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

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

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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: Journal Article
Publication: Biochemical and Biophysical Research Communications
Publisher: Elsevier Science
Additional Information: Copyright of this article belongs to Elsevier Science.
Keywords: EGCG;Plasmodium falciparumMalaria;Enoyl-ACP reductase;Slow; Tight-binding inhibitor;PfENR;Triclosan
Department/Centre: Division of Biological Sciences > Molecular Biophysics Unit
Date Deposited: 29 Mar 2010 11:46
Last Modified: 19 Sep 2010 05:57
URI: http://eprints.iisc.ac.in/id/eprint/26291

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