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Hesperidin- Curcumin- and Amphotericin B- Based Nano-Formulations as Potential Antibacterials

机译:基于橙皮苷、姜黄素和两性霉素 B 的纳米制剂作为潜在的抗菌剂

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摘要

To combat the public health threat posed by multiple-drug-resistant (MDR) pathogens, new drugs with novel chemistry and modes of action are needed. In this study, several drugs including Hesperidin (HES), curcumin (CUR), and Amphotericin B (AmpB) drug–nanoparticle formulations were tested for antibacterial strength against MDR Gram-positive bacteria, including Bacillus cereus, Streptococcus pyogenes, Methicillin-resistant Staphylococcus aureus (MRSA), and Streptococcus pneumoniae, and Gram-negative bacteria, including Escherichia coli K1, Pseudomonas aeruginosa, Salmonella enterica, and Serratia marcescens. Nanoparticles were synthesized and subjected to Atomic force microscopy, Fourier transform-infrared spectroscopy, and Zetasizer for their detailed characterization. Antibacterial assays were performed to determine their bactericidal efficacy. Lactate dehydrogenase (LDH) assays were carried out to measure drugs’ and drug–nanoparticles’ cytotoxic effects on human cells. Spherical NPs ranging from 153 to 300 nm were successfully synthesized. Results from antibacterial assays revealed that drugs and drug–nanoparticle formulations exerted bactericidal activity against MDR bacteria. Hesperidin alone failed to exhibit antibacterial effects but, upon conjugation with cinnamic-acid-based magnetic nanoparticle, exerted significant bactericidal activity against both the Gram-positive and Gram-negative isolates. AmpB-LBA-MNPs produced consistent, potent antibacterial efficacy (100% kill) against all Gram-positive bacteria. AmpB-LBA-MNPs showed strong antibacterial activity against Gram-negative bacteria. Intriguingly, all the drugs and their conjugated counterpart except AmpB showed minimal cytotoxicity against human cells. In summary, these innovative nanoparticle formulations have the potential to be utilized as therapeutic agents against infections caused by MDR bacteria and represent a significant advancement in our effort to counter MDR bacterial infections.
机译:为了应对多重耐药 (MDR) 病原体构成的公共卫生威胁,需要具有新型化学成分和作用方式的新药。在这项研究中,测试了包括橙皮苷 (HES)、姜黄素 (CUR) 和两性霉素 B (AmpB) 药物纳米颗粒制剂在内的几种药物对 MDR 革兰氏阳性菌的抗菌强度,包括蜡样芽孢杆菌、化脓性链球菌、耐甲氧西林金黄色葡萄球菌 (MRSA) 和肺炎链球菌,以及革兰氏阴性菌,包括大肠杆菌 K1、铜绿假单胞菌、肠道沙门氏菌和粘质沙雷氏菌。合成纳米颗粒并进行原子力显微镜、傅里叶变换红外光谱和 Zetasizer 进行详细表征。进行抗菌测定以确定其杀菌效果。进行乳酸脱氢酶 (LDH) 测定以测量药物和药物纳米颗粒对人体细胞的细胞毒性作用。成功合成了 153 至 300 nm 的球形 NPs。抗菌测定结果表明,药物和药物纳米颗粒制剂对 MDR 细菌具有杀菌活性。单独的橙皮苷未能表现出抗菌作用,但在与基于肉桂酸的磁性纳米颗粒结合后,对革兰氏阳性和革兰氏阴性分离株均具有显着的杀菌活性。AmpB-LBA-MNPs 对所有革兰氏阳性菌产生一致、有效的抗菌功效 (100% 杀灭)。AmpB-LBA-MNPs 对革兰氏阴性菌具有很强的抗菌活性。有趣的是,除 AmpB 外,所有药物及其偶联对应物对人类细胞的细胞毒性都很小。总之,这些创新的纳米颗粒制剂有可能用作治疗 MDR 细菌引起的感染的药物,并代表了我们在对抗 MDR 细菌感染方面的重大进步。

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