中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Rapid Screening for alpha-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration-HPLC-MS

文献类型:期刊论文

作者Chen, Guilin2,3; Guo, Mingquan1,3
刊名FRONTIERS IN PHARMACOLOGY
出版日期2017-04-27
卷号8页码:8
关键词Gymnema sylvestre gymnemic acid alpha-glucosidase UF-HPLC-MS high-throughput screening
ISSN号1663-9812
DOI10.3389/fphar.2017.00228
英文摘要Gymnema sylvestre R. Br. (Asclepiadaceae) has been known to posses potential anti-diabetic activity, and the gymnemic acids were reported as the main bioactive components in this plant species. However, the specific components responsible for the hypoglycemic effect still remain unknown. In the present study, the in vitro study revealed that the extract of G. sylvestre exhibited significant inhibitory activity against alpha-glucosidase with IC50 at 68.70 +/- 1.22 mu g/mL compared to acarbose (positive control) at 59.03 +/- 2.30 it,g/mL, which further indicated the potential anti-diabetic activity. To this end, a method based on affinity ultrafiltration coupled with liquid chromatography mass spectrometry (UF-HPLC-MS) was established to rapidly screen and identify the alpha-glucosidase inhibitors from G. sylvestre. In this way, 9 compounds with higher enrichment factors (EFs) were identified according to their MS/MS spectra. Finally, the structure-activity relationships revealed that glycosylation could decrease the potential antisweet activity of sapogenins, and other components except gymnemic acids in G. sylvestre could also be good alpha-glucosidase inhibitors due to their synergistic effects. Taken together, the proposed method combing (x-glucosidase and UF-HPLC-MS presents high efficiency for rapidly screening and identifying potential inhibitors of alpha-glucosidase from complex natural products, and could be further explored as a valuable high-throughput screening (HTS) platform in the early anti-diabetic drug discovery stage.
资助项目Natural science foundation of China[81673580] ; Chinese Academy of Sciences[29Y429291a0129]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000400242900001
出版者FRONTIERS MEDIA SA
源URL[http://202.127.146.157/handle/2RYDP1HH/1386]  
专题中国科学院武汉植物园
通讯作者Guo, Mingquan
作者单位1.Chinese Acad Sci, Sinoafrica Joint Res Ctr, Wuhan, Peoples R China
2.Chinese Acad Sci, Grad Univ, Wuhan, Peoples R China
3.Chinese Acad Sci, Wuhan Bot Garden, Key Lab Plant Germplasm Enhancement & Specialty A, Wuhan, Peoples R China
推荐引用方式
GB/T 7714
Chen, Guilin,Guo, Mingquan. Rapid Screening for alpha-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration-HPLC-MS[J]. FRONTIERS IN PHARMACOLOGY,2017,8:8.
APA Chen, Guilin,&Guo, Mingquan.(2017).Rapid Screening for alpha-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration-HPLC-MS.FRONTIERS IN PHARMACOLOGY,8,8.
MLA Chen, Guilin,et al."Rapid Screening for alpha-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration-HPLC-MS".FRONTIERS IN PHARMACOLOGY 8(2017):8.

入库方式: OAI收割

来源:武汉植物园

浏览0
下载0
收藏0
其他版本

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。