VEGFR inhibitor and blood pressure reducing medicine composition and application thereof
A technology of a composition and antihypertensive drug, applied in the field of medicine, can solve the problems that the combination use has not received extensive attention, and the side effects of targeted drugs are less concerned, and achieve significant curative effect, broad research prospects, and the effect of reducing blood pressure elevation.
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Embodiment 1
[0026] Inhibitory effects of axitinib and losartan monomers and combined drugs on the growth of kidney cancer in the subcutaneous xenograft tumor model of Balb / c nude mice. The compounds in each group were administrated with 0.5% sodium carboxymethylcellulose suspension Administration for 15 days. Axitinib has two drug concentrations of low dose 30mg / kg and high dose 60mg / kg, and losartan is administered at 10mg / kg. The experimental results are shown in Table 1.
[0027] Table 1 Inhibitory effects of axitinib and losartan monomers and combined drugs on the growth of renal cell carcinoma
[0028]
[0029] It can be seen from the above results that axitinib has a significant inhibitory effect on the growth of renal cancer in a dose-dependent manner, and the combination of losartan will not significantly reduce its anti-tumor effect. Kidney cancer also has an inhibitory effect.
Embodiment 2
[0031] Effects of axitinib and losartan alone and in combination on skin vascular permeability (Miles test)
[0032] Axitinib (10mg / kg), losartan (10mg / kg) and its combination axitinib (10mg / kg) + losartan (10mg / kg) were administered to C57BL / 6N small Rats were injected with Evans blue dye through the tail vein. After anesthesia, both sides of the abdomen were shaved. PBS and 1% VEGFA were injected into the skin on both sides. After 4 hours, a vertical incision of about 3-4 cm was made from the lower abdomen to the chest with scissors. . Remove areas of dye accumulation. After the sample is dried, formamide is added to extract the Evans blue dye, and the absorbance value is detected.
[0033] The result is attached figure 1 As shown, it can be seen from the control group that VEGFA can significantly increase vascular permeability. This effect was blocked by the VCGFR inhibitor axitinib, which reduced VEGFA-induced hypervascular permeability, which is one of the mechanisms ...
Embodiment 3
[0035] Effects of axitinib and losartan alone and in combination on blood pressure in Wistar rats
[0036] Randomly select 8 7-week-old Wistar rats, 2 in each group, orally administer axitinib (25mg / kg), losartan (10mg / kg), axitinib (25mg / kg) + loxa Tan (10mg / kg) and control sodium carboxymethylcellulose, twice a day for 7 consecutive days. Changes in systolic blood pressure were monitored daily.
[0037] The results of the systolic blood pressure test on the 7th day are attached figure 2 As shown, compared with the control group, axitinib significantly increased the systolic blood pressure of rats by about 20%, and the combined administration of losartan significantly reduced the increase in blood pressure caused by axitinib.
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