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In vitro, in vivo metabolism and pharmacokinetic profile evaluation of the alkaloid govaniadine

Grant number: 13/16496-5
Support Opportunities:Scholarships in Brazil - Doctorate
Effective date (Start): December 01, 2013
Effective date (End): February 28, 2017
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Organic Chemistry
Principal Investigator:Norberto Peporine Lopes
Grantee:Lucas Maciel Mauriz Marques
Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
Associated scholarship(s):15/02592-8 - Evaluation of the cytotoxicity of the alkaloid govaniadine in human cell lines, BE.EP.DR

Abstract

Biodiversity is a source of new chemical entities and bottom line in the discovery of new drugs. The genus Corydalis (family Fumariaceae) comprises 470 species, it is native to China, the Himalayas of Nepal, Pakistan and India, and also found in mountainous regions of Eastern Africa. Tetrahydroprotoberberine-type alkaloids, especially govaniadine isolated from Corydalis are identified as a new category of dopamine receptor ligands and anti-malarial and antileishmanicidal agents, which makes its study relevant to employment in therapy. For such purpose, the knowledge regarding its pharmacokinetic profile as well as its metabolism is needed in assessing its safety and efficacy. The oxidative metabolism of xenobiotics has been extensively researched through the use of organometallic complexes and liver microsomes. This study aims to evaluate the in vitro, in vivo metabolism and the pharmacokinetic profile of this alkaloid. Mass Spectrometry (MS) coupled or not to Liquid Chromatography (LC) it will be used to assign structures for the metabolites and Nuclear Magnetic Resonance (NMR) for confirmation of the proposed structures. (AU)

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Scientific publications (5)
(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)
MOREIRA, FERNANDA L.; MARQUES, LUCAS M. M.; LOPES, NORBERTO P.; DE OLIVEIRA, ANDERSON R. M.. In vitro metabolism studies of natural products are crucial in the early development of medicines. PHYTOCHEMISTRY REVIEWS, v. 16, n. 2, p. 355-373, . (13/04188-4, 13/16496-5, 16/07597-0, 14/50265-3)
BAUERMEISTER, ANELIZE; AGUIAR, FERNANDO ARMANI; MAURIZ MARQUES, LUCAS MACIEL; MALTA, JR., JOSE DOS SANTOS; BARROS, FABIO; CALLEJON, DANIEL ROBERTO; MORAES DE OLIVEIRA, ANDERSON RODRIGO; LOPES, NORBERTO PEPORINE. In Vitro Metabolism Evaluation of the Ergot Alkaloid Dihydroergotamine: Application of Microsomal and Biomimetic Oxidative Model. Planta Medica, v. 82, n. 15, p. 1368-1373, . (13/16496-5, 14/50265-3)
WANG, MINGXUN; CARVER, JEREMY J.; PHELAN, VANESSA V.; SANCHEZ, LAURA M.; GARG, NEHA; PENG, YAO; NGUYEN, DON DUY; WATROUS, JERAMIE; KAPONO, CLIFFORD A.; LUZZATTO-KNAAN, TAL; et al. Sharing and community curation of mass spectrometry data with Global Natural Products Social Molecular Networking. NATURE BIOTECHNOLOGY, v. 34, n. 8, p. 828-837, . (14/18052-0, 12/18031-7, 14/01651-8, 13/16496-5, 14/01884-2, 14/50265-3)
MARQUES, LUCAS M. M.; CALLEJON, DANIEL R.; PINTO, LARISSA G.; DE CAMPOS, MICHEL L.; DE OLIVEIRA, ANDERSON R. M.; VESSECCHI, RICARDO; ADHIKARI, ACHYUT; SHRESTHA, RAM L. S.; PECCININI, ROSANGELA G.; LOPES, NORBERTO P.. Pharmacokinetic properties, in vitro metabolism and plasma protein binding of govaniadine an alkaloid isolated from Corydalis govaniana Wall. Journal of Pharmaceutical and Biomedical Analysis, v. 131, p. 464-472, . (13/17658-9, 13/16496-5, 14/13192-8, 14/23604-1)
MARQUES, LUCAS M. M.; BEHRENS, MATTHIAS; KALININA, SVETLANA; ROTTKORD, ULRIKE; ADHIKARI, ACHYUT; SHRESTHA, RAM L. S.; HUMPF, HANS-ULRICH; LOPES, NORBERTO P.. Govaniadine Evaluation of Cytotoxicity and Permeability in Cell Culture. REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY, v. 30, n. 3, . (15/02592-8, 13/16496-5)
Academic Publications
(References retrieved automatically from State of São Paulo Research Institutions)
MARQUES, Lucas Maciel Mauriz. Kinetic disposition, in vitro metabolism and intestinal permeability of the govaniadine alkaloid. 2017. Doctoral Thesis - Universidade de São Paulo (USP). Faculdade de Ciências Farmacêuticas de Ribeirão Preto (PCARP/BC) Ribeirão Preto.

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