| Description: |
1-Decarboxy-3-oxo-ceanothic acid shows in vitro cytotoxic activity in a human ovarian adenocarcinoma cell line, the cytotoxic effect is mediated, at least in part, by the induction of apoptosis. It shows cytotoxic against OVCAR-3 and HeLa cancer cell lines, with an IC50 of 2.8 and 6.6 microg/mL, respectively, and an IC50 of 11.3 microg/mL against normal cell line FS-5. |
| In vitro: |
| Res Commun Mol Pathol Pharmacol. 1998 Jun;100(3):313-26. | | In vitro cytotoxic activity of 1-decarboxy-3-oxo-ceanothic acid in a human ovarian adenocarcinoma cell line.[Pubmed: 9730010] |
METHODS AND RESULTS:
The effect of a novel pentacyclic triterpene, 1-Decarboxy-3-oxo-ceanothic acid (DOCA) on DNA synthesis, DNA degradation and programmed cell death was examined in human ovarian adenocarcinoma (OVCAR-3) cells. OVCAR-3 cells exposed to various concentrations of DOCA for 30 h displayed a dose-dependent inhibition of DNA synthesis. Morphologically, treatment with 10 microg/ml of 1-Decarboxy-3-oxo-ceanothic acid for 24 h and 72 h resulted respectively in reduction in cell volume and condensation of nuclear structures. By agarose gel analysis, DNA fragmentation with the characteristic pattern of inter-nucleosomal ladder was observed after cells were treated with 2.5 microg/ml of 1-Decarboxy-3-oxo-ceanothic acid for 24 h. Both cell death and DNA fragmentation caused by this compound were partially inhibited by the protein synthesis inhibitor cycloheximide, suggesting that the apoptotic process caused by 1-Decarboxy-3-oxo-ceanothic acid requires synthesis of new proteins. On the other hand, no apparent double-stranded DNA breaks were detected after cells were incubated with 2.5 microg/ml of 1-Decarboxy-3-oxo-ceanothic acid for 24 h, indicating that DNA damage was not a preceding event for apoptosis induced by this compound.
CONCLUSIONS:
Taken together, our results demonstrate that the cytotoxic effect of 1-Decarboxy-3-oxo-ceanothic acid is mediated, at least in part, by the induction of apoptosis. | | J Nat Prod. 1998 Nov;61(11):1343-7. | | Preparation and cytotoxic effect of ceanothic acid derivatives.[Pubmed: 9834149] |
METHODS AND RESULTS:
Six ceanothane and 1-norceanothane derivatives (1, 2, 8-11) were prepared from ceanothic acid dibenzyl ester. These ring-A homologues of betulinic acid exhibited cytotoxic effects.
CONCLUSIONS:
Among these, 1-Decarboxy-3-oxo-ceanothic acid (2) was found to be the most cytotoxic against OVCAR-3 and HeLa cancer cell lines, with an IC50 of 2.8 and 6.6 microg/mL, respectively, and an IC50 of 11.3 microg/mL against normal cell line FS-5. |
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