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

BMC Complementary and Alternative Medicine

Research Article

Letícia Veras Costa-Lotufo¹  Hans-Ulrich Humpf²  Aline Cavalli Bizaro³  João Luis Callegari Lopes⁴  Norberto Peporine Lopes⁴  Lucas Rossi Sartori⁵  Denise Brentan Silva⁶  Thais Guaratini⁶ 

[1] Departamento de Fisiologia e Farmacologia, Faculdade de Medicina, Universidade Federal do Ceará, 60430-270, Fortaleza, CE, Brazil;Institute of Food Chemistry, Westfälische Wilhelms-Universität Münster, Corrensstrasse 45, 48149, Münster, Germany;Lychnoflora Pesquisa e Desenvolvimento em Produtos Naturais LTDA, Rua Ângelo Mestriner 263, Ribeirão Preto,Ribeirão Preto, SP,SP, Brazil, Brazil;Núcleo de Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/nº, 14040-903, Ribeirão Preto, SP, Brazil;Núcleo de Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/nº, 14040-903, Ribeirão Preto, SP, Brazil;Institute of Food Chemistry, Westfälische Wilhelms-Universität Münster, Corrensstrasse 45, 48149, Münster, Germany;Núcleo de Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/nº, 14040-903, Ribeirão Preto, SP, Brazil;Lychnoflora Pesquisa e Desenvolvimento em Produtos Naturais LTDA, Rua Ângelo Mestriner 263, Ribeirão Preto,Ribeirão Preto, SP,SP, Brazil, Brazil;

关键词: Spirocyclic alkaloids;    Erythraline;    in vitro;    Erythrina verna;    Fabaceae;    Jacobsen catalyst;    Erythrina alkaloids;   

DOI  :  10.1186/1472-6882-14-61

 received in 2013-10-02, accepted in 2014-02-12,  发布年份 2014

来源: Springer

【 摘 要 】

BackgroundErythrina 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.MethodsIn 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).ResultsErythraline 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.ConclusionsThe 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.

【 授权许可】

Unknown   
© Guaratini et al.; licensee BioMed Central Ltd. 2014. This article is published under license to BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.