Chemistry and Biology of Synthetic and Naturally Occurring Antiamoebic Agents

Singh, Samunder; Bharti, Neelam; Mohapatra, Prabhu P.

doi:10.1021/cr068217k

Cited by 97 publications

(48 citation statements)

References 283 publications

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“…positive charge with the ligand which reduces the polarity of the metal atom [33]. Finally, it is of interest that HL1-HL6 and their corresponding nickel(II) complexes did not significantly affect the normal cell line HDF (human dermal fibroblast cell line), Fig.…”

Section: Cytotoxicitymentioning

confidence: 98%

Synthesis, structural characterization and cytotoxicity of nickel(II) complexes containing 3,3-dialkyl/aryl-1-benzoylthiourea ligands

Selvakumaran

Pratheepkumar

et al. 2013

Inorganica Chimica Acta

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Section: Cytotoxicitymentioning

confidence: 98%

Synthesis, structural characterization and cytotoxicity of nickel(II) complexes containing 3,3-dialkyl/aryl-1-benzoylthiourea ligands

Selvakumaran

Pratheepkumar

et al. 2013

Inorganica Chimica Acta

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“…5 TSCs and their metal complexes have many examples of pharmacological applications including antimalarial, antiviral, antiamoebic, antiprotozoal, antibacterial, antifungal and anticancer activities. [3][4][5][6][7][8] Their biological activities are considered to play a vital role in biological systems due to the TSCs to chelate with trace metal ions. 8,9 Optimization of these type molecules can result in discovery of new class therapeutic agents.…”

Section: Introductionmentioning

confidence: 99%

“…[3][4][5][6][7][8] Their biological activities are considered to play a vital role in biological systems due to the TSCs to chelate with trace metal ions. 8,9 Optimization of these type molecules can result in discovery of new class therapeutic agents. There has been great regard in the chemistry and medicine of organometallic ruthenium(II)-arene complexes as the improvement of effective synthetic precursors.…”

Section: Introductionmentioning

confidence: 99%

p-Cymene Based Organometallic Ruthenium(II)-Arene Complexes with Benzaldehyde Derived Thiosemicarbazones: Synthesis, Characterization and Antimicrobial Activity

Yavuz¹,

Yaman²,

Öztürk³

et al. 2017

Dicle Tıp Dergisi

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Objective: Thiosemicarbazone (TSC) containing three new mononuclear ruthenium(II)-arene complexes were synthesized so as to contribute to the development of ruthenium complexes with pharmacologically attracted properties.Conclusion: The TSC 1-3 containing ruthenium(II)-arene complexes were successfully synthesized and their molecular structures were also determined by the spectroscopic methods. All ruthenium(II)-arene complexes showed higher antibacterial activities against Gram-positive bacterial strains than the Gram-negative ones. Original Article/Özgün AraştırmaKeywords: Half-sandwich Ru(II)-arene complexes, benzaldehyde thiosemicarbazone, p-cymene, antimicrobial activity, clinical isolate.Results: The spectroscopic data indicated that TSC 1 was bounded to the metal as a tridentate ligand with its thione sulfur atom, phenolic oxygen atom and azomethine nitrogen atom in the complex I, while TSC 2 and TSC 3 were bounded to metal center as bidentate manner through their thione sulfur atom and imine nitrogen (C=N) atom in the complexes II and III, respectively. The obtained antimicrobial activity results showed that these complexes efficiently inhibit the growth of Gram-positive bacterial strains.

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“…In 1975, Reeves and Guthrie (23) identified a PP i -dependent ACK activity in E. histolytica, an amitochondriate protist that is the causative agent of human amebiasis. Amebiasis is the third leading cause of morbidity and the fourth leading cause of mortality due to protozoan infections, resulting in approximately 70,000 deaths worldwide (30). E. histolytica lacks compartmentalized, ATP-generating mitochondria and hydrogenosomes, and glycolysis serves as the major pathway for ATP generation (26).…”

mentioning

confidence: 99%

Novel Pyrophosphate-Forming Acetate Kinase from the Protist Entamoeba histolytica

2012

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Acetate kinase (ACK) catalyzes the reversible synthesis of acetyl phosphate by transfer of the ␥-phosphate of ATP to acetate. Here we report the first biochemical and kinetic characterization of a eukaryotic ACK, that from the protist Entamoeba histolytica. Our characterization revealed that this protist ACK is the only known member of the ASKHA structural superfamily, which includes acetate kinase, hexokinase, and other sugar kinases, to utilize inorganic pyrophosphate (PP i )/inorganic phosphate (P i ) as the sole phosphoryl donor/acceptor. Detection of ACK activity in E. histolytica cell extracts in the direction of acetate/PP i formation but not in the direction of acetyl phosphate/P i formation suggests that the physiological direction of the reaction is toward acetate/PP i production. Kinetic parameters determined for each direction of the reaction are consistent with this observation. The E. histolytica PP i -forming ACK follows a sequential mechanism, supporting a direct in-line phosphoryl transfer mechanism as previously reported for the well-characterized Methanosarcina thermophila ATP-dependent ACK. Characterizations of enzyme variants altered in the putative acetate/acetyl phosphate binding pocket suggested that acetyl phosphate binding is not mediated solely through a hydrophobic interaction but also through the phosphoryl group, as for the M. thermophila ACK. However, there are key differences in the roles of certain active site residues between the two enzymes. The absence of known ACK partner enzymes raises the possibility that ACK is part of a novel pathway in Entamoeba.A cetate kinase (ACK; EC 2.7.2.12; CH 3 COO Ϫ ϩ ATP % CH 3 COPO 4 2Ϫ ϩ ADP) is a key enzyme in prokaryotic metabolism for the activation of acetate as a carbon and energy source or for the generation of ATP during fermentative growth. ACK is a member of the ASKHA phosphotransferase superfamily, which includes acetate kinase, hexokinase, and other sugar kinases, as well as the Hsc70 heat shock cognate and actin (5,6,14,15). In 2001, Buss et al. (9) published the first structure for an ACK, that from the archaeon Methanosarcina thermophila, and they suggested that ACK is the urkinase for the ASKHA superfamily.Several crystal structures have now been solved for the well-characterized M. thermophila ACK (9, 13), and the roles of a number of active site residues in substrate binding and catalysis have been examined experimentally (16,17,21,22,28,29). Kinetic and structural studies support a direct in-line transfer of the phosphoryl group of ATP to acetate. An MgADP-AlF 3 -acetate transition state analog resulted in an abortive complex (22) and was found to be in a linear array in the active site (13). Based on analysis of site-altered enzyme variants and structural studies, Gorrell et al. (13) postulated a mechanism detailing the roles of active site residues in catalysis. The active site residues implicated in this mechanism are well conserved among the ACKs, consistent with their key roles in catalysis.Here we report the biochemical...

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Chemistry and Biology of Synthetic and Naturally Occurring Antiamoebic Agents

Cited by 97 publications

References 283 publications

Synthesis, structural characterization and cytotoxicity of nickel(II) complexes containing 3,3-dialkyl/aryl-1-benzoylthiourea ligands

Synthesis, structural characterization and cytotoxicity of nickel(II) complexes containing 3,3-dialkyl/aryl-1-benzoylthiourea ligands

p-Cymene Based Organometallic Ruthenium(II)-Arene Complexes with Benzaldehyde Derived Thiosemicarbazones: Synthesis, Characterization and Antimicrobial Activity

Novel Pyrophosphate-Forming Acetate Kinase from the Protist Entamoeba histolytica

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