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Progress in Chemistry 2009, Vol. 21 Issue (01): 66-76 Previous Articles   Next Articles

• Special issues •

The Structure-Activity Relationship of Dibenzo (a,c) cyclooctene Lignans Isolated from Fructus schizandrae and Innovation of Novel Anti-Hepatitis Drugs

Yu Linghong;Liu Gengtao*   

  1. (Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China)
  • Received: Revised: Online: Published:
  • Contact: Liu Gengtao E-mail:liugt@imm.ac.cn
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Fructus schizandrae (FS) has been used as a corroborative for about two thousands of years in traditional Chinese medicines. In the early 1970’s, Chinese clinicians found that the whole powder and the honey pill of FS improved the abnormal liver function of chronic viral hepatitis. Following this clinical lead, the chemistry and pharmacology of FS are systematically studied in author's institute. Twenty dibenzo (a, c) cyclooctene lignans are isolated from different species of FS. The lignans have multiple pharmacological actions, mainly against liver injury, antioxidant, enhancing detoxification function, stimulating protein and glycogen biosynthesis, overcome multidrug resistance of cancer cells to chemotherapy as well as sedation on the central nervous system. Based on the study of the pharmacology and chemistry of FS, two novel anti-hepatitis drugs (DDB and bicyclol) are sequentially created through synthesizing analogues of schizandrin C, the most effective component of FS in anti-liver injury. The pharmacological action of different lignans and the relationship between structure and activity are reviewed in this paper.

Contents
1 Introduction
2 Chemical constituents of Fructus schizandrae (FS)
3 The structure-activity relationship of dibenzo (a,c) cyclooctene Lignans isolated from FS
3.1 Protective action of dibenzocyclooctene lignans isolated from schizandrae against liver injury and its mechanism
3.2 Antioxidant activity of the dibenzocyclooctene lignans isolated from FS
3.3 Protective effect of Sal on ox-LDL induced bovine aortic endothelium damage and oxidative stress induced neurotoxicity
3.4 Enhancing liver detoxification function—induction of the hepatic microsomal cytochrome P450
3.5 Stimulation of protein biosynthesis and glycogenesis in liver
3.6 Inhibitory effect on the central nervous system
3.7 Reversal multi-drug resistance to anti-cancer drugs
3.8 Summary
4 Synthesis of dibenzo (a,c) cyclooctene lignans and derivatives and innovation of novel anti-hepatitis drug
4.1 Innovation of novel DDB as anti-hepatitis drug
4.2 Innovation of second generative anti-hepatitis drug-bicyclol
5 Perspective

Key words: Fructus schizandrae, dibenzo (a,c)cyclooctene lignans, liver injury, hepatitis, bicyclol, anti-oxidative stress

CLC Number: 

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