Abstract
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.
Highlights
Erythrina verna, popularly known as “mulungu”, is a Brazilian medicinal plant used to treat anxiety
Erythrina alkaloids are characteristic of this genus with over one hundred structural derivatives described to date [3,4,5,6,7]
Under the chosen experimental conditions, no significant degradation of erythraline was observed in the pig cecum model when comparing activated and deactivated ceca after 8 hours of incubation (Figure 2)
Summary
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. Erythrina alkaloids are characteristic of this genus with over one hundred structural derivatives described to date [3,4,5,6,7]. E. verna is one of the 11 species that occur in Brazil and it has being previously classified as E. mulungu. These plants are used in Brazil as a sedative, to treat sleep disorders and anxiety [8]. Systematic studies have supported the popular use by confirming the anxiolytic effects of a series of erythrina alkaloids [9,10,11] and recently a mechanism of action was
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