Epigallocatechin gallate is a slow-tight binding inhibitor of enoyl-ACP reductase from Plasmodium falciparum

Banerjee, Tanushree ; Sharma, Shailendra Kumar ; Surolia, Namita ; Surolia, Avadhesha (2008) Epigallocatechin gallate is a slow-tight binding inhibitor of enoyl-ACP reductase from Plasmodium falciparum Biochemical and Biophysical Research Communications, 377 (4). pp. 1238-1242. ISSN 0006-291X

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Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1016/j.bbrc.2008.10.135

Abstract

Epigallocatechin gallate (EGCG) is known to have numerous pharmacological properties. In the present study, we have shown that EGCG inhibits enoyl-acyl carrier protein reductase of Plasmodium falciparum (PfENR) by following a two-step, slow, tight-binding inhibition mechanism. The association/isomerization rate constant (k5) of the reversible and loose PfENR-EGCG binary complex to a tight [PfENR-EGCG] or EI complex was calculated to be 4.0×10−2 s−1. The low dissociation rate constant (k6) of the [PfENR-EGCG] complex confirms the tight-binding nature of EGCG. EGCG inhibited PfENR with the overall inhibition constant (Ki) of 7.0±0.8 nM. Further, we also studied the effect of triclosan on the inhibitory activity of EGCG. Triclosan lowered the k6 of the EI complex by 100 times, lowering the overall Ki of EGCG to 97.5±12.5 pM. The results support EGCG as a promising candidate for the development of tea catechin based antimalarial drugs.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:EGCG; Plasmodium falciparum; Malaria; Enoyl-ACP Reductase; Slow; Tight-binding Inhibitor; PfENR; Triclosan
ID Code:56486
Deposited On:24 Aug 2011 11:34
Last Modified:03 Oct 2011 14:10

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