In vitro shistosomicidal activity of (-)-6,6-dinitrohinokinin: a semi-synthetic lignan derivative obtained from (-)-hinokinin

Context: (−)-6,6′-Dinitrohinokinin (DNHK) display remarkable antiparasitic activity and was, therefore, incorporated into a nanoparticle formulation.Objective: Incorporation of DNHK in poly lactic-co-glycolic acid (PLGA) nanoparticles aiming to improve its biological activities.Materials and methods: Synthesis, characterization and incorporation of DNHK into glycolic acid (PLGA) nanoparticles by nanoprecipitation method. The nanoparticles were characterized by ultraviolet-visible spectroscopy, X-ray diffraction, field emission electron microscopic scanning mansoni (FESEM), and dynamic light scattering (DLS). For the in vitro test with Schistosoma mansoni, the DNHK-loaded PLGA was diluted into the medium, and added at concentrations 10–200 µM to the culture medium containing one adult worm pair. The parasites were kept for 120 h and monitored every 24 h to evaluate their general condition, including: pairing, alterations in motor activity and mortality.Results: The loaded PLGA nanoparticles gave an encapsulation efficiency of 42.2% and showed spherical characteristics in monodisperse polymeric matrix. The adult worm pairs were separated after 120 h of incubation for concentrations higher than 50 µM of DNHK-loaded PLGA. The groups incubated with 150 and 200 µM of DNHK-loaded PLGA for 24 and 120 h killed 100% of adult worms, afforded LC50 values of 137.0 ± 2.12 µM and 79.01 ± 1.90 µM, respectively, which was similar to the effect displayed by 10 µM of praziquantel.Discussion and conclusions: The incorporation of DNHK-loaded showed schistosomicidal activity and allowed its sustained release. The loaded PLGA system can be administered intravenously, as well as it may be internalized by endocytosis by the target organisms.

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“… 2005 ; Jeng and Hou 2005 ; Silva et al. 2007 , 2009 ). In addition, the (−)-6,6′-dinitrohinokinin (DNHK) obtained by Silva et al.…”

Section: Introductionmentioning

confidence: 99%

“…In addition, the (−)-6,6′-dinitrohinokinin (DNHK) obtained by Silva et al. ( 2009 ) by partial synthesis of (−)-hinokinin, displayed schistosomicidal activity against S. mansoni in both in vitro and in vivo (Pereira et al. 2015 ).…”

Section: Introductionmentioning

confidence: 99%