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两种安息香属植物中类黄酮对曼氏血吸虫成虫的杀血吸虫活性评价。

Schistosomicidal evaluation of flavonoids from two species of Styrax against Schistosoma mansoni adult worms.

机构信息

Universidade de Franca, Av Dr Armando Salles de Oliveira, Franca, São Paulo, Brazil.

出版信息

Pharm Biol. 2012 Jul;50(7):925-9. doi: 10.3109/13880209.2011.649857. Epub 2012 Apr 6.

DOI:10.3109/13880209.2011.649857
PMID:22480261
Abstract

CONTEXT

Schistosomiasis is a major health problem worldwide. Thus, the search for new schistosomicidal agents from natural sources can provide prototypes for drug discovery.

OBJECTIVE

The present study investigated the chemical composition of the EtOAc fractions of Styrax pohlii Pohl (Styracaceae) (EF-SP) aerial parts and S. camporum A. DC. leaves (EF-SC), as well as schistosomicidal activities against Schistosoma mansoni adult worms, which have not yet been studied.

MATERIALS AND METHODS

The crude ethanol extracts of S. camporum leaves and S. pohlii aerial parts (EE-SC and EE-SP) were partitioned with n-hexane, EtOAc, and n-BuOH. The EtOAc fractions were purified by preparative HPLC. The crude extracts, EtOAc fractions and pure compounds were tested against S. mansoni adult worms in vitro.

RESULTS

The purification procedure resulted in the isolation of kaempferol-3-O-(2'',4''-di-O-(E)-p-coumaroyl)-β-d-glucopyranoside (1), kaempferol-3-O-(2'',6''-di-O-(E)-p-coumaroyl)-β-d-glucopyranoside (2), quercetin (3), and kaempferol (4). The bioassay results indicated that EE-SC, EF-SC, EF-SP, and compounds 2 and 4 are able to separate coupled S. mansoni adult worms. Additionally, EE-SC, EF-SP, and compound 4 killed the adult schistosomes in vitro at 100 µg/mL and 100 µM.

DISCUSSION AND CONCLUSION

This is the first time that the presence of compounds 1-2 in S. pohlii and 3-4 in S. camporum has been reported. Additionally, biological results indicated that S. pohlii and S. camporum have great potential as a source of active compounds.

摘要

背景

血吸虫病是全球的一个主要卫生问题。因此,从天然来源中寻找新的杀血吸虫药物可以为药物发现提供原型。

目的

本研究调查了Styrax pohlii Pohl(Styracaceae)(EF-SP)空中部分和 S. camporum A. DC.叶(EF-SC)的 EtOAc 部分的化学成分,以及尚未研究过的对曼氏血吸虫成虫的杀血吸虫活性。

材料和方法

S. camporum 叶和 S. pohlii 空中部分(EE-SC 和 EE-SP)的粗乙醇提取物用正己烷、EtOAc 和正丁醇进行分配。EtOAc 部分通过制备型 HPLC 进行纯化。粗提取物、EtOAc 部分和纯化合物在体外测试了对 S. mansoni 成虫的作用。

结果

纯化程序导致分离出 kaempferol-3-O-(2'',4''-di-O-(E)-p-coumaroyl)-β-d-glucopyranoside(1)、kaempferol-3-O-(2'',6''-di-O-(E)-p-coumaroyl)-β-d-glucopyranoside(2)、槲皮素(3)和 kaempferol(4)。生物测定结果表明,EE-SC、EF-SC、EF-SP 以及化合物 2 和 4 能够分离曼氏血吸虫成虫。此外,EE-SC、EF-SP 和化合物 4 在 100 µg/mL 和 100 µM 时在体外杀死成虫。

讨论和结论

这是首次报道在 S. pohlii 中存在化合物 1-2,在 S. camporum 中存在化合物 3-4。此外,生物学结果表明 S. pohlii 和 S. camporum 具有作为活性化合物来源的巨大潜力。

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