title: Synthesis of novel triterpenoid (lupeol) derivatives and their in vivo antihyperglycemic and antidyslipidemic activity.
abstract: 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.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, UP, India.
authors.forename: K
authors.initials: K
authors.lastname: Papi Reddy
authors.forename: A B
authors.initials: AB
authors.lastname: Singh
authors.forename: A
authors.initials: A
authors.lastname: Puri
authors.forename: A K
authors.initials: AK
authors.lastname: Srivastava
authors.forename: T
authors.initials: T
authors.lastname: Narender
mesh_terms: 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
chemical_list: 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