Licarin A, a neolignan isolated from Nectandra oppositifolia Nees & Mart. (Lauraceae), exhibited moderate preclinical efficacy against Schistosoma mansoni infection

Abstract

Schistosomiasis is a widespread human parasitic disease currently affecting over 200 million people, particularly in poor communities. Chemotherapy for schistosomiasis relies exclusively on praziquantel (PZQ). Previous studies have shown that licarin A (LIC‐A), a dihydrobenzofuran neolignan, exhibited in vitro antiparasitic activity against Schistosoma mansoni adult worms. This study aimed to investigate the potential of LIC‐A, isolated as main metabolite from leaves of Nectandra oppositifolia Nees & Mart. (Lauraceae), as an antischistosomal agent orally active in schistosomiasis animal model. PZQ was used as a reference compound. As result, LIC‐A showed, at a single dose of 400 mg/kg, to be able to partially cure infected mice (worm burden reductions of ~50%). Parasite eggs, that are responsible for a variety of pathologies and transmission of schistosomiasis, were also moderately inhibited by LIC‐A (egg burden reductions of ~50%–60%). Furthermore, it was observed that LIC‐A achieved a slight reduction of hepatomegaly and splenomegaly. Collectively, although LIC‐A was partially active when administered orally, these results give support for the antiparasitic potential LIC‐A as lead compound for novel antischistosomal agent.

Therapeutic Efficacy of Carvacrol-Loaded Nanoemulsion in a Mouse Model of Schistosomiasis

“…In recent years, many natural compounds have attracted attention for their interesting antischistosomal activities (Mafud et al, 2018;Mengarda et al, 2020;Sessa et al, 2020;Mengarda et al, 2021). In addition, natural compound-loaded nanoparticles have recently emerged as a promising alternative for the treatment of schistosomiasis.…”

Pyrazoline derivatives as promising novel antischistosomal agents

“…d Muegge filter 27 : 200 ≤ MW ≤ 600; − 2 ≤ XLOGP ≤ 5; TPSA ≤ 150; rings ≤ 7; carbon > 4; heteroatoms > 1; rotatable bonds ≤ 15; HBA ≤ 10; HBD ≤ 5. e Ghose filter 44 : 160 ≤ MW ≤ 480; -0.4 ≤ WLOGP ≤ 5.6; − 0.4 ≤ MR ≤ 130; 20 ≤ atoms ≤ 70.…”

“…Values were expressed as percentage of the control and 50% cytotoxic concentration (CC 50 ) values were calculated 27 . The selectivity indices (SI) of tested compounds were calculated by dividing CC 50 values obtained on mammalian cells with EC 50 values determined on S. mansoni 44 .…”

Antiparasitic Properties of Cardiovascular Agents against Human Intravascular Parasite Schistosoma mansoni

“…Thus, our data suggest that amiodarone should have antischistosomal properties under its current antiarrhythmic drug regimen. Although the amiodarone is commonly used in clinical practice, the risk of adverse effects acts as a limiting factor to its utilization [34][35][36][37][38][39][40][41][42][43][44][45][46][47]. As community-wide treatment would be expected at least in most endemic areas for schistosomiasis, this would be a problem.…”

“…For additional evaluation of the therapeutic efficacy, the percentages of different egg developmental stages (oogram pattern) were studied according to Pellegrino and colleagues [44], in which eggs at different stages of maturity were identified and the mean number of each stage was calculated. The percentage of worm and egg reduction was calculated by means of the following equation [45]: % R = ([UC − TC]/UC) × 100%…”