title: Binding to PLA2 may contribute to the anti-inflammatory activity of catechol.
abstract: Inhibiting PLA(2)  activity should, in theory, be an effective approach to control the inflammation. Several naturally occurring polyphenolic compounds have been reported as inhibitors of PLA(2) . Among the naturally occurring polyphenols, catechol (1,2-dihydroxybenzene) possesses anti-inflammatory activity. Catechol can inhibit cyclooxygenase and lipo-oxygenase. By means of enzyme kinetic study, it was revealed that catechol can inhibit PLA(2)  also. Crystal structure showed that catechol binds to PLA(2)  at the opening of the active site cleft. This might stop the entry of substrate into the active site. Hence, catechol can be used as a lead compound for the development of novel anti-inflammatory drugs with PLA(2)  as the target.
authors: Department of Biotechnology and Microbiology, Kannur University, Thalassery Campus, Palayad, Kerala, India.
authors: Kalarickal V
authors: KV
authors: Dileep
authors: Ignatius
authors: I
authors: Tintu
authors: Pradeep K
authors: PK
authors: Mandal
authors: Ponnuraj
authors: P
authors: Karthe
authors: Madathilkovilakathu
authors: M
authors: Haridas
authors: Chittalakkottu
authors: C
authors: Sadasivan
mesh_terms: D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000494:pharmacology*; D001665:Binding Sites; D020134:Catalytic Domain; D002396:Catechols / Q000737:chemistry* / Q000494:pharmacology; D003198:Computer Simulation; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D007700:Kinetics; D064801:Phospholipase A2 Inhibitors; D054467:Phospholipases A2 / Q000737:chemistry / Q000378:metabolism; D011485:Protein Binding / Q000187:drug effects
chemical_list: D000893:Anti-Inflammatory Agents; D002396:Catechols; D004791:Enzyme Inhibitors; D064801:Phospholipase A2 Inhibitors; D054467:Phospholipases A2; C034221:catechol