2apos; application of-O-kurarinone in preparation of medicine for treating colon cancer

Abstract

The invention discloses application of 2 '-O-kurarinone in preparation of a medicine for treating colon cancer. Belongs to the technical field of pharmaceutical chemistry. The 2 '-O-kurarinone can significantly inhibit the growth of colon cancer cells in the in-vitro cell administration concentration range of 1-256 [mu] M / mL, which proves that the 2'-O-kurarinone has the 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 2'-O-matrine in the preparation of drugs for treating cancer. Background Art

[0002] Colon cancer is one of the most common malignant tumors in the world and the second leading cause of cancer death. According to statistics from the World Health Organization (WHO), the incidence and mortality of colon cancer continue to rise, especially in Western countries and some developing countries. Since the early symptoms of colon cancer are not obvious, many patients are already in the middle and late stages when diagnosed, which increases the difficulty and challenge of treatment.

[0003] The treatment of colon cancer usually depends on the stage of cancer and the patient's health condition. Common methods include surgery, chemotherapy, radiotherapy, and targeted therapy. However, although these treatments can prolong patient survival, the effects are still limited due to the toxic side effects and drug resistance of chemotherapy drugs. Traditional chemotherapy is often accompanied by side effects such as immunosuppression and liver and kidney damage, and tumor cells may develop resistance to drugs, leading to treatment failure. Therefore, the development of new, highly effective and low-toxic drugs for the treatment of colon cancer has become an important goal of medical research.

[0004] Natural products, especially plant-derived compounds, have become a hot topic in anti-cancer research due to their diverse biological activities and relatively low toxicity. Many natural products have shown significant inhibitory effects on colon cancer cells. For example, quercetin inhibits the growth of tumor cells by regulating signaling pathways such as PI3K / Akt, MAPK, and NF-κB; curcumin slows down the proliferation of colon cancer cells and increases the sensitivity of chemotherapeutic drugs by inhibiting the NF-κB pathway; resveratrol exhibits a powerful anti-tumor effect by regulating the cell cycle, inducing tumor cell apoptosis, and enhancing immune response.

[0005] Therefore, effective compounds in natural products provide new ideas for the treatment of colon cancer, especially their low toxic side effects and multi-target anti-cancer mechanisms, making them strong candidates for drug development. Current research focuses on exploring the anti-cancer potential of natural products and screening out compounds with multi-target effects. These natural compounds can not only enrich the selection of anti-colon cancer drugs, but also provide new possibilities for overcoming the limitations of existing treatment options.

[0006] Therefore, the anti-cancer potential and relatively low toxic side effects of effective compounds in natural products make it a direction worthy of further exploration. Current research is still in the exploratory stage. Developing new natural compounds that have inhibitory effects on colon cancer, especially screening out compounds with multi-target inhibitory effects from natural products with unique chemical structures, is an important direction for future drug development.

[0007] 2'-O-matrine is a traditional Chinese medicine Sophora flavescens Aiton), there is no report on the anti-colon cancer research on the biological activity of 2'-O-matrine and its derivatives. Summary of the invention

[0008] In view of this, the present invention provides the use of 2'-O-matrine in the preparation of a drug for treating colon cancer. Through previous in vitro cell experiments, it was found that 2'-O-matrine can significantly inhibit the growth of colon cancer cells. Therefore, the 2'-O-matrine of the present invention can be used for the treatment of colon cancer.

[0009] 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 the use of 2'-O-matrine in preparing a drug for treating colon cancer. The structure of the 2'-O-matrine is shown in formula (1).

[0010] (1) 2'-O-Kurarinone, English name: 2'-O-Methylkurarinone, English alias: (2S)-7-hydroxy-2-(4-hydroxy-2-methoxyphenyl)-5-methoxy-8-[(2R)-5-methyl-2-prop-1-en-2-ylhex-4-enyl]-2,3-dihydrochromen-4-one, CAS NO.: 270249-38-2, molecular formula: C 27 H 32 O6, molecular weight: 452.54.

[0012] The present inventors provided a study on the use of 2'-O-matrine in the preparation of drugs for treating colon cancer and conducted an activity inhibition test of 2'-O-matrine on HT-29 colon cancer cells. The test results showed that 2'-O-matrine had a good inhibitory effect on HT-29 cells (see Example 1).

[0013] The second aspect of the embodiments of the present invention provides the use of 2'-O-matrine and its derivatives or pharmaceutically acceptable salts thereof in the preparation of drugs for treating colon cancer.

[0014] The use of 2'-O-matrine in the preparation of a drug for treating colon cancer, and the use of 2'-O-matrine 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.).

[0015] The present invention discovers for the first time that 2'-O-matrine can be used for the treatment of colon cancer, and provides a new use of 2'-O-matrine. BRIEF DESCRIPTION OF THE DRAWINGS

[0016] 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.

[0017] Figure 1 This is the chemical structure diagram of 2'-O-matrine.

[0018] Figure 2 IC is the half inhibitory concentration of 2'-O-matrine on colon cancer cells 50 Test result graph. DETAILED DESCRIPTION

[0019] 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 1

[0020] The inhibitory effect of 2'-O-matrine 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 2'-O-matrine were added, with gradient concentrations of 0 μM, 1 μM, 2 μM, 4 μM, 8 μM, 16 μM, 32 μM, 64 μM, 128 μM, and 256 μM. 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 The IC of 2'-O-matrine 50 Test results. The results show that the IC value of 2'-O-matrine for colon cancer cells 50 The value was 35.38 μM, which was comparable to the positive anti-colon cancer drug 5-fluorouracil (IC 50 The above shows that 2'-O-matrine has a strong inhibitory effect on the growth of colon cancer cells, that is, 2'-O-matrine can be used to prepare drugs for the treatment of colon cancer.

[0021] 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 2'-O-matrine in the preparation of a drug for treating colon cancer, characterized in that: The structure of the 2'-O-matrine 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 2'-O-matrine 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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