Silva-Silva João Victor, Moragas-Tellis Carla Junqueira, Chagas Maria do Socorro Dos Santos, de Souza Paulo Victor Ramos, de Souza Celeste da Silva Freitas, Hardoim Daiana de Jesus, Taniwaki Noemi Nosomi, Moreira Davyson de Lima, Dutra Behrens Maria, Calabrese Kátia da Silva, Almeida-Souza Fernando
Laboratory of Immunomodulation and Protozoology, Oswaldo Cruz Institute, Oswaldo Cruz Foundation, Rio de Janeiro, Brazil.
Laboratory of Natural Products for Public Health, Pharmaceutical Techonology Institute - Farmanguinhos, Oswaldo Cruz Foundation, Rio de Janeiro, Brazil.
Front Pharmacol. 2021 Jul 20;12:703985. doi: 10.3389/fphar.2021.703985. eCollection 2021.
Acknowledging the need of identifying new compounds for the treatment of leishmaniasis, this study aimed to evaluate, from trials, the activity of flavones from against . The chromatographic profiles of the hydroethanolic extract and a flavone-rich fraction (ACFF) from were determined by high-performance liquid chromatography coupled with a diode-array UV-Vis detector (HPLC-DAD-UV) and electrospray ionization mass spectrometry in tandem (LC-ESI-MS-MS). The flavones luteolin () and apigenin (), isolated from chromatographic techniques and identified by Nuclear Magnetic Resonance of H and C, were also quantified in ACFF, showing 190.7 mg/g and apigenin 12.4 mg/g, respectively. The other flavones were identified by comparing their spectroscopic data with those of the literature. The activity was assayed against promastigotes and intramacrophagic amastigote forms of . Cytotoxicity tests were performed with peritoneal macrophages of BALB/c mice. Nitrite quantification was performed with Griess reagent. Ultrastructural investigations were obtained by transmission electron microscopy. Anti- assays indicated that the IC values for ACFF, apigenin, and luteolin were obtained at 40.42 ± 0.10 and 31.51 ± 1.13 μg/mL against promastigotes, respectively. ACFF and luteolin have concentration-dependent cytotoxicity. ACFF and luteolin also inhibited the intra-macrophagic parasite (IC 3.575 ± 1.13 and 11.78 ± 1.24 μg/mL, respectively), with a selectivity index of 11.44 for ACFF. Promastigotes exposed to ACFF and luteolin exhibited ultrastructural changes, such as intense cytoplasm vacuolization and mitochondrial swelling. These findings data evidence the antileishmanial action of flavone-rich fractions of against , encouraging further studies.
认识到需要鉴定用于治疗利什曼病的新化合物,本研究旨在通过试验评估来自[植物名称未给出]的黄酮类化合物对[病原体名称未给出]的活性。采用高效液相色谱结合二极管阵列紫外可见检测器(HPLC-DAD-UV)和串联电喷雾电离质谱(LC-ESI-MS-MS)测定了[植物名称未给出]的水乙醇提取物和富含黄酮的部分(ACFF)的色谱图。从色谱技术中分离并通过氢和碳的核磁共振鉴定的黄酮木犀草素([含量未给出])和芹菜素([含量未给出])也在ACFF中进行了定量,分别显示为190.7mg/g和芹菜素12.4mg/g。通过将其光谱数据与文献数据进行比较鉴定了其他黄酮类化合物。针对[病原体名称未给出]的前鞭毛体和巨噬细胞内无鞭毛体形式测定了[活性未明确]活性。用BALB/c小鼠的腹腔巨噬细胞进行细胞毒性试验。用格里斯试剂进行亚硝酸盐定量。通过透射电子显微镜进行超微结构研究。抗[活性未明确]试验表明,ACFF、芹菜素和木犀草素对前鞭毛体的IC值分别为40.42±0.10和31.51±1.13μg/mL。ACFF和木犀草素具有浓度依赖性细胞毒性。ACFF和木犀草素还抑制巨噬细胞内寄生虫(IC分别为3.575±1.13和11.78±1.24μg/mL),ACFF的选择性指数为11.44。暴露于ACFF和木犀草素的前鞭毛体表现出超微结构变化, 如强烈的细胞质空泡化和线粒体肿胀。这些研究结果证明了[植物名称未给出]富含黄酮的部分对[病原体名称未给出]的抗利什曼作用,鼓励进一步研究。