Mupirocin
(Synonyms: 莫匹罗星; BRL-4910A; Pseudomonic acid) 目录号 : GC15238
Mupirocin是一种由荧光假单胞菌产生的次级代谢产物，对部分链球菌具有优异的体外抑制活性。
Cas No.:12650-69-0
Sample solution is provided at 25 µL, 10mM.
Mupirocin, a secondary metabolite, naturally produced by Pseudomonas fluorescens, with an excellent in vitro activity against some streptococci[1]. Mupirocin acts on isoleucyl-tRNA synthetase and inhibits bacterial protein synthesis[2]. Mupirocin is widely used as antibacterial agent against methicillin-resistant Staphylococcus aureus (MRSA)[3].
In vitro, Mupirocin treatment for 72h showed the potent cytotoxic activity against the UCT-Mel 1 melanoma cell line with an IC50 value of 5.4μg/ml[4]. 0.2mM of Mupirocin treatment for 18 hours significantly enhanced the viability of HaCat cells and significantly accelerated wound healing[5]. 0.05mM of Mupirocin treatment for 48 hours inhibited the proliferation of psoriasis lesion epidermal keratinocytes (PLEKs), promoting cell apoptosis[6].
In vivo, applying 0.1ml of Mupirocin ointment (20mg/g) to the wound daily for 12 days significantly promoted wound healing, resulting in a significant increase in epidermal thickness and a reduction in the growth of Staphylococcus aureus in a mouse model of superficial skin infection caused by Staphylococcus aureus [7].
References:
[1] Bencardino D, Amagliani G, Brandi G. Carriage of Staphylococcus aureus among food handlers: An ongoing challenge in public health[J]. Food control, 2021, 130: 108362.
[2] Gisby J, Bryant J. Efficacy of a new cream formulation of mupirocin: comparison with oral and topical agents in experimental skin infections[J]. Antimicrobial agents and chemotherapy, 2000, 44(2): 255-260.
[3] Tucaliuc A, Blaga A C, Galaction A I, et al. Mupirocin: applications and production[J]. Biotechnology letters, 2019, 41(4): 495-502.
[4] Reva O N, Rademan S, Visagie M H, et al. Comparison of structures and cytotoxicity of mupirocin and batumin against melanoma and several other cancer cell lines[J]. Future medicinal chemistry, 2019, 11(7): 677-691.
[5] Twilley D, Reva O, Meyer D, et al. Mupirocin promotes wound healing by stimulating growth factor production and proliferation of human keratinocytes[J]. Frontiers in Pharmacology, 2022, 13: 862112.
[6] Yan B X, Chen X Y, Wang Z Y, et al. Mupirocin blocks imiquimod-induced psoriasis-like skin lesion by inhibiting epidermal isoleucyl-tRNA synthetase[J]. Cell Communication and Signaling, 2022, 20(1): 185.
[7] Pérez M, Robres P, Moreno B, et al. Comparison of antibacterial activity and wound healing in a superficial abrasion mouse model of Staphylococcus aureus skin infection using photodynamic therapy based on methylene blue or mupirocin or both[J]. Frontiers in Medicine, 2021, 8: 673408.
Mupirocin是一种由荧光假单胞菌产生的次级代谢产物，对部分链球菌具有优异的体外抑制活性[1]。Mupirocin通过作用于异亮氨酰-tRNA合成酶抑制细菌蛋白质合成[2]。Mupirocin被广泛用于抗耐甲氧西林金黄色葡萄球菌（MRSA）的抗菌治疗[3]。
在体外，Mupirocin处理72小时对UCT-Mel 1黑色素瘤细胞系具有强效细胞毒性，IC50值为5.4μg/ml[4]。0.2mM的Mupirocin处理HaCat细胞18小时可显著增强细胞活力并加速伤口愈合[5]。0.05mM的Mupirocin处理银屑病皮损表皮角质形成细胞（PLEKs）48小时能抑制细胞增殖并促进凋亡[6]。
在体内，金黄色葡萄球菌引起的浅表皮肤感染小鼠模型每日局部涂抹0.1ml的Mupirocin软膏（20mg/g；持续12天）可显著促进伤口愈合，增加表皮厚度并减少金黄色葡萄球菌生长[7]。
| Cell experiment [1]: | |
Cell lines | HaCat cells |
Preparation Method | HaCat cells were seeded at a concentration of 1.5×105 cells/mL in a 24-well plate and incubated overnight at 37°C and 5% CO2 to form confluent monolayers. Subsequently, a cross was drawn in the center of each well to simulate a wound using a 1000-pipette tip. Cell debris was removed by aspirating the culture medium and adding fresh complete medium. Then, the cells were treated with Mupirocin at a final concentration of 0.2mM for 18 hours. The control group included cells grown in the culture medium (untreated) and cells treated with 0.25% DMSO (vehicle control). Images were captured using an optical microscope with a 4× magnification at the time of the initial scratch (0 hours) and 18 hours after treatment. |
Reaction Conditions | 0.2mM; 18h |
Applications | Mupirocin treatment significantly increased wound healing in HaCat cells. |
| Animal experiment [2]: | |
Animal models | SKH-1 hairless mice |
Preparation Method | Female SKH-1 hairless mice (6-8 weeks old) were individually housed in cages for a few days before the experiment to adapt to the environment. The cages were placed close to the ground to allow the mice to adapt to low light levels, and commercial feed and water were freely provided. Under general anesthesia, 20 mice were disinfected with 70% alcohol on their skin, and abrasions were made with a surgical knife until redness appeared and the epidermis was significantly lost. The wound diameter was approximately 0.6cm, located in the back area, 1cm away. Approximately 0.1ml of Mupirocin ointment (20mg/g) was applied to the wound daily (using a separate ointment each time), and gentle massage was performed until the ointment was fully absorbed. The entire process lasted for 12 days, and the pathological characteristics of the wounds were evaluated daily. |
Dosage form | 20mg/g/day for 12 days; apply to the wound |
Applications | Mupirocin treatment significantly promoted wound healing and led to thickening of the epidermis in mice. |
References: | |
| Cas No. | 12650-69-0 | SDF | |
| 别名 | 莫匹罗星; BRL-4910A; Pseudomonic acid | ||
| 化学名 | 9-[(E)-4-[(2S,3R,4R,5S)-3,4-dihydroxy-5-[[(2S,3S)-3-[(2S,3S)-3-hydroxybutan-2-yl]oxiran-2-yl]methyl]oxan-2-yl]-3-methylbut-2-enoyl]oxynonanoic acid | ||
| Canonical SMILES | CC(C1C(O1)CC2COC(C(C2O)O)CC(=CC(=O)OCCCCCCCCC(=O)O)C)C(C)O | ||
| 分子式 | C26H44O9 | 分子量 | 500.62 |
| 溶解度 | ≥ 100mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9975 mL | 9.9876 mL | 19.9752 mL |
| 5 mM | 0.3995 mL | 1.9975 mL | 3.995 mL |
| 10 mM | 0.1998 mL | 0.9988 mL | 1.9975 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
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Quality Control & SDS
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- Purity: >98.00%
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