Antiparasitic, structural, pharmacokinetic, and toxicological properties of riparin derivatives

Toxicology in Vitro : an International Journal Published in Association with BIBRA
Ana C MafudJosué de Moraes

Abstract

Schistosomiasis, caused by helminth flatworms of the genus Schistosoma, is one of the most important parasitic diseases in the world, affecting over 200 million people in developing countries. Riparins are natural alkamides found in Aniba riparia (Lauraceae) fruits that possess several pharmacological properties. In this study, we reported the synthesis, characterization and structural analysis of six riparin derivatives (A-F), as well as their schistosomicidal activity against S. mansoni worms together with a biological, pharmacokinetic and toxicological in silico evaluation. Firstly, these compounds were synthesized, purified and characterized by elemental analysis, FT-IR spectroscopy, X-ray diffraction and theoretical calculations to evaluate their stability and conformation. Next, the schistosomicidal activity of the riparins was tested against S. mansoni worms. Bioassays revealed that Riparins E and F were the most active compounds, showing half-maximum inhibitory concentration at low micromolar ranges (IC50 values ~10 μM). Also, confocal laser scanning microscopy studies revealed tegumental damage in parasites after exposition with Riparins B, E and F. Additionally, based on MTT assay, all tested riparins showed no cytoto...Continue Reading

Citations

Oct 3, 2018·Chemistry & Biodiversity·Vinícius R D PereiraAdemar A Da Silva Filho
Dec 19, 2018·Antimicrobial Agents and Chemotherapy·Rafael A GuerraJosué de Moraes
Jun 22, 2019·Current Topics in Medicinal Chemistry·Josué de MoraesDaniel B Roquini
Aug 21, 2020·Antimicrobial Agents and Chemotherapy·Mariana G de BritoJosué de Moraes
Jan 24, 2021·Chemico-biological Interactions·Luciana Muratori CostaFernando Aécio de Amorim Carvalho
Apr 27, 2021·Future Medicinal Chemistry·Tais C SilvaJosué de Moraes
May 25, 2021·Microbial Pathogenesis·Luciana Muratori CostaHumberto Medeiros Barreto
Aug 22, 2021·Chemistry & Biodiversity·Paulo U CarnaúbaJosué de Moraes

❮ Previous
Next ❯

Related Concepts

Related Feeds

Anthelmintics (ASM)

Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. Discover the latest research on anthelmintics here.

Antiparasitics

Antiparasitics are medications which are indicated for the treatment of parasitic diseases. Discover the latest research on antiparasitics here.

Anthelmintics

Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. Discover the latest research on anthelmintics here.