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A new Cu(II)-O-Carvacrotinate complex: Synthesis, characterization and biological activity.
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2018-09-29 , DOI: 10.1016/j.jinorgbio.2018.09.018
Manas Sutradhar 1 , Alexandra R Fernandes 2 , Fabiana Paradinha 3 , Patricia Rijo 4 , Catarina Garcia 4 , Catarina Roma-Rodrigues 3 , Armando J L Pombeiro 1 , Adília Januário Charmier 5
Affiliation  

Herein, we report the first example of the synthesis of a novel type of Cu(II) complex based on a natural product ligand derived from carvacrol. The copper(II) complex [Cu(DCA)2(EtOH)]2·2EtOH (1, HDCAO-carvacrotinic acid) has been synthesized and characterized by elemental analysis, IR spectroscopy, ESI-MS and single crystal X-ray analysis. Complex 1 and the carvacrotinic acid (2, HDCA) have been studied towards their antimicrobial and antiproliferative activities. For both compounds the antimicrobial activity was assessed against a panel of Gram-positive and Gram-negative bacteria and yeasts. The microdilution method allowed the determination of their Minimum Inhibitory Concentration (MIC) and minimum bactericidal concentration (MBC). Interestingly, both compounds seem to be more effective on yeasts rather than bacteria especially against C. albicans. Regarding the antimicrobial properties, the compounds appear to present a bacteriostatic behaviour, rather than bactericide. The antiproliferative effect of complex 1, O-carvacrotinic acid (HDCA) 2 and carvacrol (CA) 3 used as a reference to compare their antitumoral activity, was examined in 4 human tumor cell lines (ovarian carcinoma (A2780), colorectal carcinoma (HCT116), lung adenocarcinoma (A549) and breast adenocarcinoma (MCF7)) and in normal human primary fibroblasts. Complex 1 exhibits a moderate cytotoxic activity against ovarian carcinoma cells (A2780), with no cytotoxicity in normal primary human fibroblasts. The moderate cytotoxicity observed in A2780 cells was due to an increase of cell apoptosis.

中文翻译:

一种新的Cu(II)-O-Carvacrotinate配合物:合成,表征和生物活性。

本文中,我们报告了基于衍生自香芹酚的天然产物配体的新型Cu(II)配合物合成的第一个实例。合成了铜(II)配合物[Cu(DCA)2(EtOH)] 2·2EtOH(1,HDCAO-香芹素酸),并通过元素分析,红外光谱,ESI-MS和单晶X射线分析对其进行了表征。已经研究了复合物1和香菜碱酸(2,HDCA)的抗微生物和抗增殖活性。对于这两种化合物,针对一组革兰氏阳性和革兰氏阴性细菌和酵母菌评估了抗微生物活性。微量稀释法可以测定其最小抑菌浓度(MIC)和最小杀菌浓度(MBC)。有趣的是,这两种化合物似乎对酵母比对细菌更有效,尤其是针对C。白色的。关于抗菌性能,这些化合物似乎具有抑菌行为,而不是杀菌剂。在4种人类肿瘤细胞系(卵巢癌(A2780),结直肠癌(HCT116) ),肺腺癌(A549)和乳腺腺癌(MCF7))和正常人原代成纤维细胞中。复合物1对卵巢癌细胞(A2780)表现出中等的细胞毒性活性,在正常的原代人成纤维细胞中没有细胞毒性。在A2780细胞中观察到的中等细胞毒性是由于细胞凋亡的增加所致。在4种人类肿瘤细胞系(卵巢癌(A2780),结直肠癌(HCT116) ),肺腺癌(A549)和乳腺腺癌(MCF7))和正常人原代成纤维细胞中。复合物1对卵巢癌细胞(A2780)表现出中等的细胞毒性活性,在正常的原代人成纤维细胞中没有细胞毒性。在A2780细胞中观察到的中等细胞毒性是由于细胞凋亡的增加所致。在4种人类肿瘤细胞系(卵巢癌(A2780),结直肠癌(HCT116) ),肺腺癌(A549)和乳腺腺癌(MCF7))和正常人原代成纤维细胞中。复合物1对卵巢癌细胞(A2780)表现出中等的细胞毒性活性,在正常的原代人成纤维细胞中没有细胞毒性。在A2780细胞中观察到的中等细胞毒性是由于细胞凋亡的增加所致。肺腺癌(A549)和乳腺腺癌(MCF7))和正常人原代成纤维细胞中。复合物1对卵巢癌细胞(A2780)表现出中等的细胞毒性活性,在正常的原代人成纤维细胞中没有细胞毒性。在A2780细胞中观察到的中等细胞毒性是由于细胞凋亡的增加。肺腺癌(A549)和乳腺腺癌(MCF7))和正常人原代成纤维细胞中。复合物1对卵巢癌细胞(A2780)表现出中等的细胞毒性活性,在正常的原代人成纤维细胞中没有细胞毒性。在A2780细胞中观察到的中等细胞毒性是由于细胞凋亡的增加所致。
更新日期:2018-09-29
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