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从不同器官中提取的生物碱提取物对利什曼原虫的抗活性。

Anti-leishmanial activity of alkaloidal extracts obtained from different organs of Aspidosperma ramiflorum.

机构信息

Departamento de Farmácia, Universidade Estadual de Maringá, Avenida Colombo, 5790, CEP 87.020-900, Maringá, PR, Brazil.

出版信息

Phytomedicine. 2012 Mar 15;19(5):413-7. doi: 10.1016/j.phymed.2011.12.004. Epub 2012 Feb 9.

DOI:10.1016/j.phymed.2011.12.004
PMID:22326547
Abstract

The present study was designated to evaluate semi-quantitative antileishmanial activity of alkaloidal extracts that were obtained from 1g of different parts of Aspidosperma ramiflorum (leaves, roots, seeds, and stem barks). Alkaloidal extracts of barks and leaves presented a good activity against the extracellular form (promastigotes) of Leishmania (L.) amazonensis. It is known that compounds responsible for the antileishmanial activity in the alkaloidal extracts from A. ramiflorum are the monoterpenoid indole alkaloids ramiflorine A and ramiflorine B, therefore extracts obtained from different plant parts were analyzed by electrospray ionization mass spectrometry (ESI-MS) in order to evidence the presence of these bioactive alkaloids. Based on these findings, alkaloidal extract from leaves was fractionated on preparative thin-layer chromatography in a bioassay-guided fractionation affording individual purified ramiflorines A and B. Both ramiflorines A and B showed significant activity against Leishmania (L.) amazonensis (LD(50) values of 18.5±6.5μg/ml and 12.63±5.52μg/ml, respectively). Our results are showing that alkaloidal extract from leaves is a promising alternative to the use of stem barks from A. ramiflorum.

摘要

本研究旨在评估从 1g 不同部分的 Aspidosperma ramiflorum(叶、根、种子和茎皮)中获得的生物碱提取物的半定量抗利什曼原虫活性。树皮和叶的生物碱提取物对 Leishmania(L.)amazonensis 的细胞外形式(前鞭毛体)表现出良好的活性。已知负责 A. ramiflorum 生物碱提取物抗利什曼原虫活性的化合物是单萜吲哚生物碱 ramiflorine A 和 ramiflorine B,因此对来自不同植物部分的提取物进行了电喷雾电离质谱(ESI-MS)分析,以证明这些生物活性生物碱的存在。基于这些发现,从叶片中分离出的生物碱提取物在生物测定指导的分步分离中进行了制备性薄层色谱分离,得到了单独的纯化 ramiflorines A 和 B。ramiflorines A 和 B 对 Leishmania(L.)amazonensis 均表现出显著的活性(LD(50)值分别为 18.5±6.5μg/ml 和 12.63±5.52μg/ml)。我们的研究结果表明,来自叶片的生物碱提取物是替代使用 A. ramiflorum 茎皮的有希望的选择。

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