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

@article{Banerjee2008EpigallocatechinGI,
  title={Epigallocatechin gallate is a slow-tight binding inhibitor of enoyl-ACP reductase from Plasmodium falciparum.},
  author={T. Banerjee and S. Sharma and N. Surolia and A. Surolia},
  journal={Biochemical and biophysical research communications},
  year={2008},
  volume={377 4},
  pages={
          1238-42
        }
}
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 (k(5)) of the reversible and loose PfENR-EGCG binary complex to a tight [PfENR-EGCG](*) or EI(*) complex was calculated to be 4.0x10(-2) s(-1). The low dissociation rate… Expand
Epigallocatechin-3-gallate potently inhibits the in vitro activity of hydroxy-3-methyl-glutaryl-CoA reductase[S]
TLDR
It is demonstrated that EGCG potently inhibits the in vitro activity of HMGR (Ki in the nanomolar range) by competitively binding to the cofactor site of the reductase. Expand
Mutational analysis of the interaction between a potential inhibitor luteolin and enoyl-ACP reductase (FabI) from Salmonella enterica
Abstract Salmonella enterica is the main cause of food-borne disease worldwide and the emergence of antibiotic-resistant Salmonella strains has become a major public health concern. To combat theExpand
Novel enoyl-ACP reductase (FabI) potential inhibitors of Escherichia coli from Chinese medicine monomers.
TLDR
Two Chinese medicine monomers, luteolin and curcumin, were proved to be uncompetitive inhibitors of enoyl-ACP reductase from Escherichia coli (EcFabI) and showed apparent antibacterial activity against E. coli, demonstrating that its antibacterial action is mediated by the inhibition of EcFabI. Expand
Green Tea and its Main Catechin, Epigallocatechin-3-Gallate, Provide Parasitic Protection
TLDR
Green tea and epigallocatechin-3-gallate have anti-oxidant, anti-microbial, and anti-cancer activities and EGCG has protective effects against parasitic infections and may be used for the treatment of such infections. Expand
Effects of epigallocatechin gallate on the cell-wall structure of Mycobacterial smegmatis mc2155
TLDR
The results show that EGCG impacts the integrity of mycobacterial cell wall and is likely be a better prophylactic agent against tuberculosis. Expand
The synthesis, antimalarial activity and CoMFA analysis of novel aminoalkylated quercetin analogs.
TLDR
The structure-activity relationship determined from the antimalarial activity data suggests the inclusion of phenethyl amine sidechains on the quercetin scaffolding is necessary for potent activity. Expand
IN-SILICO SCREENING AGAINST ANTIMALARIAL TARGET PLASMODIUM FALCIPARUM ENOYL-ACYL CARRIER PROTEIN REDUCTASE
TLDR
There are two candidate inhibitor compounds from tea, which have potential for development as an antimalarial drug, which are kaempferol 3-rhamnosyl- (1-3)-rham Nosyl-(1-6)-glucoside and epigallocatechin 3,5,-di-O-gallate, with a GOLD score of 94.73 and 85.39, respectively. Expand
Detection of Escherichia coli enoyl-ACP reductase using biarsenical-tetracysteine motif.
TLDR
It is demonstrated for the first time that the binding between FlAsH reagent and TC motif was stable against high pressure, high field strength, high temperature, and ultrasound. Expand
Design, development, synthesis, and docking analysis of 2′‐substituted triclosan analogs as inhibitors for Plasmodium falciparum Enoyl‐ACP reductase
TLDR
The binding energies of the 2′ substituted analogs of triclosan for enoyl‐acyl carrier protein reductase (ENR) of Plasmodium falciparum were determined using Autodock and three potential compounds exhibited good potencies. Expand
Identification of novel antiplasmodial compound by hierarquical virtual screening and in vitro assays
TLDR
Represented structures of P. falciparum ENR can be used in a study to propose new derivatives for evaluation of biological activity in vitro and in vivo, and could be accelerated the drug development process. Expand
...
1
2
...

References

SHOWING 1-10 OF 26 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
Combined effect of epigallocatechin gallate and triclosan on enoyl-ACP reductase of Mycobacterium tuberculosis.
TLDR
For the first time, it is shown 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. Expand
Discovery of a rhodanine class of compounds as inhibitors of Plasmodium falciparum enoyl-acyl carrier protein reductase.
TLDR
A rhodanine (2-thioxothiazolidin-4-one) class of compounds are found to inhibit PfENR at low nanomolar to low micromolar concentrations, expanding the scope for developing new antimalarial drugs. Expand
Kinetic and structural analysis of the increased affinity of enoyl-ACP (acyl-carrier protein) reductase for triclosan in the presence of NAD+.
TLDR
The dramatic enhancement in the binding affinity of both triclosan and NAD+ in the ternary complex can be explained by increased van der Waals contacts in theTERNary complex, facilitated by the movement of residues 318-324 of the substrate-binding loop and the nicotinamide ring of NAD+. 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
Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids.
TLDR
Polyphenols of C-3 gallic acid esters of catechins showed in vitro activity against chloroquine-sensitive and -resistant P. falciparum strains in the low to submicromolar range. Expand
Mutational analysis of the triclosan-binding region of enoyl-ACP (acyl-carrier protein) reductase from Plasmodium falciparum.
TLDR
Modelling studies and crystal structure studies point out significant differences in the triclosan-binding region of the P. falciparum enzyme from those of its bacterial counterparts. Expand
Kinetic determinants of the interaction of enoyl-ACP reductase from Plasmodium falciparum with its substrates and inhibitors.
TLDR
The initial characterization of Plasmodium FabI expressed in Escherichia coli is reported, which shows that the binding of triclosan to the enzyme is facilitated in the presence of NAD(+) and competitive kinetics with respect to NADH are shown. 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
Novel diphenyl ethers: design, docking studies, synthesis and inhibition of enoyl ACP reductase of Plasmodium falciparum and Escherichia coli.
TLDR
Some novel diphenyl ethers designed and determined their binding energies for Enoyl-Acyl Carrier Protein Reductase (ENR) of Plasmodium falciparum using Autodock show nanomolar inhibition of PfENR and low micromolar inhibitory activity against EcENR. Expand
...
1
2
3
...