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毛果芸香碱和金纽扣(菊科)提取物对曼氏血吸虫感染的疗效。

Efficacy of spilanthol and Acmella oleracea (L.) R. K. Jansen (Asteraceae) extract against Schistosoma mansoni infection.

作者信息

Souza Costa Danilo de, Cajas Rayssa A, Leal Carla Monteiro, Carvalho Lara S Aleixo de, Souza Lara Cruz de, Fukui-Silva Lucas, Moraes Josué de, Da Silva Filho Ademar A

机构信息

Faculdade de Farmácia, Departamento de Ciências Farmacêuticas, Universidade Federal de Juiz de Fora, R. José Lourenço Kelmer s/n, Campus Universitário, Juiz de Fora, MG, 36036-900, Brazil.

Núcleo de Pesquisa Em Doenças Negligenciadas, Universidade Guarulhos, Guarulhos, SP, 07023-070, Brazil.

出版信息

J Ethnopharmacol. 2025 Feb 10;338(Pt 1):119028. doi: 10.1016/j.jep.2024.119028. Epub 2024 Nov 1.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Acmella oleracea (L.) R. K. Jansen, commonly referred to as "Jambu", is a valuable medicinal plant native to the Amazon regions. Inflorescences of A. oleracea is utilized as local anesthetic properties and for its insecticidal, antiparasitic, and anthelmintic attributes.

AIMS OF THIS STUDY

This study aimed to evaluate the in vitro and in vivo antiparasitic properties of A. oleracea extract and spilanthol (SPL) against Schistosoma mansoni.

MATERIALS AND METHODS

The ethanolic extract of A. oleracea inflorescences (AoE) was prepared, analyzed by HPLC-DAD, and characterized by UHPLC-HRMS/MS. SPL was isolated from AoE by chromatographic fractionation. The antischistosomal properties of AoE and SPL were evaluated in vitro against adult schistosomes and in preclinical assays using murine models of patent S. mansoni infection.

RESULTS

Through UHPLC-HRMS/MS analysis, 14 alkamides were annotated in AoE. HPLC-DAD analysis of AoE revealed a peak with a substantial relative area of ∼85%, which was isolated and identified as SPL. AoE and SPL caused mortality of adult schistosomes ex vivo, showing EC values of 32.6 μg/mL and 27.8 μM, respectively, without affected Vero cells or Caenorhabditis elegans. In preclinical studies, the oral administration (400 mg/kg) of AoE and SPL resulted in significant reductions in worm burden of 28% and ∼42%, respectively. Additionally, SPL exhibits remarkable effects on oogram, decreasing egg burden and the number of immature eggs by over 80%, while also promoting significant reductions in hepato- and splenomegaly.

CONCLUSIONS

The research underscores the antischistosomal activity of A. oleracea highlighting the potential of SPL as a lead for the development of new schistosomicidal drugs and encouraging further studies to validate the traditional anthelmintic use of A. oleracea inflorescences.

摘要

民族药理学相关性

金纽扣(Acmella oleracea (L.) R. K. Jansen),通常被称为“Jambu”,是一种原产于亚马逊地区的珍贵药用植物。金纽扣的花序具有局部麻醉特性,并具有杀虫、抗寄生虫和驱虫属性。

本研究目的

本研究旨在评估金纽扣提取物和毛果芸香碱(SPL)对曼氏血吸虫的体外和体内抗寄生虫特性。

材料与方法

制备了金纽扣花序的乙醇提取物(AoE),通过高效液相色谱 - 二极管阵列检测法(HPLC - DAD)进行分析,并通过超高效液相色谱 - 高分辨质谱/质谱法(UHPLC - HRMS/MS)进行表征。通过色谱分离从AoE中分离出SPL。在体外针对成年血吸虫评估了AoE和SPL的抗血吸虫特性,并在曼氏血吸虫感染的小鼠模型的临床前试验中进行了评估。

结果

通过UHPLC - HRMS/MS分析,在AoE中鉴定出14种链状酰胺。AoE的HPLC - DAD分析显示一个相对面积约为85%的主峰,该峰被分离并鉴定为SPL。AoE和SPL在体外导致成年血吸虫死亡,其半数效应浓度(EC)值分别为32.6μg/mL和27.8μM,且未影响非洲绿猴肾细胞(Vero细胞)或秀丽隐杆线虫。在临床前研究中,口服给予AoE(400mg/kg)和SPL分别使虫负荷显著降低了28%和约42%。此外,SPL对虫卵图谱有显著影响,使虫卵负荷和未成熟虫卵数量减少超过80%,同时还显著减轻了肝脏和脾脏肿大。

结论

该研究强调了金纽扣的抗血吸虫活性,突出了SPL作为开发新型杀血吸虫药物先导物的潜力,并鼓励进一步研究以验证金纽扣花序传统驱虫用途的有效性。

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