Cytotoxicity, apoptosis-inducing effects and structure-activity relationships of four natural xanthones from Gentianopsis paludosa Ma in HepG2 and HL-60 cells.
Four xanthones were isolated from Gentianopsis paludosa Ma and were identified by modern spectroscopic methods. Cytotoxicity of the four xanthones was tested on HepG2 cells and HL-60 cells by sulphorhodamine B (SRB) assay. Clonogenic survival assay, trypan blue exclusion method, AO/EB staining and DNA fragmentation assay were conducted to investigate the effect on growth inhibition and apoptosis in the two cell lines in vitro. At the same time, structure-activity relationships (SARs) of the xanthones were investigated. The results showed that the xanthones had significant cytotoxicity and inhibition of proliferation in both HepG2 cells and HL-60 cells, and could induce apoptosis in these two cell lines. SARs indicated that the methoxy group had more cytotoxic contribution than the hydroxyl group at site C-8 in the structural scaffold of xanthone. The glycosidea at site C-1 may aggravate the stereospecific blockade of compound 4 and reduced its cytotoxic activity.
Ding
Lan
L
College of Life Sciences, Northwest Normal University, Lanzhou 730070, People's Republic of China. dinglan@nwnu.edu.cn
Liu
Bo
B
Zhang
Shi-dong
SD
Hou
Qian
Q
Qi
Lin-lin
LL
Zhou
Qi-yin
QY
D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D029965:Gentianaceae / Q000737:chemistry*; D005960:Glucosides / Q000302:isolation & purification* / Q000494:pharmacology*; D018922:HL-60 Cells; D006801:Humans; D010936:Plant Extracts / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry; D013329:Structure-Activity Relationship; D044004:Xanthones / Q000302:isolation & purification / Q000494:pharmacology*
C568198:1,7-dihydroxy-3,8-dimethoxyxanthone; C568197:1-O-beta-D-glucoside-7-hydroxyl-3,8-dimethoxyxanthone; D000970:Antineoplastic Agents; D005960:Glucosides; D010936:Plant Extracts; D044004:Xanthones