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采用超滤液相色谱-电喷雾电离多级质谱法筛选黄连提取物中潜在的α-葡萄糖苷酶抑制剂

Screening for potential -α -Glucosidase inhibitors in Coptis chinensis franch extract using ultrafiltration LC-ESI-MSn.

作者信息

Zhou Hui, Jiang Tao, Wang Zhengyang, Ren Shen, Zhao Xi, Wu Wei, Jiang Lianhai, Liu Zhiqiang, Teng Lirong

机构信息

Department of Chemistry and Pharmacy, Zhuhai College of Jilin University, Zhuhai, P.R. China / Changchun Center of Mass Spectrometry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, P.R. China.

Department of Chemistry and Pharmacy, Zhuhai College of Jilin University, Zhuhai, P.R. China.

出版信息

Pak J Pharm Sci. 2014 Nov;27(6 Suppl):2007-12.

Abstract

Naturally existing -α -glucosidase inhibitors from traditional herbal medicines have attracted considerable interest to treat type 2 diabetes mellitus (T2DM). Hundreds of herbs have been reported to have the potential to inhibit -α -glucosidase. However, most common methods to examine the inhibitors of -α -glucosidase are usually time-consuming. In the current study, the screening of -α -glucosidase ligands from Coptis chinensis Franch extract was undertaken by ultrafiltration liquid chromatography coupled to electrospray ionization tandem mass spectrometry (ultrafiltration LC-ESI-MS(n)). Resultantly, the enzyme inhibition studies showed that Coptis chinensis Franch extract carries the strongest -α -glucosidase inhibitory activity among the five kinds of Chinese herbal extracts. Subsequently, five compounds that could bind to -α -glucosidase in the Coptis chinensis Franch extract were found using ultrafiltration liquid chromatography, and their structures were identified by ESI-MS(n) to be coptisine, epiberberine, jatrorrhizine, berberine, palmatine. Cumulatively, these results were anticipated to be encouraging for applying the Coptis chinensis Franch extracts as efficient anti-diabetic drug candidates.

摘要

来自传统草药的天然存在的α-葡萄糖苷酶抑制剂已引起治疗2型糖尿病(T2DM)的广泛关注。据报道,数百种草药具有抑制α-葡萄糖苷酶的潜力。然而,检测α-葡萄糖苷酶抑制剂的最常用方法通常很耗时。在当前研究中,通过超滤液相色谱-电喷雾电离串联质谱联用技术(超滤LC-ESI-MS(n))从黄连提取物中筛选α-葡萄糖苷酶配体。结果,酶抑制研究表明,黄连提取物在五种中草药提取物中具有最强的α-葡萄糖苷酶抑制活性。随后,利用超滤液相色谱法在黄连提取物中发现了五种能与α-葡萄糖苷酶结合的化合物,通过ESI-MS(n)鉴定其结构分别为黄连碱、表小檗碱、药根碱、小檗碱、巴马汀。总的来说,这些结果有望为将黄连提取物作为有效的抗糖尿病候选药物提供鼓舞。

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