Programa de Pós-Graduação em Biotecnologia, PPGBIOTEC, Universidade Federal do Delta do Parnaíba, UFDPar, Parnaíba, Piauí, PI, Brasil; Núcleo de Pesquisa em Biodiversidade e Biotecnologia, BIOTEC, Universidade Federal do Delta do Parnaíba, UFDPar, Parnaíba, Piauí, PI, Brasil; Grupo de Pesquisa em Química Medicinal e Biotecnologia, QUIMEBIO, Universidade Federal do Maranhão, UFMA, São Bernardo, Maranhão, MA, Brasil.
Programa de Pós-Graduação em Biotecnologia, PPGBIOTEC, Universidade Federal do Delta do Parnaíba, UFDPar, Parnaíba, Piauí, PI, Brasil; Núcleo de Pesquisa em Biodiversidade e Biotecnologia, BIOTEC, Universidade Federal do Delta do Parnaíba, UFDPar, Parnaíba, Piauí, PI, Brasil; Laboratório de Doenças Infecciosas, LADIC, Universidade Federal do Delta do Parnaíba, UFDPar, Parnaíba, Piauí, PI, Brasil.
Int J Biol Macromol. 2024 Aug;274(Pt 2):133048. doi: 10.1016/j.ijbiomac.2024.133048. Epub 2024 Jun 8.
Epiisopiloturine (EPI) is a compound found in jaborandi leaves with antiparasitic activity, which can be enhanced when incorporated into nanoparticles (NP). Cashew Gum (CG), modified by carboxymethylation, is used to produce polymeric nanomaterials with biological activity. In this study, we investigated the antimicrobial potential of carboxymethylated CG (CCG) NP containing EPI (NPCCGE) and without the alkaloid (NPCCG) against bacteria and parasites of the genus Leishmania. We conducted theoretical studies, carboxymethylated CG, synthesized NP by nanoprecipitation, characterized them, and tested them in vitro. Theoretical studies confirmed the stability of modified carbohydrates and showed that the EPI-4A30 complex had the best interaction energy (-8.47 kcal/mol). CCG was confirmed by FT-IR and presented DS of 0.23. NPCCG and NPCCGE had average sizes of 221.94 ± 144.086 nm and 247.36 ± 3.827 nm, respectively, with homogeneous distribution and uniform surfaces. No NP showed antibacterial activity or cytotoxicity to macrophages. NPCCGE demonstrated antileishmanial activity against L. amazonensis, both in promastigote forms (IC = 9.52 μg/mL, SI = 42.01) and axenic amastigote forms (EC = 6.6 μg/mL, SI = 60.60). The results suggest that nanostructuring EPI in CCG enhances its antileishmanial activity.
表小檗碱(EPI)是存在于贯叶连翘叶中的一种具有抗寄生虫活性的化合物,当它被纳入纳米颗粒(NP)时,其活性可以增强。腰果胶(CG)经羧甲基化修饰后,可用于制备具有生物活性的聚合纳米材料。在本研究中,我们研究了含有 EPI 的羧甲基化 CG(CCG)NP(NPCCGE)和不含生物碱的 NPCCG 对利什曼原虫属细菌和寄生虫的抗菌潜力。我们进行了理论研究、羧甲基化 CG 的合成、纳米沉淀法制备 NP,并对其进行了表征和体外测试。理论研究证实了修饰碳水化合物的稳定性,并表明 EPI-4A30 复合物具有最佳的相互作用能(-8.47 kcal/mol)。FT-IR 证实了 CCG 的存在,其取代度为 0.23。NPCCG 和 NPCCGE 的平均粒径分别为 221.94 ± 144.086nm 和 247.36 ± 3.827nm,具有均匀的分布和均匀的表面。没有 NP 表现出对细菌的抗菌活性或对巨噬细胞的细胞毒性。NPCCGE 对 L. amazonensis 的前鞭毛体形式(IC = 9.52 μg/mL,SI = 42.01)和无细胞内阿米巴形式(EC = 6.6 μg/mL,SI = 60.60)均具有抗利什曼原虫活性。结果表明,EPI 在 CCG 中的纳米结构增强了其抗利什曼原虫活性。