Bleomycin hydrochloride
(Synonyms: 盐酸博来霉素) 目录号 : GC60089
Bleomycinhydrochloride是一种DNA损伤剂，抑制DNA合成。Bleomycinhydrochloride是一种抗肿瘤抗生素(antibiotic)。
Cas No.:67763-87-5
Sample solution is provided at 25 µL, 10mM.
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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]。
References:
[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.
| Cas No. | 67763-87-5 | SDF | |
| 别名 | 盐酸博来霉素 | ||
| Canonical SMILES | NC(C[C@H](NC[C@@H](N)C(N)=O)C1=NC(N)=C(C)C(C(N[C@H](C(N[C@@H](C)[C@@H]([C@@H](C)C(N[C@@H](C(NCCC2=NC(C3=NC(C(NCCC[S+](C)C)=O)=CS3)=CS2)=O)[C@H](O)C)=O)O)=O)C(C4=CNC=N4)O[C@@H]5[C@]([H])(O[C@@H]6[C@@H](O)[C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O6)[C@H](O)[C@@H](O)[C@@H](CO)O5)=O)=N1)=O.[Cl-] | ||
| 分子式 | C55H84ClN17O21S3 | 分子量 | 1451 |
| 溶解度 | DMSO: 125 mg/mL (86.15 mM) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.6892 mL | 3.4459 mL | 6.8918 mL |
| 5 mM | 0.1378 mL | 0.6892 mL | 1.3784 mL |
| 10 mM | 0.0689 mL | 0.3446 mL | 0.6892 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Amphiregulin attenuates bleomycin-induced pneumopathy in mice
Am J Physiol Lung Cell Mol Physiol 2010 Feb;298(2):L131-8.PMID:19915156DOI:10.1152/ajplung.90576.2008.
Amphiregulin, an EGF receptor (EGFR) ligand, is essential for epithelial development in various organs. A recent report suggested that amphiregulin acts as a protective factor in a liver injury model. Little is known about the roles of amphiregulin in lung injury and pulmonary fibrosis. The purpose of the present study was to investigate the role of amphiregulin in an experimental model of bleomycin-induced pneumopathy in mice. C57BL/6 mice were administered a Bleomycin hydrochloride solution intratracheally. Recombinant human amphiregulin was injected intraperitoneally at 6, 8, 10, and 12 days after the bleomycin instillation. The grades of inflammation and fibrosis were assessed histologically and biochemically, and the numbers of apoptotic cells were counted after TdT-mediated dUTP nick end labeling (TUNEL) staining in the lung tissues. We also examined downstream survival signals of EGFR, namely phosphorylated Akt and phosphorylated Erk, in lung tissues by Western blotting analysis and immunohistochemistry. Expression of intrinsic amphiregulin was increased in murine lung tissues after bleomycin instillation. Administration of recombinant amphiregulin improved the survival rate and suppressed the degrees of inflammation and fibrosis and the number of TUNEL-positive cells in lung tissues. Amphiregulin treatment enhanced the activation of Akt and Erk in lung epithelial cells. Amphiregulin may play a protective role in bleomycin-induced pneumopathy in mice, probably through the activation of survival signals. Administration of amphiregulin may be a novel therapeutic strategy against lung injury and fibrosis.
Synergistic anticancer activity of dietary tea polyphenols and Bleomycin hydrochloride in human cervical cancer cell: Caspase-dependent and independent apoptotic pathways
Chem Biol Interact 2016 Mar 5;247:1-10.PMID:26800624DOI:10.1016/j.cbi.2016.01.012.
Bleomycin is a chemotherapeutic agent that is frequently used in the treatment of various cancers. Bleomycin causes serious adverse effects via antioxidant defense abnormalities against reactive oxygen species (ROS). However, the current cervical cancer monodrug therapy strategy has failed to produce the expected outcomes; hence, combinational therapies are gaining great interest. Tea polyphenols are also effective antioxidative and chemo-preventive agents. However, the combined effect of tea polyphenol (TPP) and bleomycin (BLM) against cervical cancer remains unknown. In this study, we focused on the potential of TPP on BLM anticancer activity against cervical cancer cells. Cervical cancer cells (SiHa) were treated with various concentrations of TPP, BLM and TPP combined with BLM (TPP-BLM), and their effects on cell growth, intracellular reactive oxygen species, poly-caspase activity, early apoptosis and the expression of caspase-3, caspase-8 and caspase-9, Bcl-2 and p53 were assessed. The MTT assay revealed that the SiHa cells were less sensitive to growth inhibition by TPP treatment compared with both BLM and the combination therapy. Nuclear staining indicated that exposure to TPP-BLM increased the percentage of apoptotic nuclei compared with a mono-agent treatment. Caspase activation assay demonstrated that proportion of early and late apoptotic/secondary necrotic cells was higher in the cells treated with the combination therapy than in those treated with either TPP or BLM alone. The TPP-BLM treatment synergistically induced apoptosis through caspase-3, caspase-8 and caspase-9 activation, Bcl-2 upregulation and p53 overexpression. This study suggests that TPP-BLM may be used as an efficient antioxidant-based combination therapy for cervical cancer.
An experimental study of the antitumour effect of Bleomycin hydrochloride microcapsules
J Microencapsul 1986 Oct-Dec;3(4):283-91.PMID:2468754DOI:10.3109/02652048609021798.
The controlled release behaviour of Bleomycin hydrochloride microcapsules was investigated by an in vitro dissolution method and an in vivo antitumour test. Bleomycin hydrochloride microcapsules prepared using the highest cooling rate exhibited sustained release characteristics and its release rate obeyed a nearly zero order release kinetics. Microcapsules containing Bleomycin hydrochloride were locally injected into the solid tumour of uterine cervix carcinoma bearing nude mice. Tumour growth was markedly inhibited by treatment using Bleomycin hydrochloride microcapsules compared to the control group and the group receiving direct local administration of Bleomycin hydrochloride. No significant differences in the changes of body weight after treatment were found between the control group and the treated group. These results suggest that controlled release microcapsules may be applicable as a drug carrier for delivery of antitumour agents in cancer chemotherapy.
Serotonin Exhibits Accelerated Bleomycin-Induced Pulmonary Fibrosis through TPH1 Knockout Mouse Experiments
Mediators Inflamm 2018 Apr 16;2018:7967868.PMID:29849496DOI:10.1155/2018/7967868.
Background: Pulmonary fibrosis is a chronic progressive fibrosis interstitial lung disease that is characterized by inflammatory infiltration and fibrotic changes. 5-Hydroxytryptamine (5-HT) is an important regulatory factor in inflammation, immunomodulation, and fibrosis. The aim of this study was to investigate the role of 5-HT in bleomycin- (BLM-) induced pulmonary fibrosis through wild-type C57BL/6 (WT) and TPH1 knockout (KO) mouse experiments. Methods: The mice were grouped as follows: WT control group, KO control group, WT BLM group, and KO BLM group. Mice were administrated Bleomycin hydrochloride through intratracheal instillation to induce pulmonary fibrosis. Mice were sacrificed 0, 7, 14, and 21 days after modeling, and bronchoalveolar lavage fluid (BALF) and lung tissues were collected to determine the severity of fibrotic changes. Results: The results showed that the weight loss of mice in the WT BLM group was more severe than that in the KO BLM group. H&E and Sirius Red staining revealed that 5-HT markedly aggravated histological damage and fibrotic changes in the lung. Significantly lower levels of hydroxyproline, Ashcroft fibrosis score, total BALF protein and cells, BALF tumor necrosis factor- (TNF-) α and interleukin- (IL-) 6, TNF-α and IL-6 mRNA, malondialdehyde (MDA), and myeloperoxidase- (MPO-) positive cells in the lung tissues, and fibrosis-associated proteins were discovered in the mice from the KO BLM group compared with the WT BLM group. Conclusion: 5-HT aggravated pulmonary fibrosis mainly by promoting the inflammation, exudation of proteins and cells, oxidative stress, and upregulation of fibrosis-associated genes in the lung tissues.
Influence of coacervation-inducing agents and cooling rates on the preparation and in vitro release of Bleomycin hydrochloride microcapsules
J Microencapsul 1985 Apr-Jun;2(2):91-101.PMID:2475603DOI:10.3109/02652048509031553.
Two types of coacervation-inducing agents (EVA, PIB) and three cooling rates (0.01998, 0.03482 and 0.06725 degrees C/min) affecting the preparation, micromeritic and drug release properties of Bleomycin hydrochloride microcapsules were investigated. Particle size distribution of microcapsules induced by EVA significantly depended on the cooling rate, but that induced by PIB was independent of the cooling rate. Higher viscosity of PIB led to a smaller particle size of microcapsules than when EVA was used. The surface topography of the microcapsules for both types of coacervation-inducing agents was obviously different. We found that the release behaviour of Bleomycin hydrochloride from the microcapsules also depended on the type of coacervation-inducing agent and the cooling rate. In general, the slower the cooling rate the more prolonged the release of the drug. Higuchi matrix model was followed for Bleomycin hydrochloride released from the microcapsules. T50 of both types of microcapsules decreased with the increase of the cooling rate. To simulate the absorption behaviour of the GI tract, the continuous flow dialysis method was modified for drug release from the microcapsules. The data indicate that the diffusion of the dissolution medium and dissolved drug through the ethylcellulose wall of the microcapsules is the rate-limiting step before dialysis. This also implies that the release rate of the drug from dosage form significantly determined the absorption in the GI tract.