Antihyperglycemic and antidyslipidemic agent from Aegle marmelos

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• 作者：T. Narender ; S. Shweta ; P. Tiwari ; K. Papi Reddy ; T. Khaliq ; P. Prathipati ; A. Puri ; A.K. Srivastava ; R. Ch ; er ; S.C. Agarwal ; et al.
• 关键词：Aegeline ; Aegle marmelos ; Antihyperglycemic activity ; Antidyslipidemic activity ; β ; ₃-AR agonist activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：15 March 2007
• 年：2007
• 卷：17
• 期：6
• 页码：1808-1811
• 全文大小：216 K

文摘

The plant Aegle marmelos belongs to the family of Rutaceae. From the leaves of A. marmelos an alkaloidal-amide, Aegeline 2, was isolated and found to have antihyperglycemic activity as evidenced by lowering the blood glucose levels by 12.9 % and 16.9 % at 5 and 24 h, respectively, in sucrose challenged streptozotocin induced diabetic rats (STZ-S) model at the dose of 100 mg/kg body weight. Aegeline 2 has also significantly decreased the plasma triglyceride (Tg) levels by 55 % (P < 0.001), total cholesterol (TC) by 24 % (P < 0.05), and free fatty acids (FFA) by 24 % , accompanied with increase in HDL-C by 28 % and HDL-C/TC ratio by 66 % in dyslipidemic hamster model at the dose of 50 mg/kg body weight. The reasonable mapping of compound 2 to validated pharmacophoric hypothesis and 3D QSAR model with an estimated activity (283 nM) suggest that the compound 2 might be a β₃-AR agonist.