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古巴苦艾精油的化学组成及其杀利什曼原虫活性

Chemistry and leishmanicidal activity of the essential oil from Artemisia absinthium from Cuba.

作者信息

Monzote Lianet, Piñón Abel, Sculli Ramón, Setzer William N

出版信息

Nat Prod Commun. 2014 Dec;9(12):1799-804.

Abstract

Historically, natural products have been a rich source of lead molecules in drug discovery. In particular, products to treat infectious diseases have been developed and several reports about potentialities of essential oils (EO) against Leishmania could be found. In this study, we report the chemical characterization, anti-leishmanial effects and cytotoxicity of the EO from Artemisia absinthium L. Chemical analysis revealed the EO to be composed of 18 compounds, 11 of which were identified, accounting for 64.1% of the composition. The main component of the EO was trans-sabinyl acetate, which made up 36.7%. In vitro anti-leishmanial screening showed that the A. absinthium EO inhibited the growth of promastigotes (14.4 ± 3.6 μg/mL) and amastigotes (13.4 ± 2.4 μg/mL) of L. amazonensis; while cytotoxicity evaluation caused 6 fold higher values than those for the parasites. In a model of experimental cutaneous leishmaniasis in BALB/c mice, five doses of EO at 30 mg/kg by intralesional route demonstrated control of lesion size and parasite burden (p< 0.05) compared with animals treated with glucantime and untreated mice. In conclusion, in vitro and in vivo results showed the potential of EO from A. absinthium as a promising source for lead or active compounds against Leishmania, which could be explored.

摘要

从历史上看,天然产物一直是药物发现中先导分子的丰富来源。特别是,已经开发出了用于治疗传染病的产品,并且可以找到几篇关于精油(EO)抗利什曼原虫潜力的报告。在本研究中,我们报告了苦艾(Artemisia absinthium L.)精油的化学特征、抗利什曼原虫作用和细胞毒性。化学分析表明,该精油由18种化合物组成,其中11种已被鉴定,占该组合物的64.1%。该精油的主要成分是反式乙酸桧酯,占36.7%。体外抗利什曼原虫筛选表明,苦艾精油抑制亚马逊利什曼原虫前鞭毛体(14.4±3.6μg/mL)和无鞭毛体(13.4±2.4μg/mL)的生长;而细胞毒性评估显示其值比寄生虫高6倍。在BALB/c小鼠实验性皮肤利什曼病模型中,与用葡聚糖铁治疗的动物和未治疗的小鼠相比,通过病灶内途径给予五剂30mg/kg的精油可控制病变大小和寄生虫负荷(p<0.05)。总之,体外和体内结果表明,苦艾精油有潜力成为一种有前景的抗利什曼原虫先导或活性化合物来源,值得进一步探索。

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