Summary
Caco-2, a human intestinal cell lines able to differentiate in long-term culture, has been used to assess the cytotoxicity of the β-agonists clenbuterol, salbutamol and isoxsuprine, also used at high doses to obtain lean meat in food producing animals, and to investigate the eventual in vitro formation of early conjugates of these compounds. For this purpose, the cells have been characterized for the activity of UDP-glucuronyltransferase, which is present and increase in the differentiated cells, and for the β-receptors’ binding characteristics, which are those of β1 and β2 subtypes. Isoxsuprine was shown to be the most toxic, followed by clenbuterol and salbutanol. Conjugates have been observed after incubation of the cells both with the lowest isoxsuprine and the highest salbutamol concentrations. No conjugates were detected in the case of clenbuterol.
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Stammati, A., Badino, P., De Angelis, I. et al. In vitro toxicity and formation of early conjugates in Caco-2 cell line treated with clenbuterol, salbutamol and isoxsuprine. European Journal of Drug Metabolism and Pharmacokinetics 22, 173–178 (1997). https://doi.org/10.1007/BF03189802
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DOI: https://doi.org/10.1007/BF03189802