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Investigation of the effects of some drugs and phenolic compounds on human dihydrofolate reductase activity.

Authors
  • Aslan, Erdem
  • Adem, Sevki
Type
Published Article
Journal
Journal of Biochemical and Molecular Toxicology
Publisher
Wiley (John Wiley & Sons)
Publication Date
Mar 01, 2015
Volume
29
Issue
3
Pages
135–139
Identifiers
DOI: 10.1002/jbt.21677
PMID: 25418905
Source
Medline
Keywords
License
Unknown

Abstract

Dihydrofolate reductase (DHFR) plays a fundamental role in cellular metabolism and cell growth. Inhibition of this enzyme will cause a decrease in the amount of folate that occurs in many metabolic processes, and the deficiency of which may cause various diseases. This study investigated the effects of some drugs and phenolic compounds on DHFR activity in vitro. To determine the inhibitory effect of compounds, enzyme activity was measured with a final concentration of an inhibitor ranging from 10 μM to 51 mM. DHFR was inhibited effectively by naringin, ferulic acid, and levofloxacin with IC50 values under 660 μM. Syringic acid, cefepime, ceftizoxime, cefazolin, ceftriaxone, and ceftazidime exhibited inhibitory effects on the enzyme activity with IC50 values in the range of 3.840-30.224 mM. K(i) constants were calculated using the Cheng-Prusoff equation. K(i) constants calculated in the range of 0.009-2.024 mM with respect to nicotinamide adenine dinucleotide phosphate oxidase (NADPH) and in the range of 0.060-5.830 mM about FH2.

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