木耳酸过渡金属羧酸盐的抗菌活性和细胞毒性

European Pharmaceutical Journal Pub Date : 2021-01-01 DOI:10.2478/afpuc-2020-0018

L. Habala, Ľ. Pašková, A. Bilková, F. Bilka, B. Oboňová, J. Valentová

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引用次数: 1

摘要

摘要以柠檬酸为原料制备了具有生物活性的天然化合物——木耳酸与羧化型过渡金属配合物，并对其抗菌活性和细胞毒性进行了体外测试。产物以及木耳酸本身是两亲性化合物，包含亲水性头部（柠檬酸部分）和疏水性尾部（非极性烷基链）。基于元素分析、红外（IR）和高分辨率质谱（HR-MS），以及与含有柠檬酸盐部分的已知配合物类似，确定了羧酸盐的推定组成。金属羧酸盐在几种微生物菌株中显示出有趣的活性，尤其是对金黄色葡萄球菌（钒络合物；MIC=0.05mg/ml）。还测试了它们在肝细胞中的细胞毒性活性，在铜（II）和锰（II）复合物中发现了最高的活性。需要在这些初步结果的基础上进行进一步的研究，以评估金属络合物在溶液中的稳定性等参数对络合物生物活性的影响。

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Antimicrobial activity and cytotoxicity of transition metal carboxylates derived from agaric acid

Abstract Carboxylato-type transition metal complexes with agaric acid, a bioactive natural compound derived from citric acid, were prepared, and tested in vitro for their antimicrobial activity and cytotoxicity. The products as well as agaric acid itself are amphiphilic compounds containing a hydrophilic head (citric acid moiety) and a hydrophobic tail (non-polar alkyl chain). The putative composition of the carboxylates was assigned on grounds of elemental analysis, infrared (IR) and high-resolution mass spectra (HR-MS), as well as in analogy with known complexes containing the citrate moiety. The metal carboxylates showed interesting activity in several microbial strains, especially against S. aureus (vanadium complex; MIC = 0.05 mg/ml). They were also tested for their cytotoxic activity in hepatocytes, the highest activity having been found in the copper(II) and manganese(II) complexes. Further research based on these preliminary results is needed in order to evaluate the influence of parameters like stability of the metal complexes in solution on the bioactivity of the complexes.

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来源期刊

European Pharmaceutical Journal Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

0.60

自引率

0.00%

发文量

期刊介绍： European Pharmaceutical Journal publishes only original articles not previously published and articles that are not being considered or have not been submitted for publication elsewhere. If parts of the results have been published as conference abstract or elsewhere, it should be stated in references. The ethical standards of the Helsinki-Tokio Declaration should be kept. This should be mentioned in the Methods of manuscript. Reviews are published only on request. Authors, whose submitted research work was performed with the support of a company, should indicate this in Conflict of Interest.