Synthesis of novel triterpenoid (lupeol) derivatives and their in vivo antihyperglycemic and antidyslipidemic activity

The triterpenoid, lupeol (1) has been isolated from the leaves extract of Aegle marmelos. Few novel derivatives (2-13) were synthesized from the naturally occurring lupeol (1) and screened for their antihyperglycemic activity (2-11) and antidyslipidemic activity (2-4 and 12-13). The derivative 4 lowered the blood glucose levels by 18.2% and 25.0% at 5 h and 24 h, respectively, in sucrose challenged streptozotocin induced diabetic rats (STZ-S) model at the dose of 100 mg/kg body weight. The compound 4 also significantly lowered 40% (P <0.001) in triglycerides, 30% (P <0.05) in glycerol, 24% (P <0.05) in cholesterol quantity and also improved the HDL-cholesterol by 5% in dyslipidemic hamster model at the dose of 50 mg/kg b.wt. (C) 2009 Elsevier Ltd. All rights reserved.