莪术醇的结构修饰研究进展.PDFVIP

现代药物与临床 Drugs Clinic 第 33 卷 第 9 期 2018 年 9 月 ·2461 · • 综 述 • 莪术醇的结构修饰研究进展 1 1 1 2 2 1* 王文倩 ，路宝庭 ，崔艳丽 ，王 义 ，田 瑜 ，陈常青 1. 天津药物研究院，天津 300193 2. 中国医学科学院 中国协和医科大学 北京药用植物研究所，北京 100193 摘 要：莪术醇是莪术挥发油中的重要活性成分，属于倍半萜类化合物，具有抗肿瘤、抗病毒、抗炎、抗早孕等广泛的生物 活性，尤其以抗肿瘤作用表现突出，临床应用广泛。但由于其独特的五元并七元环化学结构，药物溶解性较差，生物利用度 不高，为了改善其物理性质，提高作用强度，通过化学合成和微生物合成途径，广泛的对其开展结构修饰与衍生物合成研究。 对莪术醇的结构修饰研究情况进行综述，以期为新的抗肿瘤药物的研发提供参考。 关键词：莪术醇；抗肿瘤；结构修饰；倍半萜类 中图分类号：R913 文献标志码：A 文章编号：1674 - 5515(2018)09 - 2461 - 05 DOI: 10.7501/j.issn.1674-5515.2018.09.066 Research progress on structural modification of curcumol 1 1 1 2 2 1 WANG Wen-qian , LU Bao-ting , CUI Yan-li , WANG Yi , TIAN Yu , CHEN Chang-qing 1. Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China 2. Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China Abstract: Curcumol is an important active ingredients in the volatile oil of Curcumae Rhizoma. Curcumol is a compound of sesquitterpenes, which has a wide range of biological activities such as anti-tumor, anti-virus, anti-inflammation, and anti-early pregnancy. Especially in antitumor action, it has been widely applicated in clinic. However, due to its unique five-element and seven-element ring chemical structure, drug solubility is poor and bioavailability is not high. In order to improve the physical properties and enhance the strength of action, the structural modification and derivative synthesis