The molecular and cellular mechanisms of enhanced toxic effects in tumor cells of the Pt(IV) derivatives of antitumor oxaliplatin containing axial dichloroacetate (DCA) ligands were investigated. DCA ligands were chosen because DCA has shown great potential as an apoptosis sensitizer and anticancer agent reverting the Wartburg effect. In addition, DCA reverses mitochondrial changes in a wide ra...

Human consumption of chlorinated drinking water has been linked epidemiologically to bladder, kidney, and rectal cancers. The disinfection by-product (DBP) dichloroacetic acid is a hepatocarcinogen in Fischer 344 rats and B6C3F1 mice. The objective of this study is to determine the effect of the DBPs dichloro-, bromochloro-, and dibromoacetic acids (DCA, BCA, DBA) on intestinal microbial popula...

In dynamic carrier allocation (DCA) strategies, carriers are assigned priorities. Based upon how priorities are assigned to carriers, DCA strategies are classified into three classes: static-priority, dynamic-priority, and hybrid-priority strategies. In this paper, we lay out a theoretical foundation for DCA strategies: we first develop the concept of optimal reuse pattern and then propose a mo...

Dichloroacetate (DCA) is a potential environmental hazard and an investigational drug. Repeated doses of DCA result in reduced drug clearance, probably through inhibition of glutathione transferase ζ1 (GSTZ1), a cytosolic enzyme that converts DCA to glyoxylate. DCA is known to be taken up by mitochondria, where it inhibits pyruvate dehydrogenase kinase, its major pharmacodynamic target. We test...

Objective: In this study carried out in Büyükçekmece Reservoir, the composition, distribution, seasonal changes of epiphytic diatoms that live on surfaces plants, and effects environmental parameters these organisms were investigated, it was aimed to reveal water quality reservoir. Materials Methods: order determine diatom species material samples collected from five stations 2019. study, tempe...

We studied the pharmacokinetics of dichloroacetate (DCA) in naive rats and rats depleted of glutathione S-transferase-zeta (GST-zeta), at doses approaching human daily exposure levels. We also compared in vitro metabolism of DCA by rat and human liver cytosol. Jugular vein-cannulated male Fischer-344 rats received graded doses of DCA ranging from 0.05 to 20 mg/kg (intravenously or by gavage), a...

The robust glycolytic metabolism of glioblastoma multiforme (GBM) has proven them susceptible to increases in oxidative metabolism induced by the pyruvate mimetic dichloroacetate (DCA). Recent reports demonstrate that the anti-diabetic drug metformin enhances the damaging oxidative stress associated with DCA treatment in cancer cells. We sought to elucidate the role of metformin's reported acti...

OBJECTIVE To investigate the effects of 3,4-dichloroaniline (3,4-DCA) on activities of testicle enzymes as biological markers in rats. METHODS Fifty male rats were randomly divided into 5 groups (n=10). One group was left untreated and used as a solvent control (administered orally by corn oil), while the other 4 groups were treated with 3, 4-DCA. Corn oil was used as a solvent, and 3,4-DCA w...

In summary, following a single oral dose of DCA to laboratory rats, peak hepatic tissue DCA concentration occurred at 3 hr. When given chronically for 7 days, DCA caused activation of the pyruvate dehydrogenase complex which returned to basal activity 24 hr following the final dose. Hepatic tissue DCA concentrations were maximally increased at 3 hr following the final dose, and the drug was eli...

The endogenous bile acid metabolite 1β-hydroxy-deoxycholic acid (1β-OH-DCA) excreted in human urine may be used as a sensitive CYP3A biomarker in drug development reflecting in vivo CYP3A activity. An efficient and stereospecific enzymatic synthesis of 1β-OH-DCA was developed using a Bacillus megaterium (BM3) cytochrome P450 (P450) mutant, and its structure was confirmed by nuclear magnetic res...