Phytochemicals in Foods: 2011

Thursday, December 1, 2011

Phytochemicals in Foods - 11 Health Benefits of Coumestrol

Coumestrol, a phytoestrogen in the class of coumestans, belonging to the group of Flavonoids (polyphenols) found abundantly in red clover, alfalfa sprouts, soy, peas, brussels sprouts, etc.

Health Benefits
1. Intestinal alkaline phosphatase activity
In the clarification of the effects of coumestrol administration on Ca metabolism during pregnancy and in lactating mice, found that coumestrol did not affect serum Ca and the expression of vitamin D receptor protein in the duodenum and jejunum. Thus, coumestrol administration during pregnancy may decrease the mRNA expression of IAP and the ALP activity in the intestine of the pre-delivery mice through ERα, but coumestrol had little effect on intestinal ALP activity at 10 days after parturition, according to "Effects of coumestrol administration to pregnant and lactating mice on intestinal alkaline phosphatase activity" by Kirihata Y, Horiguchi Y, Ueda M, Sugimoto M, Ikeda S, Kume S.(1)

2. Cervical cancer
In the evaluation of Endogenous estrogens dramatic and differential effects on classical endocrine organ and proliferation, found that Using human cervical cancer cells (HeLa cells) as a model, the effects of representative xenoestrogens (Coumestrol-a phytoestrogen, tetrachlorodioxin (TCDD)-a herbicide and DDT-a pesticide) on proliferation, cell cycle, and apoptosis were examined. These xenoestrogens and estrogen inhibited the proliferation of Hela cells in a dose dependent manner from 20 to 120 nM suggesting, that 17-beta-estrtadiol and xenoestrogens induced cytotoxic effects. Coumestrol produced accumulation of HeLa cells in G2/M phase, and subsequently induced apoptosis. Similar effects were observed in estrogen treated cells, according to "Estrogenic activity of coumestrol, DDT, and TCDD in human cervical cancer cells" by Ndebele K, Graham B, Tchounwou PB.(2)

3. Anti-inflammatory activities
In the investigation of A new coumestan (solalyratin A, 1) and a novel cyclic eight-membered α,β-unsaturated ketone (solalyratin B, 3), together with three known compounds, puerariafuran (2), coumestrol (4) and 9-hydroxy-2',2'-dimethylpyrano[5',6':2,3]-coumestan (5), isolated from the whole plant of Solanum lyratum, found that in vitro, compounds 1-5 showed anti-inflammatory activities, with IC(50) values in the range 6.3-9.1 μM, according to "Solalyratins A and B, new anti-inflammatory metabolites from Solanum lyratum" by Zhang DW, Yang Y, Yao F, Yu QY, Dai SJ.(3)

4. Neuroprotective effects
In the investigation in vitro of protective effects of coumestrol on mice astrocytes, found that coumestrol induced a modest but significant increase in viability of astrocytes, while the viability of astrocytes was reduced following exposure to LPS and amyloid-beta peptide. The addition of coumestrol could reverse the toxic effect induced by LPS and amyloid-beta peptide. Both the LPS and amyloid-beta peptide enhanced interleukin 1, interleukin 6, and tumor necrosis factor-alpha synthesis and these effects were inhibited by 10(-9)M coumestrol, according to "The protective effects of coumestrol against amyloid-beta peptide- and lipopolysaccharide-induced toxicity on mice astrocytes" by Liu MH, Tsuang FY, Sheu SY, Sun JS, Shih CM.(4)

5. Antiseizure effects
In the investigation of the effects of 3alpha-diol (1 mg/kg, SC) and/or an androgen receptor blocker (flutamide 10 mg, SC), 1 hour prior to administration of pentylenetetrazol (85 mg/kg, IP), found that selective estrogen receptor modulators that favor ERalpha (propyl pyrazole triol, 17alpha-E(2)) or ERbeta (diarylpropionitrile, coumestrol, 3alpha-diol), or both (17beta-E(2)), were administered (0.1 mg/kg, SC) to juvenile male rats 1 hour before pentylenetetrazol. Estrogens with activity at ERbeta, but not those selective for ERalpha, produced antiseizure effects. Actions at ERbeta may underlie some antiseizure effects of T's metabolites, according to "Antiseizure effects of 3alpha-androstanediol and/or 17beta-estradiol may involve actions at estrogen receptor beta" by Frye CA, Ryan A, Rhodes M.(5)

6. Gastric cancer (GC)
In the estimation the risk of gastric cancer (GC) in relation to the individual and combined consumption of polyphenols and NOC precursors (nitrate and nitrite), found that for the first time, a protective effect for GC because of higher intake of cinnamic acids, secoisolariciresinol and coumestrol, and suggest that these polyphenols reduce GC risk through inhibition of endogenous nitrosation. The main sources of these polyphenols were pears, mangos and beans for cinnamic acids; beans, carrots and squash for secoisolariciresinol and legumes for coumestrol, according to "Dietary intake of polyphenols, nitrate and nitrite and gastric cancer risk in Mexico City" by Hernández-Ramírez RU, Galván-Portillo MV, Ward MH, Agudo A, González CA, Oñate-Ocaña LF, Herrera-Goepfert R, Palma-Coca O, López-Carrillo L.(6)

7. Pituitary tumor
In the investigation of the activation of different nongenomic pathways, and determine the involvement of mERalpha, with measurement the prolactin (PRL) release by radio-immunoassay, MAPK activations (ERK1/2 and JNK1/2/3) via a quantitative plate immunoassay, and intracellular [Ca2+] by Fura-2 fluorescence imaging in cells treated with E2 or four different phytoestrogens (coumestrol, daidzein, genistein, and trans-resveratrol), found that phytoestrogens were much more potent in mediating these nongenomic responses (activation of MAPKs, PRL release, and increased intracellular [Ca2+]) via mERalpha than was previously reported for genomic responses. The unique non-monotonic dose responses and variant signaling patterns caused by E2 and all tested phytoestrogens suggest that complex and multiple signaling pathways or binding partners could be involved. By activating these different nongenomic signaling pathways, phytoestrogens could have significant physiological consequences for pituitary cell functions, according to "Membrane estrogen receptor-alpha-mediated nongenomic actions of phytoestrogens in GH3/B6/F10 pituitary tumor cells" by Jeng YJ, Kochukov MY, Watson CS.(7)

8. Bone health
In the investigation of the effects of coumestrol on osteoblasts and osteoclasts, inducated that phytoestrogen coumestrol has a direct enhancing effect on the proliferation and osteogenic differentiation of bone marrow stromal cells, which would lead to stimulation of bone formation, and it can also protect the whole skeletal system by regulating OPG/RANKL expression, and these effects may be mediated by ERalpha, according to "Coumestrol promotes proliferation and osteoblastic differentiation in rat bone marrow stromal cells" by Wu XT, Wang B, Wei JN.(8)

9. Ovarian apoptosis
In the examination of the increased apoptosis in the adult rat ovary after lactational exposure to coumestrol (COU), a potent phytoestrogen. Lactating dams were gavaged at doses of 0.01, 0.1, 1, and 10 mg/kg COU during the lactation period and the reproductive effects of female pups in young adults, found that Ovarian weights were reduced significantly at 0.1 and 1.0 mg/kg COU. The reduction in the ovarian weight occurred in parallel with an increase in the apoptosis at PND 135-140. A marked dose-dependent increase in the expressions of active caspase-3 and -7 was observed in ovarian granulosa cells. Immunostaining for active caspase-3 and the TUNEL staining of apoptotic cells were also increased in ovaries exposed to COU in a dose-dependent manner, according to "Lactational coumestrol exposure increases ovarian apoptosis in adult rats" by Moon HJ, Seok JH, Kim SS, Rhee GS, Lee RD, Yang JY, Chae SY, Kim SH, Kim JY, Chung JY, Kim JM, Chung SY.(9)

10. Breast cancer
In the evaluation of the associations between dietary phytoestrogen (isoflavonoids, lignans, and coumestrol) intake and risk of breast cancer and whether the ER/PR statuses of the tumor influence this relationship, found that the effects of lignans or isoflavonoids were independent of receptor status. However, intake of coumestrol was associated with decreased risk of receptor negative tumors (ER-PR-) but not positive tumors. The risk of ER-PR- tumors was significantly lower (50%) in women with intermediate coumestrol intake compared with those who did not consume any, according to "Dietary phytoestrogens are not associated with risk of overall breast cancer but diets rich in coumestrol are inversely associated with risk of estrogen receptor and progesterone receptor negative breast tumors in Swedish women" by Hedelin M, Löf M, Olsson M, Adlercreutz H, Sandin S, Weiderpass E.(10)

11. Antimicrobial activity
in the determination of the effects of the isoflavonoids coumestrol, genistein and daidzein isolated and identified by bioassay-guided fractionation from the acetone extract of Erythrina crista galli young twigs infected with Phomopsis sp, found that these compounds showed antimicrobial activity against Bacillus brevis (MIC values 16.3, 64.8 and 137.8 microM, respectively), according to "Antimicrobial isoflavonoids from Erythrina crista galli infected with Phomopsis sp" by Redko F, Clavin ML, Weber D, Ranea F, Anke T, Martino V.(11)

12. Etc.

Pharmacy In Vegetables
Use the science behind the health benefits of vegetables
to improve your health, delay aging and cure major diseases.

Phytochemicals - 10 Health Benefits of Coumestans

Coumestans (phytoestrogens) a derivative of coumarin, are orgic compound in the class of Flavonoids (polyphenols), found abundantly in split peas, pinto beans, lima beans, alfalfa and clover sprouts, etc.

Health Benefits
1. Hepatoprotective effect
In the investigation of the effect of coumestans isolated form the leaves of W. calendulacea in paracetamol induced liver damage, revealed that coumestans of W. calendulacea afforded a significant protective action in the alleviation of paracetamol induced hepatocellular injury, according to "Hepatoprotective effect of coumestans isolated from the leaves of Wedelia calendulacea Less. in paracetamol induced liver damage" by

Emmanuel S, Amalraj T, Ignacimuthu S.(1)

2. Breast cancer
In the evaluation whether phytoestrogen intake associated with reduced breast cancer risk, using a novel phytoestrogen database, found that Among all women, lignan intake was associated with a reduced breast cancer risk (Q5 vs. Q1 MVOR: 0.81, 95% CI: 0.65, 0.99); however, following stratification by BMI, this reduction in risk was statistically significant only among overweight (BMI > 25) women. Total phytoestrogen intake was also associated with a risk reduction among overweight women only. Among pre-menopausal women, total phytoestrogen intake was associated with a significant reduction in breast cancer risk among overweight women only (Q5 vs. Q1 MVOR: 0.51, 95% CI: 0.30, 0.87). Among post-menopausal women, no statistically significant association was observed between breast cancer risk and isoflavones or lignans, according to "Dietary phytoestrogen intake--lignans and isoflavones--and breast cancer risk (Canada)" by Cotterchio M, Boucher BA, Kreiger N, Mills CA, Thompson LU.(2)

3. Colorectal cancer
In the evaluation of the suggestion of dietary phytoestrogens may reduce the risk of certain hormonal cancers (e.g. breast and prostate), found that Dietary lignan intake was associated with a significant reduction in colorectal cancer risk [OR (T3 vs. T1) = 0.73; 95% CI: 0.56, 0.94], as was isoflavone intake [OR (T3 vs. T1) = 0.71; 95% CI: 0.58, 0.86], according to "Dietary phytoestrogen intake is associated with reduced colorectal cancer risk" by

Cotterchio M, Boucher BA, Manno M, Gallinger S, Okey A, Harper P.(3)

4. Anticoccidial effects
In the examination of the anticoccidial efficacy of a product containing coumestans from Eclipta alba, found that Coumestan-treated groups showed a significant decrease in the oocyst counting since the 21 th day of life and displayed a reduced number of macroscopic lesions. Histopathological evaluations of cecum fragments showed that both treatments induced the migration of defense cells at the site of infection. A severe destruction of the cecal lining was found in the intestinal tract of broilers fed with a coumestans dose of 180 ppm, according to "Anticoccidial effects of coumestans from Eclipta alba for sustainable control of Eimeria tenella parasitosis in poultry production" by Michels MG, Bertolini LC, Esteves AF, Moreira P, Franca SC.(4)

5. Inhibition of snake venoms
In the investigation of the effect against phospholipase A(2) and the myotoxic activities of snake venomextracts from in natura aerial parts and roots, both native and genetically modified (in vitro), Among the modified roots, clone 19 showed higher concentrations of these coumestans. Our results show that the in natura extracts of plants collected from Botucatu and Ribeirão Preto were efficient in inhibiting snake venom phospholipase A(2) activity. Regarding in vitro material, the best effect against Crotalus durissus terrificus venom was that of clone 19. Clone 19 and isolated coumestans (wedelolactone and demethylwedelolactone) inhibited the myotoxic activity induced by basic phospholipases A(2) isolated from the venoms of Crotalus durissus terrificus (CB) and Bothrops jararacussu (BthTX-I and II), according to "Inhibition of snake venoms and phospholipases A(2) by extracts from native and genetically modified Eclipta alba: isolation of active coumestans" by Diogo LC, Fernandes RS, Marcussi S, Menaldo DL, Roberto PG, Matrangulo PV, Pereira PS, França SC, Giuliatti S, Soares AM, Lourenço MV.(5)

6. Cardioprotective effects
In nthe review of higher dietary intake of phytoestrogens, plant-derived compounds with partial estrogen agonist properties, have a lower incidence of cardiovascular disease and breast and uterine cancer than women with a lower dietary intake of these substances, indicated that Food and food supplements containing phytoestrogens are often advocated as an alternative to hormone replacement therapy (HRT) in women with contraindications to the use of conventional estrogen replacement or those wanting a natural alternative. In light of the recent trial results with HRT (estrogen plus progesterone), it would be prudent not to recommend phytoestrogens as cardioprotective substances until adequate safety and efficacy studies are completed, according to "Phytoestrogens as cardioprotective agents" by
Park D, Huang T, Frishman WH.(6)

7. Bone health
In the review of many studies performed on soyabean isoflavones (genistein and daidzein), either in the purified form or as a soyabean-based product or extract and in vitro studies using primary cell cultures or stabilised cell lines indicate that treatment with genistein may lead to a reduction in bone resorption, but effects on bone formation have also been shown. Investigations using animal models have provided convincing evidence of major improvements in bone mass or bone turnover following soyabean feeding.
found that cross-sectional observations in South-East Asian populations with moderately high intakes of soyabean isoflavones (50 mg/d) have shown that women in the high quartile of intake have higher bone mineral density (BMD) and reduced bone turnover, an effect that has not been shown in populations with low average intakes. Human trials have given an indication of a possible effect on lumbar spine BMD, although they have been either short term (<6 months) or methodologically weak. Unresolved issues are: the optimal dose compatible with safety; the individual differences in response that can be related to diet and genotypes; the duration of exposure, according to "Dietary phyto-oestrogens and bone health" by Branca F.(7)

8. Endometrial cancer
In the investigationof three classes of phytoestrogens (isoflavones, coumestans, and lignans) and the risk of endometrial cancer found that some phytoestrogenic compounds, at the levels consumed in the typical American-style diet, are associated with reduced risk of endometrial cancer in doses depending manner, according to "Phytoestrogen intake and endometrial cancer risk" by Horn-Ross PL, John EM, Canchola AJ, Stewart SL, Lee MM.(8)

9. Metabolic syndrome
In the proposal of AMP-activated protein kinase (AMPK)as a therapeutic target for the treatment of metabolic syndrome including obesity and type-2 diabetes, found that he bioassay-guided fractionation of an EtOAc-soluble extract of the stem bark of Erythrina abyssinica led to the isolation of a new coumestan, erythribyssin N (1), and two new benzofurans, erythribyssin F (2) and erythribyssin H (3), along with five known compounds (4-8). When tested for their stimulatory effects on AMPK activity at a concentration of 10 muM, compounds 4 and 5 showed potent activation, while compounds 1, 2, and 7 had moderate effects. These results suggest that benzofurans and coumestans may be new lead compounds for regulating the AMPK enzyme, according to "AMP-activated protein kinase (AMPK) activation by benzofurans and coumestans isolated from Erythrina abyssinica" by Nguyen PH, Nguyen TN, Dao TT, Kang HW, Ndinteh DT, Mbafor JT, Oh WK.(9)

10. Long-term postmenopausal diseases
In the review of whether, Phytoestrogens (PEs) a natural compounds, with a biological activity like estrogen, which comprise isoflavones, lignans and coumestans associated with a lower incidence of breast cancer and postmenopausal illness, found that indicates that PEs prevent bone resorption, increase bone density and reduce cholesterol. The estrogenic effects of phytoestrogens can be useful in preventing postmenopausal osteoporosis and cardiovascular disease, according to "Dietary phytoestrogens in the prevention of long-term postmenopausal diseases" by Chiechi LM.(10)

Pharmacy In Vegetables
Use the science behind the health benefits of vegetables
to improve your health, delay aging and cure major diseases.

Phytochemicals in Foods - 10 Health Benefits of Chalconoids

Chalconoids, also known as chalcones are natural phenols, in the class of Flavonoids (polyphenols), found abundantly in some foods and many plants, including hops.

Health Benefits
1. Anti cancers
In the review focus primarily on prominent members of the chalcone family with an 1,3-diphenyl-2-propenon core structure, indicated that compounds of this family have been shown to interfere with each step of carcinogenesis, including initiation, promotion and progression. Moreover, numerous compounds from the family of dietary chalcones appear to show activity against cancer cells, suggesting that these molecules or their derivatives may be considered as potential anticancer drugs, according to "Dietary chalcones with chemopreventive and chemotherapeutic potential" by Orlikova B, Tasdemir D, Golais F, Dicato M, Diederich M.(1)

2. Antimicrobial activities
In the observation of 2-Acetylbenzofuran 1 on treatment with substituted aldehydes affords the corresponding chalcones 2a-c, found that Treatment of the chalcones with nitromethane under Michael addition condition furnished the corresponding Michael adducts 3a-c. Cyclocondensation of the chalcones 2a and 2b with thiosemicarbazide under basic refluxing conditions gave 3-(benzofuran-2-yl)-5-(4-aryl)-4,5-dihydropyrazole-1-carbothioamides 4a,b. All the synthesized compounds were screened for their antibacterial and antifungal activities at 100 microg concentration. Some of our compounds showed excellent antimicrobial activities than control drugs, according to "Synthesis and antimicrobial evaluation of 1-(benzofuran-2-yl)-4-nitro-3-arylbutan-1-ones and 3-(benzofuran-2-yl)-4,5-dihydro-5-aryl-1-[4-(aryl)-1,3-thiazol-2-yl]-1H-pyrazoles" by Abdel-Wahab BF, Abdel-Aziz HA, Ahmed EM.(2)

3. Anti tuberculosis
In a series of twenty seven novel aryloxy azolyl chalcones synthesized and evaluated in vitro for the growth inhibition of Mycobacterium tuberculosis H37Rv, found that compound 19, an imidazolyl chalcone with a 2,4-difluorobenzyloxy moiety also exhibited moderate in vivo activity in mice against virulent M. tuberculosis, thus providing a new structural lead towards TB drug development, according to "Novel aryloxy azolyl chalcones with potent activity against Mycobacterium tuberculosis H37Rv" by Marrapu VK, Chaturvedi V, Singh S, Singh S, Sinha S, Bhandari K.(3)

4. Liver fibrosis
In the investigation of the effect of xanthohumol, the major prenylated chalcone found in hops, in an acute model of liver injury as a result of Carbon tetrachloride (CCl(4)), an industrial solvent, is a hepatotoxic agent and its administration is widely used as an animal model of toxin-induced liver injury, found that the protective effects of xanthohumol in this toxic liver injury model involves direct mechanisms related to its ability to block both hepatic inflammation and the activation of hepatic stellate cells, presumable at least in part via decreasing NFκB activity. Thus, this study further indicates the potential of xanthohumol application to prevent or ameliorate the development and progression of liver fibrosis in response to hepatic injury, according to "Protective effect of xanthohumol on toxin-induced liver inflammation and fibrosis" by Dorn C, Heilmann J, Hellerbrand C.(4)

5. Anti Inflammatory and neuroprotective effects
In the evaluation of oxidative stress and neuroinflammation on the progression of neurodegenerative diseases, found that Lico-E is a potential activator of the Nrf2/ARE-dependent pathway and is therapeutically relevant not only to oxidative-stress-related neurodegeneration but also inflammatory responses of microglial cells both in vitro and in vivo, according to "Licochalcone E activates Nrf2/antioxidant response element signaling pathway in both neuronal and microglial cells: therapeutic relevance to neurodegenerative disease" by Kim SS, Lim J, Bang Y, Gal J, Lee SU, Cho YC, Yoon G, Kang BY, Cheon SH, Choi HJ.(5)

6. Antiplasmodial activity
In the observation of Chalcone derivatives on an estradiol framework for their ability to inhibit the growth and development of the malaria parasite, found that a positive correlation was also observed among the antiplasmodial activity and inhibition of new permeation pathway. These observations suggest that steroidal chalcones with selective activity for the parasite may be considered as antimalarial leads for further optimization and preclinical study, according to "Antiplasmodial activity of steroidal chalcones: evaluation of their effect on hemozoin synthesis and the new permeation pathway of Plasmodium falciparum-infected erythrocyte membrane" by Sisodia BS, Negi AS, Darokar MP, Dwivedi UN, Khanuja SP.(6)

7. Prostate cancer
In the study of a number of cyclohexenyl chalcone Diels-Alder natural products possess promising biological properties including strong cytotoxicity in various human cancer cells found that Herein, which is a natural products in this class including panduratin A and nicolaioidesin C inhibit cysteine cathepsins as indicated by protease profiling assays and cell-free cathepsin L enzyme assays. Owing to the critical roles of cathepsins in the biology of human tumor progression, invasion, and metastasis, these findings should pave the way for development of novel antitumor agents for use in clinical settings, according to "Synthetic cyclohexenyl chalcone natural products possess cytotoxic activities against prostate cancer cells and inhibit cysteine cathepsins in vitro" by Deb Majumdar I, Devanabanda A, Fox B, Schwartzman J, Cong H, Porco JA Jr, Weber HC.(7)

8. Antioxidants
In the observation of aseries of new coumarin derivatives 4 containing a 4-arylbut-3-en-2-one moiety synthesized by condensation of 3-acetylcoumarin 1 with aryl aldehydes 2 in chloroform in the presence of piperidine, found that the coumarinic chalcone 4a has been found to be the most active (IC₅₀ = 2.07 μM), according to "Synthesis of new substituted chromen[4,3-c]pyrazol-4-ones and their antioxidant activities" by Al-Ayed AS.(8)

9. Breast cancer
In the evaluation of the different multi-substituted chalcones for their BCRP inhibitionto investigate different multi-substituted chalcones for their BCRP inhibition, synthesized chalcones and benzochalcones with different substituents (viz. OH, OCH(3), Cl) on ring A and B of the chalcone structure found that substituents at position 2' and 4' on chalcone ring A were found to be essential for activity; additionally there was a great influence of substituents on ring B. Presence of 3,4-dimethoxy substitution on ring B was found to be optimal, while presence of 2- and 4-chloro substitution also showed a positive effect on BCRP inhibition, according to "Investigation of chalcones and benzochalcones as inhibitors of breast cancer resistance protein" by Juvale K, Pape VF, Wiese M.(9)

10. Xanthohumol (XN) and liver and intestinal cells
In the study of Xanthohumol (XN) a the major prenylated chalcone of hops and hence an ingredient of beer found that fluorescent microscopy allowed for the first time visualization and tracing of the uptake and intracellular distribution of XN. A rapid accumulation of XN concentrations that were up to >60-fold higher than the concentration present in the ambient culture medium was observed. Fluorescence recovery after photobleaching experiments revealed that most XN molecules are bound to cellular proteins, which may alter properties of cellular factors, according to "Xanthohumol uptake and intracellular kinetics in hepatocytes, hepatic stellate cells, and intestinal cells" by Wolff H, Motyl M, Hellerbrand C, Heilmann J, Kraus B.(10)

11. Platelet aggregation
In an effort to develop potent antiplatelet agents, 12 O-prenylated (2-13) and 10 O-allylated (14-23) chalcones were synthesized and screened for in vitro inhibitory effects on aggregation of washed rabbit platelets induced by ADP (20 μM) and collagen (10 μg/mL), found that the preliminary structure-activity relationships suggested that the antiplatelet activity was governed to a great extent by the presence of a pyridyl ring-B and a hydroxy group at position C-3' in ring-A of the MBHC templates, according to "Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation" by Vijaya Bhaskar Reddy M, Tsai WJ, Qian K, Lee KH, Wu TS.(11)

12. Etc.

Pharmacy In Vegetables
Use the science behind the health benefits of vegetables
to improve your health, delay aging and cure major diseases.

Phytochemicals in Foods - 8 Health Benefits of Flavanonols

Flavanonols (with two "o"s aka 3-hydroxyflavanone or 2,3-dihydroflavonol) are a class of flavonoids that use the 3-hydroxy-2,3-dihydro-2-phenylchromen-4-one (IUPAC name) backbone(a), found in Japanese Raisin Tree, the wood of Pinus sibirica, Prunus domestica, brazilian green propolis, Black mulberry, etc.

Health Benefits
1. Antioxidant capacity
In the determination of the antioxidant of the polyphenolic constituents in some fruits, using the total oxidant scavenging capacity (TOSC) assay, found that cutite showed the highest antioxidant capacity followed by jambolão, araçá, and muruci and antioxidant turned out to be primarily good sources of hydrolyzable tannins and/or flavonols, according to "Phenolic constituents and antioxidant capacity of four underutilized fruits from the Amazon region"by Gordon A, Jungfer E, da Silva BA, Maia JG, Marx F.(1)

2. Antibacterial and antiandrogen
In the demonstration of sixteen flavanones, three flavanonols, and four pterocarpans were isolated from the MeOH extract of the roots of Sophora flavescens, found that twelve of these were new compounds, including eight prenylflavanones (1-8), one prenylflavanonol (9) and three novel pterocarpane derivatives (10-12) have exhibited significant antibacterial activities against the Gram-positive bacteria Staphylococcus aureus, Bacillus subtilis, S. epidermidis, and Propionibacterium acnes. They also exhibited antiandrogen activities, according to 'Antibacterial and antiandrogen flavonoids from Sophora flavescens" by Kuroyanagi M, Arakawa T, Hirayama Y, Hayashi T.(2)

3. Anti viral effects
In testing several flavonoids effects on Moloney murine leukemia virus reverse transcriptase activity and studies of four groups of flavonoids, namely flavones, flavanones, flavonols, and flavanonols, found that flavonols and flavanonols were very active in this regard while flavones and flavanones displayed very low activity, according to "Inhibitory effects of flavonoids on Moloney murine leukemia virus reverse transcriptase activity" by Chu SC, Hsieh YS, Lin JY.(3)

4. Hepatic and intestinal microsomes
In the investigation of fifteen flavonoids for their effects on the activity of 7-ethoxycoumarin O-deethylase in rat hepatic and intestinal microsomes, found that Polyhydroxylated flavonoids with a C2-C3 double bond (flavones and flavonols) were more effective inhibitors of the enzyme in both hepatic and intestinal microsomes than were the reduced homologues (flavanonols, flavanones and flavan-3-ols). In contrast, flavones lacking hydroxyl substituents (e.g. 5,6-benzoflavone, 7,8-benzoflavone and flavone) increased ethoxycoumarin deethylase activity in liver microsomes although they had an inhibitory effect in intestinal microsomes, according to "Comparison of the effects of various flavonoids on ethoxycoumarin deethylase activity of rat intestinal and hepatic microsomes" by Vernet A, Siess MH.(4)

5. Insulin-stimulated glucose uptake
In the assessment of the effects of different classes of flavonoids on insulin-stimulated 2-deoxy-D-[1-(3)H]glucose uptake by mouse MC3T3-G2/PA6 cells differentiated into mature adipose cells, found that the flavones, apigenin and luteolin, the flavonols, kaempferol, quercetin and fisetin, an isoflavone, genistein, a flavanonol, silybin, and the flavanols, (-)-epigallocatechin gallate (EGCG) and theaflavins, significantly inhibited insulin-stimulated glucose uptake, according to "Inhibitory mechanisms of flavonoids on insulin-stimulated glucose uptake in MC3T3-G2/PA6 adipose cells" by Nomura M, Takahashi T, Nagata N, Tsutsumi K, Kobayashi S, Akiba T, Yokogawa K, Moritani S, Miyamoto K.(5)

6. Anti cancers
In the investigation of Flavonoids and their protective effects against cancer development through several biological mechanisms, found that intake of individual flavonols (quercetin, kaempferol, and myricetin) and flavones (apigenin and luteolin) was assessed and found that The multivariate RRs of total cancer across increasing quintiles of total quantified flavonoid intake were 1.00, 1.00, 0.93, 0.94, and 0.97 (P for trend = 0.72). For site-specific cancers, the multivariate RRs in the highest quintile of total quantified flavonoid intake compared with the lowest quintile were 1.03 for breast cancer, 1.01 for colorectal cancer, 1.03 for lung cancer, 1.15 for endometrial cancer, and 1.09 for ovarian cancer (all P > 0.05), according to "Dietary intake of selected flavonols, flavones, and flavonoid-rich foods and risk of cancer in middle-aged and older women" by Wang L, Lee IM, Zhang SM, Blumberg JB, Buring JE, Sesso HD.(6)

7. Colon caner
In the observation of quercetin enhancing the activity of the differentiation markers alkaline phosphatase and dipeptidyl peptidase in Caco-2 colon cancer cells, found that flavonols can have pro-oxidant effects, but our data suggested that this action was not the sole determinant of growth inhibitory or differentiating effects on Caco-2 cells. Our data indicated that effects of quercetin on colon cancer cell lines can be greatly affected by glycoside modification, according to "Inhibition of growth and induction of alkaline phosphatase in colon cancer cells by flavonols and flavonol glycosides" by Lea MA, Ibeh C, Deutsch JK, Hamid I, desBordes C.(7)

8. Anti inflammatory effects
In the examination in a double-blind intervention study conducted with two groups of non-smoking, un-treated sarcoidosis patients, matched for age and gender. One group was given 4x500 mg quercetin (n = 12) orally within 24 h, the other one placebo (n = 6). Plasma malondialdehyde levels were used as marker of oxidative damage, plasma ratios of TNFα/IL-10 and IL-8/IL-10 as pro-inflammatory markers, found that Sarcoidosis patients might benefit from the use of antioxidants, such as quercetin in the group of Flavonols, to reduce the occurring oxidative stress as well as inflammation. The effects of long-term use of antioxidant supplementation in sarcoidosis, using e.g. quercetin, on improvement of lung function remain to be investigated, according to "Quercetin reduces markers of oxidative stress and inflammation in sarcoidosis" by Boots AW, Drent M, de Boer VC, Bast A, Haenen GR.(8)

Sources
(a) http://en.wikipedia.org/wiki/Dihydroflavonol
(1) http://www.ncbi.nlm.nih.gov/pubmed/21662239
(2) http://www.ncbi.nlm.nih.gov/pubmed/10654410
(3) http://www.ncbi.nlm.nih.gov/pubmed/1378087
(4) http://www.ncbi.nlm.nih.gov/pubmed/3491024
(5) http://www.ncbi.nlm.nih.gov/pubmed/18591783
(6) http://www.ncbi.nlm.nih.gov/pubmed/19158208
(7) http://www.ncbi.nlm.nih.gov/pubmed/20944146
(8) http://www.ncbi.nlm.nih.gov/pubmed/21324570

Phytochemicals in Foods - 13 Health Benefits of Glycitein

Glycitein is a phytochemical in the Isoflavones, belonging to the group of Flavonoids (polyphenols), found abundantly in food of the family of legumes, soy, peanuts, chick peas, fava beans, alfalfa, kudzu, etc.

Health Benefits
1. Prostate cancer
In the examination of the effects of the soy isoflavone glycitein on cellular differentiation in prostate epithelial cells (RWPE-1, WPE1-NB14, and RWPE-2), found that Glycitein significantly inhibited RWPE-1 cellular proliferation at concentrations ranging from 0.4 to 50 microM. Expression of the luminal epithelial cell marker cytokeratin 18 was not affected by glycitein treatment in the WPE1-NB14 and RWPE-2 cell line, according to "Basal cell induced differentiation of noncancerous prostate epithelial cells (RWPE-1) by glycitein" by Clubbs EA, Bomser JA(1)

2. Endometrial cancer
In the observation of the effects of Phytochemicals found in soy and other legumes in reducing the risk of endometrial cancer, found that a reduced risk of endometrial cancer was associated with total isoflavone intake (highest vs lowest quintile, ≥7.82 vs <1.59 mg per 1000 kcal/d, RR = 0.66, 95% CI = 0.47 to 0.91), daidzein intake (highest vs lowest quintile, ≥3.54 vs <0.70 mg per 1000 kcal/d, RR = 0.64, 95% CI = 0.46 to 0.90), and genistein intake (highest vs lowest quintile, ≥3.40 vs <0.69 mg per 1000 kcal/d, RR = 0.66, 95% CI = 0.47 to 0.91). No statistically significant association with endometrial cancer risk was observed for increasing intake of legumes, soy, tofu, or glycitein. Truncated age-adjusted incidence rates of endometrial cancer for the highest vs lowest quintile of total isoflavone intake were 55 vs 107 per 100 000 women per year, respectively, according to "Legume, soy, tofu, and isoflavone intake and endometrial cancer risk in postmenopausal women in the multiethnic cohort study" by Ollberding NJ, Lim U, Wilkens LR, Setiawan VW, Shvetsov YB, Henderson BE, Kolonel LN, Goodman MT.(2)

3. Ovarian cancer
In the evaluation of the impact of phytoestrogen consumption on breast cancer risk and its role on ovarian cancer, found that No statistically significant associations were found with any of the phytoestrogens under evaluation. However, there was a suggestion of an inverse association with total phytoestrogen consumption (from foods and supplements), with an odds ratio (OR) of 0.62 (95% CI: 0.38-1.00; p for trend: 0.04) for the highest vs. lowest tertile of consumption, after adjusting for reproductive covariates, age, race, education, BMI, and total energy. Further adjustment for smoking and physical activity attenuated risk estimates (OR: 0.66; 95% CI: 0.41-1.08), according to "Phytoestrogen consumption from foods and supplements and epithelial ovarian cancer risk: a population-based case control study" by Bandera EV, King M, Chandran U, Paddock LE, Rodriguez-Rodriguez L, Olson SH.(3)

4. Antioxidants
in the evaluation of the antioxidant activity and contents of various polyphenol classes in the seeds of seven soybean varieties of different seed color and one yellow seed cultivar, found that antioxidant activity of seed extracts was evaluated by the 2,2-diphenyl-1-picrylhydrazyl free radical scavenging activity assay. A positive linear correlation between antioxidant activity and contents of total polyphenols and anthocyanins was established. The highest antioxidant activity was observed in the extracts of black and brown varieties, which also showed high levels of all polyphenol classes examined. Yellow seed had the highest total isoflavone content (3.62 mg/g of dry material). The highest concentration of total daidzein was determined in black seeds (>2.0 mg/g of dry material), and the highest total glycitein and genistein contents occurred in the yellow cultivar (0.53 and 1.49 mg/g of dry material, respectively). According to our results, varieties of black and brown seeds could be of special interest not only for their large content of total polyphenols, ranging from 4.94 to 6.22 mg of gallic acid equivalents/g of dry material, but also for their high content of natural antioxidants such as anthocyanins, according to "Polyphenol content and antioxidant properties of colored soybean seeds from central europe" by Malenčić D, Cvejić J, Miladinović J.(4)

5. Cervical cancer
In the evaluation of the effect of a soy-derived isoflavone mixture (designated as SI-I, containing 71% daidzein, 14.3% genistein and 14.7% glycitein) on HeLa cells and its mechanism were investigated. SI-I in concentration range 5-80 μg/ml significantly reduced the survival rate of HeLa cells by MTT assay, found that SI-I inhibited HeLa cell growth through inducing apoptosis via the mitochondrial pathway and comparisons with reported data indicated that synergistic effect existed between the isoflavone species contained in SI-I. It is proposed that natural soy-derived isoflavones are potential candidates as chemotherapeutic agents against human cervical cancer, according to "Soy-derived isoflavones inhibit HeLa cell growth by inducing apoptosis" by Xiao JX, Huang GQ, Geng X, Qiu HW.(5)

6. Colon cancer
In the investigation of the cellular effects of soy isoflavones (composed of genistein, daidzein, and glycitein) in DLD-1 human colon adenocarcinoma cells with or without ER-β gene silencing by RNA interference (RNAi), found that maintaining the expression of ER-β is crucial in mediating the growth-suppressive effects of soy isoflavones against colon tumors. Thus upregulation of ER-β status by specific food-borne ER-ligands such as soy isoflavones could potentially be a dietary prevention or therapeutic strategy for colon cancer, according to "Estrogen receptor-β mediates the inhibition of DLD-1 human colon adenocarcinoma cells by soy isoflavones" by Bielecki A, Roberts J, Mehta R, Raju J.(6)

7. Osteoclast differentiation and apoptosis
In the investigation of the effects of glycitein on osteoclast differentiation and apoptosis in vitro,
found that Osteoclast generation was inhibited by glycitein in a biphasic-dose-dependent manner and showed the greatest inhibitory effects at 10 nM (-70%, p < 0.01). Glycitein increased caspase 3/7 activity by 15% at a concentration of 10 nM (p < 0.001). Further, 10 nM glycitein significantly decreased the expression of IL-6 (-53%, p < 0.05) and RANKL (-64%, p < 0.05) in osteoblasts but did not change mRNA levels of OPG, according to "Glycitein decreases the generation of murine osteoclasts and increases apoptosis" by Winzer M, Rauner M, Pietschmann P.(7)

8. Anti allergic effects
in the investigation of the production of beta-maltooligosaccharides of glycitein and daidzein using Lactobacillus delbrueckii and cyclodextrin glucanotransferase (CGTase) as biocatalysts,
found that The 7-O-beta-glucosides of glycitein and daidzein and 7-O-beta-maltoside of glycitein showed inhibitory effects on IgE antibody production. On the other hand, beta-glucosides of glycitein and daidzein exerted 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging activity and supeoxide-radical scavenging activity, according to "Synthesis of beta-maltooligosaccharides of glycitein and daidzein and their anti-oxidant and anti-allergic activities" by Shimoda K, Hamada H.(8)

9. Anti-photoaging effects
In the evaluation of purified soy isoflavone extract from soybean cake for the protective effects on UVB-induced damage, Fraction 3, which contains the aglycone group (daidzein, genistein and glycitein) and acetylglucoside group (acetyldaidzin, acetylgenistin and acetylglycitin) of soy isoflavones, could inhibit UVB-induced death of human keratinocytes and reduce the level of desquamation, transepidermal water loss (TEWL), erythema and epidermal thickness in mouse skin, according to "Anti-photoaging effects of soy isoflavone extract (aglycone and acetylglucoside form) from soybean cake" by Huang CC, Hsu BY, Wu NL, Tsui WH, Lin TJ, Su CC, Hung CF.(9)

10. Hypolipidemic effects
In the comprison of whether Monascus-fermented soybean extracts (MFSE) enriched with bioactive mevinolins (natural statins) and aglycone isoflavones (daidzein, glycitein, and genistein) perform an additive hypolipidemic effect in hyperlipidemic ratsand unfermented soybean extracts (UFSE), which have a higher level of glucoside isoflavones (daidzin, glycitin, and genistin) without mevinolin, found that treatment with both MFSE200 and MFSE400 groups for 40 days significantly reduced the activities of serum aspartate aminotransferase and alanine aminotransferase by averages of 35.6 and 43.2%, respectively, as compared to the high-fat diet group (p < 0.01). The results indicate that MFSE performs a more potent hypolipidemic action via improvement of the lipid profiles and down-regulated HMG-CoA reductase activity than UFSE in hyperlipidemic rats, according to "Hypolipidemic effects of Monascus-fermented soybean extracts in rats fed a high-fat and -cholesterol diet" by Pyo YH, Seong KS.(10)

11. Metabolic and inflammatory markers
in the measurement of glucose, insulin, and adipokines/cytokines in 75 healthy postmenopausal women who were randomized to receive 20 g of soy protein with 160 mg of total isoflavones (64 mg genistein, 63 mg daidzein, and 34 mg glycitein) or 20 g of soy protein placebo for 12 weeks. Women taking estrogen discontinued therapy at least 3 months before the study, found that after 12 weeks of treatment, there were significant positive changes in tumor necrosis factor alpha levels within the placebo group (P < 0.0001) and adiponectin levels within the isoflavone group (P = 0.03). Comparison of pre-post change between the groups showed a small but significant increase in serum adiponectin levels in the isoflavone group (P = 0.03) compared with the placebo group. No significant changes were seen in any other parameter between the two groups, according to "Effects of high-dose isoflavones on metabolic and inflammatory markers in healthy postmenopausal women" by Charles C, Yuskavage J, Carlson O, John M, Tagalicud AS, Maggio M, Muller DC, Egan J, Basaria S.(11)

12. Post-menopausal effects
found that high-dose isoflavones is associated with improved QOL among women who have become menopausal recently. Hence, the timing of isoflavone supplementation with regards to the onset of menopause appears to be important. The use of isoflavones, as an alternative to estrogen therapy, may be potentially useful and seemingly safe in this group of women who are looking for relief from menopausal symptoms, according to "Effect of high-dose isoflavones on cognition, quality of life, androgens, and lipoprotein in post-menopausal women" by Basaria S, Wisniewski A, Dupree K, Bruno T, Song MY, Yao F, Ojumu A, John M, Dobs AS.(12)

13. Obesity
In the investigation of Soygerm isoflavones fermentated by Bifidobacterium breve with most of isoflavone glycosides (daidzin, glycitin and genistin) in soygerms were deglycosylated to their corresponding isoflavone aglycones (daidzein, glycitein and genistein) within 24 h fermentation, found that ral administration of fermented isoflavones effectively suppressed absorption of excessive lipid into a body. Addition of either unfermented or fermented soygerm isoflavones effectively inhibited adipocyte differentiation from 3T3-L1 in a dose dependent manner., according to "Anti-obesity activities of fermented soygerm isoflavones by Bifidobacterium breve" by Choi I, Kim Y, Park Y, Seog H, Choi H.(13)

Phytochemicals in Foods - 11 Health Benefits of Genistein

Genistein is a phytochemical in the Isoflavones, belonging to the group of Flavonoids (polyphenols), found abundantly in food of the family of legumes, soy, alfalfa sprouts, red clover, chickpeas, peanuts, etc.

Health Benefits
1. Bladder Cancer
In a phase 2 randomized, placebo-controlled trial investigated whether daily, oral genistein (300 or 600 mg/day as the purified soy extract G-2535) for 14-21 days before surgery alters molecular pathways in bladder epithelial tissue in 59 subjects diagnosed with urothelial bladder cancer (median age 71), found that G-2535 treatment was well tolerated; observed toxicities were primarily mild to moderate gastrointestinal or metabolic and usually not attributed to study drug. Genistein was detected in plasma and urine of subjects receiving G-2535 at concentrations greater than placebo subjects' but were not dose-dependent. Reduction in bladder cancer tissue p-EGFR staining between the placebo arm and the combined genistein arms was significant at the protocol-specified significance level of 0.10 (p=0.07), according to "A Phase 2 Cancer Chemoprevention Biomarker Trial of Isoflavone G-2535 (Genistein) in Presurgical Bladder Cancer Patients" by Messing E, Gee JR, Saltzstein DR, Kim K, Disant'agnese PA, Kolesar J, Harris L, Faerber A, Havighurst TC, Young JM, Efros M, Getzenberg RH, Wheeler MA, Tangrea J, Parnes HL, House M, Busby JE, Hohl RJ, Bailey HH.(1)

2. Immunomodulation And Anti-Inflammation
In the review of new concepts have emerged in relation to mechanisms that contribute to the regulation of carcinogenesis processes and associated inflammatory effects, found that the effects of polyphenols on the adaptative and innate immune cells that could infiltrate the tumor. Reduction of chronic inflammation or its downstream consequences may represent a key mechanism in the fight of cancer development and polyphenols could reduce various pro-inflammatory substance productions through targeting signal transduction or through antioxidant effects, according to "Immunomodulation And Anti-Inflammatory Roles Of Polyphenols As Anticancer Agents" by Ghiringhelli F, Rébé C, Hichami A, Delmas D.(2)

3. Bone density
In the investigation of the association between habitual phyto-oestrogen intake and broadband ultrasound attenuation (BUA) of the calcanaeum as a marker of bone density, found that the non-soya isoflavones formononetin and biochanin A were marginally significant or significantly associated with BUA in postmenopausal women (β = 1·2; P < 0·1) and men (β = 1·2; P < 0·05), respectively; enterolignans and equol were positively associated with bone density in postmenopausal women, but this association became non-significant when dietary Ca was added to the model. In the lowest quintile of Ca intake, soya isoflavones were positively associated with bone density in postmenopausal women (β = 1·4; P < 0·1), according to "Association between dietary phyto-oestrogens and bone density in men and postmenopausal women" by Kuhnle GG, Ward HA, Vogiatzoglou A, Luben RN, Mulligan A, Wareham NJ, Forouhi NG, Khaw KT.(3)

4. Antioxidant effects
In the testing effects of the soy isoflavone genistein on antioxidant enzymes in DU145 prostate cancer cells, found that Genistein significantly decreased reactive oxygen species levels and induced the expression of the antioxidant enzymes manganese (Mn) superoxide dismutase (SOD) and catalase, which were associated with AMP-activated protein kinase (AMPK) and phosphatase and tensin homolog deleted from chromosome 10 (PTEN) pathways. The induced expression of catalase, MnSOD, and PTEN were attenuated by pretreatment with a pharmacological inhibitor for AMPK. Furthermore, PTEN is essential for genistein activity, as shown by PTEN transfection in PTEN-deficient PC3 cells. Thus, genistein induces antioxidant enzymes through AMPK activation and increased PTEN expression. indicating the effects of genistein primarily depend on AMPK, according to "The antioxidant effects of genistein are associated with AMP-activated protein kinase activation and PTEN induction in prostate cancer cells" by Park CE, Yun H, Lee EB, Min BI, Bae H, Choe W, Kang I, Kim SS, Ha J.(4)

5. Anti cancers
In the determination of Genistein, the predominant isoflavones found in soy, has been shown to inhibit the carcinogenesis in animal models, indicated that there are growing body of experimental evidence that show the inhibition of human cancer cells by genistein through the modulation of genes that are related to the control of cell cycle and apoptosis. Moreover, it has been shown that genistein inhibits the activation of NF-kappa B and Akt signaling pathways, both of which are known to maintain a homeostatic balance between cell survival and apoptosis. Genistein is commonly known as phytoestrogen, which targets estrogen- and androgen-mediated signaling pathways in the processes of carcinogenesis, according to "Soy isoflavones and cancer prevention" by Sarkar FH, Li Y.(5)

6. Prostate cells
In the investigation of the hypothesis that the soy-isoflavone genistein could protect DNA of LAPC-4 prostate cells from oxidative stress-related damage by enhancing the expression of antioxidative genes and proteins, found that genistein protects prostate cells from oxidative stress-related DNA damage presumably by inducing the expression of antioxidative products, such as metallothioneins. Genistein, therefore, might counteract the age-related decline of important antioxidative defence systems which in turn maintain DNA integrity, according to "Genistein protects prostate cells against hydrogen peroxide-induced DNA damage and induces expression of genes involved in the defence against oxidative stress" by

Raschke M, Rowland IR, Magee PJ, Pool-Zobel BL(6)

7. Breast cancer
In the investigation of the potential preventive effects of lycopene and genistein, alone and in combination, on breast cancer development in female Wistar rats treated with 7,12-dimethylbenz[a]anthracene (DMBA), a carcinogen known to induce breast tumors.
found that treatment was continued for 20 wk. Rats treated with DMBA developed mammary tumors with 100% tumor incidence during the 20-wk study. Inhibition of mammary cancer incidence by lycopene (70%), genistein (60%) and their combination (40%) was observed. Tumor weight decreased by 48%, 61%, and 67%, and mean tumor volume decreased by 18%, 35%, and 65% with lycopene, genistein, and lycopene + genistein, respectively (P < 0.01 for the combination). The proportions of adenocarcinoma masses decreased with lycopene and genistein combination (P < 0.05). Administration of lycopene and genistein combination suppressed breast cancer development and was associated with a decrease in MDA, 8-isoprostane, and 8-OhdG levels and with an increase in serum lycopene and genistein levels. Animals administered DMBA developed breast cancer, which was associated with increased expression of Bcl-2 and decreased expression of Bax, caspase 3, and caspase 9 in mammary tissues, according to "Inhibitory effects of combination of lycopene and genistein on 7,12- dimethyl benz(a)anthracene-induced breast cancer in rats" by Sahin K, Tuzcu M, Sahin N, Akdemir F, Ozercan I, Bayraktar S, Kucuk O.(7)

8. Neuroprotective effects
in the investigation of whether GEN could alleviate oxidative damage induced by beta-amyloid peptides 25-35 (Abeta25-35) in PC12 cells, found that GEN attenuated the cytotoxicity and partially prevented apoptosis induced by Abeta25-35. GEN dramatically attenuated ROS levels induced by Abeta25-35 in PC12 cells. In addition, GEN significantly reversed the reduction of MMP caused by Abeta25-35 to maintain the normal levels of the cells. The GSH/GSSG ratio in GEN pretreated groups significantly increased compared to the groups without GEN pretreatment. GEN reversed Abeta25-35 induced down regulation of the protein expression of gamma-GCS, Nrf2 and HO-1, according to "Genistein as a neuroprotective antioxidant attenuates redox imbalance induced by beta-amyloid peptides 25-35 in PC12 cells" by Ma W, Yuan L, Yu H, Ding B, Xi Y, Feng J, Xiao R.(8)

9. Anti diabetes
In the investigation of the effect of genistein on beta-cell proliferation and cellular signaling related to this effect and further determined its antidiabetic potential in insulin-deficient diabetic mice, found that genistein induced protein expression of cyclin D1, a major cell-cycle regulator essential for beta-cell growth. Dietary intake of genistein significantly improved hyperglycemia, glucose tolerance, and blood insulin levels in streptozotocin-induced diabetic mice, concomitant with improved islet beta-cell proliferation, survival, and mass. These results demonstrate that genistein may be a natural antidiabetic agent by directly modulating pancreatic beta-cell function via activation of the cAMP/PKA-dependent ERK1/2 signaling pathway, according to "Genistein induces pancreatic beta-cell proliferation through activation of multiple signaling pathways and prevents insulin-deficient diabetes in mice" by Fu Z, Zhang W, Zhen W, Lum H, Nadler J, Bassaganya-Riera J, Jia Z, Wang Y, Misra H, Liu D.(9)

10. Bone homeostasis
In the deiermination of the effect of genistein on bone homeostasis in mandibular subchondral bone of rats.Methods:Female SD rats were administered with genistein (10 and 50 mg/kg) or placebo by oral gavage for 6 weeks, found that the low and high doses of genistein significantly increased the expression of ERβ, while ERα expression was increased by the low dose genistein and decreased by the high dose genistein. ERβ silencing abrogated most of the effects of genistein treatment.Conclusion:In rat mandibular condylar subchondral bone, low-dose genistein increases bone formation and inhibit bone resorption, while excess genistein inhibits both bone formation and resorption, according to"Dose-dependent effects of genistein on bone homeostasis in rats' mandibular subchondral bone" by

Li YQ, Xing XH, Wang H, Weng XL, Yu SB, Dong GY.(10)

11. Obesity
In the study of the role of ER alpha and ER beta in a model of nutrition induced obesity, found that Treatment with E2 and Alpha decreased body weight, total cholesterol and VLDL. Visceral fat mass, adipocyte size, and serum leptin were reduced by E2, Alpha and Beta. In the soleus muscle, treatment with E2 and Beta modulated Igf1 and Pax7 gene expression and resulted in larger muscle fibers, according to "Impact of estradiol, ER subtype specific agonists and genistein on energy homeostasis in a rat model of nutrition induced obesity" by
Weigt C, Hertrampf T, Zoth N, Fritzemeier KH, Diel P.(11)

Etc.

Phytochemicals in Foods - 11 Health Benefits of Daidzein

Daidzein is a phytochemical in the Isoflavones, belonging to the group of Flavonoids (polyphenols), found abundantly in food of the family of legumes, soy, alfalfa sprouts, red clover, chickpeas, peanuts, etc.

Health Benefits
1. Breast cancer
In the investigation of the anticancer effects and cellular apoptosis pathways induced by daidzein, using human MCF-7 breast cancer cell line, found that daidzein-induced ROS generation was accompanied by disruption of mitochondrial transmembrane potential, down-regulation of bcl-2, and up-regulation of bax, which led to the release of cytochrome C from the mitochondria into the cytosol, which, in turn, resulted in the activation of caspase-9 and caspase-7, and ultimately in cell death, The induction of the mitochondrial caspase-dependent pathway was confirmed by pretreatment with pan-caspase inhibitor z-VAD-fmk and antioxidant N-acetyl-L-cysteine, according to "Daidzein induces MCF-7 breast cancer cell apoptosis via the mitochondrial pathway" by Jin S, Zhang QY, Kang XM, Wang JX, Zhao WH.(1)

2. Ameliorative effect

In the investigation of Estrogen deficiency was produced in female Sprague-Dawley rats by surgical removal of both the ovaries and these animals were used 4 weeks later and observation of Endothelium-dependent and endothelium-independent relaxations due to acetylcholine and sodium nitroprusside, found that Administration of daidzein (0.2 mgkg(-1)day(-1), sc 0.4 mgkg(-1)day(-1), sc and 0.8 mgkg(-1)day(-1), sc) and Atorvastatin (30 mgkg(-1)day(-1), po Positive Control) for one week markedly improved vascular endothelial dysfunction due to increase in nitric oxide bioavailability perhaps by inhibiting caveolin-1 and activation of PI3K-AKT pathway, according to 'Ameliorative effect of daidzein: a caveolin-1 inhibitor in vascular endothelium dysfunction induced by ovariectomy" by Sharma S, Singh M, Sharma PL.(2)

3. Prostate cancer

In evaluation of a mixture of soy isoflavones (genistein, daidzein, glycitein) and theirs effect on Prostate cancer, found that Daidzein could be the component of soy that protects against genistein-induced metastasis. Daidzein inhibited cell growth and synergized with radiation, affecting APE1/Ref-1, NF-kappaB and HIF-1alpha, but at lower levels than genistein and soy, in AR+ and AR- PCa cells, suggesting it is an AR-independent mechanism, according to "Daidzein effect on hormone refractory prostate cancer in vitro and in vivo compared to genistein and soy extract: potentiation of radiotherapy" by Singh-Gupta V, Zhang H, Yunker CK, Ahmad Z, Zwier D, Sarkar FH, Hillman GG.(3)

4. Cellular Integrity

In the investigation of the protective effect of two major soy isoflavones, genistein and daidzein, in combination on the status of glycoconjugates in plasma, found that Oral administration of genistein + daidzein (20 mg + 20 mg kg(-1) bw/day) to DMBA treated rats significantly (p< 0.05) brought back the status of glycoconjugates to near normal range. The present study thus demonstrated that genistein and daidzein in combination, according to "Genistein and Daidzein, in Combination, Protect Cellular Integrity during 7,12-Dimethylbenz[a]anthracene (DMBA) Induced Mammary Carcinogenesis in Sprague-Dawley Rats" by Pugalendhi P, Manoharan S, Suresh K, Baskaran N.(4)

5. Anti tumors

In the establishment of the chromatographic fingerprints for the anti-tumor flavonoids of Caulis spatholobi (SSCE)(16 characteristic peaks from 10 batches of medicinal materials. Among them, the peaks 1, 3, 4, 5, 8, 9, 10, 12, 13, and 16 were identified 3,4-dihodroxybenzoic acid, 4-Hydroxybenzoic Acid, epicatechin, puerarin, daidzein, liquiritigenin, calycosin, genistein, formononetin, and prunetin, respectively.) indicatedthat The method is convenient, reproducibility and stability. It can used for quality control of the anti-tumor flavonoids of C. spatholobi (SSCE), according to '[Study on HPLC chromatographic fingerprint of anti-tumor active site SSCE of Caulis spatholobi].[Article in Chinese]" by Wang H, Liu Y, Zeng Z, He W.(5)

6. Endometrial cancer

In the evaluation of Legume, soy, tofu, and isoflavone intake and endometrial cancer risk in postmenopausal women, found that reduced risk of endometrial cancer was associated with total isoflavone intake (highest vs lowest quintile, ≥7.82 vs <1.59 mg per 1000 kcal/d, RR = 0.66, 95% CI = 0.47 to 0.91), daidzein intake (highest vs lowest quintile, ≥3.54 vs <0.70 mg per 1000 kcal/d, RR = 0.64, 95% CI = 0.46 to 0.90), and genistein intake (highest vs lowest quintile, ≥3.40 vs <0.69 mg per 1000 kcal/d, RR = 0.66, 95% CI = 0.47 to 0.91). No statistically significant association with endometrial cancer risk was observed for increasing intake of legumes, soy, tofu, or glycitein, according to "Legume, soy, tofu, and isoflavone intake and endometrial cancer risk in postmenopausal women in the multiethnic cohort study" by Ollberding NJ, Lim U, Wilkens LR, Setiawan VW, Shvetsov YB, Henderson BE, Kolonel LN, Goodman MT.(6)

7. Anti-allergic activities
In the investigation of the biocatalytic synthesis of xylooligosaccharides of daidzein, using cultured cells of Catharanthus roseus and Aspergillus sp. β-xylosidase, found that The cultured cells of C. roseus converted daidzein into its 4'-O-β-glucoside, 7-O-β-glucoside, and 7-O-β-primeveroside, which was a new compound. The 7-O-β-primeveroside of daidzein was further xylosylated by Aspergillus sp. β-xylosidase to daidzein trisaccharide, i.e., 7-O-[6-O-(4-O-(β-d-xylopyranosyl))-β-d-xylopyranosyl]-β-d-glucopyranoside, which was a new compound. The 4'-O-β-glucoside, 7-O-β-glucoside, and 7-O-β-primeveroside of daidzein exerted DPPH free-radical scavenging and superoxide radical scavenging activity. On the other hand, 7-O-β-glucoside and 7-O-β-primeveroside of daidzein showed inhibitory effects on IgE antibody production, according to "Synthesis of xylooligosaccharides of daidzein and their anti-oxidant and anti-allergic activities" by Shimoda K, Hamada H, Hamada H.(7)

8. Menopausal symptoms
In the examination of the efficacy of a supplement containing natural S-(-)equol, a daidzein metabolite, in reducing menopausal symptoms, found that the beneficial effects of a 10-mg natural S-(-)equol supplement is consumed daily for 12 weeks on major menopausal symptoms, specifically, hot flushes and neck or shoulder muscle stiffness, in postmenopausal Japanese women. This supplement offers a promising alternative for management of menopausal symptoms, according to "A natural s-equol supplement alleviates hot flushes and other menopausal symptoms in equol nonproducing postmenopausal Japanese women" by Aso T, Uchiyama S, Matsumura Y, Taguchi M, Nozaki M, Takamatsu K, Ishizuka B, Kubota T, Mizunuma H, Ohta H.(8)

9. Anti skin aging
In the explanation of Oestrogen (17β estradiol) and the dietary antioxidants resveratrol, genistein and S-equol, an isoflavone produced from the gut biotransformation of soy daidzein, are effective agents to reduce ageing in skin, indicated that the evidence to date suggests that the primary mechanism of action of these antioxidants is to activate oestrogen receptor β (ERβ), which in turn enhances the expression of antioxidant enzymes and inhibits the expression of snail, a transcription factor that regulates keratinocyte cell proliferation and migration. Based on their selectivity, ERβ agents provide a treatment option for ageing skin without the potential safety issues associated with oestrogen therapy, according to "Ageing skin: oestrogen receptor β agonists offer an approach to change the outcome" by Jackson RL, Greiwe JS, Schwen RJ.(9)

10.
In the investigation of the involvement of caveolin in attenuation of the cardioprotective effect of IPC during DM in rat, found that attenuation of the cardioprotection in diabetic heart may be due to decrease the IPC mediated release of NO in the diabetic myocardium, which may be due to up -regulation of caveolin and subsequently decreased activity of eNOS, according to "Possible involvement of caveolin in attenuation of cardioprotective effect of ischemic preconditioning in diabetic rat heart" by Ajmani P, Yadav HN, Singh M, Sharma PL.(10)

11. Bone density
In the observation of the association between habitual phyto-oestrogen intake and broadband ultrasound attenuation (BUA) of the calcanaeum as a marker of bone density, found that enterolignans and equol were positively associated with bone density in postmenopausal women, but this association became non-significant when dietary Ca was added to the model. In the lowest quintile of Ca intake, soya isoflavones were positively associated with bone density in postmenopausal women (β = 1·4; P < 0·1). The present results therefore suggest that non-soya isoflavones are associated with bone density independent of Ca, whereas the association with soya or soya isoflavones is affected by dietary Ca, according to "Association between dietary phyto-oestrogens and bone density in men and postmenopausal women" by Kuhnle GG, Ward HA, Vogiatzoglou A, Luben RN, Mulligan A, Wareham NJ, Forouhi NG, Khaw KT.(11)

12. Etc.

Sources

(1) http://www.ncbi.nlm.nih.gov/pubmed/19889614
(2) http://www.ncbi.nlm.nih.gov/pubmed/22279937

(3) http://www.ncbi.nlm.nih.gov/pubmed/20309614

(4) http://www.ncbi.nlm.nih.gov/pubmed/22238489

(5) http://www.ncbi.nlm.nih.gov/pubmed/22256759

(6) http://www.ncbi.nlm.nih.gov/pubmed/22158125
(7) http://www.mdpi.com/1422-0067/12/9/5616/
(8) http://www.ncbi.nlm.nih.gov/pubmed/21992596
(9) http://www.ncbi.nlm.nih.gov/pubmed/21913999
(10) http://www.ncbi.nlm.nih.gov/pubmed/21745415
(11) http://www.ncbi.nlm.nih.gov/pubmed/21736835

Phytochemicals in Foods - 8 Health Benefits of Petunidin

Petunidin, a dark-red or purple water-soluble pigment, is an anthocyanins (flavonals), in the group of Flavonoids (polyphenols), found abundantly in many redberries and some species of grape, etc.

Health Benefits
1. Antioxidants
In the investigation of a newly developed nongenetically modified purple tomato V118 was investigated for its phytochemical compositions and antioxidant activities, found that three major anthocyanins, which were mainly acylglycosides of petunidin and malvidin. This study showed that purple tomatoes such as V118 possess additional phytochemicals like anthocyanins, which can potentially have added health benefits, according to "Characterization of phytochemicals and antioxidant activities of a purple tomato (Solanum lycopersicum L.)" by Li H, Deng Z, Liu R, Young JC, Zhu H, Loewen S, Tsao R.(1)

2. Anti diabetes
In the determination of the methanolic extracts of whole fruit and skin of the muscadine and theirs effect on the α-glucosidase with their IC(50) values at 1.50 and 2.73 mg/mL, and those against the lipase at 16.90 and 11.15 mg/mL, respectively, showed that that the muscadine extracts possessed strong antidiabetic activities. Particularly, the ethyl acetate (EtoAc) extract and the butanol (BuOH) extract exhibited much higher inhibitory activities against both enzymes than the CHCl(3) and water extracts, while the majority of anthocyanins existed in the BuOH fractions. Moreover, cyanidin exhibited a much stronger antidiabetic activity than cyanidin-3,5-diglucoside, suggesting that anthocyanins may have higher inhibitory activities after being digested. Further chromatographic analysis by high-performance liquid chromatography-mass spectrometry identified five individual anthocyanins, including cyanidin, delphinidin, petunidin, peonidin, and malvidin glycosides, according to "Inhibitory effects of muscadine anthocyanins on α-glucosidase and pancreatic lipase activities" by You Q, Chen F, Wang X, Luo PG, Jiang Y.(2)

3. Antioxidant and Eye strain
In the registration of New red leaf tea cultivar 'Sunrouge' (Camellia taliensis × Camellia sinensis), for which an application of an anthocyanin-rich tea was made in 2009, found that the four anthocyanins were identified were delphinidin-3-O-β-D-(6-(E)-p-coumaroyl)galactopyranoside (2), delphinidin-3-O-β-D-(6-(E)-p-coumaroyl)glucopyranoside (3), cyanidin-3-O-β-D-(6-(E)-p-coumaroyl)galactopyranoside (4), and cyanidin-3-O-β-D-(6-(E)-p-coumaroyl)glucopyranoside (5), and the other two were estimated as delphinidin-(Z)-p-coumaroylgalactopyranoside (1), petunidin-(E)-p-coumaroylgalactopyranoside (6). Compound 3 was found in tea for the first time. In general, anthocyanins have various bioactivities, including relieving eyestrain and antioxidative effects, so it is expected that drinking 'Sunrouge' tea brings in similar bioactivities, according to "Anthocyanins from new red leaf tea 'Sunrouge'" by Saito T, Honma D, Tagashira M, Kanda T, Nesumi A, Maeda-Yamamoto M.(3)

4. Oxidative stress
In the analyzing procyanidins B1, B2, and A2 identified by UPLC/ESI-MS(2) along with the presence of other flavanol oligomers, showed that processing induced the release of large amounts of aglycones for ferulic acid, p-coumaric acid, and quercetin. The described anthocyanic composition of lingonberry was completed with hexoside derivatives of peonidin, petunidin, malvidin, and delphinidin. Besides confirmation of in vitro antioxidant activity, in vivo study was performed on rats fed a diet inducing oxidative stress. Supplementation with lingonberry extract significantly decreased the total oxidant status and favorably affected antioxidant defense enzymes in red blood cells and liver, according to "Food grade lingonberry extract: polyphenolic composition and in vivo protective effect against oxidative stress" by
Mane C, Loonis M, Juhel C, Dufour C, Malien-Aubert C.(4)

5. Anti cancers
In the evaluation the anti cancers effect of extracted Vaccinium uliginosum Anthocyanins (A(V.uli)), a type of blueberry found in the Chinese Changbai Mountains, found that The optimum process of A(V.uli) extraction involved conditions of temperature 20°C, pH 2.0, and diatomaceous earth 1.0 g/50 g of fruit weight. A(V.uli) contained 5 main components: delphinidin (40.70 ± 1.72)%, cyanidin (3.40 ± 0.68)%, petunidin (17.70 ± 0.54)%, peonidin (2.90 ± 0.63)% and malvidin (35.50 ± 1.11)%. The malvidin percentage was significantly higher (P < 0.05) than it in A(V.myr). A(V.uli) complied with a dose-dependent repression of cancer cell proliferation with an IC(50) (50% inhibitory concentration) value of 50 µg/ml, and showed greater anticancer efficiency than A(L.cae) and A(V.myr) under the same cell treatment conditions, according to "Anthocyanins extracted from Chinese blueberry (Vaccinium uliginosum L.) and its anticancer effects on DLD-1 and COLO205 cells" by
Zu XY, Zhang ZY, Zhang XW, Yoshioka M, Yang YN, Li J.(5)

6. Liver cancer
In the identication, if the anthocyanins (delphinidin-3,5-diglucoside: cyanidin-3,5-diglucoside: petunidin-3,5-diglucoside: delphinidin-3-glucoside: malvdin-3,5-diglucoside: peonidin-3,5-diglucoside: cyanidin-3-glucoside: petunidin-3-glucoside: peonidin-3- glucoside: malvidin-3- glucoside = 27:63:8.27:1:2.21:2.21:6.7:1.25:5.72:1.25) [corrected] isolated from meoru (Vitis coignetiae Pulliat) exerted antiproliferative and anti-invasive and apoptotic effects on human hepatoma Hep3B cells, found that the anthocyanins from meoru have antiproliferative and anti-invasive effects and may induce apoptosis through the activation of the mitochondrial pathway and inhibition of antiapoptotic proteins. This study provides evidence that the anthocyanins isolated from meoru might be useful in the treatment of human hepatitis B-associated hepatoma, according to "Induction of apoptosis and inhibition of invasion in human hepatoma cells by anthocyanins from meoru" by Shin DY, Ryu CH, Lee WS, Kim DC, Kim SH, Hah YS, Lee SJ, Shin SC, Kang HS, Choi YH.(6)

7. Photoaging
In the investigation of the capacity of anthocyanin-rich extract from bog blueberry (ATH-BBe) to inhibit photoaging in UV-B-irradiated human dermal fibroblasts. BBe anthocyanins were detected as cyanidin-3-glucoside, petunidin-3-glucoside, malvidin-3-glucoside, and delphinidin3-glucoside. ATH-BBe attenuated UV-B-induced toxicity accompanying reactive oxygen species (ROS) production and the resultant DNA damage responsible for activation of p53, found that ATH-BBe dampens UV-B-triggered collagen destruction and inflammatory responses through modulating NF-kappaB-responsive and MAPK-dependent pathways. Therefore, anthocyanins from edible bog blueberry may be protective against UV-induced skin photoaging, according to "Bog blueberry anthocyanins alleviate photoaging in ultraviolet-B irradiation-induced human dermal fibroblasts" by Bae JY, Lim SS, Kim SJ, Choi JS, Park J, Ju SM, Han SJ, Kang IJ, Kang YH.(7)

8. Breast cancer
In the standardization of Jamun fruit extract (JFE) to anthocyanin content using the pH differential method, and individual anthocyanins were identified by high performance liquid chromatography with ultraviolet (HPLC-UV) and tandem mass spectrometry (LC-MS/MS) methods, showed that JFE contained 3.5% anthocyanins (as cyanidin-3-glucoside equivalents) which occur as diglucosides of five anthocyanidins/aglycons: delphinidin, cyanidin, petunidin, peonidin and malvidin, found that JFE was most effective against MCF-7aro (IC(50) = 27 microg/mL), followed by MDA-MB-231 (IC(50) = 40 microg/mL) breast cancer cells. Importantly, JFE exhibited only mild antiproliferative effects against the normal MCF-10A (IC(50) > 100 microg/mL) breast cells. Similarly, JFE (at 200 microg/mL) exhibited pro-apoptotic effects against the MCF-7aro.

9. Etc.

Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/21905736
(2) http://www.ncbi.nlm.nih.gov/pubmed/21797278
(3) http://www.ncbi.nlm.nih.gov/pubmed/21480597
(4) http://www.ncbi.nlm.nih.gov/pubmed/21375302
(5) http://www.ncbi.nlm.nih.gov/pubmed/21034658
(6) http://www.ncbi.nlm.nih.gov/pubmed/19723048
(7) http://www.ncbi.nlm.nih.gov/pubmed/19199288
(8) http://www.ncbi.nlm.nih.gov/pubmed/19166352

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Thursday, December 1, 2011