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 (K∗i) 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 K∗i 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 |
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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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