title: Phenolic Compounds from Clinopodium chinense (Benth.) O. Kuntze and Their Inhibitory Effects on α-Glucosidase and Vascular Endothelial Cells Injury.
abstract: Following an in vitro bioactivity-guided fractionation procedure, 14 compounds including eight flavonoids and six phenylpropanoids were isolated and identified from the AcOEt fraction of Clinopodium chinense (Benth.) O. Kuntze. All constituents were tested for α-glucosidase and high glucose-induced injury in human umbilical vein endothelial cells (HUVECs) inhibitory activities. All constituents exhibited varying degrees α-glucosidase inhibitory activity and protective activity on HUVECs. Among them, luteolin (2), eriodictyol (5), ethyl rosmarinate (13), and clinopodic acids B (14) were proved to be potent α-glucosidase inhibitors with IC50 value ranging from 0.6 to 2.0 μm. Additionally, luteolin (2), naringenin (4), eriodictyol (5), ethyl (2R)-3-(3, 4-dihydroxyphenyl)-2-hydroxypropanate (9), caffeic acid (11), ethyl rosmarinate (13), and clinopodic acids B (14) significantly ameliorate HUVECs injury induced by high glucose with an approximate EC50 value of 3 - 36 μm. These results suggest that the 14 bioactive constituents were responsible for hypoglycemic and protective vascular endothelium effect of C. chinense (Benth.) O. Kuntze and their structure-activity relationship was also analyzed briefly. Eriodictyol, luteolin, ethyl rosmarinate, and clinopodic acids B were the potential lead compounds of antidiabetic drugs.
authors.affiliation: School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Jiangning District, Nanjing, 211198, P. R. China.
authors.forename: Biao
authors.initials: B
authors.lastname: Zeng
authors.affiliation: School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Jiangning District, Nanjing, 211198, P. R. China.
authors.forename: Kai
authors.initials: K
authors.lastname: Chen
authors.affiliation: Department of Pharmacy, Jiangsu Provincial Chinese Medicine Hospital, Nanjing, 210029, P. R. China.
authors.forename: Ping
authors.initials: P
authors.lastname: Du
authors.affiliation: School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Jiangning District, Nanjing, 211198, P. R. China.
authors.forename: Shan-Shan
authors.initials: SS
authors.lastname: Wang
authors.affiliation: School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Jiangning District, Nanjing, 211198, P. R. China.
authors.forename: Bei
authors.initials: B
authors.lastname: Ren
authors.affiliation: School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Jiangning District, Nanjing, 211198, P. R. China.
authors.forename: Yan-Li
authors.initials: YL
authors.lastname: Ren
authors.affiliation: School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Jiangning District, Nanjing, 211198, P. R. China.
authors.forename: Hang-Song
authors.initials: HS
authors.lastname: Yan
authors.affiliation: Nanjing Sanhome Pharmaceutical Co., Ltd., No. 222 Zhujiang Road, Nanjing, 210018, P. R. China. yanl66@sina.cn.
authors.forename: Yan
authors.initials: Y
authors.lastname: Liang
authors.affiliation: School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Jiangning District, Nanjing, 211198, P. R. China. fhwu2000@sina.com.
authors.forename: Fei-Hua
authors.initials: FH
authors.lastname: Wu
mesh_terms: D004305:Dose-Response Relationship, Drug; D005947:Glucose / Q000494:pharmacology; D065089:Glycoside Hydrolase Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D061307:Human Umbilical Vein Endothelial Cells / Q000187:drug effects* / Q000473:pathology; D006801:Humans; D019686:Lamiaceae / Q000737:chemistry*; D015394:Molecular Structure; D010636:Phenols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D000520:alpha-Glucosidases / Q000378:metabolism*
chemical_list: D065089:Glycoside Hydrolase Inhibitors; D010636:Phenols; D000520:alpha-Glucosidases; D005947:Glucose
keywords: Clinopodium chinense; Flavonoids; Phenylpropanoids; Protective effect on endothelial cells; α-Glucosidase inhibitor