Pharmacognosy Department, College of Pharmacy, Cairo University, Kasr El-Einy Street, 11562, Cairo, Egypt.
Biomed Pharmacother. 2020 Jul;127:110143. doi: 10.1016/j.biopha.2020.110143. Epub 2020 Apr 24.
As ongoing investigation of Huernia saudi-arabica D.V.Field (Asclepiadaceae), a new steroidal pregnane glycoside (Huernioside A) was isolated from dichloromethane fraction (DCM); it was identified as 3β, 11, 14β, 20(R)-tetrahydroxy-pregna-5,9(11)-diene-3-O-β-D-thevetopyranosyl-(1-4)-β-D-cymaropyranoside(HCP) through analysis of 1D, 2D NMR besides ESI-MS data. The alcoholic extract of the aerial part (ALE), DCM and HCP showed inhibitory potential against pancreatic lipase compared to orilstat. Among the tested samples, the ALE and HCP exhibited a promising pancreatic lipase inhibitory commotion through IC values of 0.61 ± 0.15, 1.23 ± 0.07 mg/ml (equivalent to 88.8 μM), respectively. HCP was prevailed to have a mixed mode of inhibition as exposed by enzyme kinetic studies. Hydrophobic interactions were the major forces involved in ligand enzyme interactions. In contrast, moderate α-glucosidase inhibitory activities were evidenced for ALE and HCP (% inhibition: 24.8 ± 1.8 and 26.6 ± 2.5, respectively) compared to acarbose. This investigation is the first to report on the possible in vitro anti-obesity and anti-diabetic impact of H. saudi-arabica.
作为对胡尔尼亚沙特阿拉伯（夹竹桃科）的持续研究，从二氯甲烷部分（DCM）分离出一种新的甾体孕烷糖苷（Huernioside A）; 通过分析 1D、2D NMR 以及 ESI-MS 数据，它被鉴定为 3β、11、14β、20(R)-四羟基-孕甾-5、9(11)-二烯-3-O-β-D-thevetopyranosyl-(1-4)-β-D-cymaropyranoside（HCP）。与奥利司他相比，地上部分（ALE）、DCM 和 HCP 的醇提取物对胰脂肪酶表现出抑制潜力。在所测试的样品中，ALE 和 HCP 通过 IC 值分别为 0.61±0.15、1.23±0.07mg/ml（相当于 88.8μM），显示出有希望的胰脂肪酶抑制作用。通过酶动力学研究表明，HCP 具有混合抑制模式。疏水相互作用是配体酶相互作用中涉及的主要力。相比之下，ALE 和 HCP 对 α-葡萄糖苷酶表现出适度的抑制活性（抑制率分别为 24.8±1.8 和 26.6±2.5），而阿卡波糖的抑制率为 24.8±1.8。这项研究首次报道了胡尔尼亚沙特阿拉伯可能具有的体外抗肥胖和抗糖尿病作用。
