Sajbidor J, Lamacka M, Baláz S, Huong L M, Ciesarova Z
Department of Biochemical Technology, Chemical Faculty, Slovak Technology University, Bratislava, Slovak Republic.
J Pharm Pharmacol. 1998 Mar;50(3):297-301. doi: 10.1111/j.2042-7158.1998.tb06864.x.
The toxicity of fenpropimorph and seven newly synthesized analogues against Saccharomyces cerevisiae has been determined in liquid media. The inhibitory effect of the most efficient derivative is 120 times more than that of standard fenpropimorph. The non-linear relationship between hydrophobicity and toxicity indicates that the binding of the compounds to the receptors does not differ and so the differences in toxicity reflect changes in the rate of metabolism. The presence of inhibitors in the fermentation medium resulted in a reduction in harvested biomass and lipid yield, and changes in sterol composition -- the amount of ergosterol decreased whereas the amounts of lanosterol, dihydroergosterol and squalene increased. The toxicity of the compounds was most influenced by their lipophilicity. Use of this information could lead to development of more potent ergosterol inhibitors.
已在液体培养基中测定了粉唑醇及其七种新合成类似物对酿酒酵母的毒性。最有效衍生物的抑制作用比标准粉唑醇高120倍。疏水性与毒性之间的非线性关系表明,这些化合物与受体的结合并无差异,因此毒性差异反映了代谢速率的变化。发酵培养基中存在抑制剂会导致收获的生物量和脂质产量降低,以及甾醇组成发生变化——麦角甾醇含量减少,而羊毛甾醇、二氢麦角甾醇和角鲨烯含量增加。这些化合物的毒性受其亲脂性影响最大。利用这些信息可能会开发出更有效的麦角甾醇抑制剂。