Evaluation of in vitro biotransformation of propranolol with HPLC, MS/MS, and two bioassays

Environmental Toxicology
G Nałecz-JaweckiJ Sawicki

Abstract

The majority of human drugs enter aquatic systems after ingestion and subsequent excretion in the form of parent compounds and metabolites. Environmental exposure to drug metabolites has not been reported so far. The goal of the present study was to apply the in vitro method of biotransformation of compounds with S9 fraction to the ecotoxicological analysis. beta-adrenoceptor antagonist propranolol was metabolized with S9 rat liver fraction. The parent compound was quantified with HPLC, and the metabolites were identified with QToF MS. Propranolol was metabolized rapidly, during the first hour its level decreased by 80 and 50% of the initial 20 and 100 mg L(-1), respectively. Ten peaks were observed on the HPLC-RF chromatogram. Four peaks were identified with QToF MS/MS propranolol (m/z = 260), N-desisopropylpropranolol (m/z = 218), hydroxypropranolol (m/z = 276), and hydroxy N-desisopropranolol glycol (m/z = 235). Then the ecotoxicity of the reaction mixture was studied with two bioassays Spirotox with the protozoan Spirostomum ambiguum and Thamnotoxkit F with the anostracean crustacean Thamnocephalus platyurus. Propranolol is twofolds more toxic to Spirotox than to Thamnotoxkit F with 24 h-EC50 = 1.77 mg L(-1) and 24 h-LC50 =...Continue Reading

References

Jul 1, 1983·Journal of Pharmaceutical Sciences·B M SilberS Riegelman
Jul 13, 2002·Archives of Environmental Contamination and Toxicology·D B HuggettD Schlenk
Oct 22, 2003·The Journal of Pharmacology and Experimental Therapeutics·I Tong Mak, William B Weglicki
Sep 15, 2004·The Science of the Total Environment·D AshtonK V Thomas
Sep 20, 2005·Chemosphere·Colleen M Flaherty, Stanley I Dodson
Nov 1, 2005·Aquatic Toxicology·Karl FentDaniel Caminada
Jan 18, 2006·Forensic Science International : Synergy·Robert D Johnson, Russell J Lewis
Jun 10, 2006·The Science of the Total Environment·Mark CraneTatiana Boucard

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Citations

Apr 17, 2014·Environmental Science & Technology·Justin T JasperDavid L Sedlak
Aug 31, 2010·Environmental Science & Technology·Damian E HelblingKathrin Fenner
Aug 10, 2010·Environmental Science & Technology·Damian E HelblingKathrin Fenner
Apr 9, 2011·Environmental Science & Technology·Beate I Escher, Kathrin Fenner
Dec 10, 2016·Environmental Science & Technology·Yi ChenSteven T J Droge

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