Department of Chemistry, Zhengzhou University, 100 Science Ave. Zhengzhou, Henan 450001, P. R. China.
Curr Top Med Chem. 2009;9(17):1660-75. doi: 10.2174/156802609789941933.
Lignans are widely distributed in nature. The earliest recorded medicinal use of lignans dated back to over 1000 years ago. Lignan-rich plant products were also active ingredients in Chinese and Japanese folk medicines for the treatment of various diseases. The dried root and stem of this plant are listed in the Chinese pharmacopoeia for the treatment of rheumatoid arthritis, gastric, duodenal ulcers and many other diseases. This review highlights synthetic strategies for the Wuweizisu C analogs and the important pharmacological activities as well as therapeutic findings related to the treatment of HBV and other diseases. Notably a significant and ongoing project on Wuweizisu C and its analogs has led to the discovery and development of two potent derivatives alpha-DDB and BICYCLOL which are currently in clinical trials against HBV, especially in lowering elevated SGPT levels. Further design, synthesis, and evaluation of Wuweizisu C analogs are discussed.
木脂素广泛存在于自然界中。最早有记载的药用木脂素可以追溯到 1000 多年前。富含木脂素的植物产品也是中、日民间药物的有效成分，用于治疗各种疾病。该植物的干燥根和茎被列入中国药典，用于治疗类风湿性关节炎、胃和十二指肠溃疡等多种疾病。本综述重点介绍了 Wuweizisu C 类似物的合成策略，以及与治疗乙型肝炎病毒（HBV）和其他疾病相关的重要药理活性和治疗发现。值得注意的是，Wuweizisu C 及其类似物的一个重要且正在进行的项目导致了两种有效的衍生物 alpha-DDB 和 BICYCLOL 的发现和开发，它们目前正在针对 HBV 的临床试验中，特别是在降低升高的 SGPT 水平方面。还讨论了 Wuweizisu C 类似物的进一步设计、合成和评估。
Zotero 插件