Comparative studies on the inhibitory activities of selected benzoic acid derivatives against secretory phospholipase A2, a key enzyme involved in the inflammatory pathway.
Inflammation is considered to be a key factor in major diseases like cancer, Alzheimer's disease, Parkinson's disease, etc. For the past few decades, pharmaceutical companies have explored new effective medications against inflammation. As a part of their detailed studies, many drug targets and drugs have been introduced against inflammation. In the present study, the inhibiting capacities of selected benzoic acid derivatives like gallic acid, vannilic acid, syringic acid and protocatechuic acid against secretory phospholipase A2 (sPLA2), a major enzyme involved in the inflammatory pathway, have been investigated. The detailed in vitro, biophysical and in silico studies carried out on these benzoic acid derivatives revealed that all the selected compounds have a uniform mode of binding in the active site of sPLA2 and are inhibitory in micromolar concentrations. The study also focuses on the non-selective inhibitory activity of an NSAID, aspirin, against sPLA2.
Department of Biotechnology and Microbiology and Inter University Centre for Biosciences, Thalassery Campus, Kannur University, Kerala 670661, India. csadsivan@gmail.com.
K V
KV
Dileep
C
C
Remya
J
J
Cerezo
A
A
Fassihi
H
H
Pérez-Sánchez
C
C
Sadasivan
D000893:Anti-Inflammatory Agents / Q000737:chemistry*; D001565:Benzoates / Q000737:chemistry*; D020134:Catalytic Domain; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D062105:Molecular Docking Simulation; D056004:Molecular Dynamics Simulation; D054497:Phospholipases A2, Secretory / Q000037:antagonists & inhibitors / Q000737:chemistry*; D017186:Titrimetry
D000893:Anti-Inflammatory Agents; D001565:Benzoates; D054497:Phospholipases A2, Secretory