Application of kushenol I in preparation of medicine for treating colon cancer

Abstract

The invention discloses application of kushenol I in preparation of a medicine for treating colon cancer. Belongs to the technical field of pharmaceutical chemistry. In the concentration range of 1-256 [mu] M / mL given to in-vitro cells, the kushenol I can significantly inhibit the growth of colon cancer cells, which proves that the kushenol I has an anti-cancer effect and can be used for treating colon cancer.

Description

Technical Field

[0001] The invention belongs to the technical field of pharmaceutical chemistry, and specifically relates to the application of matrine I in preparing drugs for treating cancer. Background Art

[0003] The treatment of colon cancer is usually based on the stage of cancer and the patient's overall health status. The main treatment methods include surgical resection, radiotherapy and chemotherapy. In terms of drug treatment, the drugs widely used in clinical practice can be divided into chemotherapy drugs, such as fluorouracil (5-FU), oxaliplatin (Oxaliplatin) and capecitabine (Capecitabine), etc.; targeted therapy drugs, such as EGFR drugs (such as cetuximab) and anti-VEGF drugs (such as bevacizumab), etc. These drugs inhibit tumor growth and metastasis by specifically targeting specific molecules in cancer cells, and have become an important part of the treatment of colon cancer. There are also immunotherapy. Although existing chemotherapy and targeted therapy drugs have improved the survival rate of patients to a certain extent, there are still many problems, including drug resistance, serious side effects and high treatment costs. Therefore, it is particularly important to find new colon cancer treatment drugs from natural products.

[0004] At present, many studies have shown the potential of natural products in the treatment of colon cancer. For example, flavonoid compounds such as quercetin and catechins have shown the effects of inhibiting colon cancer cell proliferation and inducing apoptosis; curcumin and allicin have been proven to inhibit the growth and metastasis of colon cancer cells. Therefore, searching for colon cancer therapeutic drugs from natural products can not only enrich the selection of anti-colon cancer drugs and improve the treatment effect, but also provide new ideas for overcoming the limitations of existing treatment options.

[0005] Matrine I is a traditional Chinese medicine Sophora flavescens ( Sophora flavescens Aiton), and so far, no research on the biological activity of matrine I and its derivatives has been reported in the anti-colon cancer aspect. Summary of the invention

[0006] In view of this, the present invention provides the use of matrine I in the preparation of a drug for treating colon cancer. Through previous in vitro cell experiments, it was found that matrine I can significantly inhibit the growth of colon cancer cells. Therefore, the matrine I of the present invention can be used for the treatment of colon cancer.

[0007] In order to achieve the above object, the present invention adopts the following technical solution: In one aspect, an embodiment of the present invention provides a use of matrine I in preparing a drug for treating colon cancer, wherein the structure of matrine I is shown in formula (1).

[0008] (1) Kushenol I, English name Kushenol I, English alias (2R,3R)-2-(2,4-dihydroxyphenyl)-3,7-dihydroxy-8-hydroxy-5-methyl-2-(prop-1-en-2-yl)hexyl]-5-methoxy-2,3-dihydro-4H-chromen-4-one, CAS number 99119-69-4, molecular formula C 26 H 30 O7, molecular weight is 454.51.

[0010] The present inventors provided a study on the use of matrine I in the preparation of drugs for treating colon cancer and carried out an activity inhibition test of matrine I on HT-29 colon cancer cells. The test results showed that matrine I had a good inhibitory effect on HT-29 cells (see Example 1).

[0011] The second aspect of the embodiments of the present invention provides the use of matrine I and its derivatives or pharmaceutically acceptable salts thereof in the preparation of drugs for treating colon cancer.

[0012] The use of matrine I in the preparation of a drug for treating colon cancer, and the use of matrine I and its derivatives or pharmaceutically acceptable salts thereof in the preparation of a drug for treating colon cancer, in addition to the drug, also include pharmaceutically acceptable excipients. The excipients include conventional diluents (such as water for injection, microcrystalline cellulose, etc.), fillers (such as mannitol, sucrose, lactose, polyethylene glycol, Tween 80, sorbitol, menthol, liquid paraffin, vaseline, stearic acid, glyceryl monostearate, lanolin, mineral oil, DMSO, etc.), binders (such as carbomer, gum arabic, starch, cellulose, gelatin, polyvinyl pyrrolidone, polyacrylamide, etc.), disintegrants (such as sodium carboxymethyl starch, cross-linked sodium carboxymethyl cellulose, hydroxypropyl methylcellulose, low-substituted hydroxypropyl cellulose, etc.), lubricants (such as talc, hard At least one of magnesium stearate, calcium stearate, solid polyethylene glycol, lecithin, silicon dioxide, micro-powdered silica gel, etc.), a wetting agent (such as at least one of propylene glycol, glycerol, ethanol, etc.), a stabilizer (such as at least one of disodium ethylenediaminetetraacetic acid, sodium thiosulfate, sodium metabisulfite, sodium sulfite, sodium bisulfite, ethanolamine, sodium bicarbonate, sodium acetate, niacinamide, vitamin C, etc.), an osmotic pressure regulator (such as at least one of sodium chloride, glucose, etc.), a pH regulator (such as at least one of triethanolamine, sodium hydroxide, sodium citrate, etc.), a preservative (such as at least one of chlorobutanol, parabens, ethylparaben, benzalkonium bromide, etc.).

[0013] The present invention discovers for the first time that matrine I can be used for the treatment of colon cancer, and provides a new use of matrine I. BRIEF DESCRIPTION OF THE DRAWINGS

[0014] In order to more clearly illustrate the embodiments of the present invention or the technical solutions in the prior art, the drawings required for use in the embodiments or the description of the prior art will be briefly introduced below. Obviously, the drawings described below are only embodiments of the present invention. For ordinary technicians in this field, other drawings can be obtained based on the provided drawings without paying creative work.

[0015] Figure 1 This is the chemical structure diagram of matrine I.

[0016] Figure 2 IC is the half inhibitory concentration of matrine I on colon cancer cells 50 Test result graph. DETAILED DESCRIPTION

[0017] The present invention is described in detail below in conjunction with the accompanying drawings and specific examples, but should not be construed as limiting the present invention. Unless otherwise specified, the technical means used in the following examples are conventional means well known to those skilled in the art, and the materials, reagents, etc. used in the following examples, unless otherwise specified, can be obtained from commercial sources. Example

[0018] Inhibitory effect of matrine I on HT-29 cells (IC 50 ). HT-29 tumor cells in the logarithmic growth phase were counted and prepared into a cell suspension with a concentration of 6×10 4 cells / mL. 100 μL was added to a 96-well plate and cultured overnight in a 37°C, 5% CO2 cell culture incubator. After the cells adhered to the wall, different concentrations of matrine I were added, with gradient concentrations of 0 μM, 1 μM, 2 μM, 4 μM, 8 μM, 16 μM, 32 μM, 64 μM, 128 μM, 256 μM, etc. Three replicates were set for each group, and the drug solvent was used as the control group. After 48 h of culture, 10 μL of CCK-8 working solution was added, and the cells were incubated in the cell culture incubator for another 3 h. The OD value was detected at 450 nm and calculated. Figure 2 IC of matrine I 50 Test result diagram. The results show that the IC of matrine I to colon cancer cells 50 The value was 77.25 μM, which was comparable to the positive anti-colon cancer drug 5-fluorouracil (IC 50 The above shows that matrine I has a strong inhibitory effect on the growth of colon cancer cells, that is, matrine I can be used to prepare drugs for the treatment of colon cancer.

[0019] The above description is only a preferred specific implementation manner of the present invention, but the protection scope of the present invention is not limited thereto. Any technician familiar with the technical field can make equivalent replacements or changes according to the technical scheme and inventive concept of the present invention within the technical scope disclosed by the present invention, which should be covered by the protection scope of the present invention.

Claims

1. The use of matrine I for preparing a drug for treating colon cancer, characterized in that: The structure of the matrine I is: 。 2. The use according to claim 1, characterized in that: The drug also includes pharmaceutically acceptable excipients.

3. A drug for treating colon cancer, characterized in that: The medicine includes matrine I and its derivatives or pharmaceutically acceptable salts thereof.

4. The drug according to claim 3, characterized in that The drug also includes pharmaceutically acceptable excipients.

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