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对微舌一枝黄(菊科)和 Cymbifera 马兜铃(马兜铃科)提取物及化合物的体外抗血吸虫活性评估

Assessment of the In Vitro Antischistosomal Activities of the Extracts and Compounds from Solidago Microglossa DC (Asteraceae) and Aristolochia Cymbifera Mart. & Zucc. (Aristolochiaceae).

作者信息

Costa Poliana da Silva, Zuza da Silva Ohana Oliveira, Costa Danilo de Souza, Silva Lara Aparecida de Oliveira, de Faria Pinto Priscila, da Silva Marcos Paulo Nascimento, de Moraes Josué, Da Silva Filho Ademar A

机构信息

Faculty of Pharmacy, Department of Pharmaceutical Sciences, Federal University of Juiz de Fora, Juiz de Fora, MG 36036-900, Brazil.

Department of Parasitology, Microbiology and Immunology, Biological Sciences Institute, Federal University of Juiz de Fora, Juiz de Fora, MG 36036-900, Brazil.

出版信息

Evid Based Complement Alternat Med. 2020 Sep 29;2020:1726365. doi: 10.1155/2020/1726365. eCollection 2020.

Abstract

Schistosomiasis, caused by helminth flatworms of the genus , is a neglected tropical disease that afflicts over 230 million people worldwide. Currently, treatment is achieved with only one drug, praziquantel (PZQ). In this regard, the roots of (Asteraceae) and (Aristolochiaceae) are popularly used as anthelmintic. Despite their medicinal use against helminthiasis, such as schistosomiasis, . , and . have not been evaluated against . . Then, in this work, the in vitro antischistosomal activity of the crude extracts of . (Ac) and . (Sm) and their isolated compounds were investigated against . adult worms. Sm (200 g/mL) and Ac (100-200 g/mL) were lethal to all male and female worms at the 24 h incubation. In addition, Sm (10-50 g/mL) and Ac (10 g/mL) caused significant reduction in the parasite's movements, showing no significant cytotoxicity to Vero cells at the same range of schistosomicidal concentrations. Confocal laser scanning microscopy revealed that Sm and Ac caused tegumental damages and reduced the numbers of tubercles of male schistosomes. Chromatographic fractionation of Sm leads to isolation of bauerenol, -amirin, and spinasterol, while populifolic acid, cubebin, 2-oxopopulifolic acid methyl ester, and 2-oxopopulifolic acid were isolated from Ac. At concentrations of 25-100 M, bauerenol, -amirin, spinasterol, populifolic acid, and cubebin showed significant impact on motor activity of . . 2-oxopopulifolic acid methyl ester and 2-oxopopulifolic acid caused 100% mortality and decreased the motor activity of adult schistosomes at 100 M. This study has reported, for the first time, the in vitro antischistosomal effects of . and . extracts, also showing promising compounds against adult schistosomes.

摘要

血吸虫病由血吸虫属的蠕虫扁虫引起,是一种被忽视的热带疾病,全球有超过2.3亿人受其折磨。目前,治疗仅使用一种药物吡喹酮(PZQ)。在这方面,菊科的[植物名称1]和马兜铃科的[植物名称2]的根被广泛用作驱虫药。尽管它们可用于治疗蠕虫病,如血吸虫病,但[植物名称1]和[植物名称2]尚未针对[血吸虫种类]进行评估。然后,在本研究中,研究了[植物名称1](Ac)和[植物名称2](Sm)粗提物及其分离化合物对[血吸虫种类]成虫的体外抗血吸虫活性。Sm(200μg/mL)和Ac(100 - 200μg/mL)在孵育24小时后对所有雄虫和雌虫均有致死作用。此外,Sm(10 - 50μg/mL)和Ac(10μg/mL)可显著降低寄生虫的活动,在相同的杀血吸虫浓度范围内对Vero细胞无明显细胞毒性。共聚焦激光扫描显微镜显示,Sm和Ac导致雄血吸虫的体表损伤并减少结节数量。Sm的色谱分离得到了羽扇豆醇、α-香树脂醇和菠菜甾醇,而从Ac中分离出了胡桐叶酸、荜澄茄素、2-氧代胡桐叶酸甲酯和2-氧代胡桐叶酸。在25 - 100μM浓度下,羽扇豆醇、α-香树脂醇、菠菜甾醇、胡桐叶酸和荜澄茄素对[血吸虫种类]的运动活性有显著影响。2-氧代胡桐叶酸甲酯和2-氧代胡桐叶酸在100μM时导致100%的死亡率并降低成虫血吸虫的运动活性。本研究首次报道了[植物名称1]和[植物名称2]提取物的体外抗血吸虫作用,还展示了对成虫血吸虫有前景的化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3141/7545429/25b4439d1fcd/ECAM2020-1726365.002.jpg

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