In vitro metabolism study of the natural product licarina A using human liver microsomes and supersomes

• Grant number: 13/24844-3
• Support Opportunities: Scholarships in Brazil - Doctorate
• Start date: April 01, 2014
• End date: March 31, 2017
• Field of knowledge: Health Sciences - Pharmacy - Toxicological Analysis
• Principal Investigator: Anderson Rodrigo Moraes de Oliveira
• Grantee: Simone Silveira Fortes
• Host Institution: Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto (FFCLRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

Many marketed drugs had their origin in natural products and their derivatives. Due to the great potential of these new pharmacological molecules, an important step in developing a new drug is the assessment of its behavior toward the cytochrome P450 (CYP450), including drug interactions studies. In this context, a substrate that is mentioned is licarin A. It is a neolignan found in some plants and have shown several promising pharmacological properties, among which highlights the anti-leishmaniasis activity. However, for this substance becomes a drug must take place, in preclinical studies, metabolic profile and drug interaction analysis. Therefore, this project aims to conduct an in vitro metabolism study with licarin A, to determine the enzymatic kinetic parameters using human liver microsomes and to perform drug interaction studies by means of enzymatic inhibition, to characterize the possible metabolites that may be formed and to search for the CYP isoform responsible for predominantly metabolizing licarin A through the use of human superssomas.

Academic Publications

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

FORTES, Simone Silveira. In vitro metabolism and enzymatic inhibition study of the natural product Licarin A employing human liver microsomes.. 2017. Doctoral Thesis - Universidade de São Paulo (USP). Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto (PCARP/BC) Ribeirão Preto.