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Sulfation of ractopamine and salbutamol by the human cytosolic sulfotransferases
- Source :
- Journal of Biochemistry. 152:275-283
- Publication Year :
- 2012
- Publisher :
- Oxford University Press (OUP), 2012.
-
Abstract
- Feed additives such as ractopamine and salbutamol are pharmacologically active compounds, acting primarily as β-adrenergic agonists. This study was designed to investigate whether the sulfation of ractopamine and salbutamol may occur under the metabolic conditions and to identify the human cytosolic sulfotransferases (SULTs) that are capable of sulfating two major feed additive compounds, ractopamine and salbutamol. A metabolic labelling study showed the generation and release of [(35)S]sulfated ractopamine and salbutamol by HepG2 human hepatoma cells labelled with [(35)S]sulfate in the presence of these two compounds. A systematic analysis using 11 purified human SULTs revealed SULT1A3 as the major SULT responsible for the sulfation of ractopamine and salbutamol. The pH dependence and kinetic parameters were analyzed. Moreover, the inhibitory effects of ractopamine and salbutamol on SULT1A3-mediated dopamine sulfation were investigated. Cytosol or S9 fractions of human lung, liver, kidney and small intestine were examined to verify the presence of ractopamine-/salbutamol-sulfating activity in vivo. Of the four human organs, the small intestine displayed the highest activity towards both compounds. Collectively, these results imply that the sulfation mediated by SULT1A3 may play an important role in the metabolism and detoxification of ractopamine and salbutamol.
- Subjects :
- Sulfotransferase
Dopamine
Biochemistry
Substrate Specificity
chemistry.chemical_compound
Cytosol
Sulfation
In vivo
Phenethylamines
Sulfur Isotopes
medicine
Humans
Albuterol
Molecular Biology
Sulfates
Chemistry
Regular Papers
Hep G2 Cells
General Medicine
Metabolism
Hydrogen-Ion Concentration
respiratory system
Small intestine
respiratory tract diseases
Ractopamine
Kinetics
medicine.anatomical_structure
Organ Specificity
Isotope Labeling
Salbutamol
Sulfotransferases
Sulfur
medicine.drug
Subjects
Details
- ISSN :
- 0021924X
- Volume :
- 152
- Database :
- OpenAIRE
- Journal :
- Journal of Biochemistry
- Accession number :
- edsair.doi.dedup.....22a794aa948bdad3a91ae7c55389e5ad