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从 Parinari excelsa 中分离得到的一种新型 ventiloquinone 和五种已知三萜的抗利什曼原虫、抗疟原虫和细胞毒性活性的体外研究。

In vitro antileishmanial, antiplasmodial and cytotoxic activities of a new ventiloquinone and five known triterpenes from Parinari excelsa.

机构信息

UFR Sciences des Structures de la Matière et Technologie, Université de Cocody-Abidjan, Côte d'Ivoire, Switzerland.

出版信息

Pharm Biol. 2012 Jul;50(7):801-6. doi: 10.3109/13880209.2011.633270. Epub 2012 Apr 3.

Abstract

CONTEXT

Parinari excelsa Sabine (Chrysobalanaceae) is an indigenous tree from West and Eastern Africa. This tree is used in Ivory Coast as an antimalaria remedy.

OBJECTIVE

The in vitro antiplasmodial and antileishmanial activities of the stem bark, the leaf and the major compounds from the stem bark were investigated.

MATERIALS AND METHODS

The leaves and stem bark from P. excelsa were separately collected, air-dried and powdered. Two extracts (methylene chloride and methanol) were realized for both powders. Every extract was tested for its antiplasmodial and antileishmanial activities. Only the stem bark crude extracts were fractionated by column chromatography and their major components were analyzed by NMR, HRESIMS and IR methods. The compounds were tested for their antiplasmodial and antileishmanial activities.

RESULTS

The comparison of the IC(50) values of the crude extracts were in this order: 3.41 (IC(50) of PeBMc) <4.10 (IC(50) of PeBMc) <4.42 (IC(50) of PeLMe) against P. falciparum and 5.19 (IC(50) of PeBMc) <12.32 (IC(50) of PeBMe) <19.33 (IC(50) of PeLMc) <32.37 (IC(50) of PeLMe) against L. donovani. The stem bark crude extracts were the most active against both parasites. Their fractionation leaded to a new ventiloquinone, five triterpenes and one chlorogenic acid. All these compounds were isolated for the first time from P. excelsa. High activities were observed with (3β)-3-hydroxyolean-12-en-28-oic acid (IC(50) = 8.2 µM) and 3β-hydroxyolean-5,12-dien-28-oic acid (IC(50) = 7.7 µM) against L. donovani. With the antiplasmodial activity, the best activity was observed with 16β-hydroxylupane-1,20(29)-dien-3-one (IC(50) = 28.3 µM).

DISCUSSION AND CONCLUSION

These findings demonstrated that the constituents of P. excelsa stem bark have in vitro antiplasmodial and antileishmanial activities.

摘要

背景

Parinari excelsa Sabine(樟科)是一种来自西非和东非的本地树种。这种树在象牙海岸被用作抗疟疾药物。

目的

研究了茎皮、叶和茎皮主要化合物的体外抗疟原虫和抗利什曼原虫活性。

材料和方法

分别采集 Parinari excelsa 的叶和茎皮,风干并粉碎。对两种粉末(二氯甲烷和甲醇)进行了两种提取物的实验。测试了每一种提取物的抗疟原虫和抗利什曼原虫活性。仅对茎皮粗提取物进行柱层析分离,并通过 NMR、HRESIMS 和 IR 方法分析其主要成分。测试了这些化合物的抗疟原虫和抗利什曼原虫活性。

结果

粗提取物的 IC50 值比较如下:3.41(PeBMc 的 IC50)<4.10(PeBMc 的 IC50)<4.42(PeLMe 的 IC50)抗疟原虫和 5.19(PeBMc 的 IC50)<12.32(PeBMe 的 IC50)<19.33(PeLMc 的 IC50)<32.37(PeLMe 的 IC50)抗利什曼原虫。茎皮粗提取物对两种寄生虫的活性最高。它们的分离导致了一种新的 ventiloquinone、五种三萜和一种绿原酸。所有这些化合物均首次从 Parinari excelsa 中分离出来。(3β)-3-羟基齐墩果-12-烯-28-酸(IC50 = 8.2 µM)和 3β-羟基齐墩果-5,12-二烯-28-酸(IC50 = 7.7 µM)对利什曼原虫具有高活性。在抗疟原虫活性方面,观察到 16β-羟基羽扇烷-1,20(29)-二烯-3-酮(IC50 = 28.3 µM)的最佳活性。

讨论与结论

这些发现表明,Parinari excelsa 茎皮的成分具有体外抗疟原虫和抗利什曼原虫活性。

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