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
a Department of Physiology, Shri. B.M. Patil Medical College , BLDE University , Bijapur , Karnataka , India .
b Department of Medicinal Chemistry .
J Enzyme Inhib Med Chem. 2016;31(1):99-105. doi: 10.3109/14756366.2015.1004061. Epub 2015 Feb 16.
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 compounds 4, 10 and reference hypoglycemic drug glipizide showed that compound 4 and glipizide had relatively similar effects on the reduction of blood glucose levels within 2 h. Thus, compound 4 might be regarded as a potential hypoglycemic agent being able to reduce glucose concentration both in vitro and in vivo.
