Gentamycin Sulfate

Gentamycin sulfate is an aminoglycoside antibiotic that inhibits the growth of Gram-positive and Gram-negative bacteria and several strains of mycoplasma in tissue culture^[1]. Gentamicin sulfate inhibits the activity of deoxyribonuclease I with an IC₅₀ value of 0.57±0.12mM^[2]. Gentamycin sulfate acts as a protein synthesis inhibitor, binding irreversibly to the small 16S rRNA of the 30S ribosomal subunit and interfering with protein synthesis, a mechanism of action similar to that of other aminoglycosides^[3]. Gentamycin sulfate is used to treat a variety of bacterial infections. It is poorly absorbed orally and can be administered intramuscularly or intravenously^[4]. Gentamycin sulfate is a potent antibiotic that is widely used in human and animal cell culture. The recommended concentration is usually 50μg/ml, but caution is required when using it in plant cell lines. The recommended concentration is 10μg/ml or lower ^{[5, 6]}.

In vitro, treatment of human neutrophils with gentamycin sulfate (0-200μM) for 1h significantly inhibited NADPH oxidase activity and concentration-dependently inhibited superoxide production in neutrophils exposed to phorbol myristate ^[5]. Gentamycin Sulfate (25, 100, 400 μg/mL) treated human osteoblasts (hFOB 1.19) for 6 hours, dose-dependently reduced alkaline phosphatase (ALP) activity, inhibited cell proliferation, survival and adhesion ability ^[6].

In vivo, gentamycin sulfate (50, 100 mg/kg/day) was intravenously injected into male Sprague Dawley rats for 7 days, which led to increased expression of kidney injury molecule 1 (KIM-1) and neutrophil gelatinase-associated lipocalin (NGAL) in a dose- and time-dependent manner, inducing a rat nephrotoxicity model ^[7].

References:
[1] Rudin A, Healey A, Phillips C A, et al. Antibacterial activity of gentamicin sulfate in tissue culture[J]. Applied microbiology, 1970, 20(6): 989-990.
[2] Xu W, Xie Z, Tong C, et al. A rapid and sensitive method for kinetic study and activity assay of DNase I in vitro based on a GO-quenched hairpin probe[J]. Analytical and Bioanalytical Chemistry, 2016, 408: 3801-3809.
[3] Kumar C, Himabindu M, Jetty A. Microbial biosynthesis and applications of gentamicin: a critical appraisal[J]. Critical reviews in biotechnology, 2008, 28(3): 173-212.
[4] Nwakile D C, Dozie-Nwakile O C, Okoye E I, et al. Non-Absorbable Oral Gentamicin Sulphate: Biopharmaceutical and Dosage Form Evaluation[J]. European Pharmaceutical Journal, 2021, 68(2): 8-15.
[5] Schafer T W, Pascale A, Shimonaski G, et al. Evaluation of gentamicin for use in virology and tissue culture[J]. Applied Microbiology, 1972, 23(3): 565-570.
[6] Dodds J H, Roberts L W. Some inhibitory effects of gentamicin on plant tissue cultures[J]. In Vitro, 1981, 17: 467-470.
[7] Umeki S. Anti-inflammatory action of gentamycin through inhibitory effect on neutrophil NADPH oxidase activity[J]. Comparative Biochemistry and Physiology Part B: Biochemistry and Molecular Biology, 1995, 110(4): 817-821.
[8] Ince A, Schütze N, Hendrich C, et al. In vitro investigation of orthopedic titanium-coated and brushite-coated surfaces using human osteoblasts in the presence of gentamycin[J]. The Journal of arthroplasty, 2008, 23(5): 762-771.
[9] Luo Q H, Chen M L, Chen Z L, et al. Evaluation of KIM-1 and NGAL as early indicators for assessment of gentamycin-induced nephrotoxicity in vivo and in vitro[J]. Kidney and Blood Pressure Research, 2016, 41(6): 911-918.