异烟肼摄取与其对结核分枝杆菌体内分枝菌酸合成作用之间的关系。
Relationship between the uptake of isoniazid and its action on in vivo mycolic acid synthesis in Mycobacterium tuberculosis.
作者信息
Wang L, Takayama K
出版信息
Antimicrob Agents Chemother. 1972 Dec;2(6):438-41. doi: 10.1128/AAC.2.6.438.
Abstract
A direct relationship was established between the rate of uptake of isoniazid and the action of this drug on in vivo mycolic acid synthesis in Mycobacterium tuberculosis H37Ra. The rate of uptake of isoniazid increased linearly with its external concentration and appeared to reach a maximal value of 52 pmoles per hr per 10(9) cells at an external concentration of about 13 mum. Correspondingly, the rate of inhibition of mycolic acid synthesis increased with the rise in the rate of uptake of the drug. A 50% inhibition of mycolic acid synthesis occurred when the uptake of isoniazid reached 5.2 pmoles per 10(9) cells. Calculations showed that this level of drug uptake represents an internal cellular concentration of 9 mum. These results show clearly that the action of isoniazid on the mycolate synthetase system of M. tuberculosis is rapid and that this enzyme system is highly sensitive to the drug.
摘要
已确定异烟肼的摄取速率与其对结核分枝杆菌H37Ra体内分枝菌酸合成的作用之间存在直接关系。异烟肼的摄取速率随其外部浓度呈线性增加，在外部浓度约为13μM时，似乎达到每10⁹个细胞每小时52皮摩尔的最大值。相应地，分枝菌酸合成的抑制速率随着药物摄取速率的增加而增加。当异烟肼的摄取量达到每10⁹个细胞5.2皮摩尔时，分枝菌酸合成受到50%的抑制。计算表明，这种药物摄取水平代表细胞内浓度为9μM。这些结果清楚地表明，异烟肼对结核分枝杆菌的分枝菌酸合成酶系统的作用迅速，并且该酶系统对该药物高度敏感。
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