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从 Aspidosperma nitidum 中提取的生物碱对 Leishmania (Leishmania) amazonensis 的活性。

Activity of alkaloids from Aspidosperma nitidum against Leishmania (Leishmania) amazonensis.

机构信息

Postgraduate Program in Pharmaceutical Innovation, Institute of Health Sciences, Federal University of Pará, Belém, PA, Brazil.

Institute Evandro Chagas, Ananindeua, PA, Brazil.

出版信息

Sci Rep. 2022 May 23;12(1):8662. doi: 10.1038/s41598-022-12396-x.

DOI:10.1038/s41598-022-12396-x
PMID:35606396
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9126982/
Abstract

This study evaluated the morphological changes caused by fractions and subfractions, obtained from barks of Aspidosperna nitidum, against L. (L.) amazonensis promastigotes. The ethanolic extract (EE) obtained through the maceration of trunk barks was subjected to an acid-base partition, resulting the neutral (FN) and the alkaloid (FA) fractions, and fractionation under reflux, yielded hexane (FrHEX), dichloromethane (FrDCL), ethyl acetate (FrACoET), and methanol (FrMEOH) fractions. The FA was fractionated and three subfractions (SF5-6, SF8, and SF9) were obtained and analyzed by HPLC-DAD and H NMR. The antipromastigote activity of all samples was evaluated by MTT, after that, scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for the active fractions were performed. Chromatographic analyzes suggest the presence of alkaloids in EE, FN, FA, and FrDCL. The fractionation of FA led to the isolation of the indole alkaloid dihydrocorynantheol (SF8 fractions). The SF5-6, dihydrocorynantheol and SF-9 samples were active against promastigotes, while FrDCL was moderately active. The SEM analysis revealed cell rounding and changes in the flagellum of the parasites. In the TEM analysis, the treated promastigotes showed changes in flagellar pocket and kinetoplast, and presence of lipid inclusions. These results suggest that alkaloids isolated from A. nitidum are promising as leishmanicidal.

摘要

本研究评估了从 Aspidosperna nitidum 树皮中获得的馏分和亚馏分对 L.（L.） amazonensis 前鞭毛体形态变化的影响。通过对树干树皮进行浸提获得的醇提物（EE）进行酸碱分配，得到中性（FN）和生物碱（FA）馏分，并在回流下进行馏分分离，得到正己烷（FrHEX）、二氯甲烷（FrDCL）、乙酸乙酯（FrACoET）和甲醇（FrMEOH）馏分。FA 被进一步分离，得到三个亚馏分（SF5-6、SF8 和 SF9），并通过 HPLC-DAD 和 1H NMR 进行分析。所有样品的抗前鞭毛体活性均通过 MTT 进行评估，之后对活性馏分进行扫描电子显微镜（SEM）和透射电子显微镜（TEM）分析。色谱分析表明 EE、FN、FA 和 FrDCL 中存在生物碱。FA 的馏分分离导致吲哚生物碱二氢考利旦醇（SF8 馏分）的分离。SF5-6、二氢考利旦醇和 SF-9 样品对前鞭毛体具有活性，而 FrDCL 则具有中等活性。SEM 分析显示细胞圆化和鞭毛变化。在 TEM 分析中，处理过的前鞭毛体显示鞭毛囊和动基体的变化，以及脂滴的存在。这些结果表明，从 A. nitidum 中分离出的生物碱具有作为杀利什曼原虫的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/546b2c9a0aeb/41598_2022_12396_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/9e7099c1f5a1/41598_2022_12396_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/585c82bf9f68/41598_2022_12396_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/642089917555/41598_2022_12396_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/2c1df21f0ad4/41598_2022_12396_Fig4a_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/546b2c9a0aeb/41598_2022_12396_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/9e7099c1f5a1/41598_2022_12396_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/585c82bf9f68/41598_2022_12396_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/642089917555/41598_2022_12396_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/2c1df21f0ad4/41598_2022_12396_Fig4a_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/9126982/546b2c9a0aeb/41598_2022_12396_Fig5_HTML.jpg

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