Author(s): Mauro, Mariana [UNESP] ; da Silva, Rodrigo Moreira ; de Campos, Michel Leandro ; Bauermeister, Anelize ; Lopes, Norberto Peporine ; de Moraes, Natalia Valadares
Date: 2022
Persistent ID: http://hdl.handle.net/11449/229388
Origin: Oasisbr
Subject(s): Copaifera sp; Copalic acid; Kaurenoic acid; Liver microsomes; Metabolism
Made available in DSpace on 2022-04-29T08:32:13Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-01-01
Copalic (CA) and kaurenoic (KA) acids are the main diterpenes found in the oleoresin extracted from the copaiba tree (Copaifera sp). This study aimed to characterize the metabolism of CA and KA in rat and human liver microsomes using liquid chromatography with tandem mass spectrometry (LC-MS/MS). The in vitro assays showed deviations from the Michaelian kinetics in the metabolism of CA and KA. Putative metabolites of CA and KA were characterized by LC-MS/MS using electrospray ionization (ESI) with time of flight (LC-ESI-TOF) and ion-trap (LC-ESI-IT) systems and identified as a CA isomer and 16,17-dihydroxy-kaurenoic acid, respectively. CA and KA are subject to extensive metabolism with each passage through the liver with extraction ratios (E) estimated as 0.97 and 0.99, respectively. In conclusion, the kinetic parameters and metabolites described here might support drug development and the traditional use.
Departamento de Fármacos e Medicamentos Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista
Departamento de Física e Química Faculdade de Ciências Farmacêuticas de Ribeirão Preto Universidade de São Paulo, SP
Instituto de Ciências da Saúde Universidade Federal de Mato Grosso
Departamento de Fármacos e Medicamentos Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista
