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从仙茅科植物仙茅( Saururus cernuus L.)中分离得到的新木脂素具有抗曼氏血吸虫的功效。

Neolignans isolated from Saururus cernuus L. (Saururaceae) exhibit efficacy against Schistosoma mansoni.

机构信息

Institute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of São Paulo, Diadema, SP, 09972-270, Brazil.

Department of Clinical Tropical Medicine, Faculty of Tropical Medicine, Mahidol University, Bangkok, 10400, Thailand.

出版信息

Sci Rep. 2022 Nov 11;12(1):19320. doi: 10.1038/s41598-022-23110-2.

Abstract

Schistosomiasis, a parasitic disease caused by the blood fluke of the genus Schistosoma, affects over 230 million people, especially in developing countries. Despite the significant economic and public health consequences, only one drug is currently available for treatment of schistosomiasis, praziquantel. Thus, there is an urgent demand for new anthelmintic agents. Based on our continuous studies involving the chemical prospection of floristic biodiversity aiming to discover new bioactive compounds, this work reports the in vitro antiparasitic activity against Schistosoma mansoni adult worms of neolignans threo-austrobailignan-6 and verrucosin, both isolated from Saururus cernuus L. (Saururaceae). These neolignans showed a significant in vitro schistosomicidal activity, with EC values of 12.6-28.1 µM. Further analysis revealed a pronounced reduction in the number of S. mansoni eggs. Scanning electron microscopy analysis revealed morphological alterations when schistosomes were exposed to either threo-austrobailignan-6 or verrucosin. These relevant antischistosomal properties were accompanied by low cytotoxicity potential against the animal (Vero) and human (HaCaT) cell lines, resulting in a high selectivity index. Considering the promising chemical and biological properties of threo-austrobailignan-6 and verrucosin, this research should be of interest to those in the area of neglected diseases and in particular antischistosomal drug discovery.

摘要

血吸虫病是一种由血吸虫属的血吸引起的寄生虫病,影响着超过 2.3 亿人,尤其在发展中国家。尽管这种疾病对经济和公共卫生造成了重大影响,但目前仅有一种药物可用于治疗血吸虫病,即吡喹酮。因此,迫切需要新的驱虫药。基于我们持续进行的涉及植物区系生物多样性化学勘探的研究,旨在发现新的生物活性化合物,这项工作报道了 threo-austrobailignan-6 和 verrucosin 这两种从 Saururus cernuus L.(天南星科)中分离出的新木脂素对曼氏血吸虫成虫的体外驱虫活性。这两种新木脂素表现出显著的体外杀血吸虫活性,EC 值分别为 12.6-28.1µM。进一步的分析显示,曼氏血吸虫的卵数量明显减少。扫描电子显微镜分析显示,当血吸虫暴露于 threo-austrobailignan-6 或 verrucosin 时,会发生形态改变。这些相关的抗血吸虫特性伴随着对动物(Vero)和人(HaCaT)细胞系的低细胞毒性潜力,导致高选择性指数。考虑到 threo-austrobailignan-6 和 verrucosin 的有前景的化学和生物学特性,这项研究应该会引起那些关注被忽视疾病领域,特别是抗血吸虫药物发现的人的兴趣。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e431/9652300/6bf959d97e5b/41598_2022_23110_Fig1_HTML.jpg

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