Green Tea Polyphenols in drug discovery - a success or failure?

Green Tea Polyphenols in drug discovery - a success or failure?
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DOI:
10.1517/17460441.2011.570750
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发表时间:
2011-06
影响因子:
6.3
通讯作者:
Smith TJ
Smith TJ
中科院分区:
医学2区
文献类型:
--
作者:
Smith TJ

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绿色茶是由未经发酵的茶树干叶制成的,数千年来一直被人类食用。几乎同样长的时间,它一直被用作一种民间疗法,用于治疗各种疾病。最近,大量的体外和体内科学研究支持了这一古老的论点,即来自绿色茶的多酚可以提供许多健康益处。由于这些化合物对人类消费是安全的,并且在食品供应中无处不在,因此它们作为药物发现计划的先导化合物非常有吸引力。然而,作为药物,它们远非最佳。它们相对不稳定,吸收差,并且容易通过肠道微生物群和人类酶进行许多代谢转化。此外,由于这些化合物靶向广泛的生物系统,体内测试相当困难,因为需要仔细消除对替代途径的影响。这篇综述的目的是讨论一些挑战和好处,追求这个家庭的化合物的药物发现。
Green tea is made from unfermented dried leaves from Camellia sinensis and has been consumed by humans for thousands of years. For nearly as long, it has been used as a folk remedy for a wide array of diseases. More recently, a large number of in-vitro and in-vivo scientific studies have supported this ancient contention that the polyphenols from green tea can provide a number of health benefits. Since these compounds are clearly safe for human consumption and ubiquitous in the food supply, they are highly attractive as lead compounds for drug discovery programs. However, as drugs, they are far from optimum. They are relatively unstable, poorly absorbed, and readily undergo a number of metabolic transformations by intestinal microbiota and human enzymes. Further, since these compounds target a wide array of biological systems, in-vivo testing is rather difficult since effects on alternative pathways need to be carefully eliminated. The purpose of this review is to discuss some of the challenges and benefits of pursuing this family of compounds for drug discovery.
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