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不同浓度羽扇醇对旧大陆利什曼原虫的体外疗效。

In vitro efficacy of different concentrations of lupeol on old world Leishmania donovani.

机构信息

University of Al-Muthana, Samawa, Almuthana, Iraq.

University of Baghdad, Baghdad, Iraq.

出版信息

Ann Parasitol. 2024;70(2):73-79. doi: 10.17420/ap7002.523.

DOI:10.17420/ap7002.523
PMID:39044604
Abstract

Leishmaniosis is a tropical neglected parasitic disease that is endemic in many countries, including Middle East, with no existing effective vaccines. The bite of female sand-fly transmits the causative agent, Leishmania spp., to humans. High toxicity, resistance and treatment failure of the available chemotherapy against visceral leishmaniosis demands the investigation of new anti-leishmanial compounds. Lupeol is a form of triterpene isolated from several medicinal plants and possesses an antimicrobial property. In this study, cytotoxic effect of lupeol was screened against the mammalian amastigotes form and insect promastigote form of Leishmania donovani, following three cycles of incubation at different concentrations by MTT assay. Results revealed the in vitro anti-leishmanial effect of lupeol on both forms of the parasite where significant decline in promastigotes and amastigotes growth was observed. This was conducted along three times of follow up (24, 48, 72) hours, in comparison to the classical sodium stibogluconate treatment. Cell viability was calculated and the minimum IC50 was detected after 48 hours for amastigotes and 24 hours for promastigotes, 12.125 μM, 102.78 μM, respectively. Given the severity of visceral leishmaniosis and the toxicity of conventional chemotherapies, the anti-leishmanial activity of lupeol suggested a promising compound for additional clinical trials.

摘要

利什曼病是一种热带被忽视的寄生虫病,在包括中东在内的许多国家流行,但目前尚无有效的疫苗。雌性沙蝇叮咬将病原体利什曼原虫传播给人类。现有的针对内脏利什曼病的化疗药物毒性高、耐药性强且治疗失败,因此需要研究新的抗利什曼病化合物。羽扇豆醇是一种从几种药用植物中分离出来的三萜类化合物,具有抗菌特性。在这项研究中,通过 MTT 测定法,在不同浓度下孵育三个周期后,筛选了羽扇豆醇对哺乳动物无鞭毛体形式和昆虫前鞭毛体形式的利什曼原虫的细胞毒性作用。结果表明,羽扇豆醇对两种形式的寄生虫均具有体外抗利什曼原虫作用,明显观察到前鞭毛体和无鞭毛体的生长下降。这是与经典的葡萄糖酸锑钠治疗相比,在三个时间点(24、48、72 小时)进行的。计算细胞活力,并在 48 小时后检测到无鞭毛体的最小 IC50 为 12.125 μM,在 24 小时后检测到前鞭毛体的最小 IC50 为 102.78 μM。鉴于内脏利什曼病的严重性和传统化疗药物的毒性,羽扇豆醇的抗利什曼病活性表明它是一种有前途的化合物,可用于进一步的临床试验。

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