R 2 consecutive weeks. Results of immunohistochemical analysis of tumor tissue sections showed that administration BPR1K653 cells Isoliquiritigenin reduces the amount of phosphorus in histone H3 positive tumor tissue compared to control. The decreased rate of tumor growth in M Mice with either BPR1K653 VX680 or 5 days / week for 2 consecutive weeks was treated for also observed. There was a decline, 73% in tumor volume at day 30 in animals treated with BPR1K653. In addition, there was a decrease, 68% of tumor volume over 30 days in animals treated with VX680. BPR1K653 was also at a dose of 15 mg / kg, with no signs of toxicity T in the KB tumor xenograft model, that weight loss after treatment was below 10% in the treated group tolerated than in the control group for comparison.
To determine whether the inhibition of tumor growth at M Treated mice BPR1K653 was connected in populations of cancer cells apoptosis Imatinib Glivec ht obtained, Tumors were surgically removed from M Mice 12 days after treatment and tissue sections were analyzed TUNEL assay. The results of TUNEL assay showed that the amount was treated in apoptotic cells in the tumor tissue of M Nozzles pr Sentieren BPR1K653 significantly h Ago than the nozzles in control aids. This is consistent with the result of the above in vitro experiment the BPR1K652 able induction of apoptosis in cancer cells. In particular, is so effective BPR1K653 MDR1-expressing tumor xenografts, as MDR1 in cultured cells. Here VIN10 KB tumor xenografts was used to investigate the effectiveness of BPR1K653 against MDR1-expressing tumor in vivo.
Due to the characteristics of slow-growing KB VIN10 who treated Mice re U or 15 mg / kg BPR1K653 or 30 mg / kg ip for 5 days a week VX680 for 3 consecutive weeks instead of two weeks, as in the KB implanted M Mice. Compared Kaempferol to control aids nozzles, Tumor growth was significantly inhibited in KB VIN10 M Nozzles with 15 mg / kg BPR1K653. There was a 50% decrease in tumor volume at day 42 in animals treated with BPR1K653. However, no significant antitumor effect VX680 growth inhibitor for M Mice transplanted with KB cells VIN10. In addition BPR1K653 was also at a dose of 15 mg / kg, without tolerate signs of toxicity T in tumor xenograft model KB VIN10 that the weight loss after treatment was below 10% to compare the treatment group, the control group. So to speak BPR1K653 exerts strong anti-tumor efficacy of both negative and MDR MDR tumor xenografts.
The pharmacokinetics of rats BPR1K653 closing Lich pharmacokinetic studies were examined by BPR1K653 w Be consulted during a period of 24 h, plasma concentrations of intravenously after a single administration S BPR1K653. After a single administration of BPR1K653 at a dose of 5 mg / kg in rats BPR1K653 a maximum plasma concentration of 10 mm to 2 min after the administration, and the shops PROTECTED BPR1K653 plasma concentration remained at a concentration of 3, 9 nM 24 h after of administration. The plasma half-life, total clearance and volume of distribution at steady state was 3.960.7 h 49.3610.6 mL kg / min / L and 10.665.1 / kg. Discussion Aurora Kinases are important regulators of mitosis and evidence emerged of abnormalities in their expression and activity of t are closely related to e