Polymyxin B1

Polymyxin B1用途

Polymyxin B1 是一种有效的抗菌脂肽,衍生自多头芽孢杆菌。Polymyxin B1 是 Polymyxin B (HY-A0248) 的主要成分。Polymyxin B1 可以通过与细菌细胞膜的相互作用来诱导细菌细胞裂解。Polymyxin B1 可用于多重耐药性革兰氏阴性菌感染的研究。

Polymyxin B1名称

[ CAS 号 ]:
4135-11-9

[ 中文名 ]:
多粘菌素B1硫酸盐

[ 英文名 ]:
Polymyxin B1

[英文别名 ]:

polymyxin B
Polymyxin B1
polymixin B1

Polymyxin B1生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[体外研究]

多粘菌素B1对铜绿假单胞菌ATCC 27853、鲍曼不动杆菌ATCC BAA 747、肺炎克雷伯菌ATCC 13883、铜绿假单胞菌9019、鲍曼假单胞菌1261和肺炎克雷伯菌VM9的MIC值分别为4μg/mL、2μg/mL、2μg/mL、4μg/mL、4μg/mL和2μg/mL具有抗菌活性[3]。多粘菌素B1强烈抑制酵母、大肠杆菌和金黄色葡萄球菌中的蛋白质合成[4]。

[体内研究]

多粘菌素B1在大鼠静脉注射(0.8mg/kg)后的药代动力学研究。多粘菌素B1的浓度-时间曲线下面积大于粘菌素A和粘菌素B,多粘菌素B1的清除率为2.39ml/min/kg,血浆蛋白结合率为82.3%,清除半衰期为79.5min,AUC0-∞为365mg•min/L[5]。

[参考文献]

[1]. Kwa AL, et al. Pharmacokinetics of polymyxin B1 in patients with multidrug-resistant Gram-negative bacterial infections. Diagn Microbiol Infect Dis. 2008 Feb;60(2):163-7.

[2]. Berglund NA, et al. Interaction of the antimicrobial peptide polymyxin B1 with both membranes of E. coli: a molecular dynamics study. PLoS Comput Biol. 2015 Apr 17;11(4):e1004180.

[3]. Tam VH, et al. In vitro potency of various polymyxin B components. Antimicrob Agents Chemother. 2011 Sep;55(9):4490-1.

[4]. Alonso MA, et al. Compounds affecting membranes that inhibit protein synthesis in yeast. Antimicrob Agents Chemother. 1979 Dec;16(6):750-6.

[5]. Sivanesan S, et al. Pharmacokinetics of the Individual Major Components of Polymyxin B and Colistin in Rats. J Nat Prod. 2017 Jan 27;80(1):225-229.

Polymyxin B1物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
1571.6±65.0 °C at 760 mmHg

[ 分子式 ]:
C₅₆H₉₈N₁₆O₁₃

[ 分子量 ]:
1203.477

[ 闪点 ]:
904.2±34.3 °C

[ 精确质量 ]:
1202.749878

[ PSA ]:
490.66000

[ LogP ]:
-2.87

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.592

[ 储存条件 ]:
-20°C，充氩

Polymyxin B1毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TR1055000

CHEMICAL NAME :: Polymyxin B1

CAS REGISTRY NUMBER :: 4135-11-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C56-H98-N16-O13

MOLECULAR WEIGHT :: 1203.70

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 19 mg/kg

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

REFERENCE :: 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 4(1),334,1980

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 80 mg/kg

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

REFERENCE :: 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 4(1),334,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 ug/kg

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

REFERENCE :: 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 4(1),334,1980

Polymyxin B1

Polymyxin B1用途

Polymyxin B1名称

Polymyxin B1生物活性

Polymyxin B1物理化学性质

Polymyxin B1毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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