Metabolic profile and safety of piperlongumine

Made available in DSpace on 2018-11-26T17:06:22Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-09-29 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) INCT-if Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) University of Sao Paulo 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. Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Dept Ciencias Farmaceut, BR-14040903 Ribeirao Preto, SP, Brazil Univ Sao Paulo, Dept Quim, Fac Filosofia Ciencias & Letras Ribeirao Preto, BR-14040901 Ribeirao Preto, SP, Brazil Univ Fed Rio de Janeiro, Lab Prod Bioat, Campus Macae IMMT, BR-27930560 Macae, RJ, Brazil Sao Paulo State Univ UNESP, Inst Chem, Dept Organ Chem, Nucleus Bioassays Biosynthesis & Ecophysiol Nat P, Araraquara, SP, Brazil Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Nucleo Pesquisa Prod Nat & Sintet NPPNS, BR-14040903 Ribeirao Preto, SP, Brazil Sao Paulo State Univ UNESP, Inst Chem, Dept Organ Chem, Nucleus Bioassays Biosynthesis & Ecophysiol Nat P, Araraquara, SP, Brazil FAPESP: 2012/0188-4 FAPESP: 2013/17658-9 FAPESP: 2014/23604-1 FAPESP: 2014/50265-3 CNPq: 010143/2011-4 CNPq: 442384/2014-9 CNPq: 306385/2011-2 University of Sao Paulo: 2012.1.17587.1.1