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Polymyxin B Sale

(Synonyms: 多粘菌素B) 目录号 : GC19581

多粘菌素B(PMB)是一种强效抗生素,可结合并中和LPS(脂多糖)。

Polymyxin B Chemical Structure

Cas No.:1404-26-8

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Description

Polymyxin B (PMB) is a potent antibiotic that binds to and neutralizes LPS (lipopolysaccharides)[1].

Polymyxin B againsts all K. pneumoniae strains for positive K. pneumoniae carbapenemase (KPC) genes with MIC of 16 to 128 μg/ml[2]. In vitro,10 µ/mL Polymyxin B was able to neutralize the effect of endotoxin, as contaminant in S. mansoni recombinant antigens produced in E. coli, in inducing TNF-alpha and IL-10 production[1]. The MIC50 and MIC90 values of polymyxin B against 217 strains of carbapenem-resistant A. baumannii were 0.5 and 1 mg/l, respectively[3]. The MIC values for polymyxin B against MRSA (Meticillin-resistant Staphylococcus aureus) was in the range of 8-64 μg/mL, while the MIC values for polymyxin B against MRSP (meticillin-resistant Staphylococcus pseudintermedius) was in the range of 0.25-4 μg/mL[4].

In vivo, mice were treated with 72 mg/kg obviously increased the level of γH2AX foci (indicative of double stranded breaks)[5]. In vivo, carvacrol 10 mg/kg plus polymyxin B 2 mg/kg exhibite antimicrobial activity in a mouse model of infection, resulting in increased survival and a significant decrease in bacterial load in the blood[6].

References:
[1] Cardoso LS, et al. Polymyxin B as inhibitor of LPS contamination of Schistosoma mansoni recombinant proteins in human cytokine analysis. Microb Cell Fact. 2007 Jan 3;6:1.
[2] Elemam A, et al. In vitro evaluation of antibiotic synergy for polymyxin B-resistant carbapenemase-producing Klebsiella pneumoniae. J Clin Microbiol. 2010 Oct;48(10):3558-62.
[3] Thamlikitkul V, et al. In vitro activity of polymyxin B against carbapenem-resistant Acinetobacter baumannii. J Med Assoc Thai. 2014 Dec;97(12):1254-8.
[4] Boyen F, et al. In vitro antimicrobial activity of miconazole and polymyxin B against canine meticillin-resistant Staphylococcus aureus and meticillin-resistant Staphylococcus pseudintermedius isolates. Vet Dermatol. 2012 Aug;23(4):381-5, e70.
[5] Yun B, et al. Polymyxin B causes DNA damage in HK-2 cells and mice. Arch Toxicol. 2018 Jul;92(7):2259-2271.
[6] de Souza GH, et al. Synergistic interaction of polymyxin B with carvacrol: antimicrobial strategy against polymyxin-resistant Klebsiella pneumoniae. Future Microbiol. 2024 Feb 8. 

多粘菌素B(PMB)是一种强效抗生素,可结合并中和LPS(脂多糖)[1]

多粘菌素B对所有K. pneumoniae carbapenemase(KPC)基因阳性的菌株均具有抗药性,MIC为16至128μg/ml[2]。在体外,10 µ/mL多粘菌素B能够中和内毒素诱导TNF-α和IL-10产生的作用[1],内毒素是在大肠杆菌中产生的S. mansoni重组抗原中的污染物。多粘菌素B对217株carbapenem-resistant A. baumannii 的MIC50和MIC90值分别为0.5和1 mg/l[3]。多粘菌素B对MRSA(耐甲氧西林Staphylococcus aureus)的MIC值在8-64 μg/mL范围内,而多粘菌蛋白B对MRSP(耐甲羟西林Staphylococcus pseudintermedius)在0.25-4 μg/mL范围内[4]

在体内,用72 mg/kg处理的小鼠明显增加了γH2AX病灶的水平(表明双链断裂)[5]。在体内,香芹酚10 mg/kg加多粘菌素B 2 mg/kg在小鼠感染模型中表现出抗菌活性,从而提高存活率并显著降低血液中的细菌载量[6]

实验参考方法

Cell experiment [1]:

Cell lines

HK-2 cells

Preparation method

HK-2 cells were incubated with polymyxin B (12.5, 50 and 100 μM) for 6 or 24 h and stained with DAPI (10 μg/mL) for assessment of micronuclei.

Reaction Conditions

12.5, 50 and 100 μM, 6 or 24 h

Applications

Human proximal tubular cells were treated with polymyxin B (12.5-100 μM) for up to 24 h and showed a significant increase in micronuclei frequency, as well as abnormal mitotic events.

Animal experiment [2]:

Animal models

Guinea pigs

Preparation method

Guinea pigs were transnasally treated with 75 µg/kg of polymyxin-B or vehicle twice a week for a total of 3 weeks. Guinea pigs were surgically cannulated and artificially ventilated 24 h after the last administration of polymyxin-B or vehicle. Ten minutes after the installation of artificial ventilation, ascending doses of methacholine, acetylcholine or histamine were inhaled for 20 s at intervals of 5 min. Subsequent study was conducted 20 min after treatment of 60 mg/kg of indomethacin in the same manner. Final study was conducted in naive guinea pigs after single inhalation of 75 µg/mL of polymyxin B.

Dosage form

75 µg/kg, transnasally

Applications

The proportion of eosinophils in bronchoalveolar lavage fluid significantly increased in guinea pigs treated with polymyxin-B compared with vehicle. Bronchial responsiveness to inhaled methacholine, acetylcholine and histamine was significantly decreased by the polymyxin-B treatment. This protective effect induced by polymyxin B was abolished by pretreatment of indomethacin. A significant increase in bronchial responsiveness was observed after a single inhalation of polymyxin B.

References:

[1] Yun B, et al. Polymyxin B causes DNA damage in HK-2 cells and mice. Arch Toxicol. 2018 Jul;92(7):2259-2271.

[2] Ishiura Y, et al. In vivo airway eosinophil accumulation induced by polymyxin-B reduces bronchial responsiveness in guinea pigs. Clin Exp Allergy. 2001 Apr;31(4):644-51.

化学性质

Cas No. 1404-26-8 SDF
别名 多粘菌素B
分子式 分子量
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