Wang Ming-Hui, Zhang Kuo-Jun, Gu Qin-Lan, Bi Xiao-Ling, Wang Jin-Xin
Key Laboratory of Drug Design and Optimization of Jiangsu Province, China Pharmaceutical University, Nanjing 210009, China.
Higher Vocational and Technical College, China Pharmaceutical University, Nanjing 210009, China.
Chin J Nat Med. 2017 Feb;15(2):81-93. doi: 10.1016/S1875-5364(17)30024-9.
Mangosteen (Garcinia mangostana Linn.) is a well-known tropical tree indigenous to Southeast Asia. Its fruit's pericarp abounds with a class of isoprenylated xanthones which are referred as mangostins. Numerous in vitro and in vivo studies have shown that mangostins and their derivatives possess diverse pharmacological activities, such as antibacterial, antifungal, antimalarial, anticarcinogenic, antiatherogenic activities as well as neuroprotective properties in Alzheimer's disease (AD). This review article provides a comprehensive review of the pharmacological activities of mangostins and their derivatives to reveal their promising utilities in the treatment of certain important diseases, mainly focusing on the discussions of the underlying molecular targets/pathways, modes of action, and relevant structure-activity relationships (SARs). Meanwhile, the pharmacokinetics (PK) profile and recent toxicological studies of mangostins are also described for further druggability exploration in the future.
山竹（Garcinia mangostana Linn.）是一种著名的热带树木，原产于东南亚。其果实的果皮富含一类异戊烯基黄酮，称为α-倒捻子素。大量的体外和体内研究表明，α-倒捻子素及其衍生物具有多种药理活性，如抗菌、抗真菌、抗疟疾、抗癌、抗动脉粥样硬化活性以及在阿尔茨海默病（AD）中的神经保护特性。这篇综述文章全面回顾了α-倒捻子素及其衍生物的药理活性，以揭示它们在治疗某些重要疾病方面的潜在用途，主要集中在对潜在分子靶点/途径、作用模式和相关构效关系（SARs）的讨论上。同时，还描述了α-倒捻子素的药代动力学（PK）概况和近期毒理学研究，以便未来进一步探索其成药潜力。
