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川西獐牙菜中的酮类化合物及其对α-糖苷酶的抑制活性。

Xanthones from Swertia mussotii and their α-glycosidase inhibitory activities.

机构信息

Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou, P. R. China.

State key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P. R. China.

出版信息

Planta Med. 2014 Feb;80(2-3):201-8. doi: 10.1055/s-0033-1360173. Epub 2013 Dec 19.

Abstract

Two new xanthones, 1,8-dihydroxy-3-methoxyxanthone 7-O-[α-L-rhamnopyranosyl(1 → 2)-β-D-glucopyranoside] (1) and 1,8- dihydroxy-3-methoxyxanthone 7-O-[α-L-rhamnopyranosyl(1 → 3)-α-L-rhamno-pyranosyl (1 → 2)-β-D-xylopyranoside] (2), together with 26 known xanthones (3-28), were isolated from the aqueous ethanol extract of the traditional Chinese herb Swertia mussotii. Their structures were elucidated via spectroscopic analyses including 2D NMR. The inhibition of α-glucosidase by the isolated xanthones was evaluated by an in vitro high-throughput screening assay. Our results indicated that 1,3,5,8-tetrahydroxyxanthone is the best inhibitor with an IC50 value of 5.33 ± 0.09 µM, while the O-glycosylated xanthones were poor α-glycosidase inhibitors.

摘要

从中国传统草药川西獐牙菜的水乙醇提取物中分离得到了两种新的紫檀烷酮,1,8-二羟基-3-甲氧基紫檀烷酮 7-O-[α-L-鼠李吡喃糖基(1→2)-β-D-吡喃葡萄糖苷] (1) 和 1,8-二羟基-3-甲氧基紫檀烷酮 7-O-[α-L-鼠李吡喃糖基(1→3)-α-L-鼠李吡喃糖基(1→2)-β-D-木吡喃糖苷] (2),以及 26 种已知的紫檀烷酮 (3-28)。通过包括 2D NMR 在内的光谱分析确定了它们的结构。通过体外高通量筛选测定了分离得到的紫檀烷酮对α-葡萄糖苷酶的抑制作用。结果表明,1,3,5,8-四羟基紫檀烷酮是最好的抑制剂,IC50 值为 5.33±0.09 μM,而 O-糖苷化紫檀烷酮对α-葡萄糖苷酶的抑制作用较差。

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