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评估二烯丙基硫醚联合葡甲胺锑合用对利什曼原虫的抗利什曼原虫活性:分子对接、体外和动物模型。

Assessment of the antileishmanial activity of diallyl sulfide combined with meglumine antimoniate on Leishmania major: Molecular docking, in vitro, and animal model.

机构信息

Leishmaniasis Research Center, Kerman University of Medical Sciences, Kerman, Iran.

Center for Research and Training in Skin Diseases and Leprosy, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

PLoS One. 2024 Aug 30;19(8):e0307537. doi: 10.1371/journal.pone.0307537. eCollection 2024.

Abstract

Currently, no safe vaccine against leishmaniasis is available. So far, different control strategies against numerous reservoir hosts and biological vectors have not been environment-friendly and feasible. Hence, employing medicinal components and conventional drugs could be a promising approach to developing novel therapeutic alternatives. This study aimed to explore diallyl sulfide (DAS), a dynamic constituent of garlic, alone and in a mixture with meglumine antimoniate (MAT as standard drug) using in vitro and animal model experiments against Leishmania major stages. The binding affinity of DAS and four major defense elements of the immune system (iNOS, IFN-ɣ, IL-12, and TNF-α) was used to predict the predominant binding mode for molecular docking configurations. Herein, we conducted a broad range of experiments to monitor and assess DAS and MAT potential treatment outcomes. DAS, combined with MAT, displayed no cytotoxicity and employed a powerful anti-leishmanial activity, notably against the clinical stage. The function mechanism involved immunomodulation through the induction of Th1 cytokine phenotypes, triggering a high apoptotic profile, reactive oxygen species (ROS) production, and antioxidant enzymes. This combination significantly decreased cutaneous lesion diameter and parasite load in BALB/c mice. The histopathological findings performed the infiltration of inflammatory cells associated with T-lymphocytes, particularly CD4+ phenotypes, as determined by biochemical markers in alleviating the amastigote stage and improving the pathological changes in L. major infected BALB/c mice. Therefore, DAS and MAT deserve further advanced therapeutic development and should be considered as possible candidates for treating volunteer cases with cutaneous leishmaniasis in designing an upcoming clinical trial.

摘要

目前,尚无针对利什曼病的安全疫苗。到目前为止,针对众多储存宿主和生物媒介的不同控制策略并不环保且不可行。因此,使用药用成分和传统药物可能是开发新型治疗替代品的有前途的方法。本研究旨在探索大蒜中的动态成分二烯丙基二硫(DAS),单独使用以及与葡甲胺锑(MAT 作为标准药物)混合使用,通过体外和动物模型实验来对抗利什曼原虫的各个阶段。DAS 与免疫系统的四个主要防御元素(iNOS、IFN-γ、IL-12 和 TNF-α)的结合亲和力用于预测分子对接构型的主要结合模式。在此,我们进行了广泛的实验来监测和评估 DAS 和 MAT 的潜在治疗效果。DAS 与 MAT 联合使用时没有细胞毒性,并具有强大的抗利什曼原虫活性,特别是对临床阶段。其作用机制涉及通过诱导 Th1 细胞因子表型来调节免疫,引发高凋亡谱、活性氧 (ROS) 产生和抗氧化酶。这种组合显著降低了 BALB/c 小鼠的皮肤病变直径和寄生虫负荷。组织病理学发现与 T 淋巴细胞(尤其是 CD4+表型)相关的炎症细胞浸润,这是通过生物化学标志物确定的,可减轻无鞭毛体阶段并改善感染利什曼原虫的 BALB/c 小鼠的病理变化。因此,DAS 和 MAT 值得进一步进行治疗开发,并且应该被认为是治疗志愿者皮肤利什曼病病例的潜在候选药物,在设计即将进行的临床试验中。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2cda/11364230/a6d84ef90b15/pone.0307537.g001.jpg

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