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（瓦尔）S. 格罗斯（紫葳科）的抗利什曼原虫活性

Antileishmanial Activity of (Vahl) S. Grose (Bignoniaceae).

作者信息

Costa Erica Vanessa Souza, Brígido Heliton Patrick Cordovil, Silva João Victor da Silva E, Coelho-Ferreira Marlia Regina, Brandão Geraldo Célio, Dolabela Maria Fâni

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, ICS, Universidade Federal do Pará, Belém, PA, Brazil.

Departamento de Botânica, Museu Paraense Emílio Goeldi, Belém, PA, Brazil.

出版信息

Evid Based Complement Alternat Med. 2017;2017:8074275. doi: 10.1155/2017/8074275. Epub 2017 Feb 12.

DOI:10.1155/2017/8074275
PMID:28286535
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5329664/
Abstract

This study aimed to evaluate the leishmanicidal activity of ethanol extract, fractions, and isolated substance from against . Furthermore, this activity was related to cytotoxicity, and the selectivity index was determined. The ethanol extract was obtained by maceration of the stem powder, and the extract was subjected to fractionation on chromatographic column. The lapachol was obtained by acid base extraction followed by purification in chromatographic column. The antipromastigote activity and cytotoxicity tests were carried out by the cell viability method (MTT). Modified THP-1 cells were infected with promastigotes and treated for 24 h with different concentrations of the extract, fractions, and lapachol. The ethanol extract, dichloromethane, and ethyl acetate fractions were not active against promastigotes (IC > 200 g/mL) or cytotoxic (CC > 500 g/mL), and the selectivity index (SI) was greater than 2.5. The ethyl acetate fraction was active only in promastigotes; it is not cytotoxic (CC > 500 g/mL, SI > 5). The lapachol was selectively active only against amastigote (IS > 2.5, CC > 500 g/mL). In summary, lapachol and ethyl acetate fraction are promising against amastigote and promastigote forms, respectively.

摘要

本研究旨在评估[植物名称]乙醇提取物、各馏分及分离出的物质对[寄生虫名称]的杀利什曼原虫活性。此外，将该活性与细胞毒性相关联，并测定选择性指数。乙醇提取物通过对茎粉进行浸渍获得，提取物在色谱柱上进行分馏。拉帕醇通过酸碱萃取，然后在色谱柱上纯化得到。抗前鞭毛体活性和细胞毒性试验采用细胞活力法（MTT）进行。用前鞭毛体感染经修饰的THP-1细胞，并用不同浓度的提取物、馏分和拉帕醇处理24小时。乙醇提取物、二氯甲烷和乙酸乙酯馏分对前鞭毛体无活性（IC>200μg/mL）或无细胞毒性（CC>500μg/mL），选择性指数（SI）大于2.5。乙酸乙酯馏分仅对前鞭毛体有活性；无细胞毒性（CC>500μg/mL，SI>5）。拉帕醇仅对无鞭毛体有选择性活性（IS>2.5，CC>500μg/mL）。总之，拉帕醇和乙酸乙酯馏分分别对无鞭毛体和前鞭毛体形态有潜在应用前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/553f/5329664/787cf6c58ff2/ECAM2017-8074275.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/553f/5329664/132988f4dd40/ECAM2017-8074275.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/553f/5329664/a48d6b44a20d/ECAM2017-8074275.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/553f/5329664/a8b7818987e6/ECAM2017-8074275.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/553f/5329664/787cf6c58ff2/ECAM2017-8074275.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/553f/5329664/132988f4dd40/ECAM2017-8074275.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/553f/5329664/a48d6b44a20d/ECAM2017-8074275.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/553f/5329664/a8b7818987e6/ECAM2017-8074275.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/553f/5329664/787cf6c58ff2/ECAM2017-8074275.004.jpg

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