In vitro metabolism studies of erythraline, the major spiroalkaloid from Erythrina verna

Autor(es)

Guaratini, Thais ^{[1, 2]} ; Silva, Denise Brentan ^{[1, 2]} ; Bizaro, Aline Cavalli ^[2] ; Sartori, Lucas Rossi ^{[1, 3]} ; Humpf, Hans-Ulrich ^[3] ; Lopes, Norberto Peporine ^[1] ; Costa-Lotufo, Leticia Veras ^[4] ; Callegari Lopes, Joao Luis ^[1]

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, FCFRP, NPPNS, BR-14040903 Ribeirao Preto, SP - Brazil

^[2] Lychnoflora Pesquisa & Desenvolvimento Prod Nat L, Ribeirao Preto, SP - Brazil

^[3] Univ Munster, Inst Food Chem, D-48149 Munster - Germany

^[4] Univ Fed Ceara, Fac Med, Dept Fisiol & Farmacol, BR-60430270 Fortaleza, Ceara - Brazil

• Tipo de documento: Artigo Científico
• Fonte: BMC COMPLEMENTARY AND ALTERNATIVE MEDICINE; v. 14, FEB 18 2014.
• Citações Web of Science: 10

Resumo

Background: Erythrina verna, popularly known as ``mulungu{''}, is a Brazilian medicinal plant used to treat anxiety. Erythrina alkaloids have been described in several species of Erythrina, which have biological and therapeutic properties well known that include anxiolytic and sedative effects. Methods: In this work, in vitro metabolism of erythraline (1), the major spirocyclic alkaloid of Erythrina verna, was studied in the pig cecum model and by biomimetic phase I reactions. The biomimetic reactions were performed with Jacobsen catalyst to produce oxidative metabolites and one metabolite was isolated and evaluated against cancer cells, as HL-60 (promyelocytic leukemia), SF-295 (Glioblastoma) and OVCAR-8 (ovarian carcinoma). Results: Erythraline exhibited no metabolization by the pig microbiota and a main putative metabolite was formed in a biomimetic model using Jacobsen catalyst. This metabolite was isolated and identified as 8-oxo-erythraline (2). Finally, erythraline and the putative metabolite were tested in MTT model and both compounds showed no important cytotoxic activity against tumor cells. Conclusions: The alkaloid erythraline was not metabolized by intestinal microbiota, but it was possible to identify its oxidative metabolite from biomimetic reactions. So these data are interesting and stimulate other studies involving this alkaloid, since it is present in phytomedicine products and there are not reported data about the metabolism of erythrina alkaloids. (AU)

• Processo FAPESP: 11/13281-2 - Avaliação do metabolismo dos alcalóides de Erythrina verna
• Beneficiário: Thais Guaratini
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado
• Processo FAPESP: 12/18031-7 - Aplicação de MALDI-MS/MS na análise da vicenina-2 e correlatos: da compreensão dos processos ionizantes à geração de imagens
• Beneficiário: Denise Brentan da Silva
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado
• Processo FAPESP: 10/07413-0 - Avaliação do metabolismo in vivo e in vitro e determinação dos parâmetros farmacocinéticos da budleína a e correlatos
• Beneficiário: Lucas Rossi Sartori
• Modalidade de apoio: Bolsas no Brasil - Doutorado