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硫酸博莱霉素

硫酸博莱霉素用途

Bleomycin sulfate是具有有效抗肿瘤活性的DNA合成抑制剂。

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硫酸博莱霉素名称

[ CAS 号 ]:
9041-93-4

[ 中文名 ]:
硫酸博莱霉素

[ 英文名 ]:
Bleomycin sulfate

[中文别名 ]:

[英文别名 ]:

Blenmycins
BleoMycin Sufate
BLEMOYCIN SULFATE
Bleomycin (sulfate)
BLENOXANE
MFCD00070310
BLEO
BLEXANE
BLEOMYCIN SULPHATE
Blocamicina

硫酸博莱霉素生物活性

[ 描述 ]:

Bleomycin sulfate是具有有效抗肿瘤活性的DNA合成抑制剂。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

研究领域 >> 癌症

[ 靶点 ]

DNA/RNA Synthesis[1]

[体外研究]

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]。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]。

[体内研究]

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的信号显着强于对照组。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。

[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]。

[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。

[参考文献]

[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.

[相关活性小分子]

硫酸博莱霉素物理化学性质

[ 熔点 ]:
197ºC (dec)

[ 分子式 ]:
C₅₅H₈₅N₁₇O₂₅S₄

[ 分子量 ]:
1512.62

[ PSA ]:
1506.34000

[ 外观性状 ]:
白色粉末

[ 储存条件 ]:
库房通风低温干燥

[ 水溶解性 ]:
H2O: 20 mg/mL

硫酸博莱霉素MSDS

详细MSDS(安全技术说明书)

硫酸博莱霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: EC5991990

CHEMICAL NAME :: Bleomycin, sulfate

CAS REGISTRY NUMBER :: 9041-93-4

LAST UPDATED :: 199706

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 20 ug/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - cyanosis Skin and Appendages - dermatitis, allergic (after systemic exposure)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 0.286 units/kg/1D-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - fibrosis (interstitial) Lungs, Thorax, or Respiration - acute pulmonary edema

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 240 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 86 mg/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - urine volume increased Skin and Appendages - hair

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 59 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 210 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 103 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 74 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14 mg/kg/68W-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Kidney, Ureter, Bladder - Kidney tumors Tumorigenic - tumors at site of application

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18 mg/kg/52W-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Kidney, Ureter, Bladder - Kidney tumors Tumorigenic - tumors at site of application

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 36 mg/kg/52W-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Kidney, Ureter, Bladder - Kidney tumors Tumorigenic - tumors at site of application

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 8 mg/kg

SEX/DURATION :: female 6-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 20400 ug/kg

SEX/DURATION :: female 14 day(s) pre-mating female 1-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 8700 ug/kg

SEX/DURATION :: female 15-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 17400 ug/kg

SEX/DURATION :: female 15-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 15600 ug/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Dominant lethal test

TYPE OF TEST :: Morphological transformation

TYPE OF TEST :: Unscheduled DNA synthesis

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 50 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 135,199,1984 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,134,1987 IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 26,97,1981 IARC Cancer Review:Group 2B IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,134,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3576 No. of Facilities: 371 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 15071 (estimated) No. of Female Employees: 10631 (estimated)

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硫酸博莱霉素安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H340-H351-H361

[ 警示性声明 ]:
P201-P280-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;Xi: Irritant;

[ 风险声明 (欧洲) ]:
R46

[ 安全声明 (欧洲) ]:
S53-S36/37-S45

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
EC5991990

硫酸博莱霉素制备

该品是从轮枝链霉菌（Str.Verticillus)提取的，我国从放线菌的72号分离出同样的抗生素。生产过程为三级发酵，培养基为淀粉，葡萄糖、黄豆饼粉、酵母粉、玉米浆，氯化钠，硫酸锌，硫酸铜，磷酸二氢钾，发酵过程中每8小时补一次葡萄糖母液，控制发酵液残糖在1%左右，待pH回升开始每8h补玉米浆，每次补入量为0.5%，博来霉素发酵中间不产生泡沫，因此不需加消沫油。提炼过程利用博来霉素在水溶液中能解离成阳离子的特性，用弱酸性丙烯酸系阳离子交换树脂进行分离，提限，在甲醇溶液中以苯肼硫羰偶氮苯为螯合剂，或以硫化氢去除铜离子，反复用丙酮沉淀，精制后过滤，真空干燥得成品。

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硫酸博莱霉素文献

Ameliorative effect of mepenzolate bromide against pulmonary fibrosis.

J. Pharmacol. Exp. Ther. 350(1) , 79-88, (2014)

Idiopathic pulmonary fibrosis is thought to involve lung injury caused by reactive oxygen species (ROS), which in turn is followed by abnormal fibrosis. A transforming growth factor (TGF)-β1-induced i...

Transcription forms and remodels supercoiling domains unfolding large-scale chromatin structures.

Nat. Struct. Mol. Biol. 20(3) , 387-95, (2013)

DNA supercoiling is an inherent consequence of twisting DNA and is critical for regulating gene expression and DNA replication. However, DNA supercoiling at a genomic scale in human cells is uncharact...

Latent transforming growth factor-β1 protects against bleomycin-induced lung injury in mice.

Am. J. Respir. Cell. Mol. Biol. 51(6) , 761-71, (2014)

Transforming growth factor (TGF)-β1 is a potent mediator known to induce lung fibrosis. However, the role of latent TGF-β1 in lung inflammation and fibrosis is unclear. To investigate the role of circ...

更多文献

硫酸博莱霉素

硫酸博莱霉素用途

硫酸博莱霉素名称

硫酸博莱霉素生物活性

硫酸博莱霉素物理化学性质

硫酸博莱霉素MSDS

详细MSDS(安全技术说明书)

硫酸博莱霉素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

硫酸博莱霉素安全信息

硫酸博莱霉素制备

硫酸博莱霉素文献

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