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 5h and 24h, respectively, in sucrose challenged streptozotocin induced diabetic rats (STZ-S) model at the dose of 100mg/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 50mg/kg b.wt.
Papi Reddy
K
K
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, UP, India.
Singh
A B
AB
Puri
A
A
Srivastava
A K
AK
Narender
T
T
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001835:Body Weight; D002626:Chemistry, Pharmaceutical / Q000379:methods; D006224:Cricetinae; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy; D015195:Drug Design; D005947:Glucose / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008956:Models, Chemical; D053978:Pentacyclic Triterpenes; D051381:Rats; D013311:Streptozocin; D014280:Triglycerides / Q000737:chemistry; D014315:Triterpenes / Q000138:chemical synthesis* / Q000494:pharmacology; D000094042:Lupanes
D000893:Anti-Inflammatory Agents; D005947:Glucose; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D053978:Pentacyclic Triterpenes; D013311:Streptozocin; D014280:Triglycerides; D014315:Triterpenes; C010480:lupeol; D000094042:Lupanes