Ivermectin presents effective and selective antileishmanial activity in vitro and in vivo against Leishmania infantum and is therapeutic against visceral leishmaniasis

Parasitological and immunological evaluation of a quinoline derivative salt incorporated into a polymeric micelle formulation against Leishmania infantum infection

“…So, the adjustment of the number of doses and/or the increase in the drug concentration should be evaluated, aiming to completely eliminate parasites in the treated animals, then making it possible to produce a sterile cure in these mice. Nonetheless, similar results have been described in other studies, where antileishmanial candidates were also evaluated in murine models, highlighting the need to improve the therapeutic schedules tested to reach the complete elimination of the parasites (Malafaia et al 2011 ; Cunha-Júnior et al 2016 ; Freitas et al 2021 ; Reis et al 2021 ). Our purpose was to evaluate treated animals longer than 15 days post-therapy; however, mice receiving saline showed high parasitism associated with relevant loss of weight and weakness.…”

“…The optical density (OD) values were read in a microplate spectrophotometer (Molecular Devices, Spectra Max Plus, San Jose, CA, USA) at 570 nm. Results were entered into Microsoft Excel (version 10.0) spreadsheets, and IC 50 values were calculated by sigmoidal regression of the dose–response curves (Reis et al 2021 ).…”

“…Treatments were performed by subcutaneous route, while miltefosine was administered by oral route. The concentration of products used for the treatments was based on previous studies, where quinoline derivatives were also evaluated as antileishmanial agents (Tavares et al 2020 ; Freitas et al 2021 ; Reis et al 2021 ; Mendonça et al 2022 ). In addition, the parasitological and immunological assays were performed 1 and 15 days after treatment.…”

Ivermectin Prophylaxis Used for COVID-19: A Citywide, Prospective, Observational Study of 223,128 Subjects Using Propensity Score Matching

“…Additional actions of ivermectin described include agonism activity to the liver X receptor (LXR) and farnesoid X receptor (FXR), with multiple potential metabolic benefits [9,10]; neuronal regeneration [11,12], prevention of muscle hypoxia [13], and actions on specific sites, including interferon (INF) [14], nuclear factor-κB (NF-κB), lipopolysaccharide (LPS) [15], and Janus kinase/signal transducer and activator of transcription (JAK-STAT) and PAI-1 pathway [16,17]; generation of P21 activated kinase 1 (PAK-1) [18,19]; reduction of interleukin-6 (IL-6) levels [15]; allosteric modulation of P2X4 receptor [20]; inhibition of high mobility group box 1 (HMGB1) [21,22]; and suppression of mucus hypersecretion, diminished recruitment of immune cells, and production of cytokines in the lung [23]. Ivermectin is also described to induce T helper 1 cell (Th1)-type immune response against protozoan infections [24], and anti-coagulant action through binding to the S protein of some viruses [25].…”

Novel chemical scaffold as potential drug against Leishmania donovani: Integrated computational and experimental approaches

“…These drugs are further taken for pharmacokinetics studies based on ADMET characteristics using the PkCSM server. 48 These investigations were required because inadequate pharmacokinetics play a major role in the majority of drug development failures, and also, it becomes crucial because the majority of the clinical trial experiments are expensive and involve animals which raises moral dilemmas. All selected ligands exhibited good water solubility except Amyral and strong CaCO-2 permeability, as their values are less than 5 and larger than 0.9. all ligands had good intestinal absorption scores, which meant that during oral uptake, they were extensively absorbed in the gut.…”