| Cancer Treat Rep. 1983 Feb;67(2):179-82. |
| Action of (S)-10-hydroxycamptothecin on P388 leukemia and distribution of the drug in mice.[Pubmed: 6825126] |
METHODS AND RESULTS:
As an inhibitor of the growth of P388 leukemia in mice, (S)-10-Hydroxycamptothecin (OPT) was as potent as the parent compound camptothecin (CPT). Incorporation of thymidine into DNA was the parameter most sensitive to OPT in vitro (ED50 approximately 4 micrograms/ml), but incorporation of cytidine into RNA and of acetate into lipids was also reduced significantly in the presence of the drug. The cytofluorometric profile suggested suppression of the S and G2/M phases. The distribution of OPT in mice at 2 and 24 hours after ip injection (10 mg/kg) was essentially similar to that of CPT, with the exception of a somewhat greater concentration of CPT in the liver.
CONCLUSIONS:
In their pharmacology, OPT and CPT appear to be very similar, despite reports that the hydroxy derivative is less toxic. |
| Anticancer Res. 1981;1(2):115-9. |
| Anti-tumor effect of (S)-10-hydroxycamptothecin on mouse hepatoma BW7756 and its possible mode of action.[Pubmed: 7347154] |
METHODS AND RESULTS:
(S)-10-Hydroxycamptothecin (OPT), an analog of camptothecin (CPT), was found to inhibit the growth of the mouse hepatoma BW7756, when given at 1.0 mg/kg/day for 14 days. Cell cycle studies using flow cytofluorometry indicated that this drug inhibited the S-Phase of the tumor cells in vivo and the S and G2/M phases in vitro. Similar studies on host liver showed little or no effect. In spite of the narrow range of the effective dose of this drug against mouse hepatoma BW7756, the use of OPT in combination with other antitumor agents may be useful in primary hepatoma or liver metastases in view of its low toxicity towards host liver.
CONCLUSIONS:
A simple cytofluorometric method useful for live cell cycle study has been adapted for this investigation and can be adopted for other drug studies. |
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