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  • Title: Cytotoxicity, apoptosis-inducing effects and structure-activity relationships of four natural xanthones from Gentianopsis paludosa Ma in HepG2 and HL-60 cells.
    Author: Ding L, Liu B, Zhang SD, Hou Q, Qi LL, Zhou QY.
    Journal: Nat Prod Res; 2011 Apr; 25(7):669-83. PubMed ID: 20182950.
    Abstract:
    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.
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