Bioscience, Biotechnology, and Biochemistry
Online ISSN : 1347-6947
Print ISSN : 0916-8451
Nicardipine and Nifedipine Inhibit Fatty Acid Desaturases in Rat Liver Microsomes
Hiroshi KAWASHIMAKengo AKIMOTOSaeree JAREONKITMONGKOLNorifumi SHIRASAKASakayu SHIMIZU
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JOURNAL FREE ACCESS

1996 Volume 60 Issue 10 Pages 1672-1676

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Abstract

Nicardipine and nifedipine, Ca channel blockers, inhibited rat liver microsomal desaturases, though verapamil, methoxyverapamil, cinnarizine, flunarizine, and diltiazem did not. However, nicardipine and nifedipine apparently did not inhibit the fungal desaturation in Mortierella alpina 1S-4. Nicardipine inhibited rat liver microsomal Δ5 desaturase specifically (50% inhibitory concentration, 170μM), and nifedipine inhibited Δ6 desaturase specifically (78μM). The inhibition by nicardipine and nifedipine is uncompetitive, the Ki values for Δ5 and Δ6 desaturases being 62 and 44μM, respectively.

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