Lai Jia-Zhuo, Zhang Meng-Han, Wu Yang-Chang, Zhang Da-Yong, Wu Xiao-Ming, Hua Wei-Yi
Center of Drug Discovery, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, PR. China.
Mini Rev Med Chem. 2017;17(4):380-397. doi: 10.2174/1389557516666160923130814.
Extracted from Euphorbia, ent-Abietane lactones can be classified into several categories, such as Jolkinolides and Helioscopinolides, according to their structural features. The study of ent- Abietane lactones could date back to 1972, when Jolkinolide A and B were first isolated from Euphorbia jolkini Boiss. Since then, many other ent-Abietane lactones have been extracted from different species of Euphorbia. Their bio-activities include anti-tumor activity, anti-inflammatory activity as well as anti-bacterial activity. Among them, derivatives of Jolkinolide B draw the most attention for their high anti-tumor activity. There are many studies focus on the syntheses of Jolkinolides. In 1989, the first and efficient synthesis of Jolkinolides was accomplished by Katsumura et al. Their strategy to construct the last ring of Jolkinolides contributes a lot to the following studies. In the following thirty years, there are also other semi-syntheses of Jolkinolides conducted, basing on different starting materials. In this review, we will give a brief clarification of ent-Abietane lactones, as well as their bio-activities and syntheses.
从大戟属植物中提取的对映-贝壳杉烷型内酯，根据其结构特征可分为几类，如乔柯内酯类和日光旋覆花内酯类。对映-贝壳杉烷型内酯的研究可追溯到1972年，当时乔柯内酯A和B首次从九芎大戟中分离出来。从那时起，许多其他对映-贝壳杉烷型内酯已从不同种类的大戟属植物中提取出来。它们的生物活性包括抗肿瘤活性、抗炎活性以及抗菌活性。其中，乔柯内酯B的衍生物因其高抗肿瘤活性而备受关注。有许多研究聚焦于乔柯内酯的合成。1989年，Katsumura等人首次完成了高效合成乔柯内酯的工作。他们构建乔柯内酯最后一环的策略对后续研究有很大贡献。在接下来的三十年里，也基于不同的起始原料进行了其他乔柯内酯的半合成。在这篇综述中，我们将简要阐述对映-贝壳杉烷型内酯及其生物活性和合成方法。
