Combined effect of epigallocatechin gallate and triclosan on enoyl-ACP reductase of Mycobacterium tuberculosis.

@article{Sharma2008CombinedEO,
  title={Combined effect of epigallocatechin gallate and triclosan on enoyl-ACP reductase of Mycobacterium tuberculosis.},
  author={S. Sharma and G. Kumar and M. Kapoor and A. Surolia},
  journal={Biochemical and biophysical research communications},
  year={2008},
  volume={368 1},
  pages={
          12-7
        }
}
Among the various inhibitors known for enoyl-acyl carrier protein (ACP) reductases, triclosan and green tea catechins are two promising candidates. In the present study, we show, for the first time that epigallocatechin gallate (EGCG), a major component of green tea catechins, inhibits InhA, the enoyl-ACP reductase of Mycobacterium tuberculosis with an IC50 of 17.4muM. EGCG interferes with the binding of NADH to InhA. We also demonstrate that EGCG increased the inhibitory activity of triclosan… Expand
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References

SHOWING 1-10 OF 24 REFERENCES
Green tea catechins potentiate triclosan binding to enoyl-ACP reductase from Plasmodium falciparum (PfENR).
TLDR
Investigation of the mechanism of inhibition of enoyl-acyl carrier protein reductase of Plasmodium falciparum by triclosan in the presence of a few important catechins and related plant polyphenols shows great promise for the development of effective antimalarial therapy. Expand
Triclosan offers protection against blood stages of malaria by inhibiting enoyl-ACP reductase of Plasmodium falciparum
TLDR
It is demonstrated that the enoyl-ACP reductase purified from P. falciparum is triclosan sensitive and the existence of the de novo fatty acid biosynthetic pathway in this parasite is established, and a key enzyme of this pathway for the development of new antimalarials is identified. Expand
Pyrrolidine carboxamides as a novel class of inhibitors of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis.
TLDR
The discovery is reported here the discovery, through high-throughput screening, of a series of pyrrolidine carboxamides as a novel class of potent InhA inhibitors, and resolution of racemic mixtures of several inhibitors indicate that only one enantiomer is active as an inhibitor of InHA. Expand
Inhibition of InhA, the enoyl reductase from Mycobacterium tuberculosis, by triclosan and isoniazid.
TLDR
It is shown that triclosan specifically inhibits InhA, the enoyl reductase from Mycobacterium tuberculosis and a target for the antitubercular drug isoniazid. Expand
Structural basis for the variation in triclosan affinity to enoyl reductases.
TLDR
Interactions between triclosan, the cofactor NADH/NAD+ and the enzyme from five different species, one plant and four of microbial origin, have been examined in the available crystal structures and it is revealed that the conformation of this flexible loop and the binding affinities of tric Losan to each of these enzymes are strongly correlated. Expand
Evaluation of Epigallocatechin Gallate and Related Plant Polyphenols as Inhibitors of the FabG and FabI Reductases of Bacterial Type II Fatty-acid Synthase*
TLDR
EGCG inhibited acetate incorporation into fatty acids in vivo, although it was much less potent than thiolactomycin, a validated fatty acid synthesis inhibitor, and overexpression of FabG, FabI, or both did not confer resistance. Expand
Enoyl reductases as targets for the development of anti-tubercular and anti-malarial agents.
TLDR
A brief description of the mechanism of action of, and resistance to, isoniazid is presented and data on inhibition of mycobacterial and plasmodial enoyl reductases by triclosan are presented. Expand
Slow-tight-binding inhibition of enoyl-acyl carrier protein reductase from Plasmodium falciparum by triclosan.
TLDR
The steady-state kinetics revealed time-dependent inhibition of FabI by triclosan, demonstrating that tricLosan is a slow-tight-binding inhibitor of Fabi, a good target for antimalarials. Expand
Isoniazid affects multiple components of the type II fatty acid synthase system of Mycobacterium tuberculosis
TLDR
The results suggest that these components of the FAS II complex are not independently regulated and that alterations in the expression level of InhA affect expression levels of KasA, which appears to be tightly correlated with INH sensitivity. Expand
inhA, a gene encoding a target for isoniazid and ethionamide in Mycobacterium tuberculosis.
TLDR
Results suggest that InhA is likely a primary target of action for INH and ETH and that it may be involved in mycolic acid biosynthesis. Expand
...
1
2
3
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