Laboratório de Imunofarmacologia Parasitária, Disciplina de Parasitologia/Faculdade de Ciências Médicas, Universidade do Estado do Rio de Janeiro, Rio de Janeiro, Brazil.
Laboratório de Bioquímica de Tripanossomatídeos, Fundação Oswaldo Cruz, Rio de Janeiro, Brazil.
Front Cell Infect Microbiol. 2023 Jan 13;12:1059168. doi: 10.3389/fcimb.2022.1059168. eCollection 2022.
Leishmaniasis is a parasitic disease caused by several species of intracellular protozoa of the genus that present manifestations ranging from cutaneous ulcers to the fatal visceral form is an important species associated with American tegumentary leishmaniasis and the main agent in Brazil, with variable sensitivity to available drugs. The search for new therapeutic alternatives to treat leishmaniasis is an urgent need, especially for endemic countries. Not only is quercetin well known for its antioxidant activity in radical scavenging but also several other biological effects are described, including anti-inflammatory, antimicrobial, and pro-oxidant activities. This study aimed to investigate the flavonoid quercetin's therapeutic potential in infection. Quercetin showed antiamastigote (IC of 21 ± 2.5 µM) and antipromastigote (25 ± 0.7 µM) activities and a selectivity index of 22. The treatment of uninfected or -infected macrophages with quercetin increased reactive oxygen species (ROS)/H0 generation without altering Nitric Oxide (NO) production. Oral treatment with quercetin of infected hamsters, starting at 1 week of infection for 8 weeks, reduced the lesion thickness (p > 0.01) and parasite load (p > 0.001). The results of this study suggest that the antiamastigote activity of the flavonoid quercetin is associated, at least in part, with the modulation of ROS production by macrophages. The efficacy of oral quercetin treatment in hamsters infected with was presented for the first time and shows its promising therapeutic potential.
利什曼病是一种由几种属的细胞内原生动物引起的寄生虫病,表现从皮肤溃疡到致命内脏形式不等。是与美洲皮肤利什曼病相关的重要物种,也是巴西的主要病原体,对现有药物的敏感性不同。寻找治疗利什曼病的新治疗方法是当务之急,特别是在流行国家。槲皮素不仅因其在自由基清除方面的抗氧化活性而广为人知,而且还描述了其他几种生物学作用,包括抗炎、抗菌和促氧化剂活性。本研究旨在研究黄酮类槲皮素在 感染中的治疗潜力。槲皮素显示出抗变形体(IC 的 21 ± 2.5 µM)和抗前变形体(25 ± 0.7 µM)活性和 22 的选择性指数。用槲皮素处理未感染或感染的巨噬细胞会增加活性氧(ROS)/H0 的产生,而不会改变一氧化氮(NO)的产生。从感染开始后 1 周开始,用槲皮素对感染的仓鼠进行 8 周的口服治疗,可减少病变厚度(p > 0.01)和寄生虫载量(p > 0.001)。这项研究的结果表明,黄酮类槲皮素的抗变形体活性至少部分与巨噬细胞中 ROS 产生的调节有关。首次报道了口服槲皮素治疗感染 的疗效,显示出其有希望的治疗潜力。