当前位置: X-MOL 学术Chem. Biodivers. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Uncovering biological application of Brazilian green propolis: a phenotypic screening against Schistosoma mansoni
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2020-08-13 , DOI: 10.1002/cbdv.202000277
Lucas A de L Paula 1 , Mario F C Santos 1 , Mariana C Pagotti 1 , Renata Faleiros 1 , Henrique P Ramos 1 , Rodrigo C S Veneziani 1 , Jairo K Bastos 2 , Conor R Caffrey 3 , Sérgio R Ambrosio 1 , Lizandra G Magalhães 1
Affiliation  

The chemotherapy of schistosomiasis remains centered in the use of praziquantel, however, there has been growing resistant parasites to this drug. Thus, the aim of this work was to evaluate in vitro schistosomicidal activity of the hexanes/dichloromethane 1 : 1 extract of Brazilian green propolis (Pex), as well as its major isolated compounds artepillin C, caffeic acid, coumaric acid and drupanin against Schistosoma mansoni. The Pex was active by displaying an IC50 value of 36.60 (26.26–51.13) μg mL−1 at 72 h against adult worms of S. mansoni. The major isolated compounds were inactive with IC50 values >100 μM, however, the combination of the isolated compounds (CM) in the same range found in the extract was active with an IC50 value of 41.17 (39.89–42.46) μg mL−1 at 72 h. Pex and CM induced alteration in the tegument of S. mansoni, and caffeic acid caused alteration in egg's maturation. Pex displayed in vitro activity against adult worms’ and eggs’ viability of S. mansoni, which opens new perspectives to better understand the synergistic and/or additive effects promoted by both Pex extract and CM against schistosomiasis features.

中文翻译:

揭示巴西绿蜂胶的生物学应用:针对曼氏血吸虫的表型筛选

血吸虫病的化疗仍然集中在吡喹酮的使用上,但是,对这种药物的耐药性寄生虫不断增加。因此,这项工作的目的是评估巴西绿蜂胶 (Pex) 的己烷/二氯甲烷 1:1 提取物及其主要分离化合物阿替匹林 C、咖啡酸、香豆酸和杜帕宁对血吸虫的体外杀血吸虫活性曼索尼 Pex 在 72 小时内对曼氏 S. 成虫的 IC50 值为 36.60 (26.26–51.13) μg mL-1,因此具有活性。主要分离的化合物无活性,IC50 值 >100 μM,然而,在提取物中发现的相同范围内的分离化合物 (CM) 的组合具有活性,IC50 值为 41.17 (39.89–42.46) μg mL-1 72 小时。Pex 和 CM 在 S. mansoni 的外皮中诱导改变,和咖啡酸导致鸡蛋成熟的改变。Pex 显示出针对 S. mansoni 的成虫和卵生存力的体外活性,这为更好地了解 Pex 提取物和 CM 对血吸虫病特征所促进的协同和/或相加作用开辟了新的视角。
更新日期:2020-08-13
down
wechat
bug