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.
Keyphrases
- density functional theory
- adverse drug
- breast cancer cells
- multidrug resistant
- molecular docking
- high resolution
- molecular dynamics
- single cell
- emergency department
- magnetic resonance imaging
- stem cells
- high intensity
- mass spectrometry
- computed tomography
- mesenchymal stem cells
- contrast enhanced
- solid state
- monte carlo