阿西维辛在无血清培养基中抑制 fasciculata 克氏锥虫的生长，并在体内使氨甲酰磷酸合成酶 II 失活。

Acivicin inhibits Crithidia fasciculata growth in a serum-free medium and inactivates carbamoyl-phosphate synthetase II in vivo.

Aoki T, Oya H

Department of Parasitology, Juntendo University School of Medicine, Tokyo, Japan.

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1988;90(2):391-6.

Abstract

Crithidia fasciculata was grown in a serum-free medium. 2. Twenty-six hours after addition of 2, 5, 20, 50, and 150 microM acivicin to logarithmically growing organisms, cell counts were decreased to 46, 23, 14, 9.1, and 8.6% of the control, respectively. 3. Guanosine plus cytidine (0.1 mM each) provided complete protection against growth inhibition by 5 microM acivicin. 4. Cells exposed to 10 microM acivicin showed a time-dependent, irreversible inactivation of L-glutamine-dependent carbamoyl-phosphate synthetase II activity; ammonia-dependent synthetase II activity was increased up to 34% of the control. 5. Glutamine (20 mM) protected the enzyme from inactivation in vivo. 6. These results indicate that acivicin acts as an affinity analog of L-glutamine in vivo as it does in vitro.

摘要

fasciculata 利什曼原虫在无血清培养基中培养。2. 在对数生长期的生物中加入2、5、20、50和150微摩尔阿西维辛26小时后，细胞计数分别降至对照的46%、23%、14%、9.1%和8.6%。3. 鸟苷加胞苷（各0.1毫摩尔）可完全保护细胞免受5微摩尔阿西维辛的生长抑制作用。4. 暴露于10微摩尔阿西维辛的细胞显示出L-谷氨酰胺依赖性氨甲酰磷酸合成酶II活性呈时间依赖性、不可逆失活；氨依赖性合成酶II活性增加至对照的34%。5. 谷氨酰胺（20毫摩尔）在体内保护该酶不被失活。6. 这些结果表明，阿西维辛在体内的作用与在体外一样，是L-谷氨酰胺的亲和类似物。