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Pentacyclic triterpenes as α-glucosidase and α-amylase inhibitors: Structure-activity relationships and the synergism with acarbose.

Authors
  • Zhang, Bo-Wei1
  • Xing, Yan1
  • Wen, Chen1
  • Yu, Xiao-Xia1
  • Sun, Wen-Long1
  • Xiu, Zhi-Long1
  • Dong, Yue-Sheng2
  • 1 School of Life Science and Biotechnology, Dalian University of Technology, Dalian 116024, Liaoning, China. , (China)
  • 2 School of Life Science and Biotechnology, Dalian University of Technology, Dalian 116024, Liaoning, China. Electronic address: [email protected] , (China)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Nov 15, 2017
Volume
27
Issue
22
Pages
5065–5070
Identifiers
DOI: 10.1016/j.bmcl.2017.09.027
PMID: 28964635
Source
Medline
Keywords
License
Unknown

Abstract

In this paper, the inhibition of α-amylase and α-glucosidase by nine pentacyclic triterpenes was determined. For α-amylase inhibitory activity, the IC50 values of ursolic acid, corosolic acid, and oleanolic acid were 22.6±2.4μM, 31.2±3.4μM, and 94.1±6.7μM, respectively. For α-glucosidase inhibition, the IC50 values of ursolic acid, corosolic acid, betulinic acid, and oleanolic acid were 12.1±1.0μM, 17.2±0.9μM, 14.9±1.9μM, and 35.6±2.6μM, respectively. The combination of corosolic acid and oleanolic acid with acarbose showed synergistic inhibition against α-amylase. The combination of the tested triterpenes with acarbose mainly exhibited additive inhibition against α-glucosidase. Kinetic studies revealed that corosolic acid and oleanolic acid showed non-competitive inhibition and acarbose showed mixed-type inhibition against α-amylase. The results provide valuable implications for the triterpenes (ursolic acid, corosolic acid, and oleanolic acid) alone or in combination with acarbose as a therapeutic agent for the treatment of diabetes mellitus.

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