Metabolic profile and safety of piperlongumine.
Piperlongumine (PPL), a natural plant product, has been extensively studied in cancer treatment going up on clinical trials. Since the first report related to its use on cancer research (in 2011) around 80 papers have been published in less than 10 years, but a gap still remaining. There are no metabolism studies of PPL in human organism. For the lack of a better view, here, the CYP450 in vitro oxidation of PPL was described for the first time. In addition, the enzymatic kinetic data, the predicted in vivo parameters, the produced metabolites, the phenotyping study and possible piperlongumine-drug interactions in vivo is presented.
Departamento de Ciências Farmacêuticas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, 14040-903, Ribeirão Preto, São Paulo, Brazil.
Fernanda
F
de Lima Moreira
Departamento de Química, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto, Universidade de São Paulo, 14040-901 Ribeirão Preto, SP, Brazil.
Maísa D
MD
Habenschus
Laboratório de Produtos Bioativos, Universidade Federal do Rio de Janeiro, Campus Macaé - IMMT, 27930-560, Macaé, RJ, Brazil.
Thiago
T
Barth
Departamento de Ciências Farmacêuticas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, 14040-903, Ribeirão Preto, São Paulo, Brazil.
Lucas M M
LM
Marques
Nucleus of Bioassays, Biosynthesis and Ecophysiology of Natural Products - NuBBE, Sao Paulo State University - UNESP - Chemistry Institute, Department of Organic Chemistry, Araraquara, Sao Paulo, Brazil.
Alan Cesar
AC
Pilon
Nucleus of Bioassays, Biosynthesis and Ecophysiology of Natural Products - NuBBE, Sao Paulo State University - UNESP - Chemistry Institute, Department of Organic Chemistry, Araraquara, Sao Paulo, Brazil.
Vanderlan
V
da Silva Bolzani
Departamento de Química, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto, Universidade de São Paulo, 14040-901 Ribeirão Preto, SP, Brazil.
Ricardo
R
Vessecchi
Núcleo de Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, 14040-903, Ribeirão Preto-SP, Brazil.
Norberto P
NP
Lopes
Departamento de Química, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto, Universidade de São Paulo, 14040-901 Ribeirão Preto, SP, Brazil.
Anderson R M
AR
de Oliveira
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