Department of Pharmacognosy, Faculty of Pharmacy Medical College, Jagiellonian University, Kraków, Poland.
Department of Food Chemistry and Nutrition, Faculty of Pharmacy Medical College, Jagiellonian University, Kraków, Poland.
Biomed Pharmacother. 2022 Oct;154:113592. doi: 10.1016/j.biopha.2022.113592. Epub 2022 Aug 24.
In the current study, the fruits of a popular ornamental tree, Sorbus intermedia, were investigated phytochemically and biologically as potential source of bioactive triterpenes. Six terpenoids were isolated and examined with respect to their cytotoxic activity using a broad screening in vitro model and multivariate analysis for better demonstration of the effects on cancer cells. This chemometric approach allowed us to confirm that the structural characteristics of the compounds significantly affected their impact on cell lines. Ursolic acid was found to be the most potent cytotoxic agent with IC predominantly < 10 μg/mL after 24 h of incubation. Its 3-acetoxy derivative was less active, however, an improvement in selectivity with regard to prostate panel was observed. Reduction of the carboxylic moiety at C28, as well as introduction of the hydroxyl group at 19α position led to complete loss of cytotoxic activity.
在本研究中,我们对一种受欢迎的观赏树——中华稠李的果实进行了植物化学和生物学研究,以探索其作为生物活性三萜类化合物的潜在来源。我们分离了六种三萜类化合物,并使用广泛的体外筛选模型和多元分析来评估它们的细胞毒性活性,以更好地展示它们对癌细胞的影响。这种化学计量学方法使我们能够确认化合物的结构特征对其对细胞系的影响有显著影响。熊果酸被发现是最有效的细胞毒性剂,在孵育 24 小时后,IC 主要 < 10 μg/mL。它的 3-乙酰氧基衍生物活性较低,但对前列腺面板的选择性有所提高。C28 位羧酸部分的还原以及 19α 位羟基的引入导致完全丧失细胞毒性活性。