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gentamicin
REACTIVE & FUNCTIONAL POLYMERS · 2019 · IF 3.074

Synthesis of gentamicin-grafted-chitosan with improved solubility and antibacterial activity

Tingting Yan,Chengpeng Li,Qianqian Ouyang,Dongying Zhang,Qingkun Zhong,Puwang Li,Sidong Li,Ziming Yang,Tao Wang,Qingxia Zhao

Due to superior properties, chitosan (CS) has been widely applied in health field. However its acid-solubility and poor antimicrobial activity compromise its safety and applications, respectively. To enhance its water-solubility and antimicrobial activity, gentamicin-grafted-chitosan (GT-CS) is synthesized for the first time, which is then confirmed by various characteristic methods and the graft ratio for gentamicin is about 22.1%. Particularly, it is the first study, disclosing there are degradation and crosslinking involved simultaneously during CS oxidation . Furthermore, GT-CS shows greatly improved water solubility (10.0w%). Compared to CS, the antibacterial activity of GT-CS is improved significantly, approaching the pure gentamicin. It should be noted that the antimicrobic mechanism may not be the target-specific interactions but the nonspecific interactions with the bacterial membrane as shown by scanning electron microscope. To sum up, GT-CS is a superior antimicrobial with good solubility.

CAS / MDL: 1405-41-0 7790-28-5
研究领域: 生物材料学 · 微生物学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2017 · IF 3.671

Gentamicin modified chitosan film with improved antibacterial property and cell biocompatibility

Yang Liu,Peihong Ji,Huilin Lv,Yong Qin,Linhong Deng

Gentamicin modified chitosan film (CS-GT) was produced using a three-step procedure comprising: (i) the chitosan solution was air-dried to form a chitosan (CS) film, (ii) using citric acid to generate the amide and carboxyl groups on the surface of CS, (iii) the CS with surface carboxyl groups was modified by grafting of gentamicin. After modification, this CS-GT film has excellent hydrophilicity and biocompatibility. It is very evident that the gentamicin grafting treatment significantly improves the antibacterial properties of the CS film. Our preliminary results suggest that this novel gentamicin modified chitosan film, which can be prepared in large quantities and at low cost, should have potential application in biomedical applications.

研究领域: 材料科学 · 生物医学工程 · 药剂学
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TOXICOLOGY AND APPLIED PHARMACOLOGY · 2016 · IF 3.847

Evaluation of novel biomarkers of nephrotoxicity in Cynomolgus monkeys treated with gentamicin

Jean-Charles Gautier,Xiaobing Zhou,Yi Yang,Thierry Gury,Zhe Qu,Xavier Palazzi,Jean-François Léonard,Mohamed Slaoui,Yaligara Veeranagouda,Isabelle Guizon,Eric Boitier,Aziz Filali-Ansary,Bart H.J. van den Berg,Oliver Poetz,Thomas Joos,Tianyi Zhang,Jufeng Wang,Philippe Detilleux,Bo Li

Most studies to evaluate kidney safety biomarkers have been performed in rats. This study was conducted in Cynomolgus monkeys in order to evaluate the potential usefulness of novel biomarkers of nephrotoxicity in this species. Groups of 3 males were given daily intramuscular injections of gentamicin , a nephrotoxic agent known to produce lesions in proximal tubules, at dose-levels of 10, 25, or 50   mg/kg/day for 10   days. Blood and 16-h urine samples were collected on Days −   7, −   3, 2, 4, 7, and at the end of the dosing period. Several novel kidney safety biomarkers were evaluated, with single- and multiplex immunoassays and in immunoprecipitation-LC/MS assays, in parallel to histopathology and conventional clinical pathology parameters. Treatment with gentamicin induced a dose-dependent increase in kidney tubular cell degeneration/necrosis, ranging from minimal to mild severity at 10   mg/kg/day, moderate at 25   mg/kg/day, and to severe at 50   mg/kg/day. The results showed that the novel urinary biomarkers, microalbumin, α1-microglobulin, clusterin , and osteopontin , together with the more traditional clinical pathology parameters, urinary total protein and N-acetyl-β-D-glucosaminidase (NAG), were more sensitive than blood urea nitrogen (BUN) and serum creatinine (sCr) to detect kidney injury in the monkeys given 10   mg/kg/day gentamicin for 10   days, a dose leading to an exposure which is slightly higher than the desired therapeutic exposure in clinics. Therefore, these urinary biomarkers represent non-invasive biomarkers of proximal tubule injury in Cynomolgus monkeys which may be potentially useful in humans.

CAS / MDL: 32986-56-4
研究领域: 毒理学 · 药理学 · 临床研究
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RSC Advances · 2016 ·Vol. 6 ·期 18 ·14483-14489 · IF 3.289

Highly specific determination of gentamicin by induced collapse of Au–lipid capsules

Qianjin Liu,Haibo Mu,Chunli Sun,Jinyou Duan

Residues of gentamicin in food pose a threat to human health. Determining gentamicin residues relies largely on adequate analytical techniques. Herein, a simple and highly specific colorimetric method for effective detection of this aminoglycoside antibiotic in milk based on gentamicin-induced collapse of an Au–lipid capsule is first proposed. The strong interaction between gentamicin and phosphatidylcholine resulted in the collapse of Au–lipid capsule and consequently, the color of AuNPs changed from wine red to blue. The concentration of gentamicin could be determined with the naked eye or a UV-vis spectrometer. The results showed that the absorption ratio (A664/A531) was liner with the gentamicin concentration in the 0–0.2 μM range with a linear 0.99 correlation coefficient. The detection limit was 7.4 nM. The coexisting substances, including L-arginine, guanidine hydrochloride, Tween-20, ammonium hydroxide, sodium chloride, potassium chloride, calcium chloride, glucose, and other common antibiotics such as streptomycin, amikacin, kanamycin, chloramphenicol, tetracycline, ampicillin and carbenicillin, did not interfere with the gentamicin determination with this method. Furthermore, the established method was successfully applied for the qualitative and quantitative analysis of gentamicin in pretreated milk products.

CAS / MDL: 97281-47-5
研究领域: 分析化学 · 食品安全 · 纳米技术
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OTOLOGY & NEUROTOLOGY · 2023 ·Vol. 45 ·期 1 ·e49 · IF 2.1

Cortisol Sensitizes Cochlear Hair Cells to Gentamicin Ototoxicity Via Endogenous Apoptotic Pathway

Li Cong,Chen Liang,Li Yingying,Li Mengxin,Zhang Xiaoling,Cui Limei,Sun Yan,Song Xicheng

Hypothesis The stress hormone cortisol affects aminoglycoside-induced ototoxicity. Background The widespread use of aminoglycosides is a prevalent cause of sensorineural hearing loss. Patients receiving aminoglycosides usually have elevated levels of circulating stress hormones due to disease or physiological stress; however, whether the stress hormone cortisol impacts aminoglycoside-mediated injury of cochlear hair cells has not been fully investigated. Methods House Ear Institute-Organ of Corti 1 (HEI-OC1) cells with or without cortisol pretreatment were exposed to gentamicin, we investigated the effect of cortisol pretreatment on gentamicin ototoxicity by assessing cell viability. Molecular pathogenesis was explored by detecting apoptosis and oxidative stress. Meanwhile, by inhibiting glucocorticoid receptors (GR) and mineralocorticoid receptors (MR), the potential roles of receptor types in cortisol-mediated sensitization were evaluated. Results Cortisol concentrations below 75 μmol/l did not affect cell viability. However, pretreatment with 50 μmol/l cortisol for 24 hours sensitized hair cells to gentamicin-induced apoptosis. Further mechanistic studies revealed that cortisol significantly increased hair cell apoptosis and oxidative stress, and altered apoptosis-related protein expressions induced by gentamicin. In addition, blockade of either GR or MR attenuated cortisol-induced hair cell sensitization to gentamicin toxicity. Conclusion Cortisol pretreatment increased mammalian hair cell susceptibility to gentamicin toxicity. Sensitization was related to the activation of the intrinsic apoptotic pathway and excessive generation of reactive oxygen species. Cortisol may exacerbate aminoglycoside ototoxicity.

CAS / MDL: 1403-66-3
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Nanomaterials · 2023 ·Vol. 13 ·期 8 ·1416 · IF 5.3

Gentamicin Sulfate Grafted Magnetic GO Nanohybrids with Excellent Antibacterial Properties and Recyclability

Xing Wu,Jingya Zhou,Zeng Liu,Wei Shao

In this study, magnetic graphene oxide (MGO) nanohybrids were first prepared by loading Fe3O4NPs onto graphene oxide (GO). Then, GS-MGO nanohybrids were prepared by grafting gentamicin sulfate (GS) onto MGO directly using a simple amidation reaction. The prepared GS-MGO had the same magnetism as MGO. They exhibited excellent antibacterial ability against Gram-negative bacteria and Gram-positive bacteria. The GS-MGO had excellent antibacterial performance againstEscherichia coli(E. coli),Staphylococcus aureus(S. aureus), andListeria monocytogenes(L. monocytogenes). When the addition concentration of GS-MGO was 1.25 mg/mL, the calculated bacteriostatic ratios againstE. coliandS. aureusachieved 89.8% and 100%, respectively. ForL. monocytogenes, only 0.05 mg/mL of GS-MGO had an antibacterial ratio as high as 99%. In addition, the prepared GS-MGO nanohybrids also exhibited excellent non-leaching activity with good recycling antibacterial ability. After eight times antibacterial tests, GS-MGO nanohybrids still exhibited an excellent inhibition effect onE. coli,S. aureus,andL. monocytogenes. Therefore, as a non-leaching antibacterial agent, the fabricated GS-MGO nanohybrid had dramatic antibacterial properties and also showed great recycling ability. Thus, it displayed great potential in the design of novel recycling antibacterial agents with non-leaching activity.Keywords:magnetic;graphene oxide;gentamicin sulfate;antibacterial;recyclable activity

研究领域: 材料科学 · 微生物学
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Science of Advanced Materials · 2014 ·Vol. 6 ·期 12 ·2603-2610 · IF 2.908

Dynamic Release of Antibiotic Drug Gentamicin Sulfate from Novel Zirconium Phosphate Nano-Platelets

Ai Jing,Chen Yan,Jing Hui,Gao Xuechuan,Liu Jiayin,Ma Kexin,Suo Jian,Yu Shiyong,Song Shuyan

The intercalation of gentamicin sulfate (GS) into novel zirconium phosphate (ZrP) nano-platelets has been achieved using a hydrated ZrP phase known as the -ZrP (Zr(HPO4)2·6H2O) which possesses six water molecules per formula unit. This paper revealed the successful intercalation of the GS into -ZrP at different molar ratios of GS: -ZrP (1:10,1:5,1:2), which were demonstrated by the emergence of a new phase in the X-ray powder diffraction (XRD) pattern with an interlayer distance of 13.1 Å. The morphologies and sizes of the samples were characterized by scanning electron microscopy (SEM) and transmission electron microscopy (TEM) which showed the characteristic platelet-like hexagonal shape of the ZrP nanoparticles. Compared to spherical shape particles the hexagonal shape may show better margination, adhesion, and binding properties. The average particle size of GS: -ZrP nano-platelets was 120 nm in diameter and the average thickness of the particles was 10 nm. The drug release in vitro on the obtained GS: -ZrP nano-platelets was carried out in pH 7.4 buffer solution at 37 °C. The cytotoxicity cell viability experiments in vitro for the GS and GS: -ZrP nanoparticles showed that GS:ZrP had low cytotoxicity. Overall, our study demonstrated that the GS: -ZrP nanoparticles possessed a moderate GS loading efficiency, low cytotoxicity and favorable biocompatibility.

研究领域: 材料科学 · 药理学 · 纳米医学
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MATERIALS & DESIGN · 2016 · IF 3.997

Gelatin-enhanced porous titanium loaded with gentamicin sulphate and in vitro release behavior

Qiuyan Li,Guo He

Porous titanium with entangled wire structure was enhanced by filling gelatin into the porous structure to form a titanium-gelatin (Ti-G) composite. The density of the composites was 1.6–2.5   g/cm 3 , similar to that of bone. The strength and elastic modulus of the composites reached 12.9–39.4   MPa and 2.5–7.4   GPa, respectively, which were comparable to that of the cortical bone. Gelatin in Ti-G composite acted as the carrier of gentamicin sulphate (GS). Antibacterial efficacy of GS-loaded Ti-G against Staphylococcus aureus strain was tested. The lack of growth of Staphylococcus aureus strains was found in Luria–Bertani (LB) medium containing GS-loaded Ti-G. GS release behavior from the GS-loaded Ti-G composites in phosphate buffer saline (PBS) was investigated. The effective GS release times from Ti30-G and Ti50-G were 120   h and 168   h, respectively. The gelatin in Ti-G was just degraded 3.2% at the immersion time of 168   h and 9.0% at 336   h. The degradation rate of gelatin was much slower than release rate of GS, indicated that the GS release from gelatin was less affected by the gelatin degradation. These Ti-G composites loaded with drug(s) are expected to be good candidates as functional bone repair materials with drug-delivery capabilities.

研究领域: 生物材料学 · 医学工程 · 药剂学
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2026 · IF 4.6

Colorimetric and fluorometric dual-response system for rapid analysis of gentamicin in real samples

Guo Wei,Rui Wang,Peile Cao,Peng Zhang,Jinhua Li,Lingxin Chen,Zhihua Song

Gentamicin (GENTA) have been extensively used by humans and animals, however, excessive GENTA resulted in environment and food contamination, and finally threatened human health. Therefore, it is very necessary to establish novel method for quantitative determination of GENTA in real samples. In this investigation, carbon dots incorporated with nitrogen and boron elements (N,B-CDs) with large stokes shift (125 nm) and high fluorescence intensity was designed, synthesized and utilized. In the process, 18 μL of the mixed solution was dropped onto the test strip each time; the test strip was tested by a smartphone and/or a miniaturized fluorimeter to achieve red (R), green (G), blue (B) and fluorescence intensity values after 1 min. The color and fluorescence intensity of the mixture changed obviously with gold nanoparticles (AuNPs) and GENTA adding. The limit of detection (LOD) of colorimetric and fluorometric dual-response system for GENTA was 0.30 μmol/L and 14.7 nmol/L, respectively. Furthermore, the selectivity and practicality of the system was assessed for other analytes (metal ions and other antibiotics) and real samples, respectively. The system showed excellent recovery (98.4%–103.9%) and outstanding repeatability (relative standard deviation (RSD), 1.2%–4.0%) for fluorometric determination of GENTA in real samples. Moreover, this system was suitable for colorimetric detection of GENTA (recovery, 94.8%–113.4%, RSD, 1.9%–7.9%). The good properties of N,B-CDs and miniaturized fluorimeter were combined for fluorescence determination of GENTA in real samples. And simple colorimetric detection of GENTA could be realized. In brief, we anticipate that this hybrid system could be useful for rapid and onsite detection of GENTA in environment, food, and pharmaceutical samples.

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INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS · 2026 · IF 5

Proteomics reveals the mechanism by which sodium oleate decreases Escherichia coli susceptibility to gentamicin

Lvyuan Fan,Jingyun Wu,Ziyi Zhang,Liting Cai,Yubin Su,Jiao Fei,Guozhu Ye

Sodium oleate reduces E. coli susceptibility to gentamicin • Sodium oleate enhances fatty acid degradation and elevates acetyl-CoA levels • Fatty acid metabolism-related substances influence antibiotic sensitivity • Reduced membrane potential and porin permeability limit drug uptake The World Health Organization has listed antibiotic resistance as one of the top ten health threats. There is an urgent need to analyze the resistance mechanism to develop novel anti-infection strategies. Fatty acids have been reported to promote antibiotic resistance; however, the underlying mechanism is complex and requires further exploration. To address this, we investigated the effect of sodium oleate-mediated resistance by proteomics. The present study corroborated that sodium oleate decreased the sensitivity of E. coli to gentamicin being visualized by fluorescence imaging, bacterial survival curve and minimum inhibitory concentration (MIC) assays. Proteomic profiles after treatment with gentamicin or sodium oleate were significantly different, with a number of proteins significantly changing. Pathway enrichment analysis showed that fatty acid biosynthesis and the stress response were upregulated under gentamicin treatment, whereas sodium oleate upregulated fatty acid degradation, amino acids metabolism, siderophore transmembrane transporter activity and enterobactin biosynthetic process. The addition of sodium oleate increased the expression levels of genes involved in the fatty acid degradation pathway by qPCR. Additionally, sodium linoleate and sodium palmitate also reduced bacterial sensitivity to gentamicin. The higher level of acetyl-CoA was found, and acetic acid/sodium acetate also reduced bacterial sensitivity to gentamicin, which was associated with protein acetylation. Moreover, sodium oleate caused a decrease in membrane potential and porin permeability, thereby affecting gentamicin uptake. This study provides new insights of fatty acid-mediated resistance, which may contribute to the development of novel strategies for addressing antibiotic resistance. Download: Download high-res image (238KB) Download: Download full-size image

CAS / MDL: 1405-41-0 822-17-3
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ACS Sustainable Chemistry & Engineering · 2025 · IF 7.3

Valorization of Gentamicin Mycelial Residues: CuCe/GMRC Catalysts for Selective Hydrogenation of Biobased Furfural

Yaoxin Xiao,Yazhuo Wang,Gangqi Cheng,Dong Liang,Zhen Huang,Rui Shan,Haoran Yuan,Yong Chen

Gentamicin mycelial residues (GMRs), hazardous organic wastes from antibiotic production, contain various valuable components, such as polysaccharides, proteins, and amino acids, making them an excellent nitrogen-rich feedstock for material synthesis. Here, we propose a strategy by utilizing GMRs as the sole nitrogen-rich carbon source to prepare Cu-based catalysts, which are employed in the catalytic transfer hydrogenation (CTH) of furfural (FFR). The catalytic performance was enhanced by trace amounts of Ce doping. Compared to the Cu/GMRC catalyst, the bimetallic CuCe/GMRC-x catalyst exhibited optimized acid–base site distribution and structural properties, resulting in superior efficiency and selectivity toward unsaturated carbonyl compounds. Especially, CuCe/GMRC-0.04 achieved near complete FFR conversion with 97.4% FA selectivity. By integrating experimental data and characterization results, it was further revealed that the critical role of metal sites and acid–base sites in determining the reactivity and product selectivity and potential reaction pathways were proposed. This work provides a sustainable approach to transform hazardous GMRs into valuable catalytic materials, offering insights into the high-value utilization of biomass-derived resources and the environmentally sustainable management of antibiotic mycelial residues.

CAS / MDL: 10031-43-3 10294-41-4
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Frontiers in Pharmacology · 2025 · IF 4.8

Combinatorial biosynthesis of novel gentamicin derivatives with nonsense mutation readthrough activity and low cytotoxicity

Lihua Yang,Hang Zhai,Tingting Tian,Botong Liu,Xianpu Ni,Huanzhang Xia*

Background: Aminoglycosides (AGs) are one of the initial classes of antibiotics that have been used clinically and possess broad spectrum of activity. Nevertheless, their clinical utilization is restricted by safety issues associated with nephrotoxicity and ototoxicity.Methods: Glycosyltransferase (GT) KanM2 was introduced into M. echinospora to produce the gentamicin derivatives, in which a kanosamine sugar ring was introduced to replace the garosamine. The premature termination codon (PTC) readthrough activity of genkamicins (GKs) was compared using dual luciferase reporter assay. The toxicity of GK was assessed in vitro in HEK-293 and NCI-H1299 cells and determined based on cell viability calculated after 48 h of treatment with different concentrations of the compounds. The NCI-H1299 cells harbouring the R213X nonsense mutation were treated with different concentrations of the derivatives to compare their expression of p53 proteins. The expression of p53 and its downstream targets p21 and BAX was detected using Western blotting and qRT-PCR in NCI-H1299 cells containing the R213X nonsense mutation treated with different concentrations of GK-Ae and G418. Finally, immunofluorescence and flow cytometry were used to determine the subcellular localization of full-length p53 protein induced by GK-Ae treatment and its effect on apoptosis in cancer cells.Results: Eight gentamicin derivatives were obtained in this study. GK-Ae displayed similar PTC readthrough activity and reduced toxicity compared to natural aminoglycoside G418. Moreover, GK-Ae increased the levels of both p53 and its downstream targets p21 and BAX, and promoted apoptosis of cancer cells.Conclusion: These results demonstrate the potential of combinatorial biosynthesis to increase the diversity of structures of AGs and provide directions for the development of new AGs with low toxicity and high PTC readthrough activity.

CAS / MDL: 65710-07-8 8063-07-8
研究领域: 药理学 · 分子生物学
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