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基本信息
博來霉素鹽酸鹽
bleomycinchlorhydrate
BLEOMYCIN HYDROCHLORIDE
BLEOMYCIN HYDROCHLORIDES
BleomycinA5/Pingyangmycin
BleoMycin A4A5 Hydrochloride
Bleomycin hydrochloride USP/EP/BP
物理化學(xué)性質(zhì)
常見問題列表
1966年，日本微生物學(xué)家梅澤賓夫首先從輪枝鏈霉菌(Streptomyces vertillus)中分離到BLM。
1969年，日本BLM，在日本授權(quán)為抗腫瘤藥物。
1973年，日本BLM獲美國(guó)FDA許可用于臨床。目前已經(jīng)發(fā)現(xiàn)了十余種博來霉素的天然成分，這些組分的機(jī)構(gòu)之間僅在其氨基取代側(cè)鏈上有所差別。
1969年，我國(guó)宋愛蘭等專家，在溫州平陽的南雁蕩山仙姑洞前的土壤中分離出一株鏈霉菌（編號(hào)72），被取名為“爭(zhēng)光霉素”，科研人員發(fā)現(xiàn)爭(zhēng)光霉素與日本博萊霉索成分和作用相近，對(duì)鱗癌療效更好，肺毒性反而低些。為了紀(jì)念這個(gè)菌種的產(chǎn)生地，后將爭(zhēng)光霉素更名為平陽霉素(Ping yang mycin)，也稱為博萊霉素A5（Bleomycin A5），是博萊霉素家族成員之一。其產(chǎn)生菌定名為“輪枝鏈霉菌平陽變種(S. Verticillus var. pingyangensis)”。
1978年，國(guó)家食品藥品監(jiān)督管理（SFDA）授權(quán)平陽霉素用于臨床。
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. The IC 50 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; IC 50 values are 14.2±2.8 nM and 13.0±1.1 nM, respectively.
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.
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.
| Animal Model: | Male Fischer 344 rats, 8-10 week old, weighing 150-250?g |
| Dosage: | 3.5-4 mg/kg |
| Administration: | Intra-tracheal |
| Result: | Body weights decreased by day 4 then increased by Day 7 through the end of the study. |