Composition with anti-tumor activity and application

Abstract

The invention belongs to the field of anti-tumor drugs, and particularly relates to a composition with anti-tumor activity and application. The composition with the anti-tumor activity is prepared from the following raw materials: an alcohol solvent and alum, the preparation method comprises the following steps: mixing, smashing, stirring and processing the humulus japonicus, the alcohol solvent and the alum into paste to obtain the composition with antitumor activity. The effect that the humulus japonicus is directly applied to tumor treatment is not remarkable, the composition with proper additives and shapes added into the humulus japonicus has an unexpected anti-tumor effect, and a safe, effective and low-cost treatment choice can be provided for tumor patients.

Description

Technical Field

[0001] The present invention belongs to the field of anti-tumor drugs, and in particular relates to a composition with anti-tumor activity and its application. Background Art

[0002] In recent years, with the increasing incidence of cancer, finding effective anti-tumor treatment methods with few side effects has become an important direction of medical research. With the continuous development of science and technology, anti-tumor technology has made significant progress. At present, common anti-tumor technologies mainly include chemotherapy, radiotherapy, surgical resection, targeted therapy and immunotherapy. Chemotherapy is a treatment method that kills tumor cells by using chemical drugs. Its principle is to interfere with the growth and division of tumor cells, so as to achieve the purpose of killing tumor cells. The advantage of chemotherapy is that it can kill tumor cells throughout the body and has a good effect on tumors that have metastasized. However, its disadvantage is that the side effects are large and may cause damage to normal cells, causing patients to experience nausea, vomiting, hair loss and other adverse reactions. Radiotherapy is a treatment method that uses radiation to irradiate the tumor site and kill tumor cells by destroying the DNA molecular structure of tumor cells. Its advantage is that it can accurately irradiate the tumor site and cause less damage to the surrounding normal tissues. However, radiotherapy may cause certain damage to normal cells and has limited efficacy for some deep tumors or tumors that have metastasized. Surgical resection is a treatment method that removes tumor tissue from the patient's body through surgery. Its advantage is that it can quickly remove tumor tissue and has a good effect on early tumors. However, surgical resection has a high risk for some deep tumors or tumors that have already metastasized, and may cause certain trauma to the patient. Targeted therapy is a method of treatment that targets specific molecular targets of tumor cells. Its technical advantage is that it can specifically kill tumor cells, cause less damage to normal cells, and has fewer side effects. However, targeted therapy may not be effective for some tumors that do not have specific molecular targets. Immunotherapy is a treatment method that fights tumors by activating or enhancing the patient's own immune system. Its advantage is that it can specifically identify and kill tumor cells, cause less damage to normal cells, and has fewer side effects. However, immunotherapy is not effective for some patients with weak immune systems.

[0003] In summary, anti-tumor technology has made significant progress in the treatment of tumors, but various treatment methods have their significant disadvantages. In comparison, traditional Chinese medicine has gradually attracted attention due to its unique efficacy and low side effects. Traditional Chinese medicine has a long history and rich experience in anti-tumor, and many Chinese herbal medicines have been proven to have anti-tumor activity.

[0004] Humulus japonicus, scientific name Humulus japonicus Sieb.et Zucc., is a perennial herbaceous plant of the genus Humulus in the Moraceae family. It was first recorded in the "Tang Materia Medica". It is cold in nature, sweet and bitter in taste, and belongs to the lung and kidney meridians. It has the effects of clearing heat, detoxification and diuresis. Humulus japonicus is recorded in many ancient prescriptions, such as the following: ① "Compendium of Materia Medica": "Treatment of fever and fever after sweating due to typhoid fever, grind and grind, take one cup of raw juice to drink." ② "Anhui Medicinal Materials": "Treat insomnia; wash hemorrhoids." [Usage and Dosage] Oral administration: decoction, 3 to 6 qian (2 to 4 liang for fresh); or mash juice. External use: mash and apply or decoct water for fumigation and washing. ③ "Compendium of Materia Medica": Treatment of chrysanthemum: mash three liters of raw juice of Humulus japonicus, two cups of vinegar. Mix them together, take them on an empty stomach, and it should be like white juice when you urinate; ④ Jiangxi "Herbal Manual": Treatment of sand and stone stranguria: four to five liang of fresh Humulus japonicus stems. Mash it, add boiling water to make juice and drink it; ⑤ "Compendium of Materia Medica": Treat new and long-term malaria: one handful of Kudzu vine (remove both ends, for autumn and winter use) and Hengshan powder in equal parts. Soak the medicine in two large cups of light starch water, let it sit overnight under the stars and moon, boil one cup at five o'clock in the morning, and take it in divided doses, and it will heal by spitting out phlegm.

[0005] Modern pharmacological studies have shown that Humulus japonicus extracts contain polysaccharides, flavonoids, terpenes and other active ingredients, which have anti-tumor, antioxidant, anti-inflammatory and other biological activities. Zhou Tingting et al. (Zhou Tingting, Zou Xiang, Ji Yubin. Study on the anti-tumor and anti-angiogenesis effects of tetrahydroisohumulone on S180 tumor-bearing mice [J]. Chinese Herbal Medicine, 2009, 40 (S1): 218-220.) Studies have shown that tetrahydroisohumulone extracted from Humulus japonicus can inhibit S 180 The growth of solid tumors in tumor-bearing mice can be inhibited, and the formation of microvessels in tumor tissues can be inhibited. Ji Yubin (Ji Yubin. Study on the effect of humulone on the activity of NAT1 enzyme in tumor cells [C] / / Collection of papers from the 3rd Academic Conference of the Professional Committee of Applied Pharmacology of the Chinese Pharmaceutical Society, the 13th Academic Conference of the Professional Committee of Pharmaceutical Industry of the Chinese Pharmacological Society and the 2008 Biomedical Academic Forum. Harbin: Professional Committee of Applied Pharmacology of the Chinese Pharmacological Society, Professional Committee of Pharmaceutical Industry of the Chinese Pharmacological Society, 2008: 149-155.) proved through cell experiments that humulone extracted from humulone can inhibit the activity of NAT1 enzyme in human gastric cancer cells and human liver cancer cells, which may be one of the mechanisms for its cytotoxicity. Zhou He (Zhou He. Effects of tetrahydroisohumulone on apoptosis-related proteins in the mitochondrial pathway of human hepatoma cell HepG-2 [C] / / Special issue of the 10th National Academic Conference of the Chinese Pharmacological Society. Tianjin: Chinese Pharmacological Society, 2009: 184.) found that tetrahydroisohumulone can induce apoptosis of human hepatoma cells by upregulating the expression of cytochrome c, Bax and Caspase-3 proteins and inhibiting the expression of Bcl-2 protein. At present, although it has been found that there are certain anti-tumor active ingredients in Humulus japonicus, the effect of Humulus japonicus directly applied to treat tumors is not significant. Summary of the invention

[0006] The purpose of the present invention is to overcome the shortcomings and deficiencies of the prior art and to provide a composition with anti-tumor activity and its application.

[0007] The first aspect of the present invention provides a composition having anti-tumor activity, the raw materials of which include, an alcohol solvent, and alum;

[0008] The preparation method comprises the following steps: the humulus, alcohol solvent and alum are mixed, crushed, stirred and prepared into a paste to obtain a composition with anti-tumor activity.

[0009] The Humulus chinensis used in the present invention is fresh Humulus chinensis, and the above-ground stem and leaf parts of the Humulus chinensis are collected and directly prepared.

[0010] The alcohol solvent of the present invention refers to alcohol solvents such as ethanol and propylene glycol that are permitted for use in pharmacy.

[0011] The mass ratio of Humulus truncatus, alcohol solvent and alum is 500:0.05-1:0.5-1.5. The above mass ratio range can achieve better results through experiments.

[0012] The second aspect of the present invention provides use of the above-mentioned composition with anti-tumor activity in preparing anti-tumor drugs.

[0013] The anti-tumor drug has any of the following preparation forms: injection, tablet, capsule, aerosol, suppository, film, pellet, ointment, controlled release or sustained release and nano preparation, and is used for cavity administration, external use, oral administration or injection.

[0014] The effect of Humulus japonicus directly applied to treat tumors is not significant. The present invention has an unexpected anti-tumor effect by adding appropriate additives to Humulus japonicus, and can provide a safe, effective and low-cost treatment option for tumor patients. BRIEF DESCRIPTION OF THE DRAWINGS

[0015] 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 some embodiments of the present invention. For ordinary technicians in this field, without paying creative labor, other drawings obtained based on these drawings still belong to the scope of the present invention.

[0016] Figure 1 The experimental results of oral administration + application group of 7721 liver cancer cells;

[0017] Figure 2 These are the experimental results of the oral administration + application group of B16F10 melanoma cells;

[0018] Figure 3The experimental results of HepG2 liver cancer cell oral administration + application group;

[0019] Figure 4 The experimental results of the HepG2 liver cancer cell smear group;

[0020] Figure 5 The experimental results of the oral administration group of HepG2 liver cancer cells;

[0021] Figure 6 The experimental results of oral administration + application group of 4T1 breast cancer cells;

[0022] Figure 7 This is the section result of mouse lung organ;

[0023] Figure 8 This is the result of the section of mouse liver organ;

[0024] Fig. 9 This is the section result of mouse spleen organ;

[0025] Fig.10 This is the section result of mouse kidney organ;

[0026] Fig.11 This is the section result of mouse heart organ;

[0027] Fig.12 This is the section result of mouse tumor;

[0028] Fig.13 This is the immunohistochemistry result of mouse tumor Tunel;

[0029] Fig.14 For the medication process. DETAILED DESCRIPTION

[0030] In order to make the objectives, technical solutions and advantages of the present invention more clear, the present invention will be further described in detail below with reference to the accompanying drawings.

[0031] Example 1 Preparation of anti-tumor active composition:

[0032] Take 500 g of Humulus japonicus, 1 mg of propylene glycol, and 1 g of alum, mix, crush, stir and make into a paste to obtain a composition.

[0033] Example 2 Acute toxicity test:

[0034] According to the national standard (GB15193.3-2014), the composition prepared in Example 1 was dissolved in distilled water and formulated into 300 mg / ml. The mice were divided into three groups, each with 10 mice (half male and half female), and were orally administered with 100 mg / Kg, 1000 mg / Kg and 10000 mg / Kg (2 mg / mouse, 20 mg / mouse, 200 mg / mouse). After 4 hours of administration, there were no dead mice in the three doses of the oral group. The mice were observed for one week and were normal. Another group of mice was given a peritoneal dose of 1000 mg / Kg. After one week of observation, the mice were normal.

[0035] Example 3 Safety Evaluation:

[0036] The blood test was performed on the mice of Example 2. The oral group was tested at the maximum dose (10000 mg / Kg). The test results are shown in Table 1, which can illustrate the composition prepared in Example 1.

[0037] Table 1 Mouse blood test results

[0038]

[0039] Example 4 Antitumor Test:

[0040] Experimental method: 7721 liver cancer cells, HepG2 liver cancer cells, B16F10 melanoma cells, and 4T1 breast cancer cells were selected as solid tumors. Balb / c white mice and Balb / c nude mice were selected for tumor bearing. Each animal was loaded with 500,000 to 1,000,000 tumor cells. The solid tumors grew to about 50-60 mm. 3 The drug was administered orally, externally, or in combination with external application. The dosage was administered orally according to the acute toxicity dose. The tumor volume and animal weight were measured during the administration period, and the drug was administered for 3 weeks.

[0041] Figure 1-Figure 6 The results of the anti-tumor effect experiment are as follows: Figure 7-Figure 13 The experimental results are from mouse organ slices, and show that the Chinese medicine ointment used in the present invention has a significant inhibitory effect on 7721 liver cancer cells, HepG2 liver cancer cells, B16F10 melanoma cells, and 4T1 breast cancer cells, and the number of tumor cells is significantly reduced, with a significant anti-tumor effect.

[0042] The above disclosure is only the preferred embodiment of the present invention, which certainly cannot be used to limit the scope of the present invention. Therefore, equivalent changes made according to the claims of the present invention are still within the scope of the present invention.

Claims

1. A composition having anti-tumor activity, characterized in that: Its raw materials include Humulus chinensis, alcohol solvent, and alum; The preparation method comprises the following steps: the humulus, alcohol solvent and alum are mixed, crushed, stirred and prepared into a paste to obtain a composition with anti-tumor activity.

2. The composition with anti-tumor activity according to claim 1, characterized in that: The mass ratio of the humulus, alcohol solvent and alum is 500:0.05-1:0.5-1.

5.

3. Use of the composition with anti-tumor activity as claimed in claim 1 or 2 in preparing anti-tumor drugs.

4. The use according to claim 3, characterized in that: The anti-tumor drug has any of the following preparation forms: injection, tablet, capsule, aerosol, suppository, film, pellet, ointment, controlled release or sustained release and nano preparation, and is used for cavity administration, external use, oral administration or injection.

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