Bleomycin Sulfate (mixture)
| 别名 | 博来霉素;争光霉素;奈拉滨;Blenmycins，硫酸博来霉素 |
| CAS | 9041-93-4/11056-06-7 |
| 分子式 | A2：C55H85N17O25S4 B2：C55H84N20O21S2 |
| 分子量 | A2：1512.62 B2：1425.51 3 |
| 储存条件 | 2-8°C |
| 纯度 | 1.5-2.0U/mg |
| 单位 | 瓶 |
| 生物活性 | Bleomycin sulfate是具有有效抗肿瘤活性的DNA合成抑制剂。博莱霉素（BLM）被选为人淋巴细胞中研究最好的微核（MN）诱导剂，具有不同的遗传毒性机制。最常见的博来霉素诱导的DNA损伤是单链和双链断裂和单个apuinic / apyrimidinic位点。同时博来霉素是真正的放射性模拟化合物，几乎完全类似于电离辐射的遗传效应。[1-4] |
| In Vitro | 硫酸博来霉素对UT-SCC-19A细胞系的IC50值为4.0±1.3nM。 UT-SCC-12A和UT-SCC-12B对博来霉素（BLM）更具抗性; IC50值分别为14.2±2.8 nM和13.0±1.1 nM [2]。与对照培养物相比，博来霉素（BLM）诱导异常细胞（即，显示至少一种像差的细胞）的百分比和每个细胞的染色体畸变频率显着增加（p <0.05）[3]。 |
| In Vivo | 与博来霉素（In-111-BLMC）组合的短程β发射放射性核素是SCC中的肿瘤靶向剂。在35天内，裸鼠体重增加2.8±0.6g。在肿瘤接种后25和35天，肿瘤体积分别为111±51mm 3和874±577mm 3。计算的倍增时间为3.86±0.76天。 SCC细胞系表现出对博来霉素的不同敏感性。我们的SCC肿瘤异种移植模型显示适合使用In-111-BLMC的放射化学治疗研究的快速生长。 In-111-BLMC在体内的摄取与增殖活性成正比，并且可以通过动物模型剂量计算预测具有高结合能力的肿瘤[2]。在博来霉素（BLM）处理后第7天和第14天，TGF-β1的信号显著强于对照组。在治疗后28天，TGF-β1信号稍微变弱。在博来霉素加Dex组的第7天和第14天，TGF-β1的信号也强于对照组。然而，在第28天，TGF-β1信号变弱并且比对照组的水平稍强。通过比较平均IOD值[4]给出所有结果。 |
| 靶点 | DNA/RNA Synthesis chemical |
| 动物实验 | 将小鼠[4]将60只CD-1小鼠随机分成以下3组（每组n = 20）：盐水;博莱霉素 – 水;博来霉素加地塞米松（Dex）。盐水组中的小鼠气管内注射2mL/kg盐水;其他患者气管内注射博来霉素（5 mg/kg，2 mL/kg，生理盐水）。在博来霉素处理后24小时，通过管饲法给予小鼠0.45mg/kg /天DEX。用博来霉素或盐水气管内注射的那天指定为第0天。 |
| 细胞实验 | ADIPO-P2细胞在补充有20％胎牛血清，青霉素（100U/mL）和链霉素（100μg/ mL）的D-MEM高葡萄糖培养基中于37℃和5％CO 2气氛中生长。在含有1.5×10 5个细胞/ mL的TC25 Corning烧瓶中将细胞培养为单层。对于每个实验，设置两个烧瓶，一个用于对照，一个用于处理的培养物。在生长的对数期期间，用30分钟的2.5μg/ mL博来霉素（溶于无菌0.9％NaCl）脉冲处理ADIPO-P2细胞。对照培养物平行设置但不暴露于博来霉素。在用博来霉素进行脉冲处理结束时，用Hank’s平衡盐溶液洗涤细胞两次，并用新鲜培养基保持培养直至收获。在5次传代或处理后的传代培养期间，细胞连续维持在培养物中。每当培养物汇合时（大约4×10 5个细胞/ mL培养基）进行亚培养。为了估计细胞生长，在传代培养时通过胰蛋白酶消化收集细胞，用0.4％台盼蓝染色约200μL的等分试样，并测定活细胞（未染色的细胞）的数量[3]。 |
| 数据来源文献 | [1]. Hovhannisyan G, et al. Comparative analysis of individual chromosome involvement in micronuclei induced by mitomycin C and 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]. Paviolo NS, et al. Telomere instability is present in the progeny of mammalian cells exposed to bleomycin. Mutat Res. 2012 Jun 1;734(1-2):5-11. [4]. Shi K, et al. Dexamethasone attenuates bleomycin-induced lung fibrosis in mice through TGF-β, Smad3 and JAK-STAT pathway. Int J Clin Exp Med. 2014 Sep 15;7(9):2645-50. |
| 规格 | 10mg 20mg |
是一类水溶性碱性糖肽类抗生素。主要抑制胸腺嘧啶核苷参入DNA，与DNA结合使之破坏分解，作用于增殖细胞周期的S期。
可用于抗性筛选和诱导肺纤维化模型。
使用本产品的应用案例（仅供参考）：
文章：Bufei Decoction Alleviated Bleomycin-Induced Idiopathic Pulmonary Fibrosis in Mice by Anti-Inflammation
作者：Shanjun Yang 1, Wenwen Cui 2, Mingye Wang 2, Luming Xing 1, Yue Wang 1, Pengyu Zhu 1, Qisheng Qu 1, Qiang Tang 1
简介：
Objective: This study aimed to investigate the mechanistic action and therapeutic effects of Bufei decoction on idiopathic pulmonary fibrosis (IPF) after inhalation of bleomycin.
Methods: Pulmonary fibrosis model in mice was prepared by atomization inhalation of bleomycin. Then, the mice were randomly divided into five groups (control group, model group, positive group, and treatment group) and administrated the drugs for 4 weeks. H&E and Masson's staining of lung tissues were used to observe the morphological changes and deposition of fibers, and the degree of fibrosis was evaluated by hydroxyproline content. The expression and activation of NF-κB were determined by western blotting and immunohistochemistry. The infiltration of macrophages was detected by immunostaining of CD45 and F4/80 in lung tissues.
Results: In mouse IPF, Bufei decoction alleviated the pathological changes and the deposition of fibrosis by decreasing the content of hydroxyproline of lung tissues. The antipulmonary fibrosis might rely on the effects of preventing the infiltration of inflammatory cells and inhibiting the expression and activation of NF-κB in lung tissue.
Conclusion: Bufei decoction improved the process of pulmonary fibrosis by regulating the activation and expression of the NF-κB signal transduction pathway, which provided a therapeutic option for IPF patients.
In vivo
Mice（male ICR mice, aged 8–12 weeks,weighting 18–22 g；雾化吸入，5 g/L（50%）博来霉素稀释液，3 小时 15 分钟，休息 7 次，每次 5 分钟）
The pulmonary fibrosis model in mice was prepared by atomization inhalation of bleomycin. When the mice were awake, they were put into a transparent plexiglass box with 30 cm × 30 cm × 20 cm connected with the atomizer and atomized 5 g/L (50%) bleomycin diluent was sprayed into the box through the atomizer tube. Three to four mice were put in the box at a time and exposed to bleomycin for a total of 3 hours and 15 minutes of bleomycin inhalation separated by 7 sessions of 5 minutes of rest. In the control group, mice received saline as a replacement for bleomycin inhalation [4, 18]. On the second day after modeling, all mice except those in the control group and model group were orally treated with saline, and the mice in the positive group and treatment group were continuously administrated with prednisone acetate (at a dose of 0.0064 mg/g) or Bufei decoction (at a dose of 1.235 mg/g) for 4 weeks.