Synthesis and biological evaluation of novel ursolic acid analogues as potential α-glucosidase inhibitors.

ABSTRACT: Ursolic acid (UA) is a major pentacyclic triterpenoid in plants, vegetables and fruits, which has been reported to have a potential anti-diabetic activity. Despite various semi-synthetic ursolic acid derivatives already described, new derivatives still need to be designed and synthesized to further improve the anti-diabetic activity. In the present study, two series of novel UA derivatives, were synthesized and their structures were confirmed. The enzyme inhibition activities of semi-synthesized analogues against α-glucosidase were screened in vitro. The results indicated that most of UA derivatives showed a significant inhibitory activity, especially analogues UA-O-i with the IC₅₀ values of 0.71 ± 0.27 μM, which was more potential than other analogues and the positive control.

SUBMITTER: Wu PP 

PROVIDER: S-EPMC5372089 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature