In this study,three new germacranolide sesquiterpenes(1–3),together with six related known analogues(4–9)were isolated from the whole plant of Carpesium cernuum.Their structures were established by a combination of ...In this study,three new germacranolide sesquiterpenes(1–3),together with six related known analogues(4–9)were isolated from the whole plant of Carpesium cernuum.Their structures were established by a combination of extensive NMR spectroscopic analysis,HR-ESIMS data,and ECD calculations.The anti-leukemia activities of all compounds towards three cell lines(HEL,KG-1a,and K562)were evaluated in vitro.Compounds 1–3 exhibited moderate cytotoxicity with IC50 values ranging from 1.59 to 5.47μmol·L^(−1).Mechanistic studies indicated that 2 induced apoptosis by decreasing anti-apoptotic protein Bcl-2 and activating the caspase family in K562 cells.These results suggest that compound 2 is a potential anti-leukemia agent.展开更多
基金supported by the Science and Technology Department of Guizhou Province(No.QKHJC[2016]1002,81872772,81960546,and U1812403)the National Natural Science Foundation of China(Nos.81872772,81960546,and U1812403)+1 种基金the Science and Technology Department of Anshun City(No.ASKP[2019]3)the 100 Leading Talents of Guizhou Province(fund for LI Yan-Mei,Nos.P2018-KF11 and QZYY-019-022).
文摘In this study,three new germacranolide sesquiterpenes(1–3),together with six related known analogues(4–9)were isolated from the whole plant of Carpesium cernuum.Their structures were established by a combination of extensive NMR spectroscopic analysis,HR-ESIMS data,and ECD calculations.The anti-leukemia activities of all compounds towards three cell lines(HEL,KG-1a,and K562)were evaluated in vitro.Compounds 1–3 exhibited moderate cytotoxicity with IC50 values ranging from 1.59 to 5.47μmol·L^(−1).Mechanistic studies indicated that 2 induced apoptosis by decreasing anti-apoptotic protein Bcl-2 and activating the caspase family in K562 cells.These results suggest that compound 2 is a potential anti-leukemia agent.
