Mercury is a widespread environmental and industrial pollutant. It is known that mercury may cause accidental and occupational exposures and consequential damage in various organs in human. The kidney is the main target sites of mercury toxicity. Our previous study demonstrated that organic cation transporters (OCTs) mediated cadmium uptake into renal proximal tubular cells. Thus it was hypothesized that the environmental contaminant Hg(2+) (as HgCl(2+)) would be uptaken into renal proximal tubular cells via OCT1 and OCT2. Uptakes of 3H-MPP+ into Chinese hamster ovary cells stably expressing OCT1 and OCT2 were reduced in a concentration-dependent manner by HgCl2, with an IC50 of 19 and 10 µM, respectively. The inhibitory mechanism of OCT1 and OCT2 were competitive inhibition as revealed by kinetic study. Inhibition of OCT1 and OCT2 by OCT inhibitors reduced Hg intracellular accumulation and subsequently reduced HgCl2-induced cytotoxicity. Taken together, OCT1 and OCT2 may be the potential to get to prevent nephrotoxicity indyced by mercury.
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