Zeng Biao, Chen Kai, Du Ping, Wang Shan-Shan, Ren Bei, Ren Yan-Li, Yan Hang-Song, Liang Yan, Wu Fei-Hua
School of Traditional Chinese Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Jiangning District, Nanjing, 211198, P. R. China.
Department of Pharmacy, Jiangsu Provincial Chinese Medicine Hospital, Nanjing, 210029, P. R. China.
Chem Biodivers. 2016 May;13(5):596-601. doi: 10.1002/cbdv.201500187.
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.
通过体外生物活性导向的分离程序，从风轮菜的乙酸乙酯部位分离并鉴定出14种化合物，包括8种黄酮类化合物和6种苯丙素类化合物。对所有成分进行了α-葡萄糖苷酶和高糖诱导的人脐静脉内皮细胞（HUVECs）损伤抑制活性测试。所有成分均表现出不同程度的α-葡萄糖苷酶抑制活性和对HUVECs的保护活性。其中，木犀草素（2）、圣草酚（5）、迷迭香酸乙酯（13）和风轮菜酸B（14）被证明是有效的α-葡萄糖苷酶抑制剂，IC50值范围为0.6至2.0μm。此外，木犀草素（2）、柚皮素（4）、圣草酚（5）、（2R）-3-（3,4-二羟基苯基）-2-羟基丙酸乙酯（9）、咖啡酸（11）、迷迭香酸乙酯（13）和风轮菜酸B（14）显著改善高糖诱导的HUVECs损伤，近似EC50值为3 - 36μm。这些结果表明，这14种生物活性成分是风轮菜降血糖和保护血管内皮作用的原因，并且还简要分析了它们的构效关系。圣草酚、木犀草素、迷迭香酸乙酯和风轮菜酸B是抗糖尿病药物的潜在先导化合物。
