Antiplasmodial Activity of Nitroaromatic and Quinoidal Compounds: Redox Potential vs Inhibition of Erythrocyte Glutathione Reductase

Grellier, Philippe; Šarlauskas, Jonas; Anusevičius, Žilvinas; Marozien≐, Audron≐; Houée-Levin⊥, Chantal; Schrével, Joseph; Č≐nas, Narimantas

doi:10.1006/abbi.2001.2487

Cited by 44 publications

(51 citation statements)

References 41 publications

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“…Nitro aromatic compounds can either be strong or weak inhibitors of erythrocyte GR [26]. Similar results were obtained in different studies [16 -18].…”

Section: Discussionsupporting

confidence: 88%

Effects of some antibiotics on human erythrocyte glutathione reductase: anin vitrostudy

Şentürk

Küfrevioğlu

Çiftçi

2008

Journal of Enzyme Inhibition and Medicinal Chemistry

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Inhibitory effects of some antibiotics on purified human erythrocyte glutathione reductase were investigated. Human erythrocyte glutathione reductase was purified 2800-fold (29% yield) at 48C using 2 0 , 5 0 -ADP Sepharose 4B affinity gel and Sephadex G-200 gel filtration chromatography. SDS polyacrylamide gel electrophoresis showed a single band for the enzyme. Imipenem, rifamycin, sulfanylacetamide, ceftazidime, chloramphenicol, seftriaxon, vancomycin, cefuroxime and ornidazole exhibited inhibitory effects but clindamycin, lincomycin, amoxicillin, amikacin exhibited activatory effects on the enzyme in vitro. The IC 50 values of imipenem, rifamycin, sulfanylacetamide, ceftazidime, chloramphenicol, seftriaxon, vancomycin, cefuroxime and ornidazole were 0.030, 0.146, 0.59, 2.476, 2.36, 2.88, 4.83, 15.43 and 19.632 mM, respectively, and the K i constants were 0.06^0.01, 0.275^0.10, 0.85^0. 05, 3.59^0.51, 3.85^0.40, 3.71^0.60, 15.11^2.50, 23.50^2.94 and 28.49^6.50 mM, respectively. While imipenem, rifamycin, sulfanylacetamide, ceftazidime, chloramphenicol and seftriaxon cefuroxime and ornidazole showed competitive inhibition, vankomycine displayed noncompetitive inhibition.

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“…Nitro aromatic compounds can either be strong or weak inhibitors of erythrocyte GR [26]. Similar results were obtained in different studies [16 -18].…”

Section: Discussionsupporting

confidence: 88%

Effects of some antibiotics on human erythrocyte glutathione reductase: anin vitrostudy

Şentürk

Küfrevioğlu

Çiftçi

2008

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…It was reported that nicotine causes competitive inhibition by binding the active site of GR. Nitro aromatic compounds can either be strong or weak inhibitors of erythrocyte GR (Grellier et al, 2001). Similar results were obtained from different studies (Erat & Ciftci, 2006;.…”

Section: Discussionsupporting

confidence: 86%

The effect of some antibiotics on glutathione reductase enzyme purified from liver and erythrocyte of Lake Van pearl mullet

Altun

Türkoğlu²,

Çelik

2015

Pharmaceutical Biology

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Context: The effect of antibiotics (amikacin, cefazolin, ivermectin, and kanamycin) on glutathione reductase (GR) isoenzymes activity in liver and erythrocyte of the fish, Chalcalburnus tarichi (Lake Van pearl mullet, Pallas 1811) (Cyprinidae) were investigated. Objective: This study determined the biochemical characterization of GR purified from the liver and erythrocytes of C. tarichi and the inhibition effect of the antibiotics on the GR isoenzymes. Materials and methods: GR was purified by affinity chromatography from the tissues of C. tarichi. The biochemical characterization of GR such as optimum temperature, optimum pH, and ionic strength were determined. The inhibition effects of the antibiotics on the isoenzymes were evaluated as IC 50 and K i values. K i constant and 50% inhibitory concentration (IC 50 ) value for antibiotics were determined by Lineweaver-Burk graphs and plotting activity % versus [I], respectively, at five different concentrations of antibiotics. Results: Optimum temperature, pH, and ionic strength were determined for isoenzymes as 40 C, 60 C; 8.0, 8.0, and 50, 50 mM, respectively. Subunit molecular weights of the isoenzymes were estimated as 55 kDa by sodium dodecyl sulfate polyacrilamide gel electrophoresis (SDS-PAGE). In addition, IC 50 and K i values were calculated for amikacin, cefazolin, ivermectin, and kanamycin. The antibiotics showed non-competitive inhibition effects. IC 50 values were calculated as 16.3, 36.6, 0.504, and 18.8 mM for liver and 20.0, 30.4, 0.787, and 31

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“…P. falciparum FcB1 strain was maintained in continuous culture of human erythrocytes (Trager and Jensen, 1976;Grellier et al, 2001). In vitro antiplasmodial activity was determined using a modification of the semiautomatic microdilution technique (Desjardins et al, 1979).…”

Section: Methodsmentioning

confidence: 99%

Role of Single-Electron Oxidation Potential and Lipophilicity in the Antiplasmodial in vitro Activity of Polyphenols: Comparison to Mammalian Cells

Grellier

Nemeikaitė-Čėnienė

Šarlauskas³

et al. 2008

Zeitschrift Für Naturforschung C

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In spite of extensive studies, the structure-activity relationships in the action of polyphenols against the malaria parasite Plasmodium falciparum are poorly understood so far. As the mammalian cell cytotoxicity of polyphenols shows a negative dependence on the potential of the phenoxyl radical/phenol redox couple (E 2 7 ), due to the involvement of prooxidant events, and a positive dependence on the octanol/water distribution coefficient at pH 7.0 (log D), we examined the role of these parameters in their antiplasmodial in vitro activity. We found that the concentrations of hydroxybenzenes causing 50% inhibition of the growth of P. falciparum strain FcB1 (IC 50 ) are described by the regression log IC 50 (μm) = 0.36 + 1.81 E , where CL 50 is the compound concentration for 50% cell survival] than on their antiplasmodial activity. Although it is unclear whether the prooxidant action is the main factor in the antiplasmodial action of polyphenols or not, our data showed that the ease of their oxidation (decrease in E 2 7 ) may enhance their activity. On the other hand, the different sensitivity of the mammalian cell cytotoxicity and the antiplasmodial activity of the hydroxybenzenes to their E 2 7 values implied that compounds with high oxidation potential may be used as relatively efficient antiplasmodial agents with low mammalian cell cytotoxicity.

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Antiplasmodial Activity of Nitroaromatic and Quinoidal Compounds: Redox Potential vs Inhibition of Erythrocyte Glutathione Reductase

Cited by 44 publications

References 41 publications

Effects of some antibiotics on human erythrocyte glutathione reductase: anin vitrostudy

Effects of some antibiotics on human erythrocyte glutathione reductase: anin vitrostudy

The effect of some antibiotics on glutathione reductase enzyme purified from liver and erythrocyte of Lake Van pearl mullet

Role of Single-Electron Oxidation Potential and Lipophilicity in the Antiplasmodial in vitro Activity of Polyphenols: Comparison to Mammalian Cells

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