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.
BMC Complement Altern Med. 2014 Feb 18;14:61. doi: 10.1186/1472-6882-14-61.
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.
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).
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.
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.
Erythrina verna，俗称“mulungu”，是一种巴西药用植物，用于治疗焦虑。Erythrina 生物碱已在几种 Erythrina 物种中被描述，这些物种具有众所周知的生物和治疗特性，包括抗焦虑和镇静作用。
在这项工作中，研究了 Erythrina verna 的主要螺环生物碱 erythraline（1）在猪盲肠模型和仿生相 I 反应中的体外代谢。仿生反应使用 Jacobsen 催化剂进行，以产生氧化代谢物，并分离出一种代谢物并对癌细胞进行评估，如 HL-60（早幼粒细胞白血病）、SF-295（神经胶质瘤）和 OVCAR-8（卵巢癌）。
erythraline 未被猪微生物群代谢，在使用 Jacobsen 催化剂的仿生模型中形成了一种主要的假定代谢物。该代谢物被分离并鉴定为 8-氧代-erythraline（2）。最后，erythraline 和假定的代谢物在 MTT 模型中进行了测试，两种化合物对肿瘤细胞均无重要的细胞毒性活性。
生物碱 erythraline 未被肠道微生物群代谢，但可以从仿生反应中鉴定出其氧化代谢物。因此，这些数据很有趣，并刺激了其他涉及该生物碱的研究，因为它存在于植物药产品中，并且没有关于 erythrina 生物碱代谢的报告数据。
