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新型具有抗菌和细胞毒性活性的铜配合物。

New Copper Complexes with Antibacterial and Cytotoxic Activity.

机构信息

Department of Inorganic Chemistry, Faculty of Pharmacy, "Iuliu-Hațieganu" University of Medicine and Pharmacy, 400012 Cluj-Napoca, Romania.

Department of Pharmaceutical Biochemistry and Clinical Laboratory, Faculty of Pharmacy, "Iuliu-Hațieganu" University of Medicine and Pharmacy, 400012 Cluj-Napoca, Romania.

出版信息

Int J Mol Sci. 2023 Sep 7;24(18):13819. doi: 10.3390/ijms241813819.

DOI:10.3390/ijms241813819
PMID:37762121
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10530662/
Abstract

The discovery of a new non-toxic metal complex with biological activity represents a very active area of research. Two Cu complexes, [Cu(L1)(OH)(DMF)(HO)] (C1) (HL1 = N-(5-ethyl-[1,3,4]-thiadiazole-2-yl)-benzenesulfonamide) and [Cu(L2)(phen)(HO)] (C2) (HL2 = N-(5-(4-methylphenyl)-[1,3,4]-thiadiazole-2-yl)-naphtalenesulfonamide), with two new ligands were synthesized. The X-ray crystal structures of the complexes were determined. In both complexes, Cu is five-coordinated, forming a CuNO and CuNO chromophore, respectively. The ligands act as monodentate, coordinating the metal ion through a single N atom; for the two complexes, the molecules from the reaction medium (phenantroline, dimethylformamide and water) are also involved in the coordination of Cu. The complexes have a distorted square pyramidal square-planar geometry. The compounds were characterized by FT-IR and UV-Vis spectroscopy. Using the microdilution method, the antibacterial activity of the complexes was determined against four Gram-positive and two Gram-negative bacteria, with Gentamicin as the positive control. Cytotoxicity studies were carried out on two tumor cell lines (HeLa, DLD-1) and on a normal cell line (HFL1) using the MTT method and Cisplatin as a positive control. Flow cytometric assessment of apoptosis induced by the complexes on the three cell lines was also performed. Both complexes present in vitro biological activities but complex C2 is more active.

摘要

具有生物活性的新型无毒金属配合物的发现代表了一个非常活跃的研究领域。合成了两个具有两个新配体的 Cu 配合物 [Cu(L1)(OH)(DMF)(HO)] (C1) (HL1 = N-(5-ethyl-[1,3,4]-thiadiazole-2-yl)-benzenesulfonamide) 和 [Cu(L2)(phen)(HO)] (C2) (HL2 = N-(5-(4-methylphenyl)-[1,3,4]-thiadiazole-2-yl)-naphtalenesulfonamide)。配合物的晶体结构通过 X 射线衍射确定。在两个配合物中,Cu 都是五配位的,分别形成 CuNO 和 CuNO 发色团。配体作为单齿配体,通过单个 N 原子与金属离子配位;对于两个配合物,来自反应介质(邻菲咯啉、二甲基甲酰胺和水)的分子也参与了 Cu 的配位。配合物具有扭曲的四方锥四方平面几何形状。通过傅里叶变换红外光谱和紫外可见光谱对化合物进行了表征。采用微量稀释法,测定了配合物对四种革兰氏阳性菌和两种革兰氏阴性菌的抗菌活性,以庆大霉素作为阳性对照。使用 MTT 法和顺铂作为阳性对照,在两种肿瘤细胞系(HeLa、DLD-1)和正常细胞系(HFL1)上进行了细胞毒性研究。还通过流式细胞术评估了配合物对三种细胞系诱导凋亡的作用。两个配合物均具有体外生物活性,但配合物 C2 的活性更高。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/375e2b8dd97c/ijms-24-13819-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/09d11a47300f/ijms-24-13819-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/ba46fd7223bc/ijms-24-13819-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/a177134d77d1/ijms-24-13819-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/00f3ad362c3e/ijms-24-13819-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/2c4d70311271/ijms-24-13819-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/375e2b8dd97c/ijms-24-13819-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/09d11a47300f/ijms-24-13819-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/74f2332b1be7/ijms-24-13819-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/83a2329dd54d/ijms-24-13819-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/b112ccb47945/ijms-24-13819-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/ba46fd7223bc/ijms-24-13819-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/a177134d77d1/ijms-24-13819-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/00f3ad362c3e/ijms-24-13819-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/2c4d70311271/ijms-24-13819-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3be0/10530662/375e2b8dd97c/ijms-24-13819-sch001.jpg

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