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结合HPLC-HRMS-SPE-NMR的高分辨率生物活性分析:来自水香桃木(桃金娘科)的α-葡萄糖苷酶抑制剂和乙酰化鞣花酸鼠李糖苷。

High-resolution bioactivity profiling combined with HPLC-HRMS-SPE-NMR: α-Glucosidase inhibitors and acetylated ellagic acid rhamnosides from Myrcia palustris DC. (Myrtaceae).

作者信息

Wubshet Sileshi G, Moresco Henrique H, Tahtah Yousof, Brighente Inês M C, Staerk Dan

机构信息

Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.

Laboratório de Química de Produtos Naturais, Departamento de Química, Universidade Federal de Santa Catarina, Campus Trindade, Florianópolis, SC 88040-900, Brazil.

出版信息

Phytochemistry. 2015 Aug;116:246-252. doi: 10.1016/j.phytochem.2015.04.004. Epub 2015 Apr 30.

Abstract

Type 2 diabetes (T2D) is an endocrine metabolic disease with a worldwide prevalence of more than 8%, and an expected increase close to 50% in the next 15-20years. T2D is associated with severe and life-threatening complications like retinopathy, neuropathy, nephropathy, and cardiovascular diseases, and therefore improved drug leads or functional foods containing α-glucosidase inhibitors are needed for management of blood glucose. In this study, leaves of Myrcia palustris were investigated by high-resolution α-glucosidase inhibition profiling combined with HPLC-HRMS-SPE-NMR. This led to identification of casuarinin, myricetin 3-O-β-d-(6″-galloyl)galactopyranoside, kaempferol 3-O-β-d-galactopyranoside, myricetin, and quercetin as α-glucosidase inhibitors. In addition, four acetylated ellagic acid rhamnosides, i.e., 4-O-(2″,4″-O-diacetyl-α-l-rhamnopyranosyl)ellagic acid, 4-O-(2″,3″-O-diacetyl-α-l-rhamnopyranosyl)ellagic acid, 4-O-(3″,4″-O-diacetyl-α-l-rhamnopyranosyl)ellagic acid, and 4-O-(2″,3″,4″-O-triacetyl-α-l-rhamnopyranosyl)ellagic acid were identified.

摘要

2型糖尿病(T2D)是一种内分泌代谢疾病,在全球的患病率超过8%,预计在未来15至20年内将增加近50%。T2D与严重且危及生命的并发症相关,如视网膜病变、神经病变、肾病和心血管疾病,因此需要改进的药物先导物或含有α-葡萄糖苷酶抑制剂的功能性食品来控制血糖。在本研究中,通过高分辨率α-葡萄糖苷酶抑制谱分析结合HPLC-HRMS-SPE-NMR对水杨梅叶进行了研究。这导致鉴定出了苏木精、杨梅素3-O-β-d-(6″-没食子酰)吡喃半乳糖苷、山奈酚3-O-β-d-吡喃半乳糖苷、杨梅素和槲皮素作为α-葡萄糖苷酶抑制剂。此外,还鉴定出了四种乙酰化鞣花酸鼠李糖苷,即4-O-(2″,4″-O-二乙酰基-α-l-吡喃鼠李糖基)鞣花酸、4-O-(2″,3″-O-二乙酰基-α-l-吡喃鼠李糖基)鞣花酸、4-O-(3″,4″-O-二乙酰基-α-l-吡喃鼠李糖基)鞣花酸和4-O-(2″,3″,4″-O-三乙酰基-α-l-吡喃鼠李糖基)鞣花酸。

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