EXPERIMENTAL AND COMPUTATIONAL STUDY OF BINDING INTERACTION OF ALKOXY DERIVATIVES OF N-ARYLHYDROXAMIC ACIDS WITH DNA
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2014, Vol 6, Issue 9
Abstract
Objective:  Binding affinity towards DNA for small molecules is very important in the development of new therapeutic reagents. Interaction between N-Arylhydroxamic acid derivatives N-p-Tolyl-4-Ethoxybenzohydroxamic acid (p-TEBHA) and N-o- Tolyl-4-Ethoxybenzohydroxamic Acid (o-TEBHA), with calf thymus DNA (CT DNA) were studied by UV–visible absorption, fluorescence,  viscosity measurement and molecular docking.Methods:  The absorption and emission spectra of DMSO solution of hydroxamic acid derivatives were studied for their binding activity with calf-thymus DNA by titration with increasing amount hydroxamic acids. Docking was performed by HEX software.Results:  Fluorescent spectra showed that CT DNA quenches the emission spectra of p-TEBHA & o-TEBHA with binding constant 1.6 Ñ… 108 M-1 and 4.3 Ñ… 103 M-1 respectively. Competitive study with ethidium bromide (EB) indicates that p-TEBHA can displace the DNA-bound EB suggesting strong competition with EB whereas o-TEBHA does not displace the DNA-bounded Ethidium bromide effectively. UV study of the interaction of the complexes with calf-thymus DNA has shown that the hydroxamic acid derivatives can bind with CT DNA. The docking studies were used to predict the mode of interaction of the drug with DNA. It was observed that as far as binding strength was concerned the computational results complemented the experimental results.Conclusion:  Investigated hydroxamic acid derivatives are found to be strong DNA binders and seem to have promising drug like nature.Â
Authors and Affiliations
Bharati Verma, Manish Pardhi, Rama Pande
Keywords
Related Articles
- EP ID EP579558
- DOI -
- Views 61
- Downloads 0
BIODIVERSITY OF ANTIBIOTIC-PRODUCING SOIL BACTERIA FROM YOGYAKARTA SPECIAL PROVINCE INDONESIA
Objective: The present study aims to evaluate the diversity of antibiotic-producing soil bacteria from Java, Indonesia.Methods: An agar diffusion method to select the active isolates against Staphylococcus aureus ATCC 25...
IDENTIFICATION OF PUTATIVE DRUG TARGETS IN MASTITIS CAUSING STAPHYLOCOCCUS AUREUS BY IN SILICO APPROACH
Objective: In the present study an attempt has been made by the use of a computational approach to investigate putative drug targets in Staphylococcus aureus.Methods: In silico comparative analysis of the metabolic pathw...
SIMULTANEOUS ESTIMATION OF PROPAFENONE AND ITS TWO METABOLITES IN HUMAN PLASMA BY LIQUID CHROMATOGRAPHY/TANDEM MASS SPECTROMETRY LC-MS/MS
Objective: A simple, sensitive and rapid performance liquid chromatography/positive ion electrospray tandem mass spectrometry method was to be developed and validated for quantification of propafenone (PPF) and its two m...
ESTROGENS IMPROVE THE CARDIOVASCULAR ALTERATIONS IN FRUCTOSE-INDUCED INSULIN RESISTANT OVARIECTOMIZED RATS
Objective: The present study aimed to investigate the possible improving effects of 17-β estradiol (EST) and genistein (GEN) on the cardiovascular changes associated with fructose (21% in drinking water for 8 weeks)-ind...
CLINICAL EVALUATION OF POTENTIAL ANTI-INFLAMMATORY EFFECT OF VITAMIN D3 ADJUVANT THERAPY FOR CHRONIC ASTHMA IN IRAQI PATIENTS
Objective: This study was designed to evaluate the potential anti-inflammatory effect of vitamin D3 supplementation in Iraqi patients with chronic asthma. Methods: Forty-four candidate patients were diagnosed with asthma...