์ฝ˜ํ…์ธ ๋กœ ๊ฑด๋„ˆ๋›ฐ๊ธฐ
Merck

In vitro inhibitory effects of some acetophenone derivatives on some metabolic enzymes and molecular docking.

Archiv der Pharmazie (2020-09-03)
Parham Taslimi
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In this study, the acetophenone derivatives 1-6 were found to be effective inhibitor molecules for ฮฑ-glycosidase, human carbonic anhydrases I and II (hCA I/II), and acetylcholinesterase (AChE), with Ki values in the range of 167.98โ€‰ยฑโ€‰25.06 to 304.36โ€‰ยฑโ€‰65.45โ€‰ยตM for ฮฑ-glycosidase, 555.76โ€‰ยฑโ€‰56.07 to 1,043.66โ€‰ยฑโ€‰98.78โ€‰ยตM for hCA I, 598.63โ€‰ยฑโ€‰90.04 to 945.76โ€‰ยฑโ€‰74.50โ€‰ยตM for hCA II, and 71.34โ€‰ยฑโ€‰11.25 to 143.75โ€‰ยฑโ€‰31.27โ€‰ยตM for AChE, and IC50 values of 73.65-101.13โ€‰ยตM for tyrosinase. In the last step, molecular docking calculations were performed to compare the biological activities of molecules with their docking scores in these enzymes. The interactions of the studied molecules against human ฮฑ-galactosidase (PDB ID: 1R47), hCA I (PDB ID: 3LXE), human AChE (PDB ID: 4M0E), hCA II (PDB ID: 5AML), and human tyrosinase (PDB ID: 5M8Q) were examined to compare the biological activity values. The ADME/T analysis (adsorption, distribution, metabolism, and discharge) was then performed for the future use of these molecules as drugs.

MATERIALS
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Sigma-Aldrich
2-Methoxyacetophenone, 95%
Sigma-Aldrich
ฮฑ-Glucosidase from Saccharomyces cerevisiae, Type I, lyophilized powder, โ‰ฅ10 units/mg protein (using p-nitrophenyl ฮฑ-D-glucoside as substrate.)
Sigma-Aldrich
4-Nitrophenyl ฮฑ-D-glucopyranoside, โ‰ฅ99%
Sigma-Aldrich
Benzoylnitromethane, 98%