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Boibessot I Tettey JN Skellern GG Watson DG Grant MH 《Journal of veterinary pharmacology and therapeutics》2006,29(6):547-553
Little is known about the metabolism and mechanism of action of the trypanocide, isometamidium (ISM), the major drug used for prophylaxis of trypanosomiasis. We have investigated its metabolism and distribution in isolated rat hepatocytes using liquid chromatography-mass spectrometry and confocal laser scanning microscopy (CLSM). Two putative metabolites were formed, which were proposed to be a mono-acetyl derivative and an oxidized metabolite (SII). This is the first demonstration of the hepatic metabolism of ISM, as previous in vivo studies were hampered by dose-limiting toxicity and insensitive analytical methods. The intrinsic fluorescence of the drug enabled its intracellular uptake to be followed by CLSM. It is taken up rapidly into the nucleolus, nuclear membrane and endoplasmic reticulum within 5 min, and retained in the nucleus for at least 24 h. Persistent binding of ISM to cellular macromolecules may contribute to its prophylactic effect in vivo. Pretreatment of rats with 3-methylcholanthrene, phenobarbitone (PB) or the widely used pyrethroid pesticide, deltamethrin, resulted in an increase in metabolism of ISM to the proposed SII after 1 h incubation with hepatocytes. 3-methylcholanthrene was the most potent inducer, causing a maximal 19.5-fold induction of SII formation after exposure of hepatocytes to ISM for 1 h compared with formation by control hepatocytes. In comparison, at the 1 h timepoint deltamethrin pre-treatment caused a 10.2-fold induction, and PB only 8.2 fold. 相似文献
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Aidoo Owusu Fordjour Cunze Sarah Guimapi Ritter A. Arhin Linda Ablormeti Fred Kormla Tettey Elizabeth Dampare Frank Afram Yayra Bonsu Osei Obeng Joshua Lutuf Hanif Dickinson Matthew Yankey Ndede 《植物病害和植物保护杂志》2021,128(5):1313-1325
Journal of Plant Diseases and Protection - Coconut is recognized for its popularity in contributing to food and nutritional security. It generates income and helps to improve rural livelihood.... 相似文献
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