School of Chemistry and Chemical Engineering, University of Jinan, Jinan, 250022, China; School of Biological Science and Technology, University of Jinan, Jinan, 250022, China.
School of Biological Science and Technology, University of Jinan, Jinan, 250022, China.
Phytochemistry. 2024 Dec;228:114233. doi: 10.1016/j.phytochem.2024.114233. Epub 2024 Aug 5.
Nine previously unreported lathyrane diterpenoids named euphorantesters A-I, along with 16 known analogues, have been separated from the tubers of Euphorbia antiquorum. Their structures were established by means of spectroscopic analyses, time-dependent density functional theory based electronic circular dichroism calculation and single crystal X-ray crystallography. Their reversal ability against P-glycoprotein-mediated multidrug resistance (MDR) in MCF-7/ADR cell line was then evaluated, and 15 ones exhibited moderate MDR reversal activity with reversal fold falling in the range of 1.12-13.15. The most active euphorantester B could effectively increase the sensitivity of MCF-7/ADR cell to adriamycin comparably to the reference drug verapamil.
从大飞扬Euphorbia antiquorum 的块根中分离得到了 9 个以前未报道的拉蒂烷二萜类化合物，命名为 euphorantesters A-I，以及 16 个已知类似物。通过光谱分析、基于时间依赖密度泛函理论的电子圆二色性计算和单晶 X 射线晶体学确定了它们的结构。然后评估了它们对 MCF-7/ADR 细胞系中 P-糖蛋白介导的多药耐药（MDR）的反转能力，其中 15 个表现出中等的 MDR 反转活性，反转倍数在 1.12-13.15 之间。最活跃的 euphorantester B 可以有效地增加 MCF-7/ADR 细胞对阿霉素的敏感性，与参比药物维拉帕米相当。
