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Evaluation of Polyhydroxybenzophenones as α‐Glucosidase Inhibitors
Author(s) -
Hu Xuesen,
Xiao Yang,
Wu Jianlong,
Ma Lin
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000147
Subject(s) - acarbose , chemistry , substrate (aquarium) , stereochemistry , non competitive inhibition , enzyme , enzyme inhibitor , biochemistry , biology , ecology
This experiment was designed to synthesize 18 kinds of polyhydroxybenzophenones by using Friedel‐Crafts reaction, and to measure the inhibitory activity on α‐glucosidase with p ‐nitrophenyl‐β‐D‐galactopyranoside (PNPG) as a substrate. Here, acarbose (IC 50 = 1674.75 µmol L −1 ) was used as the reference inhibitor. The results demonstrated that most of the target compounds had remarkable inhibitory activities on α‐glucosidase. Among all these compounds, 2,4,4′,6‐butahydroxydiphenylketone ( 11 ) was found to be the most potent α‐glucosidase inhibitor with an IC 50 value of 10.62 µmol L −1 . In addition, we found these compounds were competitive inhibitors through the kinetic analysis. The results suggested that such compounds might be utilized for the development of new candidates for diabetes treatment.