天然产物研究与开发 ›› 2020, Vol. 32 ›› Issue (8): 1357-1362.doi: 10.16333/j.1001-6880.2020.8.011

• 研究简报 • 上一篇    下一篇

藏药材诃子中3种α-葡萄糖苷酶抑制剂的分离与鉴定

马家麟，陈涛，谭亮，王环，李玉林*


  

  1. 中国科学院西北高原生物研究所 中国科学院三江源国家公园研究院，西宁 810008

  • 出版日期:2020-08-28 发布日期:2020-09-02
  • 基金资助:
    青海省科技基础条件平台建设项目（2020-ZJ-T02）;青海省重点研发与转化计划（2019-SF-123）;中国科学院兰州区域中心自主知识课题（lz201904）

Isolation and identification of three α-glucosidase inhibitors from Terminalia chebula Retz.

MA Jia-lin,CHEN Tao,TAN Liang,WANG Huan,LI Yu-lin*#br#

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  1. Northwest Institute of Plateau Biology,Chinese Academy of Sciences,Ecological Protection and Adaptive Management Academic Seminar of Three-River-Sourse National Park,Xining 810008,China

  • Online:2020-08-28 Published:2020-09-02

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摘要：

通过超滤-高效液相色谱法筛选诃子提取物中具有α-葡萄糖苷酶抑制活性的化合物，采用大孔吸附树脂和半制备高效液相色谱对其进行富集和分离制备，1H NMR和13C NMR鉴定其化学结构，最后采用以4-硝基酚-α-D-吡喃葡萄糖苷（pNPG）为底物的酶抑制剂筛选模型检测目标化合物的活性。结果显示：诃子提取物中含有的3个主要成分具有潜在的α-葡萄糖苷酶抑制活性；经筛选，AB-8大孔树脂对目标化合物富集效果最好，富集后目标化合物的峰面积比分别达到29.6%、40.3%和21.9%；由半制备高效液相色谱对目标化合物进一步纯化后，得到纯度分别为96.6%、98.1%和96.4%的化合物1（27 mg）、2（35 mg）和3（22 mg）；经1H NMR和13C NMR鉴定得出3个化合物分别为诃黎勒酸、诃子酸、鞣花酸；活性测试结果表明，3个化合物均具有良好的α-葡萄糖苷酶抑制作用，其中诃黎勒酸（IC50=39.2±0.7 mg/L）和诃子酸（IC50=35.8±0.4 mg/L）抑制活性大于阳性对照阿卡波糖（IC50=41.2±0.6 mg/L）。本试验为开发诃子中的α-葡萄糖苷酶抑制剂提供了科学依据。

关键词: 诃子, α-葡萄糖苷酶抑制剂, 超滤-高效液相色谱, 分离, 鉴定

Abstract:

In this study,the compounds with α-glucosidase inhibitory activity in the extract from Terminalia chebula were screened by ultrafiltration-HPLC,in addition,macroporous resin (MR) combined with semi-preparative HPLC were used to isolate the target compounds.The inhibitory effect of the compounds on α-glucosidase was determined by using 4-nortiphenyl-α-D-glucopyranoside (pNPG) as a substrate.The results showed that three components from T. chebula had potential α-glucosidase inhibitory activities.It was found that AB-8 resin showed a ideal purifying profile,the peak area ratios of the target compounds raised at 29.6%,40.3%,21.9% respectively.After further purification by semi-preparative HPLC,compound 1(27 mg),2(35 mg) and 3(22 mg) with purity of 96.6%,98.1% and 96.4% were obtained.Finally,the three compounds were identified by 1H NMR and 13C NMR spectra as chebulagic acid,chebulinic acid and ellagic acid.The activity screening tests showed that the three compounds had strong α-glucosidase inhibitory activities,chebulagic acid(IC50=39.2±0.7 mg/L)and chebulinic acid(IC50=35.8±0.4 mg/L) showed greater activity than that of acarbose(IC50=41.2±0.6 mg/L).This study provided a scientific basis for the development of α-glucosidase inhibitors in T. chebula .

Key words: Terminalia chebula , Retz.,  , α-glucosidase inhibitor, ultrafiltration HPLC, isolation, identification

中图分类号:  R914.1

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