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巴西亚马孙西部帕拉州植物的体外和体内抗疟活性、细胞毒性和植物化学 HRMS 特征。

In Vitro and in Vivo Antimalarial Activity, Cytotoxicity and Phytochemical HRMS Profile of Plants from the Western Pará State, Brazilian Amazonia.

机构信息

Laboratório de Bioprospecção e Biologia Experimental - LabBBEx, Universidade Federal do Oeste do Pará, Rua Vera Paz, s/n, Salé, 68035-110, Santarém, PA, Brazil.

Programa de Pós-Graduação Doutorado em Rede de Biodiversidade e Biotecnologia - BIONORTE/Polo Pará, Universidade Federal do Pará, Rua Augusto Corrêa, 01, Guamá, 66075-110, Belém, PA, Brazil.

出版信息

Chem Biodivers. 2024 Jan;21(1):e202301082. doi: 10.1002/cbdv.202301082. Epub 2023 Dec 5.

Abstract

Ethnopharmacology and botanical taxonomy are valid criteria used to selecting plants for antimalarial bioprospection purposes. Based on these two criteria, ethanol extracts of 11 plants from Santarém City vicinities, Western Pará State, Brazilian Amazonia, had their in vitro antiplasmodial activity against chloroquine-resistant Plasmodium falciparum (W2 clone) assessed by the PfLDH method, whereas their cytotoxicity to HepG2-A16 cells was assessed through MTT assay. Acmella oleracea, Siparuna krukovii and Trema micrantha extracts disclosed the highest rate of parasite growth inhibition (90 %) in screening tests. In vivo antimalarial assays were conducted with these extracts against Plasmodium berghei (NK 65 strain) infected mice. Inhibition rate of parasite multiplication ranged from 41.4 % to 60.9 % at the lowest extract dose (25 mg/kg). HPLC-ESI-HRMS analyses allowed the putative identification of alkylamides, fatty acids, flavonoid glycosides and alkaloids in ethanol extracts deriving from these three plant species. Results pointed towards A. oleracea flowers ethanol extract as the most promising potential candidate to preclinical studies aiming the development of antimalarial phytomedicine.

摘要

基于民族药理学和植物分类学这两个标准,从巴西亚马逊地区帕拉州西部圣塔伦市附近的 11 种植物中提取了乙醇提取物,并用 PfLDH 法检测了这些提取物对氯喹耐药恶性疟原虫(W2 克隆)的体外抗疟活性,并用 MTT 法检测了它们对 HepG2-A16 细胞的细胞毒性。在筛选试验中,Acmella oleracea、Siparuna krukovii 和 Trema micrantha 的提取物显示出对寄生虫生长的最高抑制率(90%)。用这些提取物对感染 Plasmodium berghei(NK 65 株)的小鼠进行体内抗疟试验。在最低提取物剂量(25mg/kg)时,寄生虫增殖的抑制率范围为 41.4%至 60.9%。HPLC-ESI-HRMS 分析允许在这三个植物物种的乙醇提取物中鉴定出烷基酰胺、脂肪酸、类黄酮糖苷和生物碱。结果表明,A. oleracea 花乙醇提取物是最有前途的候选药物,可用于开发抗疟植物药的临床前研究。

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