<i>Trans</i>-resveratrol-mediated inhibition of β-oestradiol conjugation in MCF-7 cells stably expressing human sulfotransferases SULT1A1 or SULT1E1, and human liver microsomes

Ung, Din; Nagar, Swati

doi:10.1080/00498250802604082

Cited by 15 publications

(4 citation statements)

References 29 publications

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“…Resveratrol was shown to be a mechanism-based inhibitor of recombinant CYP3A4 (Chan and Delucchi, 2000). High resveratrol concentrations (10-500 mM) inhibited estradiol glucuronidation in human liver microsomes (Ung and Nagar, 2009). Resveratrol inhibited SULT1E1 activity in primary human mammary epithelial cells, as measured by the formation of 17b-estradiol-3-sulfate (Otake et al, 2000).…”

Section: Case Study: Milk Thistlementioning

confidence: 99%

Herb–Drug Interactions: Challenges and Opportunities for Improved Predictions

et al. 2013

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Supported by a usage history that predates written records and the perception that "natural" ensures safety, herbal products have increasingly been incorporated into Western health care. Consumers often self-administer these products concomitantly with conventional medications without informing their health care provider(s). Such herb-drug combinations can produce untoward effects when the herbal product perturbs the activity of drug metabolizing enzymes and/or transporters. Despite increasing recognition of these types of herb-drug interactions, a standard system for interaction prediction and evaluation is nonexistent. Consequently, the mechanisms underlying herb-drug interactions remain an understudied area of pharmacotherapy. Evaluation of herbal product interaction liability is challenging due to variability in herbal product composition, uncertainty of the causative constituents, and often scant knowledge of causative constituent pharmacokinetics. These limitations are confounded further by the varying perspectives concerning herbal product regulation. Systematic evaluation of herbal product drug interaction liability, as is routine for new drugs under development, necessitates identifying individual constituents from herbal products and characterizing the interaction potential of such constituents. Integration of this information into in silico models that estimate the pharmacokinetics of individual constituents should facilitate prospective identification of herb-drug interactions. These concepts are highlighted with the exemplar herbal products milk thistle and resveratrol. Implementation of this methodology should help provide definitive information to both consumers and clinicians about the risk of adding herbal products to conventional pharmacotherapeutic regimens.

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Section: Case Study: Milk Thistlementioning

confidence: 99%

Herb–Drug Interactions: Challenges and Opportunities for Improved Predictions

et al. 2013

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“…4 Recent in vitro and animal studies also showed that resveratrol enhances testosterone levels in rabbits and inhibits estradiol (E2), indicating that resveratrol may alter the homeostasis of endogenous hormones. 5,6…”

Section: Adverse Effects Of Resveratrolmentioning

confidence: 99%

“…In a healthy volunteer study, resveratrol (1 g/day) was shown to inhibit the cytochrome P450 isoforms CYP2C9, CYP2D6, and CYP3A4, potentially leading to increased adverse drug reactions of coadministered CYP substrates . Recent in vitro and animal studies also showed that resveratrol enhances testosterone levels in rabbits and inhibits estradiol (E2), indicating that resveratrol may alter the homeostasis of endogenous hormones …”

Section: Adverse Effects Of Resveratrolmentioning

confidence: 99%

Interplay between metabolism and transport of resveratrol

Maier‐Salamon

Böhmdorfer

Riha

et al. 2013

Annals of the New York Academy of Sciences

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Resveratrol exhibits a variety of biological and pharmacological activities despite its extensive metabolism to sulfates and glucuronides in the intestine and liver. The metabolism of resveratrol is cell specific and strongly correlates with enzyme expression levels. However, a high rate of biotransformation, in concert with the action of the efflux transporters MRP2, MRP3, and ABCG2, reduces intracellular resveratrol concentrations, and may thereby decrease its pharmacological activity. Interestingly, biotransformation is also dependent on disease status. For example, significantly greater sulfation of resveratrol occurs in human breast tumor tissue than in adjacent nonmalignant tissue. The observed differences, however, do not correlate with the expression of sulfotransferases responsible for catalyzing resveratrol sulfation, but rather with significantly higher steroid sulfatase mRNA levels. The in vitro activity of resveratrol sulfates may not necessarily reflect their in vivo function, given the fact that ubiquitously existing human sulfatases can convert the metabolites back to active resveratrol in humans.

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“…Furthermore, EDCs can act through feedback mechanisms that can result in up-or down-regulation of aromatase activity while they do not necessarily interact directly with the enzyme. For example, if an EDC disrupts the metabolism of estradiol and results in changes in estradiol levels, aromatase activity might also be affected by an organism's attempt to maintain E2 homeostasis by regulating its production (Ung and Nager 2009).…”

Section: Introductionmentioning

confidence: 99%