Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity
Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity
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DOI：
10.1021/np8000255
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发表时间：
2008-07-01
影响因子：
5.1
通讯作者：
Kinghorn, A. Douglas
中科院分区：
文献类型：
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作者：
Balunas, Marcy J.;Su, Bin;Kinghorn, A. Douglas
使用非细胞、基于酶的微粒体芳香酶抑制测定法筛选植物膳食补充剂山竹（藤黄果的果皮）的 12 种呫吨酮成分。在这些化合物中，garcinone D (3)、garcinone E (5)、α-mangostin (8) 和 γ-mangostin (9) 表现出剂量依赖性抑制活性。在使用表达高水平芳香酶的 SK-BR-3 乳腺癌细胞进行的后续细胞测定中，这四种氧杂蒽酮中最有效的是 γ-山竹素 (9)。由于市售的山竹产品中可能会消耗大量的氧杂蒽酮，因此经常摄入山竹植物膳食补充剂的后果。需要进一步研究以确定它们在乳腺癌化学预防中的可能作用。
Twelve xanthone constituents of the botanical dietary supplement mangosteen (the pericarp, of Garcinia mangostana) were screened using a noncellular, enzyme-based microsomal aromatase inhibition assay. Of these compounds, garcinone D (3), garcinone E (5), alpha-mangostin (8), and gamma-mangostin (9) exhibited dose-dependent inhibitory activity. In a follow-up cell-based assay using SK-BR-3 breast cancer cells that express high levels of aromatase, the most potent of these four xanthones was gamma-mangostin (9). Because xanthones may be consumed in substantial amounts from commercially available mangosteen products, the consequences of frequent intake of mangosteen botanical dietary supplements. require further investigation to determine their possible role in breast cancer chemoprevention.