Rapid Screening for alpha-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration-HPLC-MS

doi:10.3389/fphar.2017.00228

CORC > 武汉植物园 > 中国科学院武汉植物园

	Rapid Screening for alpha-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration-HPLC-MS
	Chen, Guilin 2,3; Guo, Mingquan 1,3
刊名	FRONTIERS IN PHARMACOLOGY
	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
DOI	10.3389/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
出版者	FRONTIERS MEDIA SA
WOS记录号	WOS:000400242900001
内容类型	期刊论文
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.