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α-GLUCOSIDASE INHIBITORY EFFECT OF SULOCHRIN FROM ASPERGILLUSTERREUS AND ITSBROMINATED DERIVATIVES
- Source :
- Malaysian Journal of Science. 37:70-81
- Publication Year :
- 2018
- Publisher :
- Univ. of Malaya, 2018.
-
Abstract
- Use of I±-glucosidase inhibitorsis one of the therapeutic approaches for decreasing postprandial hyperglycemia. Sulochrin (1) from Aspergillus terreus as well as two synthetic sulochrin derivatives were assessed for antidiabetic activity against yeast and rat intestine I±-glucosidase. Sulochrin showed potential inhibition against yeast I±-glucosidase, through a non-competitive mode with an IC50 value of 133.79 µM, and rat intestine I±-glucosidase by uncompetitive mode with an IC50 value of 144.59 µM.. Two synthetic derivatives of sulochrin were also prepared by bromination which resulted in dibromo-sulochrin (2) and tribromo-sulochrin (3). Preliminary SAR studies of sulochrin derivatives revealed that the yeast I±-glucosidase inhibitory activity of compound 2 and 3 increased than 1 due to substitution of hydrogen atom with bromine with IC50 values of 122.65 and 49.08 µM, respectively. However, the inhibitory activity against rat intestine I±-glucosidase of 2 and 3 was decreased compared to 1. To the best our knowledge, this is the first report of structure-activity relationship of sulochrin and its derivatives as I±-glucosidase inhibitors. These results suggested that sulochrin can potentially be used as a lead compound to develop new I±-glucosidase inhibitor from microorganisms. Keywords: Aspergillus terreus, I±-glucosidase inhibitory activity, sulochrin, bromination
- Subjects :
- 0301 basic medicine
030109 nutrition & dietetics
Multidisciplinary
biology
Synthetic derivatives
Halogenation
biology.organism_classification
01 natural sciences
Yeast
0104 chemical sciences
010404 medicinal & biomolecular chemistry
03 medical and health sciences
chemistry.chemical_compound
Biochemistry
chemistry
Ic50 values
Aspergillus terreus
IC50
Inhibitory effect
Lead compound
Subjects
Details
- ISSN :
- 13943065
- Volume :
- 37
- Database :
- OpenAIRE
- Journal :
- Malaysian Journal of Science
- Accession number :
- edsair.doi...........fd24a6f08f03baff3f65c5495d61a468