Department of Chemical Biology and Genetics, Centre of the Region Haná for Biotechnological and Agricultural Research, Palacký University, Šlechtitelů 27, CZ-783 71, Olomouc, Czech Republic.
Central Laboratories and Research Support, Centre of the Region Haná for Biotechnological and Agricultural Research, Palacký University, Šlechtitelů 27, CZ-783 71, Olomouc, Czech Republic.
Phytochem Anal. 2018 Jan;29(1):23-29. doi: 10.1002/pca.2711. Epub 2017 Aug 7.
Various species of the Euphorbia genus contain diterpene ingenol and ingenol mebutate (ingenol-3-angelate), a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death. A gel formulation of the drug has been approved by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the topical treatment of actinic keratosis.
To develop a rapid and reliable method for quantification of ingenol in various plant extracts.
Methanolic extracts of 38 species of the Euphorbia genus were analysed via ultra-high performance liquid chromatography with tandem mass spectrometry (UHPLC-MS/MS) after methanolysis and solid-phase extraction (SPE) purification. The O-labelled ingenol analogue was prepared and used as an internal standard for ingenol content determination and method validation.
The highest ingenol concentration (547 mg/kg of dry weight) was found in the lower leafless stems of E. myrsinites. The screening confirms a substantial amount of ingenol in species studied previously and furthermore, reveals some new promising candidates.
The newly established UHPLC-MS/MS method shows to be an appropriate tool for screening of the Euphorbia genus for ingenol content and allows selection of species suitable for raw material production and/or in vitro culture initiation. Copyright © 2017 John Wiley & Sons, Ltd.
大戟属的各种物种都含有二萜醇 ingenol 和 ingenol mebutate（ingenol-3-angelate），这是一种在植物大戟属植物汁液中发现的物质，也是细胞死亡的诱导剂。该药物的凝胶制剂已获得美国食品和药物管理局 (FDA) 和欧洲药品管理局 (EMA) 的批准，用于局部治疗光化性角化病。
开发一种快速可靠的方法来定量分析各种植物提取物中的 ingenol。
通过超高效液相色谱-串联质谱 (UHPLC-MS/MS) 分析 38 种大戟属植物的甲醇提取物，经过甲醇解和固相萃取 (SPE) 纯化。制备了 ¹³C 标记的 ingenol 类似物，并将其用作 ingenol 含量测定和方法验证的内标。
最高的 ingenol 浓度（547mg/kg 干重）出现在无叶下茎的 E. myrsinites 中。筛选证实了先前研究的物种中存在大量 ingenol，此外，还发现了一些有前途的新候选物。
新建立的 UHPLC-MS/MS 方法可用于筛选大戟属植物中的 ingenol 含量，并可选择适合原材料生产和/或体外培养启动的物种。版权所有©2017 年 John Wiley & Sons, Ltd.
