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镍(II)氯化物席夫碱配合物的合成、表征、毒性、抗菌和杀利什曼原虫活性。

Nickel (II) chloride schiff base complex: Synthesis, characterization, toxicity, antibacterial and leishmanicidal activity.

机构信息

Agrarian and Environmental Sciences Center, Federal University of Maranhão, Chapadinha, Maranhão, Brazil.

Department of Biological Chemistry, Regional University of Cariri, Crato, Ceará, Brazil.

出版信息

Chem Biol Interact. 2022 Jan 5;351:109714. doi: 10.1016/j.cbi.2021.109714. Epub 2021 Oct 25.

DOI:10.1016/j.cbi.2021.109714
PMID:34710376
Abstract

The use of schiff base complex against microbial agentes a has recently received more attention as a strategy to combat infections caused by multidrug-resistant bacteria and leishmania. This study aimed to evaluate the toxicity, antibacterial and leishmanicidal activities of the nickel (II) chloride schiff base complex ([Ni(L2)] against Leishmania amazonensis promastigote, multi-resistant bacterial strains and evaluate to modulate antibiotic activity against multi-resistant bacterial. The schiff base complex was characterized by the techniques of elemental analysis, Fourier transform infrared spectroscopy (FTIR), UV-vis absorption spectroscopy and thermal analysis (TGA/DTG/DSC). The [Ni(L2)] complex presented moderate toxicity in saline artemia (LC = 150.8 μg/mL). In leishmanicidal assay, the NiL2 complex showed values of IC of (6.079 μg/mL ± 0.05656 at the 24 h), (0.854 μg/mL ± 0.02474, 48 h) and (1.076 μg/mL ± 0.04039, 72 h). In antibacterial assay, the [Ni(L2)] complex presented significant inhibited the bacterial growth of P. aeruginosa (MIC = 256 μg/mL). However, [Ni(L2)] complex did not present clinically relevant minimum inhibitory concentration (MIC ≥1024 μg/mL) against S. aureus and E. coli. The combination of [Ni(L2)] complex and antibacterial drugs resulted in the increased antibiotic activity of gentamicin and amikacin against S. aureus and E.coli multi-resistant strains. Thus, our results showed that [Ni(L2)] complex is a promising molecule for the development of new therapies associated with aminoglycoside antibiotics and in disease control related to resistant bacteria and leishmaniasis.

摘要

席夫碱配合物在医学领域的应用

席夫碱配合物作为一种对抗多药耐药菌和利什曼原虫感染的策略,最近受到了更多的关注。本研究旨在评估氯化镍(II)席夫碱配合物([Ni(L2)])对利什曼原虫无鞭毛体、多耐药菌的毒性、抗菌和杀利什曼原虫活性,并评估其对抗多耐药菌的抗生素活性的调节作用。席夫碱配合物采用元素分析、傅里叶变换红外光谱(FTIR)、紫外可见吸收光谱和热分析(TGA/DTG/DSC)进行表征。[Ni(L2)]配合物在盐水丰年虾(LC=150.8μg/mL)中表现出中等毒性。在杀利什曼原虫试验中,NiL2 配合物在 24 小时时的 IC 值为(6.079μg/mL±0.05656),在 48 小时时为(0.854μg/mL±0.02474),在 72 小时时为(1.076μg/mL±0.04039)。在抗菌试验中,[Ni(L2)]配合物显著抑制了铜绿假单胞菌的生长(MIC=256μg/mL)。然而,[Ni(L2)]配合物对金黄色葡萄球菌和大肠杆菌没有表现出临床相关的最小抑菌浓度(MIC≥1024μg/mL)。[Ni(L2)]配合物与抗菌药物联合使用,增加了庆大霉素和阿米卡星对金黄色葡萄球菌和大肠杆菌多耐药株的抗生素活性。因此,我们的结果表明,[Ni(L2)]配合物是一种很有前途的分子,可用于开发与氨基糖苷类抗生素相关的新疗法,并可控制与耐药菌和利什曼病相关的疾病。

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