Greenspan M D, Germershausen J I
J Bacteriol. 1973 Feb;113(2):847-55. doi: 10.1128/jb.113.2.847-855.1973.
Halofenate-free acid (HFA) inhibited the growth of Saccharomyces cerevisiae by 50% at a concentration of 0.34 mm. This inhibitory effect was prevented by addition of either oleate or acetate, but not by pyruvate. When cell growth was supported by oleate, HFA inhibited the incorporation of radioactive carbon from glucose-U-(14)C or pyruvate-2-(14)C into fatty acids and sterols. The incorporation of radioactive carbon into fatty acids and sterols from acetate-2-(14)C was unaffected by the compound. When cell growth was supported by either oleate or acetate, HFA inhibited the conversion of pyruvate-1-(14)C to (14)CO(2). These results suggest that HFA inhibits the conversion of pyruvate to acetate in yeast. Partially purified yeast pyruvate dehydrogenase was inhibited 50% by 5.5 mm HFA; however, the concentration required for 50% inhibition was considerably reduced when the enzyme was preincubated with the compound at room temperature. In a similar manner, the hypolipidemic agent clofibrate-free acid inhibited the growth of yeast by 50% at 3.0 mm. This inhibition was also prevented by acetate and not by pyruvate. In addition, clofibrate-free acid inhibited partially purified pyruvate dehydrogenase by 50% at a concentration of 37.0 mm.
无卤泛酸盐(HFA)在浓度为0.34 mM时可抑制酿酒酵母生长50%。添加油酸或乙酸盐可阻止这种抑制作用,但丙酮酸盐不能。当细胞生长由油酸支持时,HFA抑制放射性碳从葡萄糖-U-(14)C或丙酮酸-2-(14)C掺入脂肪酸和甾醇。放射性碳从乙酸盐-2-(14)C掺入脂肪酸和甾醇不受该化合物影响。当细胞生长由油酸或乙酸盐支持时,HFA抑制丙酮酸-1-(14)C转化为(14)CO₂。这些结果表明HFA抑制酵母中丙酮酸向乙酸盐的转化。部分纯化的酵母丙酮酸脱氢酶被5.5 mM HFA抑制50%;然而,当酶在室温下与该化合物预孵育时,50%抑制所需的浓度显著降低。以类似方式,降血脂药物无氯贝酸在3.0 mM时可抑制酵母生长50%。这种抑制作用也可被乙酸盐阻止,而丙酮酸盐不能。此外,无氯贝酸在浓度为37.0 mM时可抑制部分纯化的丙酮酸脱氢酶50%。