Binding to PLA2 May Contribute to the Anti-Inflammatory Activity of Catechol

被引：15

作者：

Dileep, Kalarickal V. ^{[1
]}

Tintu, Ignatius ^{[1
]}

Mandal, Pradeep K. ^{[3
]}

Karthe, Ponnuraj ^{[3
]}

Haridas, Madathilkovilakathu ^{[1
,2
]}

Sadasivan, Chittalakkottu ^{[1
,2
]}

机构：

[1] Kannur Univ, Dept Biotechnol & Microbiol, Kannur 670661, Kerala, India

[2] Kannur Univ, Inter Univ Ctr Biosci, Kannur 670661, Kerala, India

[3] Univ Madras, Ctr Adv Study Crystallog & Biophys, Madras 600025, Tamil Nadu, India

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2012年 / 79卷 / 01期

关键词：

anti-inflammatory; catechol; crystal structure; enzyme inhibition; PLA2; PHOSPHOLIPASE A(2) ACTIVITY; INHIBITION; BRAIN; MODEL;

D O I：

10.1111/j.1747-0285.2011.01258.x

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Inhibiting PLA2 activity should, in theory, be an effective approach to control the inflammation. Several naturally occurring polyphenolic compounds have been reported as inhibitors of PLA2. 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 PLA2 also. Crystal structure showed that catechol binds to PLA2 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 PLA2 as the target.

引用

页码：143 / 147

页数：5

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