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.
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。
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。
