In vitro metabolism study of the piplartine alkaloid using rat liver microsomes

• Grant number: 11/13560-9
• Support Opportunities: Scholarships in Brazil - Master
• Start date: April 01, 2012
• End date: July 31, 2013
• Field of knowledge: Health Sciences - Pharmacy - Toxicological Analysis
• Principal Investigator: Anderson Rodrigo Moraes de Oliveira
• Grantee: Lucas Maciel Mauriz Marques
• Host Institution: Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto (FFCLRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
• Associated research grant: 09/51812-0 - Development of a platform for the study of in vitro and in vivo metabolism of natural products, a need for pre-clinical testing system, AP.BTA.TEM

Abstract

The medicinal plants are the source for thousands of years. Species from Genus Piper has been highlighted because of its diverse pharmacological activities presented. Its prevalence is in tropical and subtropical regions of the globe. The Family Piperaceae has shown great diversity of secondary metabolites with biological activity, such as lignans, neolignans, terpenes, propenyl phenoles, chalcones, flavones, benzopyrans, lactones and amides alkaloids, which are characteristic metabolites. Among them, piplartine has significant cytotoxic activity in tumor cells, antifungal properties, anti platelet aggregation, anxiolytic, antidepressant and antiparasitic. The xenobiotics oxidative metabolism has been extensively researched in the last two decades by means of biological models, using perfused organs, isolated cells or cell fragments (microsomes). Its importance lies on the fact that new drug candidates, must pass through studies, to affect its safety and efficacy, making efforts to be taken in order to describe the involved metabolic pathway and also the characterization of enzymatic kinetics. The present work aims to develop and validate an analytical method for subsequent application in a study of piplartine in vitro metabolism using rat liver microsomes as well as characterization of enzymatic kinetics and the possible metabolites formed. The objectives of this project are as part of the FAPESP 2009/51812-0 project.

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)

MAURIZ MARQUES, LUCAS MACIEL; DA SILVA-JUNIOR, EDUARDO AFONSO; GOUVEA, DAYANA RUBIO; VESSECCHI, RICARDO; PUPO, MONICA TALLARICO; LOPES, NORBERTO PEPORINE; KATO, MASSUO JORGE; MORAES DE OLIVEIRA, ANDERSON RODRIGO. In vitro metabolism of the alkaloid piplartine by rat liver microsomes. Journal of Pharmaceutical and Biomedical Analysis, v. 95, p. 113-120, JUL 2014. (11/17508-1, 11/13560-9, 09/51812-0)

Academic Publications

(References retrieved automatically from State of São Paulo Research Institutions)

MARQUES, Lucas Maciel Mauriz. In vitro metabolism study of the piplartine alkaloid using rats liver microsomes. 2013. Master's Dissertation - Universidade de São Paulo (USP). Faculdade de Ciências Farmacêuticas de Ribeirão Preto (PCARP/BC) Ribeirão Preto.