Novel Piperine Derivatives with Antidiabetic Effect as PPAR‐γ Agonists. (27th May 2016)

• Record Type: Journal Article
• Authors: Kharbanda, Chetna; Alam, Mohammad Sarwar; Hamid, Hinna; Javed, Kalim; Bano, Sameena; Ali, Yakub; Dhulap, Abhijeet; Alam, Perwez; Pasha, M. A. Qadar
• Is Part Of: Chemical biology & drug design. Volume 88:Number 3(2016)
• Page Start: 354
• Page End: 362
• Publication Date: 2016-05-27
• Subjects: amide linkage -- antidiabetic -- gene expression -- piperine -- PPAR‐γ; Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12760
• Languages: English
• ISSNs: 1747-0277

Abstract

Abstract : Piperine is an alkaloid responsible for the pungency of black pepper. In this study, piperine isolated from Piper nigrum L. was hydrolyzed under basic condition to obtain piperic acid and was used as precursor to carry out the synthesis of twenty piperine derivatives containing benzothiazole moiety. All the benzothiazole derivatives were evaluated for their antidiabetic potential by OGT test followed by assessment of active derivatives on STZ‐induced diabetic model. It was observed that nine of twenty novel piperine analogues (5b, 6a‐h), showed significantly higher antidiabetic activity in comparison with rosiglitazone (standard). Furthermore, these active derivatives were evaluated for their action as PPAR‐γ agonists demonstrating their mechanism of action. The effects on body weight, lipid peroxidation, and hepatotoxicity after administration with active derivatives were also studied to further establish these derivatives as lead molecules for treatment of diabetes with lesser side‐effects. Abstract : Twenty synthesized piperine derivatives are potential antidiabetic agents. Maximum antidiabetic effect was observed for compounds6c and6d .