Bleomycinhydrochloride是一种DNA损伤剂，抑制DNA合成。Bleomycinhydrochloride是一种抗肿瘤抗生素(antibiotic)。
Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic[1].
Bleomycin is chosen as the best-studied micronucleus inducers in human lymphocytes with different mechanisms of genotoxicity. The most frequent Bleomycin-induced DNA lesions are single and double strand breaks and single apuinic/apyrimidinic sites. At the same time Bleomycin is true radiomimetic compound, resembling almost completely the genetic effect of ionizing radiation[1]. The IC50 value of Bleomycin for UT-SCC-19A cell line is 4.0±1.3 nM. UT-SCC-12A and UT-SCC-12B are both more resistant to Bleomycin; IC50 values are 14.2±2.8 nM and 13.0±1.1 nM, respectively[2].
Bleomycin treatment (3.5-4.0 mg/kg; intra-tracheal) on day 0, body weights decreases by day 4 then increases by Day 7 through the end of the study[3].Bleomycin (3.5-4.0 mg/kg; intra-tracheal) produces a statistically significant increase in lung hydroxyproline levels, and also increases right caudal lung lobe mass[3]. Animal Model: Male Fischer 344 rats, 8-10 week old, weighing 150-250 g[3]
Bleomycin hydrochloride是DNA合成抑制剂。Bleomycin hydrochloride是一种DNA损伤剂。Bleomycin hydrochloride是一种抗肿瘤抗生素[1]。
Bleomycin被选为最好研究的微核诱导剂之一，具有不同的遗传毒性机制。最常见的Bleomycin诱导的DNA损伤是单链和双链断裂以及单个无嘌呤/嘧啶位点。同时，Bleomycin是真正的放射模拟化合物，几乎完全类似于电离辐射的遗传效应[1]。Bleomycin对UT-SCC-19A细胞系的IC50值为4.0±1.3 nM。UT-SCC-12A和UT-SCC-12B对Bleomycin都更具有抗性；其IC50值分别为14.2±2.8 nM和13.0±1.1 nM[2]。
Bleomycin治疗（3.5-4.0 mg/kg；经气管内给药）在第0天进行，到第4天体重降低，然后在第7天到研究结束时开始增加[3]。Bleomycin（3.5-4.0 mg/kg；经气管内给药）会导致肺羟脯氨酸水平显著增加，并且会增加右下肺叶的质量[3]。动物模型：雄性Fischer 344大鼠，8-10周龄，体重150-250 g[3]。
参考文献:
[1]. Hovhannisyan G, et al. Comparative analysis of individual chromosome involvement in micronuclei induced by bleomycin in human leukocytes. Mol Cytogenet. 2016 Jun 21;9:49.
[2]. Jaaskela-Saari HA, et al. Squamous cell cancer cell lines: sensitivity to bleomycin and suitability for animal xenograft studies. Acta Otolaryngol Suppl. 1997;529:241-4.
[3]. Corboz MR, et al. Therapeutic administration of inhaled INS1009, a treprostinil prodrug formulation, inhibits bleomycin-induced pulmonary fibrosis in rats. Pulm Pharmacol Ther. 2018 Apr;49:95-103.
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