Neves Monica Araujo das, Jesus Caroline Martins de, Oliveira Jhones Luiz de, Buna Samuel Dos Santos Soares, Silva Lucilene Amorim, Fraceto Leonardo Fernandes, Rocha Cláudia Quintino da
PostGraduate Program in Chemistry, Center for Exact Sciences and Technology (CCET), UFMA-Federal University of Maranhão, São Luís 65080-805, Brazil.
PostGraduate Program in Health Sciences, Center for Biological and Health Sciences (CCBS), UFMA-Federal University of Maranhão, São Luís 65080-805, Brazil.
Pharmaceutics. 2024 Dec 16;16(12):1603. doi: 10.3390/pharmaceutics16121603.
Leishmaniasis, caused by protozoa of the genus , is a major global health issue due to the limitations of current treatments, which include low efficacy, high costs, and severe side effects. This study aimed to develop a more effective and less toxic therapy by utilizing zein nanoparticles (ZNPs) in combination with a nonpolar fraction (DCMF) from (Syn. ), a plant rich in dimeric flavonoids called brachydins. Zein nanoparticles were used as carriers to encapsulate DCMF. The system was characterized by measuring particle diameter, polydispersity index, zeta potential, and encapsulation efficiency. Analytical techniques such as FTIR, DSC, and AFM were employed to confirm the encapsulation and stability of DCMF. Antileishmanial activity was assessed against promastigotes and amastigotes, while cytotoxicity was tested on RAW264.7 macrophages. The ZNP-DCMF system exhibited favorable properties, including a particle diameter of 141 nm, a polydispersity index below 0.2, and a zeta potential of 11.3 mV. DCMF was encapsulated with an efficiency of 94.6% and remained stable for 49 days. In antileishmanial assays, ZNP-DCMF inhibited the viability of promastigotes with an IC50 of 36.33 μg/mL and amastigotes with an IC50 of 0.72 μg/mL, demonstrating higher selectivity (SI = 694.44) compared to DCMF alone (SI = 43.11). ZNP-DCMF was non-cytotoxic to RAW264.7 macrophages, with a CC50 > 500 μg/mL. Combining DCMF with zein nanoparticles as a carrier presents a promising approach for leishmaniasis treatment, offering improved efficacy, reduced toxicity, and protection of bioactive compounds from degradation.
利什曼病由利什曼原虫属的原生动物引起，由于当前治疗方法存在局限性，包括疗效低、成本高和严重副作用，它成为了一个重大的全球健康问题。本研究旨在通过将玉米醇溶蛋白纳米颗粒（ZNPs）与来自 （同义词 ）的非极性馏分（DCMF）联合使用来开发一种更有效且毒性更小的疗法， 是一种富含名为短柄双黄酮的二聚体黄酮类化合物的植物。玉米醇溶蛋白纳米颗粒被用作载体来包裹DCMF。通过测量粒径、多分散指数、zeta电位和包封率对该系统进行表征。采用傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和原子力显微镜（AFM）等分析技术来确认DCMF的包封和稳定性。针对前鞭毛体和无鞭毛体评估抗利什曼活性，同时在RAW264.7巨噬细胞上测试细胞毒性。ZNP-DCMF系统表现出良好的特性，包括粒径为141 nm、多分散指数低于0.2以及zeta电位为11.3 mV。DCMF的包封率为94.6%，并且在49天内保持稳定。在抗利什曼试验中，ZNP-DCMF抑制前鞭毛体活力的IC50为36.33 μg/mL，抑制无鞭毛体活力的IC50为0.72 μg/mL，与单独的DCMF（SI = 43.11）相比，显示出更高的选择性（SI = 694.44）。ZNP-DCMF对RAW264.7巨噬细胞无细胞毒性，CC50 > 500 μg/mL。将DCMF与玉米醇溶蛋白纳米颗粒作为载体结合，为利什曼病治疗提供了一种有前景的方法，具有提高疗效、降低毒性以及保护生物活性化合物不被降解的优点。
