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]。