Department of Biotechnology and Microbiology, Kannur University, Thalassery Campus, Palayad, Kerala, India.
Chem Biol Drug Des. 2012 Jan;79(1):143-7. doi: 10.1111/j.1747-0285.2011.01258.x. Epub 2011 Nov 16.
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.
理论上，抑制 PLA(2) 的活性应该是控制炎症的有效方法。已经有报道称，几种天然存在的多酚化合物可以抑制 PLA(2)。在天然存在的多酚中，儿茶酚（1,2-二羟基苯）具有抗炎活性。儿茶酚可以抑制环加氧酶和脂加氧酶。通过酶动力学研究表明，儿茶酚也可以抑制 PLA(2)。晶体结构表明，儿茶酚结合在 PLA(2)的活性位点裂隙开口处。这可能阻止底物进入活性位点。因此，儿茶酚可用作新型抗炎药物的先导化合物，以 PLA(2) 为靶点。
