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传统中药五味子具有多种药理活性。20世纪70年代以来,我国临床发现五味子能改善慢性肝炎病人的肝功能异常,在此基础上,我所化学家和药理学家对五味子分离得到的20余种联苯环辛烯类木脂素成分和其药理作用进行了大量研究。五味子的药理活性主要有:保肝,抗氧化,诱导肝药酶,增强解毒功能,促进蛋白质、糖原合成,克服肿瘤耐药性,增强对抗药癌的敏感性以及对中枢神经系统的镇静作用。在这些研究基础上,合成了保肝作用最强的五味子丙素结构类似物,相继研制出两种抗肝炎新药联苯双酯(DDB)和双环醇(bicyclol)。本文对五味子木脂素类成分的结构与药理活性关系以及两种新药的创制做一综述。
Traditional Chinese medicine Schisandra has a variety of pharmacological activities. Since the 1970s, China has found that Chinese schisandra can improve liver function abnormalities in patients with chronic hepatitis. Based on this, more than 20 types of biphenyl cyclooctene lignans isolated by chemists and pharmacologists from our institute have been obtained. The composition and its pharmacological effects have been extensively studied. The pharmacological activities of schisandra include: hepatoprotection, antioxidation, inducing liver drug enzymes, enhancing detoxification function, promoting protein, glycogen synthesis, overcoming tumor resistance, increasing sensitivity to anticancer drugs, and sedating the central nervous system . On the basis of these studies, the structural analogues of schisandrin, which has the strongest hepatoprotective effect, were synthesized, and two novel anti-hepatitis drugs, biphenyl ester (DDB) and bicyclol, were developed in succession. This article reviews the structure and pharmacological activity of lignans and the creation of two new drugs.