Four previously undescribed ent-abietane diterpenoids(1—4),along with eleven known analogues(5—15),were isolated from the roots of wild Euphorbia fischeriana.Their gross structures were determined via extensive spec...Four previously undescribed ent-abietane diterpenoids(1—4),along with eleven known analogues(5—15),were isolated from the roots of wild Euphorbia fischeriana.Their gross structures were determined via extensive spectroscopic data,and the absolute configurations were elucidated by means of single-crystal X-ray diffraction analysis,Rh2(OCOCF3)4-induced CD spectrum and ECD calculations.Their cervical carcinoma inhibition activities counteract HeLa cells were screened by MTT assay,and the structure-activity relationships were further examined.The results demonstrated that 2(IC50 value at 3.75μmol/L)was more potent than cisplatin.The underlying mechanism study revealed that 2 could distinctly induce apoptosis accompanied by increasing reactive oxygen species(ROS)production,Ca^(2+)influx and decreasing mitochondrial membrane potential.Furthermore,signal pathways including MAPKs/AKT might play a significant role in 2-induced cervical cancer cells death.展开更多
基金This work was supported by the National Key R&D Program of China(2017YFC1701200)the National Natural Science Foundation of China(81903789)。
文摘Four previously undescribed ent-abietane diterpenoids(1—4),along with eleven known analogues(5—15),were isolated from the roots of wild Euphorbia fischeriana.Their gross structures were determined via extensive spectroscopic data,and the absolute configurations were elucidated by means of single-crystal X-ray diffraction analysis,Rh2(OCOCF3)4-induced CD spectrum and ECD calculations.Their cervical carcinoma inhibition activities counteract HeLa cells were screened by MTT assay,and the structure-activity relationships were further examined.The results demonstrated that 2(IC50 value at 3.75μmol/L)was more potent than cisplatin.The underlying mechanism study revealed that 2 could distinctly induce apoptosis accompanied by increasing reactive oxygen species(ROS)production,Ca^(2+)influx and decreasing mitochondrial membrane potential.Furthermore,signal pathways including MAPKs/AKT might play a significant role in 2-induced cervical cancer cells death.
