Inhibitory Effect of Melinamide on Cholesterol Solubility in Mixed Micellar Solution of Sodium Taurocholate

The inhibitory effect of melinamide, N-(α-methylbenzyl)-linoleamide, on cholesterol solubility in a mixed micellar solution of sodium taurocholate was investigated in vitro by the solubility method. At pH 7.4, melinamide decreased the amount of cholesterol by 30-40% without influencing the concentra...

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Veröffentlicht in:Chemical & pharmaceutical bulletin 1986/10/25, Vol.34(10), pp.4273-4279
Hauptverfasser: NAKAJIMA, TAKESHI, NATORI, KAZUICHI, HIROHASHI, TOSHIYUKI, AONO, SHUNJI
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Sprache:eng
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Zusammenfassung:The inhibitory effect of melinamide, N-(α-methylbenzyl)-linoleamide, on cholesterol solubility in a mixed micellar solution of sodium taurocholate was investigated in vitro by the solubility method. At pH 7.4, melinamide decreased the amount of cholesterol by 30-40% without influencing the concentration of oleic acid in bile salt-rich micelles with a molar ratio of more than 10 : 10 : 5 of bile salt : oleic acid : monolein, while it had no effect on oleic acid-monolein-rich micelles. Further, the effect of melinamide was independent of the pH of the medium. Melinamide seems to exhibit its effect as a result of releasing cholesterol from the micellar phase. On the other hand, it is assumed that neomycin reduces the amount of cholesterol by destroying micellar structure, as it was shown to completely eliminate oleic acid as well as cholesterol from micellar solution.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.34.4273