Comparative CYP1A1 and CYP1B1 substrate and inhibitor profile of dietary flavonoids

Androutsopoulos, Vasilis P.; Papakyriakou, Athanasios; Vourloumis, Dionisios; Spandidos, Demetrios Α.

doi:10.1016/j.bmc.2011.03.042

Cited by 90 publications

(63 citation statements)

References 42 publications

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“…Previous investigations have demonstrated that the structure of flavonoids is also associated with mutagen metabolism. For example, flavonoids containing a methoxyl group can induce CYP1A1 enzyme, which is an enzyme involved in benzo(a)pyrene metabolism (Androutsopoulos 2011). Moreover, some flavonols and flavones inhibited CYP1A2 activity, but enhanced CYP1A1 acitivity (Moon et al, 2006;Chatuphonprasert and Jarukamjorn, 2012).…”

Section: Mutagenicity and Antimutagenicity Of Seed And Hull Extracts mentioning

confidence: 99%

Mutagenicity and Antimutagenicity of Hydrophilic and Lipophilic Extracts of Thai Northern Purple Rice

Punvittayagul¹,

Sringarm²,

Chaiyasut³

et al. 2014

Asian Pacific Journal of Cancer Prevention

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Section: Mutagenicity and Antimutagenicity Of Seed And Hull Extracts mentioning

confidence: 99%

Mutagenicity and Antimutagenicity of Hydrophilic and Lipophilic Extracts of Thai Northern Purple Rice

Punvittayagul¹,

Sringarm²,

Chaiyasut³

et al. 2014

Asian Pacific Journal of Cancer Prevention

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“…Plants produce flavonoids as secondary metabolites for protection against micro organisms, U.V.light, spread of disease and gives colour to flowers. Chrysin is 5,7-dihydroxy flavone that was found to be cytotoxic with EC 50 value of 100 μM in wide range of cell lines such as breast (MCF-7, MDA-MB-231 cells), colon (Lovo, DLD-1) and prostate cancer cells [23,24]. Emerging evidences have shown that Histone deacetylase inhibitors (HDACi) such as Trichostatin A (TSA), NBM-HD-1, 3, 3' Diindolyl methane (DIM) were found to be not only inhibit histone deacetylase activity but also decrease the Akt activity that eventually lead to growth inhibition as well as apoptosis [25]‐[28].…”

Section: Introductionmentioning

confidence: 99%

Plant HDAC inhibitor chrysin arrest cell growth and induce p21 WAF1 by altering chromatin of STAT response element in A375 cells

et al. 2012

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BackgroundChrysin and its analogues, belongs to flavonoid family and possess potential anti-tumour activity. The aim of this study is to determine the molecular mechanism by which chrysin controls cell growth and induce apoptosis in A375 cells.MethodsEffect of chrysin and its analogues on cell viability and cell cycle analysis was determined by MTT assay and flowcytometry. A series of Western blots was performed to determine the effect of chrysin on important cell cycle regulatory proteins (Cdk2, cyclin D1, p53, p21, p27). The fluorimetry and calorimetry based assays was conducted for characterization of chrysin as HDAC inhibitor. The changes in histone tail modification such as acetylation and methylation was studied after chrysin treatment was estimated by immuno-fluorescence and western blot analysis. The expression of Bcl-xL, survivin and caspase-3 was estimated in chrysin treated cells. The effect of chrysin on p21 promoter activity was studied by luciferase and ChIP assays.ResultsChrysin cause G1 cell cycle arrest and found to inhibit HDAC-2 and HDAC-8. Chrysin treated cells have shown increase in the levels of H3acK14, H4acK12, H4acK16 and decrease in H3me2K9 methylation. The p21 induction by chrysin treatment was found to be independent of p53 status. The chromatin remodelling at p21WAF1 promoter induces p21 activity, increased STAT-1 expression and epigenetic modifications that are responsible for ultimate cell cycle arrest and apoptosis.ConclusionChrysin shows in vitro anti-cancer activity that is correlated with induction of histone hyperacetylation and possible recruitment of STAT-1, 3, 5 proteins at STAT (−692 to −684) region of p21 promoter. Our results also support an unexpected action of chrysin on the chromatin organization of p21WAF1 promoter through histone methylation and hyper-acetylation. It proposes previously unknown sequence specific chromatin modulations in the STAT responsive elements for regulating cell cycle progression negatively via the induction of the CDK inhibitor p21WAF1.

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“…Formononetin also significantly inhibits CYP 2D6, and biochanin A also inhibits human CYP 2C9 [147]. CYP 1B1 is inhibited by flavone [148], chrysin [148], apigenin [148], genistein [148], luteolin [149], quercetein [149], galangin [149], myricetin [150], and many others. CYP 1A1 is irreversibly inhibited by the binding of two flavones (3-flavone propargyl etherE and 7-Hydroxy flavone) [151].…”

Section: Challenges In Flavonoids In Cancer Chemoprevention Developmentmentioning

confidence: 99%

Cancer chemoprevention through dietary flavonoids: what’s limiting?

2017

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Flavonoids are polyphenols that are found in numerous edible plant species. Data obtained from preclinical and clinical studies suggest that specific flavonoids are chemo-preventive and cytotoxic against various cancers via a multitude of mechanisms. However, the clinical use of flavonoids is limited due to challenges associated with their effective use, including (1) the isolation and purification of flavonoids from their natural resources; (2) demonstration of the effects of flavonoids in reducing the risk of certain cancer, in tandem with the cost and time needed for epidemiological studies, and (3) numerous pharmacokinetic challenges (e.g., bioavailability, drug–drug interactions, and metabolic instability). Currently, numerous approaches are being used to surmount some of these challenges, thereby increasing the likelihood of flavonoids being used as chemo-preventive drugs in the clinic. In this review, we summarize the most important challenges and efforts that are being made to surmount these challenges.

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Comparative CYP1A1 and CYP1B1 substrate and inhibitor profile of dietary flavonoids

Cited by 90 publications

References 42 publications

Mutagenicity and Antimutagenicity of Hydrophilic and Lipophilic Extracts of Thai Northern Purple Rice

Mutagenicity and Antimutagenicity of Hydrophilic and Lipophilic Extracts of Thai Northern Purple Rice

Plant HDAC inhibitor chrysin arrest cell growth and induce p21 WAF1 by altering chromatin of STAT response element in A375 cells

Cancer chemoprevention through dietary flavonoids: what’s limiting?

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