Jaju M, Jaju M, Ahuja Y R
Mutat Res. 1982 Mar;101(1):57-66. doi: 10.1016/0165-1218(82)90165-3.
Cephaloridine is a semi-synthetic broad-spectrum bactericidal antibiotic derived from cephalosporin C. The drug was tested for its clastogenic effects on human chromosomes in vitro at various concentrations and for various periods of treatment (24, 48, 72 h) in 72-h lymphocyte cultures. 2 concentrations of the drug used in the tests (20 and 60 micrograms/ml) were similar to those found in the plasma of individuals after receipt of therapeutic doses of 500 mg and 2 g, respectively. 2 other concentrations tested were either below (10 micrograms/ml) or above (120 micrograms/ml) the plasma level. Control cultures were set up simultaneously for each batch of experimental cultures. The aberration frequency was increased with increasing concentration of the drug, irrespective of the duration of the exposure. In other words, there was a dose-effect relationship. No increase in chromosomal aberrations was observed with lower doses of 10 and 20 micrograms/ml. Significant increases were seen with higher doses of 60 and 120 micrograms/ml. Aberrations were mostly of the chromatid type. The results show that cephaloridine is clastogenic at the upper levels of permissible therapeutic doses.
头孢菌素I是一种从头孢菌素C衍生而来的半合成广谱杀菌抗生素。在72小时淋巴细胞培养中,对该药物在体外不同浓度和不同处理时间(24、48、72小时)下对人类染色体的致断裂作用进行了测试。测试中使用的2种药物浓度(20和60微克/毫升)分别与接受500毫克和2克治疗剂量后个体血浆中的浓度相似。测试的另外2种浓度要么低于(10微克/毫升)要么高于(120微克/毫升)血浆水平。每批实验培养物同时设置对照培养物。无论暴露时间长短,畸变频率都随着药物浓度的增加而增加。换句话说,存在剂量效应关系。在10和20微克/毫升的较低剂量下未观察到染色体畸变增加。在60和120微克/毫升的较高剂量下观察到显著增加。畸变大多为染色单体类型。结果表明,在允许治疗剂量的上限水平时,头孢菌素I具有致断裂作用。