Structural Diversity and Structure-Activity Relationship-New Drug Research and Development of Tripterygium wilfordii Hook. f. | |
Li Zheng; Li Yuanchao | |
刊名 | PROGRESS IN CHEMISTRY |
2009-12 | |
卷号 | 21期号:12页码:2483-2491 |
关键词 | triptolide structure modification structure-activity relationship (SAR) |
ISSN号 | 1005-281X |
文献子类 | Article |
英文摘要 | Tripterygium wilfordii Hook. f. (TWHF alpha), commonly known as Lei Gong Teng (Thunder God Vine), is a vine used in traditional Chinese herbal medicine. Triptolide, the major component responsible for the clinical properties of TWHF, is characterized as an abeo-abietane-typed diterpenoid with a unique triepoxide structure and alpha, beta-unsaturated-5-membered lactone. Right after its isolation, triptolide is shown to possess a broad spectrum of pharmacological activities including anticancer, anti-fertility besides its remarkable anti-inflammatory and immunosuppressive activities, which led to extensive studies. Through the modification of different functional groups in triptolide, including the C14-hydroxyl group, C12 beta, C13 beta-epoxy group, alpha, beta-unsaturated-5-membered-lactone ring, C7 beta, C8 beta-epoxy group, C5, C6- position, and three epoxy ring-opening transformation etc., a series of derivatives are synthesized and their related pharmacological activities are tested. Some preliminary structure-activity relationship (SAR) characteristics are summarized from the pharmacological test results. With the accumulation and deepening of chemical and biological study of 1, its SAR will be clearer. Low toxicity, high activity, and wide therapeutic window derivatives of 1 will definitely make 1 a broad application prospect in many fields. |
WOS关键词 | TRIPTOLIDE ; ANALOGS |
WOS研究方向 | Chemistry |
语种 | 中文 |
CSCD记录号 | CSCD:3774071 |
出版者 | CHINESE ACAD SCIENCES |
WOS记录号 | WOS:000273314100001 |
内容类型 | 期刊论文 |
源URL | [http://119.78.100.183/handle/2S10ELR8/279080] |
专题 | 药物化学研究室 |
通讯作者 | Li Yuanchao |
作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
推荐引用方式 GB/T 7714 | Li Zheng,Li Yuanchao. Structural Diversity and Structure-Activity Relationship-New Drug Research and Development of Tripterygium wilfordii Hook. f.[J]. PROGRESS IN CHEMISTRY,2009,21(12):2483-2491. |
APA | Li Zheng,&Li Yuanchao.(2009).Structural Diversity and Structure-Activity Relationship-New Drug Research and Development of Tripterygium wilfordii Hook. f..PROGRESS IN CHEMISTRY,21(12),2483-2491. |
MLA | Li Zheng,et al."Structural Diversity and Structure-Activity Relationship-New Drug Research and Development of Tripterygium wilfordii Hook. f.".PROGRESS IN CHEMISTRY 21.12(2009):2483-2491. |
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