Binding to PLA2 may contribute to the anti-inflammatory activity of catechol.

Authors :: Dileep KV
Tintu I
Mandal PK
Karthe P
Haridas M
Sadasivan C
Source :: Chemical biology & drug design [Chem Biol Drug Des] 2012 Jan; Vol. 79 (1), pp. 143-7. Date of Electronic Publication: 2011 Nov 16.
Publication Year :: 2012
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.<br /> (© 2011 John Wiley & Sons A/S.)