Pharmacology and Therapeutics Department, Medical Faculty, Universitas Sumatera Utara, Medan 20155, Indonesia.
Department of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang 11800, Malaysia.
Molecules. 2022 Oct 12;27(20):6814. doi: 10.3390/molecules27206814.
(1) Background: An earlier study on the hypoglycemic activity of S. polyanthum (Wight.) leaf methanol extract identified squalene as the major chemical compound. The present study was conducted to assess the hypoglycemic effect of fractions and subfractions of the methanol extract of S. polyanthum compared to the squalene using a bioassay-guided in vivo study. (2) Methods: The methanol extract was fractionated using the liquid−liquid fractionation method. Streptozotocin-induced type 1 diabetic rat was used to study the hypoglycemic effect. (3) Results: The findings showed that chloroform fraction significantly (p < 0.05) lowered blood glucose levels of diabetic rats as compared to the control. Further fractionation of chloroform fraction yielded subfraction-1 and -2, whereby subfraction-1 exhibited a higher blood-glucose-lowering effect. The lipid profile test showed that the total cholesterol level of subfraction-1 and squalene-treated groups decreased significantly (p < 0.05). An immunohistochemistry study revealed that none of the treatments regenerated pancreatic β-cells. Gas chromatography−mass spectrophotometer analysis identified the presence of squalene in the active methanol extract, chloroform fraction, and subfraction-1. In silico analysis revealed a higher affinity of squalene against protein receptors that control lipid metabolism than metformin. (4) Conclusions: Data obtained from the present work suggested the crude methanol extract exerted the highest hypoglycemic effect compared to fraction, subfraction, and squalene, confirming synergistic effect may be responsible for the hypoglycemic activity of S. polyanthum.
(1) 背景：先前对 S. polyanthum（Wight.）叶甲醇提取物的降血糖活性的研究表明，角鲨烯是主要的化学化合物。本研究旨在评估 S. polyanthum 甲醇提取物的馏分和亚馏分与角鲨烯相比的降血糖作用，采用生物测定指导的体内研究。
(2) 方法：使用液-液分馏法对甲醇提取物进行分级。采用链脲佐菌素诱导的 1 型糖尿病大鼠研究降血糖作用。
(3) 结果：研究结果表明，与对照组相比，氯仿馏分显著（p<0.05）降低了糖尿病大鼠的血糖水平。进一步对氯仿馏分进行分级得到亚馏分-1 和 -2，其中亚馏分-1 表现出更高的降血糖作用。脂质谱测试显示，亚馏分-1 和角鲨烯处理组的总胆固醇水平显著降低（p<0.05）。免疫组织化学研究表明，没有一种治疗方法可以再生胰岛β细胞。气相色谱-质谱联用分析表明，活性甲醇提取物、氯仿馏分和亚馏分-1 中均存在角鲨烯。计算机模拟分析表明，角鲨烯与控制脂质代谢的蛋白受体的亲和力高于二甲双胍。
(4) 结论：本工作获得的数据表明，与馏分、亚馏分和角鲨烯相比，粗甲醇提取物表现出最高的降血糖作用，证实协同作用可能是 S. polyanthum 降血糖活性的原因。
