Cytotoxic phenolic constituents from Hypericum japonicum.


State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang, 550014, PR China; School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang, 550025, PR China; Key Laboratory of Chemistry for Natural Products of Guizhou Province, And Chinese Academy of Sciences, Guiyang, 550014, PR China. Electronic address: [Email]


Nine undescribed compounds, including five xanthone derivatives, two flavonoids, one 2-pyrone derivative, and one undescribed naturally occurring compound, along with 30 known phenolic compounds, were isolated from Hypericum japonicum. In addition, hyperjaponols A and B were identified as racemates. The structures and absolute configurations of the undescribed compounds were determined by comprehensive MS, NMR spectroscopy, and electronic circular dichroism (ECD) calculations. The cytotoxic effects of the isolated compounds on two human tumour cell lines (HEL and MDA-MB-231) were evaluated by the MTT assay. Eighteen compounds showed good inhibitory activities against the HEL cell line, with IC50 values of 3.53-18.7 μM, while nine compounds exhibited moderate cytotoxicity against the MDA-MB-231 cancer cell line, with IC50 values ranging from 4.92 to 10.75 μM. Their preliminary structure-activity relationship of the isolated compounds was also discussed.


Cytotoxic activities,Hypericum japonicum thunb. (Hypericaceae),Phenolic compounds,Structure-activity relationship,Xanthone and flavonoid derivatives,