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具有强胰岛素分泌作用的尼泊尔产獐牙菜中的獐牙菜苦苷。

Potent Insulin Secretagogue from Scoparia dulcis Linn of Nepalese Origin.

机构信息

H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences (ICCBS), University of Karachi, Karachi, 75270, Pakistan.

Central Department of Chemistry, Tribhuvan University, Kirtipur, Kathmandu, Nepal.

出版信息

Phytother Res. 2015 Oct;29(10):1672-5. doi: 10.1002/ptr.5412. Epub 2015 Jul 14.

Abstract

Ethno-botanical inspired isolation from plant Scoparia dulcis Linn. (Sweet Broomweed) yielded six compounds, coixol (1), glutinol (2), glutinone (3), friedelin (4), betulinic acid (5), and tetratriacontan-1-ol (6). There structures were identified using mass and 1D- and 2D-NMR spectroscopy techniques. Compounds 1-6 were evaluated for their insulin secretory activity on isolated mice islets and MIN-6 pancreatic β-cell line, and compounds 1 and 2 were found to be potent and mildly active, respectively. Compound 1 was further evaluated for insulin secretory activity on MIN-6 cells. Compound 1 was subjected to in vitro cytotoxicity assay against MIN-6, 3T3 cell lines, and islet cells, and in vivo acute toxicity test in mice that was found to be non-toxic. The insulin secretory activity of compounds 1 and 2 supported the ethno-botanic uses of S. dulcis as an anti-diabetic agent.

摘要

从植物 Scoparia dulcis Linn.(甜艾菊)中提取的民族植物学启示,得到了六种化合物,分别是 coixol(1)、谷醇(2)、谷甾酮(3)、羽扇豆醇(4)、齐墩果酸(5)和三十烷醇(6)。利用质谱和 1D-和 2D-NMR 波谱技术确定了它们的结构。对化合物 1-6 进行了分离小鼠胰岛和 MIN-6 胰腺β细胞系的胰岛素分泌活性评价,发现化合物 1 和 2 分别具有较强和温和的活性。进一步对化合物 1 在 MIN-6 细胞上的胰岛素分泌活性进行了评价。对化合物 1 进行了体外对 MIN-6、3T3 细胞系和胰岛细胞的细胞毒性试验,以及在小鼠体内的急性毒性试验,结果表明无毒性。化合物 1 和 2 的胰岛素分泌活性支持了 S. dulcis 作为抗糖尿病药物的民族植物学用途。

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