Thursday, December 1, 2011

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.

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