Department of Pharmacy, Jining No. 1 People's Hospital, Jining, 272011, Shandong Province, China.
Jining Medical University, Jining, 272011, Shandong Province, China.
Rapid Commun Mass Spectrom. 2020 Apr 15;34(7):e8661. doi: 10.1002/rcm.8661.
Erianin, a bioactive component isolated from Dctidrobium chrysotoxum Lindl, was demonstrated to have many biological properties relevant to cancer prevention and therapy. However, the metabolic profiles of erianin remain unknown. This study was carried out to investigate the metabolic profiles of erianin in rats and humans.
Erianin was orally administered to rats at a single dose of 50 mg/kg. Urine and bile samples were collected. For in vitro metabolism, erianin was co-incubated with rat or human hepatocytes at 37°C for 2 h. The samples from incubations and rat were analyzed by liquid chromatography combined with electrospray ionization high-resolution mass spectrometry. The data were processed by MetWorks software. The structures of the metabolites were proposed by comparing the mass spectra with that of the parent compound.
A total of twenty-four metabolites were detected in vitro and in vivo, including seven phase I and eighteen phase II metabolites. The phase I metabolic pathways of erianin were hydroxylation, demethylation and dehydrogenation. Erianin undergoes metabolic activation to form reactive metabolites quinoid intermediates, which were further trapped by glutathione (GSH) or N-acetylcysteine. The phase II metabolic pathways were glucuronidation, glutathione and N-acetylcysteine conjugation.
The present study provides an overview pertaining to the in vitro and in vivo metabolic profiles of erianin, which is indispensable for us to understand the efficacy and safety of erianin, as well as the herbal medicine D. chrysotoxum.
从金钗石斛中分离得到的生物活性成分鸢尾宁被证明具有许多与癌症预防和治疗相关的生物学特性。然而，鸢尾宁的代谢谱仍然未知。本研究旨在探讨鸢尾宁在大鼠和人体内的代谢谱。
将鸢尾宁以 50mg/kg 的单剂量口服给予大鼠。收集尿液和胆汁样本。对于体外代谢，将鸢尾宁与大鼠或人肝细胞在 37°C 下共孵育 2 小时。用液相色谱-电喷雾电离高分辨质谱法分析孵育物和大鼠的样品。使用 MetWorks 软件处理数据。通过将质谱与母体化合物进行比较，提出代谢物的结构。
在体内和体外共检测到 24 种代谢物，包括 7 种 I 相和 18 种 II 相代谢物。鸢尾宁的 I 相代谢途径为羟化、去甲基化和脱氢。鸢尾宁发生代谢激活，形成反应性代谢物醌中间产物，进一步被谷胱甘肽（GSH）或 N-乙酰半胱氨酸捕获。II 相代谢途径为葡萄糖醛酸化、谷胱甘肽和 N-乙酰半胱氨酸缀合。
本研究提供了鸢尾宁在体内和体外代谢谱的概述，这对于我们了解鸢尾宁的功效和安全性以及金钗石斛草药至关重要。
