In vitro effect of alpha-bisabolol and its synthetic derivatives on macrophages, promastigotes, and amastigotes of Leishmania amazonensis and Leishmania infantum

IF 1.9 3区化学 Q3 CHEMISTRY, APPLIED Natural Product Research Pub Date : 2025-02-16 DOI:10.1080/14786419.2023.2288232

Livia Reisen Perin , Luciana Alves Parreira , Estevão Carlos Silva Barcelos , Mario Ferreira Conceição Santos , Luciano Menini , Daniel de Oliveira Gomes , Francisco de Paula Careta

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Abstract

Cutaneous and visceral leishmaniasis are public health problems in Africa, Asia, Europe, and America. The treatment has a high cost and toxicity. Thus, this work aims to evaluate the leishmanicidal activity of alpha-bisabolol and its three synthetic derivatives, P1, P2, and P3, on the promastigotes and amastigotes Leishmania infantum and L. amazonensis forms. Alpha-bisabolol showed the lowest IC₅₀ with 3.43 for L. amazonensis promastigotes, while P1 was the most toxic for L. infantum with an IC₅₀ of 9.10. The derivative P3 was better for the amastigote form, with an IC₅₀ of 3.39 for L. amazonensis. All the compounds effectively decreased the intracellular load of amastigote and its ability to turn promastigote again. Thus, alpha-bisabolol and its three synthetic derivatives were effective in their leishmanicidal activity. Therefore, it can be an option for developing new treatments against leishmaniasis.

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α -双abolol及其合成衍生物对亚马逊利什曼原虫和幼利什曼原虫巨噬细胞、原鞭毛体和无鞭毛体的体外影响。

皮肤和内脏利什曼病是非洲、亚洲、欧洲和美洲的公共卫生问题。这种治疗方法成本高且有毒性。因此，本研究旨在评价α -双abolol及其三种合成衍生物P1、P2和P3对幼利什曼原虫和亚马逊利什曼原虫的杀灭活性。α -bisabolol对亚马孙乳杆菌的IC50最低，为3.43;P1对婴儿乳杆菌的IC50最高，为9.10。P3衍生物对亚马孙无性系的IC50为3.39，对亚马孙无性系的IC50为3.39。所有化合物都有效地降低了无纺锤体的胞内负荷及其再次转化promastigote的能力。因此，-比索洛尔及其三个合成衍生物具有有效的利什曼尼杀虫活性。因此，它可以成为开发对抗利什曼病的新疗法的一种选择。

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来源期刊

Natural Product Research 化学-医药化学

CiteScore

5.10

自引率

9.10%

发文量

605

审稿时长

2.1 months

期刊介绍： The aim of Natural Product Research is to publish important contributions in the field of natural product chemistry. The journal covers all aspects of research in the chemistry and biochemistry of naturally occurring compounds. The communications include coverage of work on natural substances of land and sea and of plants, microbes and animals. Discussions of structure elucidation, synthesis and experimental biosynthesis of natural products as well as developments of methods in these areas are welcomed in the journal. Finally, research papers in fields on the chemistry-biology boundary, eg. fermentation chemistry, plant tissue culture investigations etc., are accepted into the journal. Natural Product Research issues will be subtitled either ""Part A - Synthesis and Structure"" or ""Part B - Bioactive Natural Products"". for details on this , see the forthcoming articles section. All manuscript submissions are subject to initial appraisal by the Editor, and, if found suitable for further consideration, to peer review by independent, anonymous expert referees. All peer review is single blind and submission is online via ScholarOne Manuscripts.