Abstract：
BACKGROUND AND OBJECTIVES:Previous studies reported that tapentadol-sulfate represented one of the major metabolites of tapentadol excreted in urine. The current study aimed to identify the human cytosolic sulfotransferases (SULTs) that is(are) capable of sulfating tapentadol and to examine whether human cells and human organ specimens are capable of sulfating tapentadol. METHODS:Thirteen human SULTs, previously expressed and purified, as well as human organ cytosols, were analyzed for tapentadol-sulfating activity using an established sulfotransferase assay. Cultured HepG2 human hepatoma cells and Caco-2 human colon carcinoma cells were labeled with [35S]sulfate in the presence of different concentrations of tapentadol. RESULTS:Three of the thirteen human SULTs, SULT1A1, SULT1A3, and SULT1C4, were found to display sulfating activity toward tapentadol. Kinetic analysis revealed that SULT1A3 displayed the highest catalytic efficiency in mediating the sulfation of tapentadol, followed by SULT1A1 and SULT1C4. Using cultured HepG2 and Caco-2 cells, the generation and release of sulfated tapentadol under metabolic conditions was demonstrated. Moreover, of the four human organ specimens (kidney, liver, lung, and small intestine) tested, the cytosols prepared from small intestine and liver showed significant tapentadol-sulfating capacity (at 0.0203 and 0.0054 nmol/min/mg, respectively). CONCLUSION:Taken together, the results derived from the current study provided a molecular basis underlying the sulfation of tapentadol in humans.
journal_name
Eur J Drug Metab Pharmacokinetjournal_title
European journal of drug metabolism and pharmacokineticsauthors
Bairam AF,Rasool MI,Kurogi K,Liu MCdoi
10.1007/s13318-016-0392-8subject
Has Abstractpub_date
2017-10-01 00:00:00pages
793-800issue
5eissn
0378-7966issn
2107-0180pii
10.1007/s13318-016-0392-8journal_volume
42pub_type
杂志文章abstract：:The influence of phenobarbital pretreatment on liver concentration of digitoxin and its metabolites was studied in guinea-pigs after i.p. administration of the cardiac glycoside. During the first hour an increase in liver uptake was observed in pretreated animals. The differences detected in the hepatic subcellular di...
journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
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