Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
Department of Medicinal Chemistry and State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
Molecules. 2018 Nov 8;23(11):2914. doi: 10.3390/molecules23112914.
Diterpenoids are widely distributed natural products and have caused considerable interest because of their unique skeletons and antibacterial and antitumor activities and so on. In light of recent discoveries, -kaurane diterpenoids, which exhibit a wide variety of biological activities, such as anticancer and anti-inflammatory activities, pose enormous potential to serve as a promising candidate for drug development. Among them, spirolactone-type 6,7---kaurane diterpenoids, with interesting molecular skeleton, complex oxidation patterns, and bond formation, exhibit attractive activities. Furthermore, spirolactone-type diterpenoids have many modifiable sites, which allows for linking to various substituents, suitable for further medicinal study. Hence, some structurally modified derivatives with improved cytotoxicity activities are also achieved. In this review, natural bioactive spirolactone-type diterpenoids and their synthetic derivatives were summarized.
二萜类化合物广泛分布于自然界，由于其独特的骨架结构以及具有抗菌、抗肿瘤等活性而引起了人们的广泛关注。鉴于最近的发现，-贝壳杉烷二萜类化合物具有广泛的生物活性，如抗癌和抗炎活性等，具有巨大的潜力成为药物开发的有前途的候选物。其中，螺内酯型 6,7---贝壳杉烷二萜类化合物具有有趣的分子骨架、复杂的氧化模式和键形成方式，表现出吸引人的活性。此外，螺内酯型二萜类化合物具有许多可修饰的位点，允许与各种取代基连接，适合进一步的药物研究。因此，还实现了一些结构修饰的衍生物，具有提高的细胞毒性活性。在本综述中，总结了天然生物活性螺内酯型二萜类化合物及其合成衍生物。
