cyanoginosin-lr and bis(4-nitrophenyl)phosphate

Microcystin-LR is a hepatotoxin produced by several cyanobacteria. Its toxicity is mainly due to a inhibition of protein phosphatase, PP1 and PP2A. Previously, we used a cell line stably expressing uptake transporter for microcystin-LR, OATP1B3 (HEK293-OATP1B3 cells). In this study, to determine whether overexpression of carboxylesterase (CES), which degrades ester-group and amide-group, attenuates the cytotoxicity of microcystin-LR, we generated the HEK293-OATP1B3/CES2 double-transfected cells. HEK293-OATP1B3/CES2 cells showed high hydrolysis activity of p-nitrophenyl acetate (PNPA), which is an authentic substrate for esterase. CES activity in HEK293-OATP1B3/CES2 cells was approximately 3-fold higher than that in the HEK293-OATP1B3 cells. HEK293-OATP1B3/CES2 cells (IC

Topics: Absorption, Physiological; Bacterial Toxins; Binding Sites; Carboxylesterase; Carcinogens, Environmental; Cell Survival; Drug Resistance; Enzyme Induction; Enzyme Inhibitors; Green Fluorescent Proteins; HEK293 Cells; Hep G2 Cells; Humans; Inactivation, Metabolic; Marine Toxins; Microcystins; Nitrophenols; Organic Anion Transporters, Sodium-Independent; Recombinant Fusion Proteins; Recombinant Proteins; Solute Carrier Organic Anion Transporter Family Member 1B3; Substrate Specificity