来自山竹树皮的抗糖尿病氧杂蒽酮类化合物。

Anti-diabetic xanthones from the bark of Garcinia xanthochymus.

作者信息

Nguyen Chi N, Trinh Binh T D, Tran Toan B, Nguyen Le-Thu T, Jäger Anna K, Nguyen Lien-Hoa D

机构信息

Natural Product and Medicinal Chemistry Lab, Faculty of Chemistry, VNUHCM-University of Science, 227 Nguyen Van Cu, Ho Chi Minh City, Viet Nam.

Natural Product and Medicinal Chemistry Lab, Faculty of Chemistry, VNUHCM-University of Science, 227 Nguyen Van Cu, Ho Chi Minh City, Viet Nam; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.

出版信息

Bioorg Med Chem Lett. 2017 Aug 1;27(15):3301-3304. doi: 10.1016/j.bmcl.2017.06.021. Epub 2017 Jun 8.

DOI:10.1016/j.bmcl.2017.06.021

PMID:28624142

Abstract

An ethyl acetate extract the bark of Garcinia xanthochymus exhibited strong inhibition towards α-glucosidase and PTP1B with IC values of 0.3±0.1μg/mL and 2.3±0.4μg/mL, respectively. Chemical constituents of the extract were therefore examined, and two new compounds, xanthochymusxanthones A (1) and B (2), along with ten known xanthones (3-12), were isolated. Their structures were determined using spectroscopic methods, mainly 1D and 2D NMR. Inhibitory activity of the isolated compounds was then tested, and subelliptenone F (12) showed significant effect towards α-glucosidase with IC value of 4.1±0.3μM (compared with acarbose, IC=900.0±3.0μM) whilst xanthochymusxanthone B (2) exhibited remarkable activity towards PTP1B with IC value of 8.0±0.6μM (compared with RK682, IC=4.4±0.3μM).

摘要

藤黄果树皮的乙酸乙酯提取物对α-葡萄糖苷酶和蛋白酪氨酸磷酸酶1B（PTP1B）表现出强烈抑制作用，其IC值分别为0.3±0.1μg/mL和2.3±0.4μg/mL。因此，对该提取物的化学成分进行了研究，分离出两种新化合物，藤黄果氧杂蒽酮A（1）和B（2），以及十种已知的氧杂蒽酮（3 - 12）。使用光谱方法，主要是一维和二维核磁共振确定了它们的结构。然后测试了分离出的化合物的抑制活性，亚椭圆酮F（12）对α-葡萄糖苷酶显示出显著作用，IC值为4.1±0.3μM（与阿卡波糖相比，IC = 900.0±3.0μM），而藤黄果氧杂蒽酮B（2）对PTP1B表现出显著活性，IC值为8.