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Application of physcion and derivative thereof in preparation of antitumor drugs

An anti-tumor drug and drug technology, applied in the field of medicine, can solve the problem of the high probability of distant metastasis and recurrence of tumors.

Inactive Publication Date: 2017-09-29
潘小平
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, even after the above treatments, the probability of distant metastasis and recurrence of the tumor remains high, making anticancer treatment one of the most challenging problems in the world

Method used

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  • Application of physcion and derivative thereof in preparation of antitumor drugs
  • Application of physcion and derivative thereof in preparation of antitumor drugs
  • Application of physcion and derivative thereof in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Example 1 Effect of Emodin Methyl Ether on Tumor Cells and Normal Cell Survival Rates

[0065] According to the above experimental method, the test results of emodin methyl ether on the survival rate of tumor cells and normal cells are shown in Table 1: Cancer, gastric cancer, oral epithelial cancer, and chronic myeloid leukemia cells all had significant inhibitory effects, and as the dose of emodin increased, the inhibitory effect on the survival rates of the above tumor cells was enhanced. The tumor suppressive effect of emodin is especially obvious in liver cancer, lung cancer and colon cancer cells. There was no significant effect on the survival rate of normal liver cells, normal bronchial epithelial cells, and normal colonic epithelial cells. From the results in Table 1, it can be seen that emodin can inhibit the activity of various tumor cells, especially effective for liver cancer, lung cancer, and colon cancer, but has no effect on the activity of normal cells...

Embodiment 2

[0069] Example 2 Effect of Emodin on Tumor Volume in Tumor-bearing Nude Mice

[0070] According to the above experimental method, the results of the effect of emodin on the tumor volume of tumor-bearing nude mice are shown in Table 2. Compared with Day0, the tumor volumes of liver cancer, lung cancer, and colon cancer on Day24 all increased significantly; Compared with the blank control group, the tumor volume of nude mice gavaged with emodin methyl ether was significantly reduced, and with the increase of gavage dose, the inhibitory effect on tumor volume was more significant. The results show that emodin can effectively inhibit the growth of tumor volume in nude mice bearing liver cancer, lung cancer and colon cancer, and has a significant inhibitory effect on tumors.

[0071] Table 2 Effect of emodin on tumor volume in tumor-bearing nude mice

[0072]

[0073] vs Day 0##p<0.01; vs Day 24 control group **p<0.01.

Embodiment 3

[0074] Example 3 Acute and subacute toxicity experiments of emodin methyl ether

[0075] 3.1 Acute toxicity test:

[0076] After intragastric administration of the test substance for one week, the survival rate of the animals was 100%, the activity, hair smoothness, diet and breathing were normal, and there were no abnormal secretions in the nose, eyes and mouth, and no obvious symptoms of poisoning were seen. One week later, the mice were dissected, and the important organs were observed with the naked eye and a microscope, and no obvious pathological changes appeared. The results of the maximum tolerated dose (MTD) test are shown in Table 3. The MTD of emodin to mice of both sexes is greater than 5.0 g / kg.bw. According to the acute toxicity grading standard, the sample is a practical non-toxic substance.

[0077] Table 3 Acute toxicity test results in mice

[0078]

[0079] 3.2 Subacute toxicity test:

[0080] During the test period, the overall growth of the animal...

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Abstract

The invention belongs to the field of medicines and particularly relates to an application of physcion and a derivative thereof in preparation of antitumor drugs. The activity of a liver cancer cell, a lung cancer cell, a breast cancer cell, a colon cancer cell, a nasopharynx cancer cell, a gastric cancer cell, a human oral epidermoid carcinoma cell and a chronic myelogenous leukemia cell can be effectively inhibited by employing a pharmaceutical composition containing the physcion and the derivative thereof as active components, and especially the pharmaceutical composition has a more significant inhibition effect on the liver cancer cell, the lung cancer cell and the colon cancer cell. The physcion and the derivative thereof have an anti-tumor effect of inhibiting transplantation tumor growth for tumor-bearing nude mice with a liver cancer, a lung cancer and a colon cancer. Furthermore, the physcion and the derivative thereof have no toxic and side effect on a normal body. A foundation is laid for development of high-efficiency and low-toxicity novel broad-spectrum anti-tumor drugs of the physcion and the derivative thereof.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of emodin methyl ether and derivatives thereof in the preparation of antitumor drugs. Background technique [0002] Rheum offcinale (Rheum offcinale Baill), Rheum palmatum L., and Rheum tanguticum Maxim.ex Balf are the dried roots and rhizomes of Polygonaceae plants. Rhubarb is cold in nature and bitter in taste. It has the functions of purging and attacking stagnation, clearing heat and purging fire, cooling blood and detoxifying, removing blood stasis and stimulating menstruation, promoting dampness and reducing jaundice. Rhubarb can also be used for excess heat stagnation, constipation, blood heat, spit at the nose, red eyes and throat, carbuncle furuncle, intestinal ulcer abdominal pain, amenorrhea due to blood stasis, postpartum stagnation, bruises, damp heat dysentery, jaundice, red urine, Lin syndrome, edema, and external treatment of burns and scalds. ...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61P35/00A61P35/02
CPCA61K31/122
Inventor 潘小平
Owner 潘小平
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