Youssef Fadia S, Ashour Mohamed L, Ebada Sherif S, Sobeh Mansour, El-Beshbishy Hesham A, Singab Abdel Nasser, Wink Michael
Department of Pharmacognosy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, Heidelberg, Germany.
J Pharm Pharmacol. 2017 Jun;69(6):733-742. doi: 10.1111/jphp.12690. Epub 2017 Mar 21.
This study was designed to evaluate the antihyperglycaemic activity of the methanol leaf extract of Eremophila maculata (EMM) both in vitro and in vivo.
The antihyperglycaemic activity was assessed in vitro using differentiated 3T3-L1 adipocytes, whereas in-vivo effect was evaluated in streptozotocin-induced diabetic rats. Chemical profiling of EMM was done using LC-ESI-MS techniques. Molecular modelling experiments of the identified compounds were performed using C-Docker protocol.
Eremophila maculata slightly enhanced cellular glucose uptake and utilization in vitro by 3.92% relative to the untreated control. A stronger in-vivo effect was observed for EMM and its dichloromethane fraction. A pronounced elevation in serum insulin by 88.89 and 66.67%, respectively, accompanied by an apparent decline in fasting blood glucose (FBG) level by 65.60 and 70.37% comparable to streptozotocin-induced diabetic rats was observed. This effect was stronger than that of the reference drug glibenclamide (GLB). Chemical profiling of EMM revealed that leucoseptoside A, verbascoside, syringaresinol-4-O-β-D-glucopyranoside, pinoresinol-4-O-β-D-glucopyranoside and pinoresinol-4-O-[6″-O-(E)-feruloyl]-β-D-glucopyranoside are the major compounds. Molecular modelling showed that martynoside, verbascoside and phillygenin exhibited the highest inhibition to human pancreatic α-amylase (HPA), maltase glucoamylase (MGAM) and aldose reductase (AR), respectively.
Eremophila maculata offers an interesting relatively safer antihyperglycaemic candidate comparable to synthetic analogues.
本研究旨在评估斑纹沙巴拉叶甲醇提取物(EMM)在体外和体内的降血糖活性。
使用分化的3T3-L1脂肪细胞在体外评估降血糖活性,而在链脲佐菌素诱导的糖尿病大鼠中评估体内效果。采用LC-ESI-MS技术对EMM进行化学分析。使用C-Docker协议对鉴定出的化合物进行分子模拟实验。
相对于未处理的对照,斑纹沙巴拉叶在体外使细胞葡萄糖摄取和利用略有增强,提高了3.92%。观察到EMM及其二氯甲烷馏分具有更强的体内作用。与链脲佐菌素诱导的糖尿病大鼠相比,血清胰岛素分别显著升高88.89%和66.67%,同时空腹血糖(FBG)水平明显下降65.60%和70.37%。这种效果比参考药物格列本脲(GLB)更强。EMM的化学分析表明,亮叶黄芩苷A、毛蕊花糖苷、紫丁香树脂醇-4-O-β-D-吡喃葡萄糖苷、松脂醇-4-O-β-D-吡喃葡萄糖苷和松脂醇-4-O-[6″-O-(E)-阿魏酰基]-β-D-吡喃葡萄糖苷是主要化合物。分子模拟表明,马钱苷、毛蕊花糖苷和连翘酯苷分别对人胰腺α-淀粉酶(HPA)、麦芽糖酶糖化酶(MGAM)和醛糖还原酶(AR)表现出最高的抑制作用。
斑纹沙巴拉叶提供了一种有趣的、相对更安全的降血糖候选物,可与合成类似物相媲美。