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希灵菊中二萜内酯和香豆素类化合物的抗利什曼原虫活性。

Antileishmanial activity of furoquinolines and coumarins from Helietta apiculata.

机构信息

Instituto de Investigaciones en Ciencias de la Salud, Department of Tropical Medicine, Asunción, Paraguay.

出版信息

Phytomedicine. 2010 Apr;17(5):375-8. doi: 10.1016/j.phymed.2009.09.009. Epub 2009 Oct 29.

DOI:10.1016/j.phymed.2009.09.009
PMID:19879121
Abstract

UNLABELLED

The bark infusion of H. apiculata are used to treat wound healing related to cutaneous leishmaniasis and as anti-inflammatory.

AIM OF THE STUDY

To isolate, purify active constituents of H. apiculata stem bark, and evaluate their in vitro and in vivo antileishmanial activities.

MATERIALS AND METHODS

Isolation by chromatographic methods and chemical identification of furoquinoline alkaloids and coumarins, then evaluation of the in vitro leishmanicidal activity of these compounds against three strains of Leishmania sp. promastigotes and in vivo against Leishmania amazonensis in Balb/c mice.

RESULTS

Furoquinoline alkaloids and coumarins presented a moderate in vitro activity against promastigote forms of Leishmania sp. with IC(50) values in the range between 17 and >50 microg/ml. Balb/c mice infected with Leishmania amazonensis were treated with gamma-fagarine by oral route, or with 3-(1'-dimethylallyl)-decursinol or (-)-heliettin by subscutaneous route for 14 days at 10mg/kg daily. In these conditions, gamma-fagarine, 3-(1'-dimethylallyl)-decursinol and (-)-heliettin showed the same efficacy as the reference drug reducing by 97.4, 95.6 and 98.6% the parasite loads in the lesion, respectively.

CONCLUSION

These compounds showed significant efficacy in L. amazonensis infected mice, providing important knowledge to improve its potential role for a future use in the treatment of cutaneous leishmaniasis.

摘要

未加标签

喇叭茶的树皮浸剂用于治疗与皮肤利什曼病相关的伤口愈合和抗炎。

研究目的

从喇叭茶的茎皮中分离、纯化活性成分,并评估其体外和体内抗利什曼原虫活性。

材料和方法

通过色谱方法分离和化学鉴定呋喃喹啉生物碱和香豆素,然后评估这些化合物对三种利什曼原虫株的体外杀利什曼原虫活性和体内对感染利什曼原虫的 Balb/c 小鼠的活性。

结果

呋喃喹啉生物碱和香豆素对利什曼原虫的前鞭毛体具有中等体外活性,IC50 值在 17 至 >50μg/ml 之间。用 gamma-fagarine 经口服、用 3-(1'-二甲基烯丙基)-去甲泽醇或(-)heliettin 经皮下途径治疗感染利什曼原虫的 Balb/c 小鼠 14 天,每日 10mg/kg。在这些条件下,gamma-fagarine、3-(1'-二甲基烯丙基)-去甲泽醇和(-)heliettin 对寄生虫负荷的减少与参比药物相同,分别减少 97.4%、95.6%和 98.6%。

结论

这些化合物在感染利什曼原虫的小鼠中显示出显著的疗效,为提高其在未来治疗皮肤利什曼病中的潜在作用提供了重要的知识。

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