Saidu Muhammad Bello, Kúsz Norbert, Berkecz Róbert, Rácz Bálint, Spengler Gabriella, Hohmann Judit, Rédei Dóra
Department of Pharmacognosy, University of Szeged, 6720, Szeged, Eötvös u. 6., Hungary.
Institute of Pharmaceutical Analysis, University of Szeged, 6720, Szeged, Somogyi u. 4., Hungary.
Phytochemistry. 2022 Dec;204:113344. doi: 10.1016/j.phytochem.2022.113344. Epub 2022 Aug 8.
Nine previously undescribed ingol-type diterpenoid polyesters with eighteen known ingol esters, two ent-atisane, and one stachane diterpenoid were isolated from the methanol extract of Euphorbia deightonii Croizat. The structures were established by extensive spectroscopic analysis involving 1D (H, C J-modulation) and 2D NMR experiments, HRESIMS measurements, and the comparison of the spectroscopic data with reported literature values. The cytotoxic concentrations of 13 isolated compounds were determined, and the compounds were investigated for multidrug resistance modulating activity on an L5178 mouse lymphoma cell line using a rhodamin 123 accumulation assay. Six ingol esters demonstrated the significant inhibition of P-glycoprotein, while the two ent-atisane diterpenoids were found to be inactive. The measured activities allowed to establish some structure-activity relationships. Notably, lower and higher-type diterpenoids simultaneously occurred in E. deightonii.
从大戟科植物德氏大戟（Euphorbia deightonii Croizat）的甲醇提取物中分离出9种先前未描述的因戈尔型二萜聚酯、18种已知的因戈尔酯、2种对映-乌散烷二萜和1种水苏烷二萜。通过涉及一维（氢、碳J调制）和二维核磁共振实验、高分辨电喷雾电离质谱测量以及将光谱数据与已报道文献值进行比较等广泛的光谱分析确定了这些化合物的结构。测定了13种分离化合物的细胞毒性浓度，并使用罗丹明123积累试验在L5178小鼠淋巴瘤细胞系上研究了这些化合物的多药耐药调节活性。6种因戈尔酯对P-糖蛋白有显著抑制作用，而2种对映-乌散烷二萜无活性。所测得的活性有助于建立一些构效关系。值得注意的是，德氏大戟中同时存在低级和高级型二萜。
