{"title":"在二维和三维肝细胞模型中评价M86和M87化合物对铅、镉和砷的毒性","authors":"Hamdi Temel , Serap Yalçın Azarkan , Serkan Şahin","doi":"10.1016/j.jtemb.2025.127665","DOIUrl":null,"url":null,"abstract":"<div><div>Increasing environmental pollution increases the risk of human exposure to toxic metals. Therefore, there is a need for substances to protect individuals against the harmful effects caused by toxic metals. Bu çalışma, 3-metoksi katekol bileşiğinin 1,4-fenil diboronik asitle 1:1 ve 1:2 mol ratios of 3-methoxy catechol compound with 1,4-phenyl diboronic acid (1:1 and 1:1) and 1,4-bis(4-methoxybenzo[<em>d</em>][1,3,2]dioxaborol-2-yl)phenyl)boronic acid (M86) and 1,4-bis(4-methoxybenzo[<em>d</em>][1,3,2]dioxaborol-2-yl)benzene (M87) against lead (Pb), cadmium (Cd) and arsenic (As) toxicity in THLE-2 liver cell line. The structures of synthesized compounds M86 and M87 were characterized by 1 H, 13 C NMR, LC-MS-IT-TOF, UV-Vis., FTIR. The biological activities of these compounds were evaluated by DPPH, ABTS, CUPRAC, anticholinesterase, antiurease and antithyrosinase tests. 2D and 3D cell models were used in THLE-2 cell line. The protective effects of M86 and M87 against Pb, Cd and As toxicity were examined by XTT test and ATP colorimetric method and IC50 values were determined. In antioxidant tests, it was observed that M86 and M87 exhibited high activity in ABTS, DPPH and CUPRAC tests compared to standard antioxidants ?-tocopherol (?-TOC) and butylated hydroxytoluene (BHT). Enzyme inhibition tests showed that M86 and M87 significantly suppressed acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzyme activities. These compounds were found to reverse the decrease in cell proliferation following Pb, Cd and As exposure. In conclusion, M86 and M87 have the potential to be versatile therapeutic agents that provide effective protection against metal toxicity. In the future, with the evaluation of the efficacy of these compounds in in vivo models and clinical studies, it is thought that their use against metal toxicity may be possible.</div></div>","PeriodicalId":49970,"journal":{"name":"Journal of Trace Elements in Medicine and Biology","volume":"89 ","pages":"Article 127665"},"PeriodicalIF":3.6000,"publicationDate":"2025-05-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Evaluation of M86 and M87 compounds against lead, cadmium, and arsenic toxicity in 2D and 3D liver cell models\",\"authors\":\"Hamdi Temel , Serap Yalçın Azarkan , Serkan Şahin\",\"doi\":\"10.1016/j.jtemb.2025.127665\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Increasing environmental pollution increases the risk of human exposure to toxic metals. Therefore, there is a need for substances to protect individuals against the harmful effects caused by toxic metals. Bu çalışma, 3-metoksi katekol bileşiğinin 1,4-fenil diboronik asitle 1:1 ve 1:2 mol ratios of 3-methoxy catechol compound with 1,4-phenyl diboronic acid (1:1 and 1:1) and 1,4-bis(4-methoxybenzo[<em>d</em>][1,3,2]dioxaborol-2-yl)phenyl)boronic acid (M86) and 1,4-bis(4-methoxybenzo[<em>d</em>][1,3,2]dioxaborol-2-yl)benzene (M87) against lead (Pb), cadmium (Cd) and arsenic (As) toxicity in THLE-2 liver cell line. The structures of synthesized compounds M86 and M87 were characterized by 1 H, 13 C NMR, LC-MS-IT-TOF, UV-Vis., FTIR. The biological activities of these compounds were evaluated by DPPH, ABTS, CUPRAC, anticholinesterase, antiurease and antithyrosinase tests. 2D and 3D cell models were used in THLE-2 cell line. The protective effects of M86 and M87 against Pb, Cd and As toxicity were examined by XTT test and ATP colorimetric method and IC50 values were determined. In antioxidant tests, it was observed that M86 and M87 exhibited high activity in ABTS, DPPH and CUPRAC tests compared to standard antioxidants ?-tocopherol (?-TOC) and butylated hydroxytoluene (BHT). Enzyme inhibition tests showed that M86 and M87 significantly suppressed acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzyme activities. These compounds were found to reverse the decrease in cell proliferation following Pb, Cd and As exposure. In conclusion, M86 and M87 have the potential to be versatile therapeutic agents that provide effective protection against metal toxicity. In the future, with the evaluation of the efficacy of these compounds in in vivo models and clinical studies, it is thought that their use against metal toxicity may be possible.</div></div>\",\"PeriodicalId\":49970,\"journal\":{\"name\":\"Journal of Trace Elements in Medicine and Biology\",\"volume\":\"89 \",\"pages\":\"Article 127665\"},\"PeriodicalIF\":3.6000,\"publicationDate\":\"2025-05-11\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Trace Elements in Medicine and Biology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0946672X25000781\",\"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 Trace Elements in Medicine and Biology","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0946672X25000781","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Evaluation of M86 and M87 compounds against lead, cadmium, and arsenic toxicity in 2D and 3D liver cell models
Increasing environmental pollution increases the risk of human exposure to toxic metals. Therefore, there is a need for substances to protect individuals against the harmful effects caused by toxic metals. Bu çalışma, 3-metoksi katekol bileşiğinin 1,4-fenil diboronik asitle 1:1 ve 1:2 mol ratios of 3-methoxy catechol compound with 1,4-phenyl diboronic acid (1:1 and 1:1) and 1,4-bis(4-methoxybenzo[d][1,3,2]dioxaborol-2-yl)phenyl)boronic acid (M86) and 1,4-bis(4-methoxybenzo[d][1,3,2]dioxaborol-2-yl)benzene (M87) against lead (Pb), cadmium (Cd) and arsenic (As) toxicity in THLE-2 liver cell line. The structures of synthesized compounds M86 and M87 were characterized by 1 H, 13 C NMR, LC-MS-IT-TOF, UV-Vis., FTIR. The biological activities of these compounds were evaluated by DPPH, ABTS, CUPRAC, anticholinesterase, antiurease and antithyrosinase tests. 2D and 3D cell models were used in THLE-2 cell line. The protective effects of M86 and M87 against Pb, Cd and As toxicity were examined by XTT test and ATP colorimetric method and IC50 values were determined. In antioxidant tests, it was observed that M86 and M87 exhibited high activity in ABTS, DPPH and CUPRAC tests compared to standard antioxidants ?-tocopherol (?-TOC) and butylated hydroxytoluene (BHT). Enzyme inhibition tests showed that M86 and M87 significantly suppressed acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzyme activities. These compounds were found to reverse the decrease in cell proliferation following Pb, Cd and As exposure. In conclusion, M86 and M87 have the potential to be versatile therapeutic agents that provide effective protection against metal toxicity. In the future, with the evaluation of the efficacy of these compounds in in vivo models and clinical studies, it is thought that their use against metal toxicity may be possible.
期刊介绍:
The journal provides the reader with a thorough description of theoretical and applied aspects of trace elements in medicine and biology and is devoted to the advancement of scientific knowledge about trace elements and trace element species. Trace elements play essential roles in the maintenance of physiological processes. During the last decades there has been a great deal of scientific investigation about the function and binding of trace elements. The Journal of Trace Elements in Medicine and Biology focuses on the description and dissemination of scientific results concerning the role of trace elements with respect to their mode of action in health and disease and nutritional importance. Progress in the knowledge of the biological role of trace elements depends, however, on advances in trace elements chemistry. Thus the Journal of Trace Elements in Medicine and Biology will include only those papers that base their results on proven analytical methods.
Also, we only publish those articles in which the quality assurance regarding the execution of experiments and achievement of results is guaranteed.