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https://doi.org/10.2478/10004-1254-60-2009-1895

D-Amphetamine Toxicity in Freshly Isolated Rat Hepatocytes: a Possible Role of CYP3A

Vessela Vitcheva ; Laboratory of Drug Metabolism and Drug Toxicity, Department of Pharmacology, Pharmacotherapy,and Toxicology, Faculty of Pharmacy, Medical University Sofia, Sofia, Bulgaria
Magdalena Kondeva-Burdina ; Laboratory of Drug Metabolism and Drug Toxicity, Department of Pharmacology, Pharmacotherapy, and Toxicology, Faculty of Pharmacy, Medical University Sofi a, Sofi a, Bulgaria
Mitka Mitcheva ; Laboratory of Drug Metabolism and Drug Toxicity, Department of Pharmacology, Pharmacotherapy, and Toxicology, Faculty of Pharmacy, Medical University Sofi a, Sofi a, Bulgaria


Puni tekst: engleski pdf 87 Kb

str. 139-145

preuzimanja: 1.072

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Sažetak

The aim of this study was to trace D-amphetamine toxicity in isolated rat hepatocytes and to elucidate a possible involvement of CYP3A in the mechanisms of its toxicity. To this end, male Wistar rats were treated with nifedipine (5 mg kg-1 i.p., 5 days), a substrate and inducer of CYP3A. Hepatocytes isolated from nifedipine-treated and control rats were incubated with D-amphetamine at a concentration of 100 µmol L-1, which was determined to be an average toxic concentration (TC50) for the compound. To evaluate the possible toxic effects of D-amphetamine on freshly isolated rat hepatocytes, we assessed the following parameters: cell viability, lactate dehydrogenase (LDH) activity, and glutathione (GSH). The results showed that nifedipine potentiated amphetamine cytotoxicity in vitro, as follows: cell viability dropped by 65 % (p<0.001), GSH by 80 % (p<0.001), and LDH activity increased by 190 % (p<0.001). To clarify the role of nifedipine in amphetamine cytotoxicity, we used amiodarone, a substrate and an inhibitor of CYP3A. Pre-incubation of nifedipine-treated hepatocytes with amiodarone (14 µmol L-1) significantly lowered amphetamine cytotoxicity. Our results confirmed the toxicity of D-amphetamine in isolated rat hepatocytes and the involvement of CYP3A in its metabolism and hepatotoxicity.

Ključne riječi

amiodarone; amphetamine cytotoxicity; nifedipine

Hrčak ID:

38380

URI

https://hrcak.srce.hr/38380

Datum izdavanja:

12.6.2009.

Podaci na drugim jezicima: hrvatski

Posjeta: 2.330 *