阅读说明：本技术 槐花散提取物及其制备和应用 (Sophora japonica powder extract and preparation and application thereof ) 是由 禹志领 符秀琼 李俊葵 于 2019-09-19 设计创作，主要内容包括：本发明提供一种槐花散提取物及其制备和应用。该制备方法包括如下步骤：(1)秤取槐花散,粉碎后用乙醇水溶液提取,过滤,得醇提液；所述槐花散包含有槐花和栀子；(2)除去所述醇提液中的乙醇并将所得产物通过大孔树脂,再用乙醇水溶液洗脱大孔树脂,收集洗脱液；(3)除去所述洗脱液中的乙醇,浓缩,干燥。本发明制备得到槐花散提取物,该槐花散提取物具有抗肿瘤的作用,能够有效地抑制肿瘤细胞的增殖、明显抑制肿瘤生长。同时,本发明的槐花散提取物还对正常细胞毒性低,在一种机体肿瘤生长的同时不影响机体的生长。(The invention provides a sophora japonica powder extract and preparation and application thereof. The preparation method comprises the following steps: (1) weighing flos Sophorae Immaturus powder, pulverizing, extracting with ethanol water solution, and filtering to obtain ethanol extractive solution; the flos Sophorae Immaturus powder contains flos Sophorae Immaturus and fructus Gardeniae; (2) removing ethanol in the ethanol extract, passing the obtained product through macroporous resin, eluting the macroporous resin with ethanol water solution, and collecting the eluate; (3) removing ethanol from the eluate, concentrating, and drying. The sophora japonica powder extract prepared by the invention has an anti-tumor effect, can effectively inhibit the proliferation of tumor cells and obviously inhibit the growth of tumors. Meanwhile, the sophora japonica powder extract has low toxicity to normal cells, and does not influence the growth of an organism while the growth of an organism tumor.)

1. The preparation method of the sophora japonica powder extract is characterized by comprising the following steps of:

(1) Weighing flos Sophorae Immaturus powder, pulverizing, extracting with ethanol water solution, and filtering to obtain ethanol extractive solution; the flos Sophorae Immaturus powder contains flos Sophorae Immaturus and fructus Gardeniae;

(2) Removing ethanol in the ethanol extract, adsorbing with macroporous resin, and eluting with ethanol water solution after adsorption.

2. the preparation method of the sophora japonica powder extract according to claim 1, wherein the weight ratio of sophora japonica to gardenia jasminoides in the sophora japonica powder is 1: (0.1-10).

3. The preparation method of the sophora japonica powder extract according to claim 1 or 2, wherein in the step (1) and/or the step (2), the volume percentage of ethanol in the ethanol aqueous solution is not higher than 95%; or/and the weight of the ethanol water solution is 5-15 times of that of the sophora japonica powder; or/and the extraction method adopts ultrasonic extraction; or/and the extraction times are at least 2 times, and each time lasts for 1-4 h; or/and the macroporous resin is D101 macroporous resin.

4. The method for preparing the sophora japonica powder extract according to claim 3, wherein the volume percentage of the ethanol in the ethanol aqueous solution is 30-95%.

5. The preparation method of the sophora japonica powder extract according to claim 1 or 2, wherein the ethanol in the eluent obtained in the step (2) is removed, and the obtained product is concentrated and dried.

6. Sophora flower powder extract obtained by the preparation method according to any one of claims 1 to 5.

7. The use of the sophora flower powder extract of claim 6 in the preparation of antitumor drugs.

8. The use of claim 7, wherein the neoplasm is melanoma, cancer of the large intestine, breast, leukemia, prostate, nasopharynx, lung, liver, esophagus, stomach, kidney, lymph, mouth, ovary, cervix, bladder, or thyroid.

9. an antitumor drug, which is characterized by comprising the sophora japonica powder extract of claim 6 and pharmaceutically acceptable auxiliary materials.

10. The antitumor agent as claimed in claim 9, wherein the agent is in the form of tablet, capsule, granule, oral liquid or paste.

Technical Field

The invention belongs to the field of medicines, and particularly relates to a sophora japonica powder extract, and preparation and application thereof.

Background

Tumors are diseases that seriously threaten human health. In 2019, 1 month, the latest national cancer statistical data released by the national cancer center indicate that the incidence and mortality of malignant tumors are in a continuously rising state in recent decades, and the medical cost caused by the malignant tumors exceeds 2,200 billion every year. The existing medicines for treating tumors are expensive and have large toxic and side effects. Therefore, the search for new effective, safe and low-cost antitumor drugs is urgently needed.

The traditional Chinese medicine has important significance in preventing and treating tumors, and most of the traditional Chinese medicines are low in price. The traditional Chinese medicine can be used for directly treating or preventing tumors, and can be matched with radiotherapy, chemotherapy and the like to play a synergistic effect. In addition, the traditional Chinese medicine treatment can also relieve the toxic and side effects of radiotherapy and chemotherapy, improve the life quality of patients, and can be taken by patients with advanced tumors to prolong the life.

The sophora flower powder is composed of sophora flower and gardenia, is recorded in experience proved recipe for the earliest time, and is recorded in experience proved recipe (quoted from Puji's prescription): 'Huai Hua san' treats toxin, alcohol disease and hematochezia. Flos Sophorae Immaturus (half raw and half fried), fructus Gardeniae (peeled and fried) and fructus Gardeniae (peeled and fried) are in powder form, and are administered before taking after being mixed with fresh water for every dose of two coins. The product has effects of clearing intestine and stopping bleeding, and can be used for treating toxin, alcoholism, and hematochezia. In ancient literature, a compound with different drug compositions is also described as sophora japonica powder.

Sophora japonica, recorded in Rihuazi Ben Cao (Rihuazi materia Medica), is the dried flower bud and flower of Sophora japonica L. Alias: sophora japonica, sophora flower bud and sophora flower seed (the flower and bud of sophora flower are used in the same way in traditional Chinese medicine). The functional indications are as follows: cool blood to stop bleeding, clear liver heat and purge fire. Can be used for treating hematochezia, hemorrhoidal bleeding, bloody dysentery, metrorrhagia, hematemesis, epistaxis, liver heat with conjunctival congestion, headache, and vertigo. Modern pharmacological research shows that the sophora japonica has the following pharmacological actions: (1) anti-inflammatory effects; (2) antiviral and antifungal effects; (3) the anti-tumor effect is as follows: researches find that the quercetin contained in the sophora flower has an anti-tumor effect; (4) effect on cardiovascular system: flos Sophorae Immaturus has effects of lowering blood pressure and dilating coronary; (5) blood fat reducing effect: rutin, the main component of flos Sophorae Immaturus, has fat removing effect on liver infiltrated with fat.

Gardenia (academic name: Gardenia jasminoides Ellis), also known as Gardenia jasminoides Ellis: gardenia jasminoides Ellis, Gardenia jasminoides Ellis and Cinobufagin are fruits of Gardenia jasminoides Ellis of Rubiaceae. It is first recorded in Shen nong Ben Cao Jing, Shang Han Lun, Min Dong Ben Cao, Pu Ji Fang and Sheng Ji Zong Lu. Gardenia is bitter and cold in nature, has the effects of purging fire, relieving restlessness, clearing heat, promoting diuresis, cooling blood and removing toxic substances, and is mainly used for treating fever, vexation, damp-heat jaundice, stranguria, blood heat, hematemesis, epistaxis, conjunctival congestion, swelling and pain, fire toxin, pyocutaneous disease, trauma, sprain, contusion and pain. Gardenia jasminoides is mainly produced in Zhejiang Pingyang, Wenling mountains, Hunan quan, Liuyang, Jiangxi Yongfeng, Pingxiang and the like, and also produced in Shandong, Henan, Jiangsu and Anhui and the like. The fruit of gardenia is a traditional Chinese medicine, belongs to the first medical and edible dual-purpose resource issued by the Ministry of health, and has the functions of protecting liver, promoting bile flow, reducing blood pressure, tranquilizing, stopping bleeding, reducing swelling and the like. Clear heat, purge fire, cool blood. It is used to treat febrile diseases, vexation, insomnia, jaundice, gonorrhea, diabetes, conjunctival congestion, pharyngalgia, hematemesis, epistaxis, dysentery with blood, hematuria, pyocutaneous disease due to heat toxin, sprain, and swelling and pain. Modern pharmacological research shows that cape jasmine has certain activity in protecting liver, benefiting gallbladder, lowering blood sugar, promoting pancreas secretion, protecting stomach function, lowering blood pressure, regulating fat, protecting nerve, resisting inflammation, resisting oxidation, resisting fatigue, resisting thrombus, etc.

modern clinical research shows that the compound containing the sophora flower powder has better curative effects on gastrointestinal hemorrhage, enteritis, allergic purpura, psoriasis and the like. So far, no research report on the anti-tumor effect of the sophora japonica powder is found.

Disclosure of Invention

based on the above, the main objective of the present invention is to provide a preparation method of sophora japonica powder extract, wherein the obtained sophora japonica powder extract has an anti-tumor effect, and can effectively inhibit proliferation of tumor cells and significantly inhibit tumor growth.

The purpose of the invention is realized by the following technical scheme:

The invention mainly aims to provide a preparation method of a sophora japonica powder extract, which comprises the following steps:

(1) Weighing flos Sophorae Immaturus powder, pulverizing, extracting with ethanol water solution, and filtering to obtain ethanol extractive solution; the flos Sophorae Immaturus powder contains flos Sophorae Immaturus and fructus Gardeniae;

(2) Removing ethanol in the ethanol extract, passing the obtained product through macroporous resin, eluting the macroporous resin with ethanol water solution, and collecting the eluate.

In one embodiment, the weight ratio of sophora japonica to gardenia in the sophora japonica powder is 1: (0.1-10).

In one embodiment, the sophora japonica powder consists of sophora japonica and gardenia.

In one embodiment, the ethanol in the ethanol aqueous solution has a volume percentage of ethanol of not higher than 95%; or/and the weight of the ethanol water solution is 5-15 times of that of the sophora japonica powder; or/and the extraction method adopts ultrasonic extraction; or/and the extraction times are at least 2 times, and each time lasts for 1-4 h; or/and the macroporous resin is D101 macroporous resin.

In one embodiment, the ethanol in the ethanol aqueous solution has a volume percentage of 30-95%.

In one embodiment, the preparation method further removes ethanol in the eluent obtained in the step (2) and concentrates and dries the obtained product.

The invention also aims to provide the sophora flower powder extract obtained by the preparation method.

the invention also aims to provide the application of the sophora flower powder extract in preparing antitumor drugs.

In one embodiment, the tumor is melanoma, carcinoma of large intestine, breast cancer, leukemia, prostate cancer, nasopharyngeal cancer, lung cancer, liver cancer, esophageal cancer, gastric cancer, renal cancer, lymphoma, oral cancer, ovarian cancer, cervical cancer, bladder cancer, or thyroid cancer.

In one embodiment, the tumor is melanoma or colon cancer.

the invention also aims to provide an anti-tumor medicament which comprises the sophora flower powder extract and pharmaceutically acceptable auxiliary materials.

In one embodiment, the medicament is a tablet, capsule, granule, oral liquid or paste.

Compared with the prior art, the invention has the following beneficial effects:

The sophora japonica powder extract prepared by the invention has an anti-tumor effect, can effectively inhibit the proliferation of tumor cells and obviously inhibit the growth of tumors. Meanwhile, the sophora japonica powder extract has low toxicity to normal cells, and does not influence the growth of an organism while the growth of an organism tumor.

Drawings

FIG. 1 Effect of Sophora flower powder extract on mouse melanoma cell proliferation;

FIG. 2 effect of the sophora flower powder extract on proliferation of human melanoma cells;

FIG. 3 effect of the sophora japonica powder extract on proliferation of human colorectal cancer cells;

FIG. 4 Effect of Sophora flower powder extract on proliferation of human normal colon epithelial cells;

FIG. 5 Effect of Sophora flower powder extract on apoptosis of human melanoma cells;

FIG. 6 shows the effect of the Sophora japonica powder extract on apoptosis of human colorectal cancer cells;

FIG. 7 Effect of the sophora flower powder extract on tumor growth of melanoma tumor-bearing mice;

FIG. 8 shows the effect of the sophora japonica powder extract on the growth of tumor in nude mice bearing tumor of human colorectal cancer.

Detailed Description

In order that the invention may be more fully understood, reference will now be made to the following description. This invention may, however, be embodied in many different forms and should not be construed as limited to the embodiments set forth herein. Rather, these embodiments are provided so that this disclosure will be thorough and complete.

Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. The terminology used in the description of the invention herein is for the purpose of describing particular embodiments only and is not intended to be limiting of the invention. As used herein, the term "and/or" includes any and all combinations of one or more of the associated listed items.

The embodiment provides a preparation method of a sophora japonica powder extract, which comprises the following steps:

(1) Weighing flos Sophorae Immaturus powder, pulverizing, extracting with ethanol water solution, and filtering to obtain ethanol extractive solution; the flos Sophorae Immaturus powder contains flos Sophorae Immaturus and fructus Gardeniae;

(2) Removing ethanol in the ethanol extract, passing the obtained product through macroporous resin, eluting the macroporous resin with ethanol water solution, and collecting the eluate.

In one embodiment, in the step (1) and the step (2), the ethanol content of the ethanol aqueous solution is not higher than 95% by volume. In order to better extract the anticancer components in the sophora japonica powder, the volume percentage of the ethanol in the ethanol aqueous solution is further preferably 30-95%, for example, in a preferred embodiment, the volume percentage of the ethanol is 70%.

In one embodiment, in the step (1), the weight of the ethanol aqueous solution is 5-15 times of that of the sophora japonica powder. Preferably 10 times.

In one embodiment, in step (1), the method of extraction employs ultrasonic extraction.

In one embodiment, in step (1), the number of times of extraction is at least 2, each time for 1-4 h. The weight of the ethanol water solution is 5-15 times of that of the flos Sophorae powder. Preferably 10 times.

in one embodiment, the sophora japonica powder consists of sophora japonica and gardenia.

In one embodiment, the weight ratio of sophora flower to gardenia is 1: (0.1-10). Preferably, it is 1: 0.8-1.2. More preferably 1: 1.

in one embodiment, the preparation method further removes ethanol in the eluent obtained in the step (2) and concentrates and dries the obtained product. In one embodiment, the concentration is to concentrate the ethanol-removed eluate into an extract, and the drying is to dry the extract until no solvent remains.

This example provides a sophora japonica powder extract obtained by the above-mentioned preparation method.

The embodiment provides an application of the sophora flower powder extract in preparing an anti-tumor medicament.

In one embodiment, the tumor includes melanoma, carcinoma of large intestine, breast cancer, leukemia, prostate cancer, nasopharyngeal cancer, lung cancer, liver cancer, esophageal cancer, gastric cancer, renal cancer, lymph cancer, oral cancer, ovarian cancer, cervical cancer, bladder cancer, thyroid cancer, and other tumors, and tumor resistant to radiotherapy and chemotherapy drugs. The kind of tumor is not limited by the above examples.

In one embodiment, the tumor comprises melanoma, colon cancer.

An anti-tumor medicine comprises the sophora flower powder extract and pharmaceutically acceptable auxiliary materials.

Adjuvants such as pharmaceutical carriers, adjuvants, etc., as described in this example.

In one embodiment, the medicament is any one dosage form of tablets, capsules, granules, oral liquid, paste and the like. The medicaments in various dosage forms can be prepared according to the conventional method in the pharmaceutical field. The present invention is not limited by the above listed dosage forms.

The anti-tumor drug described in this embodiment includes a tumor prevention drug and a tumor treatment drug, and may also be an auxiliary drug of an anti-tumor drug. The antitumor adjuvant can be used for adjuvant radiotherapy or other antitumor chemotherapeutic drugs, targeting preparation, immunotherapy, biotherapy, etc. for treating cancer.