Abstract:
Aim: Octyl gallate (OG) loaded into a nanostructured lipid system (NLS) was tested for antifungal activity and in vitro and in vivo toxicity. Methods & Results: The features of NLS-OG were analyzed by dynamic light scattering and showed adequate size (132.1 nm) and homogeneity (polydispersity index = 0.200). OG was active against Paraccoccidioides spp., and NLS-OG did not affect antifungal activity. NLS-OG demonstrated reduced toxicity to lung cells and zebrafish embryos compared with OG, whereas NLS was toxic to hepatic cells. OG and NLS-OG did not show toxicity in a Galleria mellonella model at 20 mg/kg. All toxic concentrations were superior to MIC (antifungal activity). Conclusion: These results indicate good anti-Paracoccidioides activity and low toxicity of NLS-OG.
Plain language summary Drugs for the treatment of fungal diseases are limited in number and present side effects, drug interactions, risks for pregnant women and fungal resistance. The authors produced a derivative compound from plants called octyl gallate (OG) and then incorporated it into a nanoparticle lipid system (NLS) for better distribution in biological fluids. NLS-OG was tested against a fungus called Paracoccidioides, which causes lung infections. The toxicity profile of NLS-OG was also evaluated in lung and hepatic cells as well as novel animal models. NLS-OG presented good antifungal activity and low toxicity in lung cells and embryos.
摘要:
目的:测试了加载到纳米结构脂质系统(NLS)中的没食子酸辛酯(OG)的抗真菌活性以及体外和体内毒性。方法和结果:通过动态光散射分析NLS-OG的特征,并显示出足够的尺寸(132.1nm)和均匀性(多分散指数=0.200)。OG对副球藻属具有活性。,和NLS-OG不影响抗真菌活性。与OG相比,NLS-OG对肺细胞和斑马鱼胚胎的毒性降低,而NLS对肝细胞有毒性。OG和NLS-OG在20mg/kg的美罗兰模型中未显示毒性。所有毒性浓度均优于MIC(抗真菌活性)。结论:这些结果表明,NLS-OG具有良好的抗副球菌活性和低毒性。
简单的语言总结治疗真菌疾病的药物数量有限,并且存在副作用,药物相互作用,孕妇的风险和真菌耐药性。作者从植物中产生了一种衍生化合物,称为没食子酸辛酯(OG),然后将其掺入纳米颗粒脂质系统(NLS)中,以便在生物流体中更好地分布。对NLS-OG进行了一种名为副球菌的真菌的测试,导致肺部感染.还在肺和肝细胞以及新型动物模型中评估了NLS-OG的毒性谱。NLS-OG在肺细胞和胚胎中具有良好的抗真菌活性和低毒性。