Hypoglycemic activity of curcumin synthetic analogues in alloxan-induced diabetic rats. (2nd January 2016)

• Record Type: Journal Article
• Authors: Das, Kusal K.; Razzaghi-Asl, Nima; Tikare, Swati N.; Di Santo, Roberto; Costi, Roberta; Messore, Antonella; Pescatori, Luca; Crucitti, Giuliana Cuzzucoli; Jargar, Jameel G.; Dhundasi, Salim A.; Saso, Luciano
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 31:Number 1(2016:Feb.)
• Page Start: 99
• Page End: 105
• Publication Date: 2016-01-02
• Subjects: Curcumin -- diabetic rats -- hypoglycemic -- in vitro -- OGTT -- synthesis; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2015.1004061
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: The currently available therapies for type 2 diabetes have been unable to achieve normoglycemic status in the majority of patients. The reason may be attributed to the limitations of the drug itself or its side effects. In an effort to develop potent and safe oral antidiabetic agents, we evaluated the in vitro and in vivo hypoglycemic effects of 10 synthetic polyphenolic curcumin analogues on alloxan-induced male diabetic albino rats. In vitro studies showed 7-bis(3, 4-dimethoxyphenyl)hepta-1, 6-diene-3, 5-dione (4 ) to be the most potential hypoglycemic agent followed by 1, 5-bis(4-hydroxy-3-methoxyphenyl)penta-1, 4-dien-3-one (10 ). Structure activity relationship (SAR) of the tested compounds was elucidated and the results were interpreted in terms of in vitro hypoglycemic activities. Furthermore, oral glucose tolerance test (OGTT) with compounds4, 10 and reference hypoglycemic drug glipizide showed that compound4 and glipizide had relatively similar effects on the reduction of blood glucose levels within 2 h. Thus, compound4 might be regarded as a potential hypoglycemic agent being able to reduce glucose concentration both in vitro and in vivo .