Abstract
Genistein, one of the most active natural flavonoids, exerts various biological effects including chemoprevention, antioxidation, antiproliferation and anticancer. More than 30 clinical trials of genistein with various disease indications have been conducted to evaluate its clinical efficacy. Based on many animals and human pharmacokinetic studies, it is well known that the most challenge issue for developing genistein as a chemoprevention agent is the low oral bioavailability, which may be the major reason relating to its ambiguous therapeutic effects and large interindividual variations in clinical trials. In order to better correlate pharmacokinetic to pharmacodynamics results in animals and clinical studies, an in-depth understanding of pharmacokinetic behavior of genistein and its ADME properties are needed. Numerous in vitro/in vivo ADME studies had been conducted to reveal the main factors contributing to the low oral bioavailability of genistein. Therefore, this review focuses on summarizing the most recent progress on mechanistic studies of genistein ADME and provides a systemic view of these processes to explain genistein pharmacokinetic behaviors in vivo. The better understanding of genistein ADME property may lead to development of proper strategy to improve genistein oral bioavailability via mechanism-based approaches.
Keywords: Genistein, Flavonoids, Isoflavone, Bioavailability, Pharmacokinetics, ADME, Metabolism, Transporter, BCRP, estrogen-dependent breast, preneoplastic cells
Anti-Cancer Agents in Medicinal Chemistry
Title:Bioavailability and Pharmacokinetics of Genistein: Mechanistic Studies on its ADME
Volume: 12 Issue: 10
Author(s): Zhen Yang, Kaustubh Kulkarni, Wei Zhu and Ming Hu
Affiliation:
Keywords: Genistein, Flavonoids, Isoflavone, Bioavailability, Pharmacokinetics, ADME, Metabolism, Transporter, BCRP, estrogen-dependent breast, preneoplastic cells
Abstract: Genistein, one of the most active natural flavonoids, exerts various biological effects including chemoprevention, antioxidation, antiproliferation and anticancer. More than 30 clinical trials of genistein with various disease indications have been conducted to evaluate its clinical efficacy. Based on many animals and human pharmacokinetic studies, it is well known that the most challenge issue for developing genistein as a chemoprevention agent is the low oral bioavailability, which may be the major reason relating to its ambiguous therapeutic effects and large interindividual variations in clinical trials. In order to better correlate pharmacokinetic to pharmacodynamics results in animals and clinical studies, an in-depth understanding of pharmacokinetic behavior of genistein and its ADME properties are needed. Numerous in vitro/in vivo ADME studies had been conducted to reveal the main factors contributing to the low oral bioavailability of genistein. Therefore, this review focuses on summarizing the most recent progress on mechanistic studies of genistein ADME and provides a systemic view of these processes to explain genistein pharmacokinetic behaviors in vivo. The better understanding of genistein ADME property may lead to development of proper strategy to improve genistein oral bioavailability via mechanism-based approaches.
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Cite this article as:
Yang Zhen, Kulkarni Kaustubh, Zhu Wei and Hu Ming, Bioavailability and Pharmacokinetics of Genistein: Mechanistic Studies on its ADME, Anti-Cancer Agents in Medicinal Chemistry 2012; 12 (10) . https://dx.doi.org/10.2174/187152012803833107
DOI https://dx.doi.org/10.2174/187152012803833107 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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