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Preparation and characterization of polymeric nanoparticles containing (-)-6,6'-dinitrohinokinin and (±)-licarina-A as potential drugs in the assessment of the schistosomicidal activity

Grant number: 11/05952-4
Support Opportunities:Scholarships in Brazil - Doctorate
Effective date (Start): September 01, 2011
Effective date (End): August 31, 2015
Field of knowledge:Physical Sciences and Mathematics - Chemistry
Principal Investigator:Márcio Luís Andrade e Silva
Grantee:Thaís Coelho Lima
Host Institution: Reitoria. Universidade de Franca (UNIFRAN). Franca , SP, Brazil


The project proposes the development of a potential drug for the treatment of schistosomiasis from the patent already deposited with the INPI. Schistosomiasis affects over 220 million people a year worldwide, of which 10 million are in Brazil. About 30% of infected individuals are resistant to treatment with drugs on the market. For this, obtained by partial synthesis from the lignan (-)-cubebin isolated from Piper cubeba, the compounds (-)-O-metilcubebina and (-)-hinokinin and (-)-dinitrohinokinin both naturally occurring as well as (±)-licarina and (±)-conocarpana and its enantiomers [(+)/(-)-licarina and (+)/(-)-conocarpana]. These substances will be used for the treatment of schistosomiasis. It is noteworthy that the derivatives of (-)-cubebin were active in biological assays in vitro and in vivo and (±)-licarina and (±)-conocarpana active in vitro. In preclinical trials, nanoparticle-based formulations of studies will be conducted. The nanoparticles are composed of biocompatible and biodegradable materials such as PLGA, MCM-41, MCM-41 amino-functionalized and lipids.

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Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
NERES, NAYARA B. R.; MONTAGNINI, DANIEL; FERREIRA, DANIELE S.; PARREIRA, RENATO L. T.; ORENHA, RENATO P.; LIMA, THAIS C.; MOLINA, EDUARDO F.; CUNHA, WILSON R.; SILVA, MARCIO L. A.; ESPERANDIM, VIVIANE R.. In Vivo and in Silico Trypanocidal Activity Evaluation of (-)-Cubebin Encapsulated in PLGA Microspheres as Potential Treatment in Acute Phase. CHEMISTRY & BIODIVERSITY, v. 18, n. 6, . (17/24856-2, 13/04880-5, 10/17378-8, 09/05049-2, 11/05952-4, 11/07623-8)
LIMA, THAIS C.; MAGALHAES, LIZANDRA G.; PAULA, LUCAS A. DE L.; CUNHA, WILSON R.; JANUARIO, ANA H.; PAULETTI, PATRICIA M.; BASTOS, JAIRO K.; DOS SANTOS, FRANSERGIO F.; FORIM, MOACIR R.; LAURENTIZ, ROSANGELA S.; et al. Evaluation of lignan-loaded poly(epsilon-caprolactone) nanoparticles: synthesis, characterization, in vivo and in silico schistosomicidal activity. NATURAL PRODUCT RESEARCH, . (09/15207-4, 10/17378-8, 18/25010-2, 11/07623-8, 11/05952-4)

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