Effect of cepharanthine on antitumor activity of 1-(2-tetrahydrofuryl)-5-fluorouracil (FT-207)--5-fluorouracil delivery into tumor tissue
Abstract
A study on the antitumor effect and distribution to tumor tissue of 1-(2-tetrahydrofuryl)-5-fluorouracil (FT-207) when administered with cepharanthine was performed using RPMI 4788 human colon cancer cell line or murine Sarcoma-180 tumor cells in vitro and in vivo. Combined treatment with FT-207 or 5-fluorouracil (5-FU) and cepharanthine showed a marked anti-proliferative effect on DNA synthesis of RPMI 4788 cells when measured by 3H-thymidine incorporation in vitro. Combination of FT-207 (1 microgram/ml) and cepharanthine (1 microgram/ml or 5 micrograms/ml) exhibited a similar antitumor effect to FT-207 (25 micrograms/ml). Also the DNA synthesis of RPMI 4788 cells was inhibited by low dose of 5-FU with cepharanthine similarly by high dose of 5-FU alone. On the other hand, Sarcoma-180 tumor was transplanted to the back of mice, and FT-207 (50 mumole/kg; 10 mg/kg) and cepharanthine were orally coadministered once at day 7 after tumor transplantation. This combined therapy significantly inhibited the growth of Sarcoma-180 tumor. Furthermore, antitumor activity of FT-207 was enhanced significantly by coadministration of cepharanthine daily for 10 days. The concentration of FT-207 or 5-FU in the tumor tissue, normal tissues and serum were measured in mice with Sarcoma-180 tumor. The mice were given FT-207 and cepharanthine orally once at day 7 (I) or daily for 10 days (II) after transplantation of Sarcoma-180 tumor cells. No remarkable difference was found in the concentration…
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