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Pharmaceutical composition containing ursolic acid and cyclophosphamide

A technology of cyclophosphamide and composition, which is applied in the field of anti-tumor pharmaceutical composition, and can solve the problems of increased toxicity of normal cells, etc.

Inactive Publication Date: 2015-06-10
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The activity of the modified ursolic acid derivatives has been improved, but the toxicity to normal cells has also been increased accordingly

Method used

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  • Pharmaceutical composition containing ursolic acid and cyclophosphamide
  • Pharmaceutical composition containing ursolic acid and cyclophosphamide
  • Pharmaceutical composition containing ursolic acid and cyclophosphamide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Cytotoxicity of ursolic acid and cyclophosphamide alone and in combination on breast cancer: The effects of ursolic acid and cyclophosphamide on different breast cancer cell lines—MCF-7 (breast cancer highly metastatic cell line), MDA- Cytotoxicity of MB-231 and 4T1.

[0021] The anticancer activity experiment was realized by cytotoxicity, and the proliferation inhibitory activities of different combinations of drugs on three tumor cell lines were measured by standard MTT colorimetry.

[0022] The specific steps are as follows: take the cells in the logarithmic growth phase and in good condition, add 0.25% trypsin to digest, make a single cell suspension, count on a cell counting plate, inoculate 100 μL per well in a 96-well plate, each well The number of cells was controlled at 5×10 4 / mL, 37℃, 5%CO 2 Cultivate overnight in the incubator, add the prepared samples of different concentrations, add 100 μL MTT (5 mg / mL) to each well after 48 hours of action, continu...

Embodiment 2

[0025] Inhibition of 4T1 tumors in mouse breast cancer by combined use of ursolic acid and cyclophosphamide

[0026] Experimental procedure: using BALB / C female mice (6-8 weeks old), 4T1 cell suspension (4*10 5 / 200μL PBS) were injected subcutaneously into the mammary fat pad (MFP) of mice. One week later, the mice were randomly divided into four groups (n=7), control group (normal saline, gavage), UA group (100 mg / kg, gavage), cyclophosphamide (20 mg / kg, gavage), UA+cyclophosphamide group (UA, 80mg / kg+CP, 20 mg / kg, orally). The administration continued for four weeks, during which the body weight of the mice was measured every two days and the long diameter (a) and short diameter (b) of the tumor were measured with a vernier caliper, according to the formula V=a×b 2 / 2, converted to tumor volume. On day 28, mice were sacrificed by cervical dislocation. The tumor tissue was dissected and weighed, and the tumor inhibition rate (TI) was calculated. TI (%) = (average tumor ...

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Abstract

The invention relates to an anti-tumor pharmaceutical composition. The pharmaceutical composition is characterized by comprising ursolic acid and cyclophosphamide with a weight ratio of (1-10):1, and the preferable ratio is (2-5):1. The ursolic acid and the cyclophosphamide are cooperatively used for treating tumors to generate an obvious synergistic effect. The composition can both reinforce the anti-tumor efficacy of a single component and reduce the toxicity on normal tissues, so as to improve the tumor treatment effect, and thus the pharmaceutical composition has a broad application prospect in the field of tumor treatment.

Description

technical field [0001] The invention belongs to the field of antitumor drugs, in particular, the invention relates to an antitumor pharmaceutical composition and application thereof. Background technique [0002] Malignant tumors and their complications are a serious threat to human life and health, and their incidence is increasing rapidly year by year. Statistics from the World Health Organization show that in 2000, there were nearly 10 million new cases of malignant tumors in the world, and its incidence rate is second only to cardiovascular and cerebrovascular diseases. Current cancer treatments include surgery, chemotherapy, and radiotherapy. Surgical resection is currently the preferred treatment method, but surgical resection is only suitable for a small number of patients with early localized tumors, and postoperative recurrence and metastasis are often accompanied. Therefore, chemotherapy is the most commonly used tumor treatment method at this stage. Conventional...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/675A61P35/00A61K31/56
Inventor 邵敬伟汤乔李涛刘亚军杨祥
Owner FUZHOU UNIV
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