{"title":"咪唑衍生物通过TrxR1、GST和GR对U-87 MG胶质瘤细胞的抑菌和抗氧化活性的影响","authors":"Işıl Nihan Korkmaz, Arzu Öztürk Kesebir","doi":"10.1002/jbt.70376","DOIUrl":null,"url":null,"abstract":"<div>\n \n <p>In the literature, it is seen that heteroaromatic imidazole compounds have many effective biological properties such as antitumor, antimicrobial, antioxidant, antihypertensive, antiallergic, anticancer, analgesic and anti-inflammatory. Due to these effects, its therapeutic effects in various types of cancer are being investigated more and more day by day. In particular, the effects of imidazole derivatives are being investigated for cancer types for which no treatment has yet been identified, such as Glioblastoma Multiforme (GBM). For this reason, the anticancer effects of imidazole derivatives on U-87 MG and HDFa cells, their inhibitory effects on TrxR1, GR and GST enzymes associated with multidrug resistance in cancer cells, and their antioxidant and antimicrobial activities were investigated. Cytotoxic effects were measured by MTT assay after U-87 MG HDFa cells were treated with imidazole compounds. The results revealed that imidazole compounds decreased the viability of cells in a dose-dependent manner compared to the control group. In addition, when imidazole compounds are used in treatments targeting enzymes in cancerous cells, it has been observed that they do not harm healthy HDFa cells, but they also have a significant effect on U-87 MG cells. It can be said that compound I3 is a selective inhibitor in the treatment of Glioblastoma. It was observed that compounds I2 and I3 have antimicrobial activity. When the antioxidant activities of imidazole derivatives were examined, we observed that compounds I2 and I3 exhibited antioxidant activity. These results show us that imidazole molecules have antioxidant, antimicrobial and anticancer effects.</p></div>","PeriodicalId":15151,"journal":{"name":"Journal of Biochemical and Molecular Toxicology","volume":"39 7","pages":""},"PeriodicalIF":3.2000,"publicationDate":"2025-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Effect of Imidazole Derivatives on U-87 MG Glioblastoma Cell Lines via TrxR1, GST and GR, Antimicrobial and Antioxidant Activities\",\"authors\":\"Işıl Nihan Korkmaz, Arzu Öztürk Kesebir\",\"doi\":\"10.1002/jbt.70376\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div>\\n \\n <p>In the literature, it is seen that heteroaromatic imidazole compounds have many effective biological properties such as antitumor, antimicrobial, antioxidant, antihypertensive, antiallergic, anticancer, analgesic and anti-inflammatory. Due to these effects, its therapeutic effects in various types of cancer are being investigated more and more day by day. In particular, the effects of imidazole derivatives are being investigated for cancer types for which no treatment has yet been identified, such as Glioblastoma Multiforme (GBM). For this reason, the anticancer effects of imidazole derivatives on U-87 MG and HDFa cells, their inhibitory effects on TrxR1, GR and GST enzymes associated with multidrug resistance in cancer cells, and their antioxidant and antimicrobial activities were investigated. Cytotoxic effects were measured by MTT assay after U-87 MG HDFa cells were treated with imidazole compounds. The results revealed that imidazole compounds decreased the viability of cells in a dose-dependent manner compared to the control group. In addition, when imidazole compounds are used in treatments targeting enzymes in cancerous cells, it has been observed that they do not harm healthy HDFa cells, but they also have a significant effect on U-87 MG cells. It can be said that compound I3 is a selective inhibitor in the treatment of Glioblastoma. It was observed that compounds I2 and I3 have antimicrobial activity. When the antioxidant activities of imidazole derivatives were examined, we observed that compounds I2 and I3 exhibited antioxidant activity. These results show us that imidazole molecules have antioxidant, antimicrobial and anticancer effects.</p></div>\",\"PeriodicalId\":15151,\"journal\":{\"name\":\"Journal of Biochemical and Molecular Toxicology\",\"volume\":\"39 7\",\"pages\":\"\"},\"PeriodicalIF\":3.2000,\"publicationDate\":\"2025-07-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Biochemical and Molecular Toxicology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://onlinelibrary.wiley.com/doi/10.1002/jbt.70376\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Biochemical and Molecular Toxicology","FirstCategoryId":"3","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/jbt.70376","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Effect of Imidazole Derivatives on U-87 MG Glioblastoma Cell Lines via TrxR1, GST and GR, Antimicrobial and Antioxidant Activities
In the literature, it is seen that heteroaromatic imidazole compounds have many effective biological properties such as antitumor, antimicrobial, antioxidant, antihypertensive, antiallergic, anticancer, analgesic and anti-inflammatory. Due to these effects, its therapeutic effects in various types of cancer are being investigated more and more day by day. In particular, the effects of imidazole derivatives are being investigated for cancer types for which no treatment has yet been identified, such as Glioblastoma Multiforme (GBM). For this reason, the anticancer effects of imidazole derivatives on U-87 MG and HDFa cells, their inhibitory effects on TrxR1, GR and GST enzymes associated with multidrug resistance in cancer cells, and their antioxidant and antimicrobial activities were investigated. Cytotoxic effects were measured by MTT assay after U-87 MG HDFa cells were treated with imidazole compounds. The results revealed that imidazole compounds decreased the viability of cells in a dose-dependent manner compared to the control group. In addition, when imidazole compounds are used in treatments targeting enzymes in cancerous cells, it has been observed that they do not harm healthy HDFa cells, but they also have a significant effect on U-87 MG cells. It can be said that compound I3 is a selective inhibitor in the treatment of Glioblastoma. It was observed that compounds I2 and I3 have antimicrobial activity. When the antioxidant activities of imidazole derivatives were examined, we observed that compounds I2 and I3 exhibited antioxidant activity. These results show us that imidazole molecules have antioxidant, antimicrobial and anticancer effects.
期刊介绍:
The Journal of Biochemical and Molecular Toxicology is an international journal that contains original research papers, rapid communications, mini-reviews, and book reviews, all focusing on the molecular mechanisms of action and detoxication of exogenous and endogenous chemicals and toxic agents. The scope includes effects on the organism at all stages of development, on organ systems, tissues, and cells as well as on enzymes, receptors, hormones, and genes. The biochemical and molecular aspects of uptake, transport, storage, excretion, lactivation and detoxication of drugs, agricultural, industrial and environmental chemicals, natural products and food additives are all subjects suitable for publication. Of particular interest are aspects of molecular biology related to biochemical toxicology. These include studies of the expression of genes related to detoxication and activation enzymes, toxicants with modes of action involving effects on nucleic acids, gene expression and protein synthesis, and the toxicity of products derived from biotechnology.