Wang Rubin, Kong John, Wang Dali, Lien Linda Lin-min, Lien Eric Jung-chi
Department of Pharmaceutical Sciences, School of Pharmacy, University of Southern California, 1985 Zonal Avenue, Los Angeles, CA 90089-9121, USA.
Chin Med. 2007 May 10;2:5. doi: 10.1186/1749-8546-2-5.
A literature survey was conducted on herbs, their preparations and ingredients with reported liver protection activities, in which a total of 274 different species and hundreds of active ingredients have been examined. These ingredients can be roughly classified into two categories according to their activities: (1) the main ingredients, such as silybin, osthole, coumarin, glycyrrhizin, saikosaponin A, schisandrin A, flavonoids; and (2) supporting substances, such as sugars, amino acids, resins, tannins and volatile oil. Among them, some active ingredients have hepatoprotective activities (e.g. anti-inflammatory, anticancer, antioxidant, immunomodulating and liver cirrhosis-regulating effects). Calculation of physicochemical parameters indicates that the main ingredients with negative and positive E(lumo) values possibly display their hepatoprotective effects through different mechanisms, such as antioxidative, anti-inflammatory and immunomodulating effects. As the combination of herbs may achieve some treatment effects synergistically and/or additively, it is common in Chinese medicine to use mixtures of various medicinal herbs with pharmacologically active compounds to have synergistic and/or additive effects, or to reduce harmful effects of some pharmacologically active compounds. In particular, the active compounds with Clog P around 2 are suitable for passive transport across membranes and accessible to the target sites. Thus, E(lumo) and Clog P values are good indicators among the calculated parameters. Seven different physicochemical parameters (MW, Clog P, CMR, mu, E(lumo), E(lumo) and H(f)) and four major biological activities (antioxidant, anti-inflammatory, antiviral/antitumor and immunomodulating) are discussed in this review. It is hoped that the discussion may provide some leads in the development of new hepatoprotective drugs.
我们对具有肝脏保护活性的草药、其制剂和成分进行了文献调研,共研究了274种不同的物种和数百种活性成分。这些成分根据其活性大致可分为两类:(1)主要成分,如西利宾、蛇床子素、香豆素、甘草酸、柴胡皂苷A、五味子醇甲、黄酮类化合物;(2)辅助物质,如糖类、氨基酸、树脂、单宁和挥发油。其中,一些活性成分具有肝脏保护活性(如抗炎、抗癌、抗氧化、免疫调节和调节肝硬化的作用)。物理化学参数的计算表明,具有负E(lumo)值和正E(lumo)值的主要成分可能通过不同机制发挥其肝脏保护作用,如抗氧化、抗炎和免疫调节作用。由于草药的组合可能协同和/或相加地产生一些治疗效果,因此在中医中,使用含有药理活性化合物的各种草药混合物以产生协同和/或相加作用,或减少某些药理活性化合物的有害作用是很常见的。特别是,Clog P约为2的活性化合物适合通过被动转运穿过膜并到达靶位点。因此,E(lumo)和Clog P值是计算参数中的良好指标。本文综述了七个不同的物理化学参数(分子量、Clog P、CMR、μ、E(lumo)、E(lumo)和H(f))和四种主要生物活性(抗氧化、抗炎、抗病毒/抗肿瘤和免疫调节)。希望该讨论能为新型肝脏保护药物的开发提供一些线索。