| In vitro: |
| Bioorg Med Chem. 2008 Apr 15;16(8):4331-40. | | Inhibitors of DNA polymerase beta: activity and mechanism.[Pubmed: 18343122 ] |
METHODS AND RESULTS:
Bioassay-guided fractionation of extracts prepared from Couepia polyandra and Edgeworthia gardneri resulted in the isolation of the DNA polymerase beta (pol beta) inhibitors oleanolic acid (1), Edgeworin (2), betulinic acid (3), and stigmasterol (4). Study of these pol beta inhibitors revealed that three of them inhibited both the lyase and polymerase activities of DNA polymerase beta, while stigmasterol inhibited only the lyase activity. Further investigation indicated that the four inhibitors had substantially different effects on the DNA-pol beta binary complex that is believed to be an obligatory intermediate in the lyase reaction. It was found that the inhibitors potentiated the inhibitory action of the anticancer drug bleomycin in cultured A549 cells, without any influence on the expression of pol beta in the cells.
CONCLUSIONS:
The results of the unscheduled DNA synthesis assay support the thesis that the potentiation of bleomycin cytotoxicity by DNA pol beta inhibitors was a result of an inhibition of DNA repair synthesis. | | Biol Pharm Bull. 2004 Aug;27(8):1312-6. | | Antiproliferative constituents in plants 14. Coumarins and acridone alkaloids from Boenninghausenia japonica NAKAI.[Pubmed: 15305045] |
METHODS AND RESULTS:
The MeOH extracts of the ground part and the root of Boenninghausenia japonica NAKAI showed inhibitory activity against tumor cell growth. Fractionation of the extracts has resulted in isolation of 1,3-dihydroxy-4-(2'-hydroxy-3'-hydroxymethyl-3',4'-epoxy-butyl)-N-methylacridone, 1,3-dihydroxy-4-[(Z)-3'-hydroxy-3'-methyl-buten-1'-yl]-N-methylacridone, 3-(1',1'-dimethylallyl)-7-hydroxy-8-methoxy-2H-1-benzopyran-2-one, casegravol, cis-casegravol, and Edgeworin in addition to 9 compounds reported from B. japonica and B. albiflora.
CONCLUSIONS:
The isolates from this plant and some related compounds were tested for antiproliferative activity against human gastric adenocarcinoma (MK-1), human uterus carcinoma (HeLa), and murine melanoma (B16F10) cells. |
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