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Bioorg Med Chem Lett. 2007 Mar 15;17(6):1808-11. Epub 2006 Dec 15.

Antihyperglycemic and antidyslipidemic agent from Aegle marmelos.

Author information

1
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226 001 (UP), India. tnarender@rediffmail.com

Abstract

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 24h, respectively, in sucrose challenged streptozotocin induced diabetic rats (STZ-S) model at the dose of 100mg/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 50mg/kg body weight. The reasonable mapping of compound 2 to validated pharmacophoric hypothesis and 3D QSAR model with an estimated activity (283nM) suggest that the compound 2 might be a beta(3)-AR agonist.

PMID:
17197179
DOI:
10.1016/j.bmcl.2006.12.037
[Indexed for MEDLINE]

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