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化学进展 2013, Vol. 25 Issue (09): 1553-1574 DOI: 10.7536/PC130729 前一篇   后一篇

• 癌症化学预防专辑 •

天然产物用于癌症化学预防的口服生物利用度问题

郜嵩1, Sumit Basu1, 杨广义1,2, Arijita Deb3, 胡明*1   

  1. 1. Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, The University ofHouston, 1441 Moursund Street, Houston, TX, 77030, USA;
    2. 太和医院 湖北医药学院附属医院 十堰420000;
    3. Department of Pharmaceutical Technology, Jadavpur University, Raja S C Mullick Road, Kolkata700032, India
  • 收稿日期:2013-05-21 出版日期:2013-09-25 发布日期:2013-07-31
  • 通讯作者: 胡明 E-mail:mhu@uy.edu
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Oral Bioavailability Challenges of Natural Products Used in Cancer Chemoprevention

Song Gao1, Sumit Basu1, Guangyi Yang1,2, Arijita Deb3, Ming Hu*1   

  1. 1. Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, The University of Houston, 1441 Moursund Street, Houston, TX, 77030, USA;
    2. Taihe Hospital, Affiliated with Hubei University of Medicine, 32 Remin South Road, Shiyan 420000, China;
    3. Department of Pharmaceutical Technology, Jadavpur University, Raja S C Mullick Road, Kolkata 700032, India
  • Received:2013-05-21 Online:2013-09-25 Published:2013-07-31

由于其低毒和易得的特点,天然产物被认为具有成为化学预防药物的巨大潜力。然而,口服生物利用度差的问题限制了许多天然产物在体内发挥其生物效应。本文综述了影响几类重要的化学预防天然产物生物利用度的因素,这些天然产物包括白藜芦醇、姜黄素、黄连素、染料木素、槲皮素、葱蒜属化合物、人参皂甙化合物K 等。最新研究数据表明,尽管化学和微生物稳定性也在其中发挥作用,细胞膜透过率、溶解性和代谢是限制天然产物口服生物利用度的主要因素。今后相关研究的一个重要方向是进一步优化天然产物的口服生物利用度,并实现其体内的化学预防和治疗效果。

关键词： 口服生物利用度, 天然产物, 癌症化学预防

Natural products hold great promises for being developed into chemopreventive drugs due to their low toxicity and high accessibility. However, poor oral bioavailability limits the biological effects of many natural products in vivo. This paper reviews the factors that affect the bioavailability of several classes of important chemopreventive natural products including resveratrol, curcumin, berberine, genistein, quercetin, allium compound, and ginsenoside compound K. The up-to-date research data suggested that membrane permeability, solubility, and metabolism are the primary factors that limit the oral bioavailability of these natural products although chemical and microbial stability may also contribute to the problem. An important direction for future investigation is to further optimize the oral bioavailabilities of these natural products and realize their chemopreventive and chemotherapeutic effects in vivo.

Key words: oral bioavailability, natural products, chemoprevention

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