Kasugamycin (hydrochloride) is an aminoglycosidic antibiotic against many different bacteria [1]. Kasugamycin binds to the 30S ribosomal subunit and the 70S ribosome of Escherichia coli, inhibiting the translation of typical transcripts with the 5' untranslated region (5'-UTR) containing the Shine-Dalgarno (SD) sequence[2]. Kasugamycin has been widely used to inhibit the growth of Escherichia coli, as well as for conducting studies on drug resistance or sensitivity analysis[3].
In vitro, Kasugamycin treatment for 24 hours significantly inhibited the growth of Pectobacterium aroidearum, with an EC50 value of 20.14μg/ml[4]. Treatment with Kasugamycin (250ng/ml) for 48 hours can eliminate the ERK and AKT activation stimulated by chitinase 3-like-1 (CHI3L1) in Calu-3 cells, and inhibit the uptake of the pseudovirus carrying the Omicron S protein mutation by Calu-3 cells[5].
In vivo, Kasugamycin treatment via intraperitoneal injection at a dose of 100mg/kg (every other day) for 30 days inhibited bleomycin-stimulated pulmonary fibrosis in mice and reduced the collagen accumulation[6]. Daily intraperitoneal injection of 400mg/kg dose of Kasugamycin combined with 10mg/kg/day rifampicin (p.o.) for 2 weeks significantly reduced the bacterial load in the lungs of mice infected with Mycobacterium tuberculosis[7].
References:
[1] Umezawa H, Okami Y, Hashimoto T, et al. A new antibiotic, kasugamycin[J]. The Journal of Antibiotics, Series A, 1965, 18(2): 101-103.
[2] Okuyama A, Tanaka N, KOMAI T. The binding of kasugamycin to the Escherichia coli ribosomes[J]. The Journal of Antibiotics, 1975, 28(11): 903-905.
[3] Lange C, Lehr M, Zerulla K, et al. Effects of kasugamycin on the translatome of Escherichia coli[J]. PloS one, 2017, 12(1): e0168143.
[4] Xiong C, Zhou X, Tu Y, et al. Kasugamycin disrupts membrane transport and reduces virulence in Pectobacterium aroidearum to control konjac soft rot[J]. Phytopathology Research, 2025, 7(1): 52.
[5] Kamle S, Ma B, Lee C M, et al. Host chitinase 3-like-1 is a universal therapeutic target for SARS-CoV-2 viral variants in COVID-19[J]. Elife, 2022, 11: e78273.
[6] Lee J H, Lee C M, Lee J H, et al. Kasugamycin is a novel chitinase 1 inhibitor with strong antifibrotic effects on pulmonary fibrosis[J]. American Journal of Respiratory Cell and Molecular Biology, 2022, 67(3): 309-319.
[7] Chaudhuri S, Li L, Zimmerman M, et al. Kasugamycin potentiates rifampicin and limits emergence of resistance in Mycobacterium tuberculosis by specifically decreasing mycobacterial mistranslation[J]. Elife, 2018, 7: e36782.
Kasugamycin (hydrochloride)是一种对多种细菌具有活性的氨基糖苷类抗生素[1]。Kasugamycin结合大肠杆菌的30S核糖体亚基和70S核糖体，抑制含有Shine-Dalgarno（SD）序列的5'非翻译区（5'-UTR）的典型转录本的翻译[2]。Kasugamycin已被广泛用于抑制大肠杆菌的生长，以及进行耐药性或敏感性分析的研究[3]。
在体外，Kasugamycin处理24小时显著抑制了Pectobacterium aroidearum的生长，EC50值为20.14μg/ml [4]。使用250ng/ml的Kasugamycin处理48小时，可消除chitinase 3-like-1 (CHI3L1)刺激的Calu-3细胞中ERK和AKT的激活，并抑制Calu-3细胞对携带Omicron S蛋白突变假病毒的摄取[5]。
在体内，每隔一天腹腔注射100mg/kg剂量的Kasugamycin，持续30天，抑制了博来霉素刺激的小鼠肺纤维化并减少了胶原沉积[6]。每日腹腔注射400mg/kg剂量的Kasugamycin，联合口服10mg/kg/day剂量的利福平，持续两周，显著降低了感染结核分枝杆菌小鼠肺部的细菌负荷[7]。