The stereospecific incorporation of fenoprofen into rat hepatocyte and adipocyte triacylglycerols

Benedetta C. Sallustio, Peter J. Meffin, Kathleen M. Knights

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    64 Citations (Scopus)

    Abstract

    The formation of triacylglycerols containing fenoprofen was studied in rat isolated adipocytes and hepatocytes incubated with [3H]glycerol and R or S fenoprofen. In both hepatocytes and adipocytes there was a high-affinity enzymatic process for the synthesis of triacylglycerol containing fenoprofen which was stereospecific for the R enantiomer. The apparent Km values for R fenoprofen were 1.0 μM in adipocytes and 2.8 μM in hepatocytes. These results are consistent with the proposed stereospecific formation of R-2-arylpropionyl-CoA thioesters resulting in the stereospecific formation of R-tri-acylglycerol at clinically relevant unbound fenoprofen concentrations. In isolated hepatocytes, but not adipocytes, a second low-affinity enzymatic process for the synthesis of triacylglycerol containing fenoprofen was also observed. However, this process (Km = 3780 μM) occurred at concentrations much higher than those found in man with usual doses.

    Original languageEnglish
    Pages (from-to)1919-1923
    Number of pages5
    JournalBiochemical Pharmacology
    Volume37
    Issue number10
    DOIs
    Publication statusPublished - 15 May 1988

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