Antineoplastic pharmaceutical composition containing piperizine and application of antineoplastic pharmaceutical composition

An anti-tumor drug, the technology of acetazine piperazine, applied in the field of tumor treatment, can solve the problems of reduced treatment effect, severe drug resistance, etc., and achieves the effect of broad market prospect, good treatment effect, and significant killing effect.

Active Publication Date: 2022-04-08
THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In view of the above problems and deficiencies, the present invention provides an antineoplastic pharmaceutical composition containing piperacetazine and its application, by using sunitinib in combination with piperacetazine to solve the problem of using conventional doses of sunitinib in the prior art. The problem of serious drug resistance brought by Tini and the problem of significantly reduced therapeutic effect after reducing the treatment dose, so as to obtain more significant clinical therapeutic effect and reduce sunitinib drug resistance and side effects

Method used

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  • Antineoplastic pharmaceutical composition containing piperizine and application of antineoplastic pharmaceutical composition
  • Antineoplastic pharmaceutical composition containing piperizine and application of antineoplastic pharmaceutical composition
  • Antineoplastic pharmaceutical composition containing piperizine and application of antineoplastic pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 In vitro anti-tumor synergy experiment

[0041] (1) Take 786-O cells in the logarithmic growth phase and plant them in a 96-well plate at a certain density (1500-2000 / well);

[0042] (2) Discard the old medium after 24 hours, divide the cells into 5 groups of 1-5 for use, add medium containing different drug concentrations, set 3 duplicate wells for each group, and add sunitinib to group 1 , group 2 was added with piperacetazine, group 3 was added with sunitinib and piperacetazine, group 4 was added with DMSO, and group 5 was used as the blank group; group 1 had an initial concentration of sunitinib of 100 μM, after which each well was sequentially diluted ; The initial concentration of piperazine in group 2 was 100 μM, after which each well was sequentially diluted; in group 3, the initial concentration of sunitinib and piperazine was 100 μM, and then each well was sequentially diluted.

[0043] (3) After culturing for 48 hours, discard the drug solution, ad...

Embodiment 2

[0054] Example 2 In vitro anti-tumor synergistic compatibility experiment

[0055] (1) 786-O, Caki-2 and OS-RC-2 cells in the logarithmic growth phase were planted in a 96-well plate at a certain density (1500-2000 / well);

[0056] (2) Discard the old medium after 24 hours, add drugs containing different compatible forms to continue the culture, and set 3 duplicate wells for each group;

[0057] (3) After culturing for 48 hours, discard the cell culture medium, add a medium containing 5% CCK-8, incubate at 37°C for 3 hours, and then use a microplate reader to detect the OD value at 450nm.

[0058] Based on the DMSO group, the corresponding synergistic effect evaluation was carried out on the inhibition rate, and the combined drug effect was analyzed by King's formula (Q value):

[0059] Q=E (A+B) / (E A +E B -E A ×E B ), that is, E (A+B) : Inhibition rate of combination drug, E A : Inhibition rate of drug A alone, E B : Inhibition rate of drug B alone. When Q>1.15, it ...

Embodiment 3

[0064] Example 3 In vivo anti-tumor experiment

[0065] Choose Balb / c mice around 5-6 weeks old for in situ tumor growth inhibition experiment in vivo, the specific experimental method is as follows:

[0066] (1) Culture murine renal carcinoma Renca cells in vitro, collect logarithmic phase cells, centrifuge and suspend;

[0067] (2) The cell suspension was injected subcutaneously into 3 Balb / c mice, and after the tumors formed, the tumors were taken out and divided into 5mm 3 Small tumors of left and right size;

[0068] (3) Re-transplant the obtained small tumors under the kidney capsule of several new Balb / c mice;

[0069] (4) After tumor formation, 24 nude mice were randomly divided into 4 groups, numbered 1-4, 6 mice in each group, and administered by intragastric administration; among them, group 1 was given sunitinib-10mg / kg· d, Group 2 was given piperacetylazine-10 mg / kg d, group 3 was given sunitinib-5 mg / kg d+piperacetazine-5 mg / kg d, group 4 was given the same am...

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Abstract

The invention provides an anti-tumor pharmaceutical composition containing piperizine and application of the anti-tumor pharmaceutical composition. On the basis of the original sunitinib, the piperazine is further added and can generate a very remarkable synergistic effect with the sunitinib, so that the proliferation of cancer cells is obviously inhibited, and the sunitinib composition has very remarkable killing efficiency on the cancer cells. According to the pharmaceutical composition provided by the invention, the problem of serious drug resistance caused by pure use of sunitinib and the problem of obviously reduced treatment effect when the conventional use amount of sunitinib is reduced in the prior art can be obviously improved, the clinical treatment efficiency is greatly improved, and the treatment toxic and side effects of a patient are reduced; a new scheme is provided for clinical treatment, and the traditional Chinese medicine composition has very wide market prospects and extremely important social significance.

Description

technical field [0001] The invention belongs to the technical field of tumor treatment, and in particular relates to an antitumor pharmaceutical composition containing piperacetazine and application thereof. Background technique [0002] Kidney cancer is one of the three major malignant tumors of the urinary system. Among them, renal cell carcinoma (Renal Cell Carcinoma, RCC) is a malignant tumor originating from renal tubular epithelial cells, accounting for 90% of all renal cancers, and is the most common type of renal malignant tumor. Due to the application of screening methods such as ultrasound and CT and the enhancement of people's awareness of health checkups, the incidence of renal cancer has increased. However, early renal cancer can be treated with radical surgery, and the prognosis is better. The overall 5-year survival rate of RCC is 49%, but its prognosis is closely related to the clinical stage and pathological grade of the disease. Patients with clinical stag...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5415A61P35/00A61P35/02A61K31/404
Inventor 岳欣彭振维王雪涔陈勇
Owner THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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