"In vitro and in vivo metabolism of the major secondary metabolites present in the extract of Lychnophora salicifolia Mart. (Asteraceae: Vernonieae) leaves"

• Grant number: 10/09137-0
• Support type: Scholarships in Brazil - Doctorate
• Effective date (Start): October 01, 2010
• Effective date (End): September 30, 2013
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Norberto Peporine Lopes
• Grantee: Dayana Rubio Gouvea
• Home Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). 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 species Lychnophora salicifolia Mart. is popularly known as "arnicão", and its frequent ethnobotanical use is the same observed for the false arnica or "arnica da serra" (Lychnophora ericoides Mart.) as anti-inflammatory and analgesic. The vicenin-2 is a flavonoid C-glycoside present in large amounts in the hydroalcoholic extract of L. salicifolia leaves. This molecule has anti-inflammatory and antioxidant activities. Another major compound in this extract is the lychnopholic acid, which presents antibacterial, antifungal and trypanocidal action. The increasing importance of natural products, and the difficulty of using the isolated compounds due to the high cost involved in the isolation and purification of substances and the need for more comprehensive studies in this area, this work aims to study these two compounds present in the extract of L. salicifolia leaves. Thus it will be studied in vitro metabolism of these compounds by rat and human liver microsomes. Reactions with metalloporphyrins also will be performed to obtaining standards for identification of metabolites formed. It will be studied the apparent permeability using Caco-2 cells as a model for evaluating the possible absorption of the compounds in humans and finally the study of the pharmacokinetic profile in rats will be performed.

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)

DAYANA R. GOUVEA; GABRIELA A. BUQUI; JOÃO LUIS C. LOPES; ANDREA DINIZ; NORBERTO P. LOPES. An UPLC-MS/MS Method for Determination of Vicenin-2 and Lychnopholic Acid in Rat Plasma and its Application to a Pharmacokinetic Study. Journal of the Brazilian Chemical Society, v. 28, n. 3, p. -, Mar. 2017.

GOUVEA, DAYANA R.; BUQUI, GABRIELA A.; LOPES, JOAO LUIS C.; DINIZ, ANDREA; LOPES, NORBERTO P. An UPLC-MS/MS Method for Determination of Vicenin-2 and Lychnopholic Acid in Rat Plasma and its Application to a Pharmacokinetic Study. Journal of the Brazilian Chemical Society, v. 28, n. 3, SI, p. 427-434, MAR 2017. Web of Science Citations: 2.

GOUVEA, DAYANA RUBIO; BELLO RIBEIRO, ARTHUR DE BARROS; THORMANN, URSULA; LOPES, NORBERTO PEPORINE; BUTTERWECK, VERONIKA. Evaluation of Intestinal Permeability of Vicenin-2 and Lychnopholic Acid from Lychnophora salicifolia (Brazilian Arnicao) Using Caco-2 Cells. Journal of Natural Products, v. 77, n. 3, p. 464-471, MAR 2014. Web of Science Citations: 5.

Academic Publications

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

GOUVEA, Dayana Rubio. In vitro and in vivo metabolism of the major secondary metabolites present in the extract of Lychnophora salicifolia Mart. (Asteraceae: Vernonieae). 2013. Doctoral Thesis - Universidade de São Paulo (USP). Faculdade de Ciências Farmacêuticas de Ribeirão Preto Ribeirão Preto.