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Resveratrol Modulates Drug- and Carcinogen-Metabolizing Enzymes in a Healthy Volunteer Study

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Chow, H-H. Sherry, Garland, Linda L., Hsu, Chiu-Hsieh, Vining, Donna R., Chew, Wade M., Miller, Jessica A., Perloff, Marjorie, Crowell, James A., Alberts, David S.·2010·Cancer Prevention Research
DOI 10.1158/1940-6207.capr-09-0155
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Abstract

Resveratrol has been shown to exhibit cancer-preventive activities in preclinical studies. We conducted a clinical study to determine the effect of pharmacologic doses of resveratrol on drug- and carcinogen-metabolizing enzymes. Forty-two healthy volunteers underwent baseline assessment of cytochrome P450 (CYP) and phase II detoxification enzymes. CYP1A2, CYP2D6, CYP2C9, and CYP3A4 enzyme activities were measured by the metabolism of caffeine, dextromethorphan, losartan, and buspirone, respectively. Blood lymphocyte glutathione S-transferase (GST) activity and GST-π level and serum total and direct bilirubin, a surrogate for UDP-glucuronosyl transferase (UGT) 1A1 activity, were measured to assess phase II enzymes. After the baseline evaluation, study participants took 1 g of resveratrol once daily for 4 weeks. Enzyme assessment was repeated upon intervention completion. Resveratrol intervention was found to inhibit the phenotypic indices of CYP3A4, CYP2D6, and CYP2C9 and to induce the phenotypic index of 1A2. Overall, GST and UGT1A1 activities were minimally affected by the intervention, although an induction of GST-π level and UGT1A1 activity was observed in individuals with low baseline enzyme level/activity. We conclude that resveratrol can modulate enzyme systems involved in carcinogen activation and detoxification, which may be one mechanism by which resveratrol inhibits carcinogenesis. However, pharmacologic doses of resveratrol could potentially lead to increased adverse drug reactions or altered drug efficacy due to inhibition or induction of certain CYPs. Further clinical development of resveratrol for cancer prevention should consider evaluation of lower doses of resveratrol to minimize adverse metabolic drug interactions. Cancer Prev Res; 3(9); 1168–75. ©2010 AACR.

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Metadata

Authors
Chow, H.-H. S., Garland, L. L., Hsu, C.-H., Vining, D. R., Chew, W. M., Miller, J. A., Perloff, M., Crowell, J. A., & Alberts, D. S.
Venue
Cancer Prevention Research
Publisher
American Association for Cancer Research (AACR)
Published
2010-09-01
Volume
3
Issue
9
Pages
1168-1175
ISSN
  • 1940-6207 (ISSN-L)
  • 1940-6215
DOI
10.1158/1940-6207.capr-09-0155
OpenAlex
W2158735110
Cited by
330
References
0
FWCI
16.07
Type
journal article
Language
en
Open access
green

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CoChat. (2026). Citation check: Resveratrol Modulates Drug- and Carcinogen-Metabolizing Enzymes in a Healthy Volunteer Study. https://app.cochat.ai/papers/10.1158/1940-6207.capr-09-0155
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Chow, H.-H. S., Garland, L. L., Hsu, C.-H., Vining, D. R., Chew, W. M., Miller, J. A., Perloff, M., Crowell, J. A., & Alberts, D. S. (2010). Resveratrol Modulates Drug- and Carcinogen-Metabolizing Enzymes in a Healthy Volunteer Study. Cancer Prevention Research. https://doi.org/10.1158/1940-6207.capr-09-0155

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