Chin Young-Won, Kinghorn A Douglas
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
Mini Rev Org Chem. 2008 Nov 1;5(4):355-364. doi: 10.2174/157019308786242223.
Mangosteen (Garcinia mangostana L., Clusiaceae) is a popular botanical dietary supplement in the United States, where it is used principally as an antioxidant. It is referred to as the "queen of fruits" in Thailand, a country of origin. The major secondary metabolites of mangosteen, the xanthones, exhibit a variety of biological activities including antibacterial, antifungal, antiinflammatory, antioxidant, antiplasmodial, cytotoxic, and potential cancer chemopreventive activities. Moreover, some of the xanthones from mangosteen have been found to influence specific enzyme activities, such as aromatase, HIV-1 protease, inhibitor κB kinase, quinone reductase, sphingomyelinase, topoisomerase and several protein kinases, and they also modulate histamine H(1) and 5-hydroxytryptamine(2A) receptor binding. Several synthetic procedures for active xanthones and their analogs have been conducted to obtain a better insight into structure-activity relationships for this compound class. This short review deals with progress made in the structural characterization of the chemical constituents of mangosteen, as well as the biological activity of pure constituents of this species and synthetic methods for the mangosteen xanthones.
山竹（藤黄科莽吉柿，学名Garcinia mangostana L.）在美国是一种广受欢迎的植物性膳食补充剂，主要用作抗氧化剂。在其原产国泰国，它被誉为“水果皇后”。山竹的主要次生代谢产物——氧杂蒽酮，具有多种生物活性，包括抗菌、抗真菌、抗炎、抗氧化、抗疟原虫、细胞毒性以及潜在的癌症化学预防活性。此外，已发现一些来自山竹的氧杂蒽酮会影响特定酶的活性，如芳香化酶、HIV-1蛋白酶、抑制因子κB激酶、醌还原酶、鞘磷脂酶、拓扑异构酶和几种蛋白激酶，并且它们还能调节组胺H(1)和5-羟色胺(2A)受体结合。已开展了几种活性氧杂蒽酮及其类似物的合成方法研究，以便更好地了解该化合物类别的构效关系。这篇简短综述论述了山竹化学成分结构表征方面取得的进展，以及该物种纯成分的生物活性和山竹氧杂蒽酮的合成方法。
