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从 中提取的孕烷糖苷作为潜在的杀血吸虫中间介质。

Pregnane glycoside from as latent schistosomicidal mediator.

机构信息

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Giza, Egypt.

Medical Parasitology Department, Kasr Al-Ainy Faculty of Medicine, Cairo University, Giza, Egypt.

出版信息

Nat Prod Res. 2020 Jan;34(2):311-316. doi: 10.1080/14786419.2018.1528584. Epub 2018 Nov 8.

DOI:10.1080/14786419.2018.1528584
PMID:30404547
Abstract

Development of a novel agent for control of schistosomiasis is a mandate. anti-schistosomal activity of the aerial parts of were examined. Chromatographic investigations of the ethanol extract (EE) were afforded three compounds. Pregnane glycoside (CI) 12--hydroxy-benzoyl-20-acetyl-boucerin-3--D-glucopyranosyl-(1→4)--D-cymaropyranosyl-(1→4)-D-cymaropyranoside, in addition to two flavonoids (CII) luteolin-4'---D-neohesperidoside and (CIII)quercetin-3-rutinoside were recognized spectral analysis. The schistosomicidal effects were evaluated using scanning electron microscope (SEM). bioassays on the viability (mobility, morphological changes and mortality) of adults, cercariae, miracidia and eggs at different concentrations 2.5, 5, 12.5, 25 and 50 μg/ml of EE and 2.6, 5.2, 13, 26 and 52 μM of CI in incubation times 1,2,4,6,12hrs were carried out. EE and CI evidenced anti-schistosomal activity with a dose and incubation time-dependent fashion. The effect of EE and CI was evident by the topography damage showed by SEM. EE proved moderate cytotoxicity with IC of 8.48 µg/ml.

摘要

开发新型血吸虫病防治药物势在必行。本研究考察了 地上部分的抗血吸虫活性。从乙醇提取物(EE)的色谱研究中得到了三种化合物。孕烷糖苷(CI)12--羟基苯甲酰-20-乙酰-布西林-3--D-吡喃葡萄糖基-(1→4)--D-橙皮吡喃糖基-(1→4)-D-橙皮吡喃糖苷,以及两种黄酮类化合物(CII)芦丁-4'---D-新橙皮糖苷和(CIII)槲皮素-3-鼠李糖苷通过光谱分析得到确认。采用扫描电子显微镜(SEM)评估杀血吸虫效果。在不同浓度 2.5、5、12.5、25 和 50μg/ml 的 EE 以及 2.6、5.2、13、26 和 52μM 的 CI 孵育 1、2、4、6、12 小时的条件下,对成虫、尾蚴、毛蚴和卵的活力(运动、形态变化和死亡率)进行了生物测定。EE 和 CI 表现出剂量和孵育时间依赖性的抗血吸虫活性。EE 和 CI 的作用通过 SEM 显示的形貌损伤得到证实。EE 表现出中等的细胞毒性,IC 为 8.48µg/ml。

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