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

IF 3.6 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Hamdi Temel , Serap Yalçın Azarkan , Serkan Şahin
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引用次数: 0

摘要

日益严重的环境污染增加了人类接触有毒金属的风险。因此,需要一些物质来保护个人免受有毒金属造成的有害影响。但是çalışma, 3-metoksi katekol bileşiğinin 1,4-fenil diboronik asitle 1:1和1:2 3-甲氧基儿茶酚化合物与1,4-苯基二硼酸(1:1和1:1)和1,4-二(4-甲氧基苯并[d][1,3,2]二恶硼醇-2-基苯)硼酸(M86)和1,4-二(4-甲氧基苯并[d][1,3,2]二恶硼醇-2-基)苯(M87)对THLE-2肝细胞系铅(Pb)、镉(Cd)和砷(As)的毒性研究。合成的化合物M86和M87的结构通过1 H、13 C NMR、LC-MS-IT-TOF、UV-Vis等手段进行了表征。红外光谱。通过DPPH、ABTS、CUPRAC、抗胆碱酯酶、抗脲酶、抗甲状腺酶等试验对化合物的生物活性进行了评价。THLE-2细胞系采用二维和三维细胞模型。采用XTT试验和ATP比色法检测了M86和M87对Pb、Cd和As的保护作用,并测定了IC50值。在抗氧化试验中,与标准抗氧化剂-生育酚(-TOC)和丁基羟基甲苯(BHT)相比,M86和M87在ABTS、DPPH和CUPRAC试验中表现出较高的活性。酶抑制试验表明,M86和M87显著抑制乙酰胆碱酯酶(AChE)和丁基胆碱酯酶(BChE)活性。这些化合物被发现可以逆转铅、镉和砷暴露后细胞增殖的下降。综上所述,M86和M87有潜力成为多功能治疗剂,对金属毒性提供有效的保护。在未来,随着这些化合物在体内模型和临床研究中的疗效评估,认为它们有可能用于抗金属毒性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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.
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来源期刊
CiteScore
6.60
自引率
2.90%
发文量
202
审稿时长
85 days
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.
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