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蒲桃叶萜类成分对亚马逊利什曼原虫的活性

Anti-Leishmania amazonensis activity of the terpenoid fraction from Eugenia pruniformis leaves.

作者信息

Albuquerque Ricardo D D G, Oliveira Adriana P, Ferreira Christian, Passos Carlos L A, Fialho Eliane, Soares Deivid C, Amaral Veronica F, Bezerra Gabrielle B, Esteves Ricardo S, Santos Marcelo G, Albert AndrÉ L M, Rocha Leandro

机构信息

Universidade Federal Fluminense, Laboratório de Tecnologia de Produtos Naturais, Faculdade de Farmácia, Rua Dr. Mário Vianna, 523, Santa Rosa, 24241-000 Niterói, RJ, Brazil.

Universidade Federal do Rio de Janeiro, Laboratório Multidisciplinar de Ciências Farmacêuticas, Faculdade de Farmácia, Av. Carlos Chagas Filho, 373, Cidade Universitária, 21941-902 Rio de Janeiro, RJ, Brazil.

出版信息

An Acad Bras Cienc. 2020 Dec 7;92(4):e20201181. doi: 10.1590/0001-3765202020201181. eCollection 2020.

Abstract

Leishmaniasis is caused by protozoan parasites belonging to the genus Leishmania and includes cutaneous, mucocutaneous and visceral clinical forms. Drugs currently available for leishmaniasis treatment present high toxicity, and development of parasite resistance. Plants constitute an important source of compounds with leishmanicidal potential. This study aimed to evaluate the anti-Leishmania amazonensis activity of the terpenoid fraction of Eugenia pruniformis leaves (TF-EpL). TF-EpL was active against the promastigote and intracellular amastigote forms of L. amazonensis with IC50(24h) value of 43.60μg/mL and 44.77μg/mL, respectively. TF-EpL altered the cell cycle of the parasite, increasing 2.32-fold the cells in the Sub-G0/G1 phase. TF-EpL also changed the ΔΨm and increased ROS and the number of annexin-V-PI positive promastigotes, which suggests incidental death. β-sitosterol, ursolic acid, corosolic acid and asiatic acid were isolated from TF-EpL. The results showed the antileishmanial activity of E. pruniformis terpenoids and its potential for further studies as a source of new drugs for leishmaniasis.

摘要

利什曼病由属于利什曼原虫属的原生动物寄生虫引起,包括皮肤型、黏膜皮肤型和内脏型临床形式。目前可用于治疗利什曼病的药物具有高毒性且会产生寄生虫耐药性。植物是具有杀利什曼原虫潜力化合物的重要来源。本研究旨在评估蒲桃叶萜类成分(TF-EpL)对亚马逊利什曼原虫的活性。TF-EpL对亚马逊利什曼原虫的前鞭毛体和细胞内无鞭毛体形式均有活性,其IC50(24小时)值分别为43.60μg/mL和44.77μg/mL。TF-EpL改变了寄生虫的细胞周期,使亚G0/G1期的细胞增加了2.32倍。TF-EpL还改变了线粒体膜电位(ΔΨm),增加了活性氧(ROS)和膜联蛋白-V-碘化丙啶(annexin-V-PI)阳性前鞭毛体的数量,这表明存在意外死亡。从TF-EpL中分离出了β-谷甾醇、熊果酸、科罗索酸和积雪草苷。结果显示了蒲桃萜类化合物的抗利什曼活性及其作为利什曼病新药来源进一步研究的潜力。

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