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解读替考拉宁的遗传毒性和细胞毒性特性:实验室与计算相结合的研究

Deciphering the genotoxic and cytotoxic properties of teicoplanin: a combined laboratory and computational investigation.

作者信息

Berber Ahmet Ali, Aliravci Işıl Deniz, Akinci Kenanoğlu Nihan, Demir Şefika Nur

机构信息

Vocational School of Health Services, Çanakkale Onsekiz Mart University, Çanakkale, Turkey.

Health Practice and Research Hospital, Infectious Diseases and Clinical Microbiology Clinic, Çanakkale Onsekiz Mart University, Çanakkale, Turkey.

出版信息

Drug Chem Toxicol. 2025 Sep;48(5):1015-1024. doi: 10.1080/01480545.2025.2502446. Epub 2025 May 8.

Abstract

In this study, the mutagenicity and carcinogenicity of the teicoplanin antibiotic were first investigated using the Vega Hub and Toxtree software through prediction. The cytotoxic and genotoxic effects were evaluated using assays, including the mitotic index (MI), micronucleus (MN), nuclear division index (NDI), and Comet Assay (CA) in human lymphocytes. In the studies, both 24-hour and 48-hour exposures were conducted for MI, and teicoplanin significantly decreased MI compared to the control at all concentrations. In addition, a significant increase was detected in the MN frequency compared to the negative control at all concentrations. In the Comet assay, tail length significantly increased compared to the control at all concentrations except for 5.6 µg/mL, while tail moment and comet tail intensity significantly increased at all concentrations compared to the control. In conclusion, within the concentration range used in this study, teicoplanin was found to have cytotoxic and genotoxic effects.

摘要

在本研究中,首先使用Vega Hub和Toxtree软件通过预测对替考拉宁抗生素的致突变性和致癌性进行了研究。使用包括人淋巴细胞有丝分裂指数(MI)、微核(MN)、核分裂指数(NDI)和彗星试验(CA)在内的试验评估细胞毒性和遗传毒性作用。在这些研究中,对MI进行了24小时和48小时的暴露试验,与对照组相比,替考拉宁在所有浓度下均显著降低了MI。此外,与阴性对照组相比,所有浓度下的MN频率均显著增加。在彗星试验中,除5.6 µg/mL外,所有浓度下的尾长与对照组相比均显著增加,而与对照组相比,所有浓度下的尾矩和彗星尾强度均显著增加。总之,在本研究使用的浓度范围内,发现替考拉宁具有细胞毒性和遗传毒性作用。

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