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硫酸粘杆菌素

硫酸粘杆菌素用途

Colistin是一种多肽抗生素,其通过与革兰氏阴性细菌的外细胞膜中的脂多糖和磷脂结合来抑制革兰氏阴性细菌。
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硫酸粘杆菌素名称

[ CAS 号 ]:
1264-72-8

[ 中文名 ]:
硫酸粘杆菌素

[ 英文名 ]:
Colistin sulfate

[中文别名 ]:

[英文别名 ]:

硫酸粘杆菌素生物活性

[ 描述 ]:

Colistin是一种多肽抗生素,其通过与革兰氏阴性细菌的外细胞膜中的脂多糖和磷脂结合来抑制革兰氏阴性细菌。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬
信号通路 >> 抗感染 >> 细菌
研究领域 >> 感染

[体外研究]

通过类似洗涤剂的机制,粘菌素对革兰氏阴性细菌具有杀菌作用。这种机制涉及通过竞争性地从膜脂的带负电荷的磷酸基团中置换二价阳离子(钙和镁)来与外膜的脂多糖和磷脂相互作用以及与外膜的静电干扰[1]。粘菌素(多粘菌素E)具有快速细菌杀伤的有利特性,活性范围窄,以及治疗由多重耐药革兰氏阴性细菌引起的感染的相关的缓慢发展。商业上有两种形式的粘菌素:主要用于局部使用的粘菌素(硫酸盐)和用于肠胃外使用的粘菌素甲磺酸盐(钠)[2]。

[体内研究]

由于在滴注后缓慢且持续的CMS转化,实现了大鼠ELF中高浓度的粘菌素[3]。粘菌素通常用于仔猪,但剂量不足和过量服用是常见的。粘菌素的剂量不足或过量不会导致仔猪粪便微生物群的任何严重干扰,并且很少选择显性大肠杆菌群体中的染色体抗性[4]。

[动物实验]

大鼠:在无菌0.9%氯化钠中新鲜制备粘菌素甲磺酸盐(钠)和粘菌素(硫酸盐)给药溶液。对于iv研究,通过颈静脉插管通过推注注射施用甲磺酸粘菌素(CMS)或硫酸盐溶液。气管内(it)滴注用作肺部给药的技术。以14mg / kg体重,28mg / kg或56mg / kg的剂量静脉内施用动物。在一项独立研究中,大鼠静脉注射粘菌素,剂量为0.21 mg / kg,0.41 mg / kg或0.62 mg / kg [3]。

[参考文献]

[1]. Hancock RE et al. Peptide antibiotics. Antimicrob Agents Chemother. 1999 Jun;43(6):1317-23.

[2]. Li J, et al. In vitro pharmacodynamic properties of colistin and colistin methanesulfonate againstPseudomonas aeruginosa isolates from patients with cystic fibrosis. Antimicrob Agents Chemother. 2001 Mar;45(3):781-5.

[3]. W S Yapa S, et al. Population pharmacokinetics of colistin methanesulfonate in rats: achieving sustained lung concentrations of colistin for targeting respiratory infections. Antimicrob Agents Chemother. 2013 Oct;57(10):5087-95.

[4]. Fleury MA, et al. Impact of two different colistin dosing strategies on healthy piglet fecal microbiota. Res Vet Sci. 2016 Aug;107:152-60.


[相关活性小分子]

嘌呤霉素二盐酸盐 | G-418 硫酸盐 | 衣霉素 | 潮霉素B | 盐霉素 | 阿维巴坦钠 | 硫酸新霉素 | 法硼巴坦 | 甲氧西林钠 | 利福平 | 甲硝唑 | 羧苄青霉素钠 | 头孢他啶 | 盐酸依拉环素 | 头孢噻肟钠

硫酸粘杆菌素物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
1537.3±65.0 °C at 760 mmHg

[ 熔点 ]:
200-220°C

[ 分子式 ]:
C52H100N16O17S

[ 分子量 ]:
1253.51

[ 闪点 ]:
883.5±34.3 °C

[ PSA ]:
573.64000

[ LogP ]:
-3.68

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.575

[ 储存条件 ]:
2-8°C

硫酸粘杆菌素MSDS

硫酸粘杆菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TR1500000
CHEMICAL NAME :
Polymyxin E sulfate
CAS REGISTRY NUMBER :
1264-72-8
LAST UPDATED :
199504
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C45-H85-N13-O10.H2-O4-S

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
72200 ug/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 13,7,1979
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
793 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,395,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
21800 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,395,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
53500 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,395,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
6 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ABANAE Antibiotics Annual. (New York, NY) 1953-60. For publisher information, see AMACCQ. Volume(issue)/page/year: 7,41,1959/1960
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
58 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 16,105,1968 *** REVIEWS *** TOXICOLOGY REVIEW ANBCB3 Antibiotics and Chemotherapy (Basel). (S. Karger AG, Postfach CH-4009 Basel, Switzerland) V.17- 1971- Volume(issue)/page/year: 31,119,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M4682 No. of Facilities: 215 (estimated) No. of Industries: 2 No. of Occupations: 6 No. of Employees: 2247 (estimated) No. of Female Employees: 1438 (estimated)
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硫酸粘杆菌素安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
Missing Phrase - N15.00950417

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
S45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
TR1500000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2309901000

硫酸粘杆菌素海关

[ 海关编码 ]: 2309901000

硫酸粘杆菌素文献

Inhibitory Effect of Epigallocatechin Gallate on the Virulence of Clostridium difficile PCR Ribotype 027.

J. Food Sci. 80 , M2925-31, (2016)

Clostridium difficile infection (CDI) is the most prevalent cause of health-care-associated infections. CDI-related health-care costs and deaths are both increasing annually on a global scale. C. diff...

Mucin Binding Reduces Colistin Antimicrobial Activity.

Antimicrob. Agents Chemother. 59 , 5925-31, (2015)

Colistin has found increasing use in treating drug-resistant bacterial lung infections, but potential interactions with pulmonary biomolecules have not been investigated. We postulated that colistin, ...

Renal disposition of colistin in the isolated perfused rat kidney.

Antimicrob. Agents Chemother. 53 , 2857-64, (2009)

Nephrotoxicity is an important limitation to the clinical use of colistin against Pseudomonas aeruginosa and other gram-negative pathogens. Previous work reported net tubular reabsorption of colistin ...


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