阅读说明：本技术 一种用于治疗胃溃疡的中药及其应用 (Traditional Chinese medicine for treating gastric ulcer and application thereof ) 是由 杨晓艳 邹玉林 崔秀明 向巧 曲媛 杨野 王承潇 于 2020-12-09 设计创作，主要内容包括：本发明提供一种用于治疗胃溃疡的中药及其应用。其中,该中药的有效成分为酱头提取物。酱头提取物的提取方法包括：将酱头用打粉机粉碎,过筛,粉末加入溶剂进行提取,过滤后收集提取液,继续加入溶剂,提取2-3次,合并提取液,使用旋转蒸发仪浓缩至浸膏；将浸膏加水溶解混匀,加入乙酸乙酯进行萃取,萃取2-3次,合并萃取液,旋转蒸发仪蒸干至浸膏,得到酱头提取物。所述酱头提取物中含有15.0-22.5％的总酚成分,本发明还公开了酱头提取物对乙醇致大鼠胃粘膜损伤的修复作用。本发明提供的中药对治疗胃溃疡具有显著作用。(The invention provides a traditional Chinese medicine for treating gastric ulcer and application thereof. Wherein the effective component of the traditional Chinese medicine is a sauce head extract. The extraction method of the Maotai extract comprises the following steps: pulverizing sauce head with a pulverizer, sieving, extracting the powder with solvent, filtering, collecting extractive solution, adding solvent, extracting for 2-3 times, mixing extractive solutions, and concentrating to obtain extract with rotary evaporator; dissolving the extract in water, mixing, adding ethyl acetate, extracting for 2-3 times, mixing extractive solutions, evaporating to dryness with rotary evaporator to obtain extract. The Maotai extract contains 15.0-22.5% of total phenol components, and the invention also discloses a repairing effect of the Maotai extract on the damage of the gastric mucosa of a rat caused by ethanol. The traditional Chinese medicine provided by the invention has a remarkable effect on treating gastric ulcer.)

1. A traditional Chinese medicine for treating gastric ulcer is characterized in that the effective components of the traditional Chinese medicine comprise a sauce head extract.

2. The traditional Chinese medicine for treating gastric ulcer is characterized in that the extraction method of the Maotai extract comprises the following steps: pulverizing sauce head with a pulverizer, sieving, extracting the powder with solvent, filtering, collecting extractive solution, adding solvent, extracting for 2-3 times, mixing extractive solutions, and concentrating to obtain extract with rotary evaporator.

Dissolving the extract in water, mixing, adding ethyl acetate, extracting for 2-3 times, mixing extractive solutions, and evaporating to obtain extract.

3. The traditional Chinese medicine according to claim 2, wherein the mass ratio of the Maotai powder to the solvent is 1:5-1: 10; the solvent is 80-95% ethanol water solution by volume percentage.

4. The traditional Chinese medicine according to claim 2, wherein the extraction is performed by any one of leaching, reflux extraction or ultrasonic extraction.

5. The traditional Chinese medicine according to claim 2, wherein the temperature of the rotary evaporator is 50 ℃ and the pressure is 0.05-0.08 MPa.

6. The traditional Chinese medicine according to claim 2, wherein the volume ratio of the amount of ethyl acetate added to water during extraction is 3:1-1: 3.

7. The traditional Chinese medicine according to claim 2, wherein the total phenols content in the Maotai extract is 15.0-22.5% of total phenols.

8. A formulation comprising the Chinese medicament for treating gastric ulcer as claimed in claims 1 to 7, wherein the formulation consists of the pharmaceutical composition and a pharmaceutically acceptable carrier or diluent.

9. The preparation of claim 8, wherein the preparation is in the form of tablet, capsule, oral liquid, pill, granule, or powder.

10. Use of a traditional Chinese medicine according to any one of claims 1 to 7 or a formulation according to any one of claims 8 to 9 in the manufacture of a medicament for the treatment of gastric ulcers.

Technical Field

The invention relates to the technical field of traditional Chinese medicines, in particular to a traditional Chinese medicine for treating gastric ulcer and application thereof.

Background

The sauce head is common Chinese herbal medicine for Yi nationality in Yunnan province, and is derived from root tuber of Fallopia densticulata (Huang) A.J.Litrans.nov. It is astringent and cool in nature and taste, has effects of astringing, stopping diarrhea, diminishing inflammation, relieving pain, etc., and can be decocted or ground into powder for oral administration for treating dysentery, dyspepsia, and chronic hepatitis; it can be administered with wine for internal hemorrhage; the fresh product is mashed or the dry powder is externally applied to the early stage of furuncle, traumatic bleeding and the like, and the root tuber of the Yi nationality has good curative effect on chronic hepatitis.

Gastric ulcer is a digestive ulcer caused by imbalance of defense factors and attack factors of gastric mucosa, and causes gastric ulcer are various, such as alcoholism, mental stress, abuse of non-steroidal anti-inflammatory drugs and invasion of helicobacter pylori. The treatment of the gastric ulcer generally needs to take western medicines for a long time, but the western medicines have great side effects on the body, and the traditional Chinese medicines have small toxic and side effects and can be taken for a long time.

Disclosure of Invention

The invention aims to overcome the defects in the prior art and provides a traditional Chinese medicine for treating gastric ulcer and application thereof.

A traditional Chinese medicine for treating gastric ulcer comprises the effective components of a Maotai extract.

A traditional Chinese medicine for treating gastric ulcer is prepared by the extraction method of a Maotai extract, which comprises the following steps: pulverizing sauce head with a pulverizer, sieving, extracting the powder with solvent, filtering, collecting extractive solution, adding solvent, extracting for 2-3 times, mixing extractive solutions, and concentrating to obtain extract with rotary evaporator.

Dissolving the extract in water, mixing, adding ethyl acetate, extracting for 2-3 times, mixing extractive solutions, and evaporating to obtain extract.

Further, according to the traditional Chinese medicine, the mass ratio of the sauce head powder to the solvent is 1:5-1: 10; the solvent is 80-95% ethanol water solution by volume percentage.

Further, the extraction method of the traditional Chinese medicine is any one of an extraction method, a reflux extraction method or an ultrasonic extraction method.

Further, the temperature of the rotary evaporator is 50 ℃, and the pressure is 0.05-0.08 MPa.

Furthermore, the volume ratio of the ethyl acetate added to the water during the extraction of the traditional Chinese medicine is 3:1-1: 3.

Further, in the traditional Chinese medicine, the total phenols contained in the Maotai extract are 15.0-22.5%.

The preparation containing the traditional Chinese medicine for treating the gastric ulcer consists of a pharmaceutical composition and a pharmaceutically acceptable carrier or diluent.

Further, the preparation is tablet, capsule, oral liquid, pill, granule or powder.

Use of a Chinese medicament as defined above or a formulation as defined above in the manufacture of a medicament for the treatment of gastric ulcer.

Has the advantages that:

the traditional Chinese medicine for treating gastric ulcer provided by the invention is prepared by extracting effective components from sauce heads serving as basic raw materials, has a large amount of total phenol components, has the effects of resisting bacteria, resisting cancer, diminishing inflammation and the like, is small in toxic and side effects, and has a remarkable effect of treating gastric ulcer.

Drawings

FIG. 1 is a graph comparing the damage of the Soy extract to the gastric mucosa of rats in each group in example 1;

wherein, a. normal group; B. a model group; C. a group of positive drugs; D. concentration group in sauce head extract; E. a high concentration group of sauce head extract;

FIG. 2 is a pathological section (HE staining) of the extract of Soy sauce head on the gastric mucosa of rats in each group 20X in example 1;

wherein, a is epithelial cell injury and necrosis; submucosal edema; c, interstitial bleeding; inflammatory cell infiltration; A. a normal group; B. a model group; C. a group of positive drugs; D. a low concentration group of Soy sauce head extract; E. concentration group in sauce head extract; F. high concentration group of sauce head extract.

Detailed Description

In order to make the objects, technical solutions and advantages of the present invention more apparent, the technical solutions of the present invention are described clearly and completely below, and it is obvious that the described embodiments are some, not all embodiments of the present invention. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.

Example 1

The method for extracting the effective components of the sauce head by adopting a cold soaking extraction method comprises the following steps:

pulverizing and sieving the sauce head, weighing 300g of sauce head powder, adding five times of 80% ethanol for extraction, extracting for 2 days at room temperature, filtering and collecting the extracting solution, extracting the filter residue for 2-3 times, combining the extracting solutions, concentrating under reduced pressure, drying to obtain 90.4g of powder, adding 3L of water for dissolving, adding ethyl acetate with the same amount as water for extraction to obtain 19.0g of ethyl acetate extract, namely the sauce head extract. The total phenol content of the sauce head extract is 16.2-22.5% as determined by Folin-Cioealteau color development method.

Example 2

The method for extracting the effective components of the sauce head by adopting a reflux extraction method comprises the following steps:

pulverizing and sieving the sauce head, weighing 300g of sauce head powder, adding ten times of 95% ethanol aqueous solution, heating and refluxing for 3h at 50 ℃ in a water bath, filtering, repeatedly extracting residues for 3 times, combining filtrates, carrying out rotary evaporation, rotary drying and drying to obtain sauce head extract powder (92.4g), adding 3L of water for dissolving, adding ethyl acetate with the same amount as water for extraction to obtain 20.9g of ethyl acetate extract, namely the sauce head extract. The total phenol content of the extract is 16.8-18.3% as determined by Folin-Cioealteau color development method.

Example 3

The method for extracting the effective components of the sauce head by adopting an ultrasonic extraction method comprises the following steps:

pulverizing and sieving sauce head, weighing 300g of sauce head powder, adding five times of 95% ethanol aqueous solution, performing ultrasonic extraction at 50 ℃ for 60min with the power of 250W and the frequency of 50KHz for 3 times, filtering, combining filtrates, concentrating under reduced pressure and drying to obtain sauce head extract (88.6g), adding 3L of water for dissolving, adding water-equivalent ethyl acetate for extraction to obtain 17.8g of ethyl acetate extract, namely the sauce head extract. The total phenol content of the Soy extract is 15.0-17.9% as determined by Folin-Cioealteau color development method.

Example 4

The method for determining the content of total phenols in the sauce head extract by adopting a Folin-Cioealteau color development method comprises the following steps:

(1) preparation of standard solution

Accurately weighing 10.0mg gallic acid, adding 1mL absolute ethyl alcohol for dissolving, adding distilled water for volume determination to 10mL, and obtaining gallic acid solution with concentration of 1.0 mg/mL. The gallic acid solution was diluted with distilled water to standard solutions at concentrations of 0.10, 0.08, 0.06, 0.04, and 0.02mg/mL, respectively.

(2) Preparation of test solution

Precisely weighing 10.0mg of the Soy head extract obtained in examples 1, 2 and 3, dissolving with 10% ethanol, and diluting to a constant volume in a 10mL volumetric flask to obtain a test solution with a concentration of 1.0 mg/mL.

(3) Establishment of standard curve linearity

Taking 0.04mL of gallic acid standard solution with concentration of 0.10, 0.08, 0.06, 0.04 and 0.02mg/mL prepared in (1), respectively, adding water to make up for 0.4mL, adding 4mL of 2.0% Na₂CO₃Mixing the solution, adding 0.2mL 50% Folin-Cioealateau reagent after 2min, mixing, standing for 30min, and measuring OD value at 750 nm. Taking gallic acid concentration as abscissa and absorbance as ordinate, its standard curveHas a regression equation of Y-4.7314X +0.0465, R²＝0.9984。

(4) Content determination of test sample

Respectively taking 0.05mL of each test solution, placing in a test tube, adding water to make up for 0.4mL, adding 4mL of 2.0% Na₂CO₃Mixing the solution, adding 0.2mL of 50% Folin-Cioealateau reagent after 2min, mixing, standing for 30min, measuring OD value at 750nm, and calculating the extraction rate of total phenol, wherein the calculation formula is as follows:

the total phenol extraction (%) - (A-0.0465)/4.7314 XB XC/D Xm₂]/m₁ ⅹ 100％

A is the OD value of the test solution; b is 8, which is the dilution multiple; c is 10.0mL, which is the volume of the test solution; d is 10.0mg of total phenol extract of the sauce head used for preparing the test solution; m is₁The mass of the sauce head powder used for the test; m is₂Is the quality of the total phenol extract of the sauce.

Example 5

The effect of the effective components of Maotai on treating gastric ulcer, the protection effect of Maotai extract on the acute gastric ulcer of rats caused by absolute ethyl alcohol is studied in the example.

The experimental method comprises the following steps:

(1) feeding 60 SPF SD male rats (weight 200 + -20 g) for 7 days to adapt to the laboratory environment;

(2) 60 SPF-grade SD male rats were divided into 6 groups of 10 rats each, which were:

blank group: regular feeding, and equal amount of physiological saline is given every day;

model group: regular feeding, and equal amount of physiological saline is given every day;

low dose group of sauce head extract: regular feeding, wherein the sauce head extract is fed daily (150 mg/kg);

soy sauce head extract medium dose group: regular feeding, wherein the sauce head extract is fed daily (300 mg/kg);

high dose group of sauce head extract: regular feeding, wherein the sauce head extract is fed daily (600 mg/kg);

positive control group: regular feeding, with ranitidine suspension feeding (150mg/kg) daily;

the extract of Maotai is the extract of Maotai in example 1, and ranitidine (Guangdong Hengjian limited company) is purchased from great drug stores of east Jun, and each administration group is administered by gavage 1 time per day for 14 days;

(3) after the medicine is drenched on day 13, the rats are fasted and are not forbidden to drink for 24 hours, 1 hour after the last administration, except for the normal group, the rats of each group are drenched with absolute ethyl alcohol with the volume of 0.5ml/100g for molding, 3 percent sodium pentobarbital is injected into the abdominal cavity after 1 hour, then the whole stomach is cut off, cut open along the greater curvature of the stomach, cleaned with ice physiological saline, the stomach is unfolded and photographed in an HAD machine, the ulcer area is measured by using Image J software, and the ulcer inhibition rate is calculated, which is specifically shown in figure 1.

The ulcer inhibition rate calculation formula is as follows: ulcer inhibition (%) - (average ulcer area of model group-average ulcer area of experiment group)/average ulcer area of model group × 100%.

After photographing the stomach tissue, the stomach mucosa tissue with a proper size is cut and placed in a marked dehydration box and soaked in 4% paraformaldehyde, so as to make a pathological section later, as shown in fig. 2.

(4) The degree of gastric mucosal damage was evaluated by the area of the ulcer. As can be seen from Table 1, the model group has significant gastric mucosa injury and the largest gastric ulcer area under the action of absolute ethyl alcohol, which indicates that the absolute ethyl alcohol causes the successful preparation of the acute gastric ulcer model of the rat, and after the administration of the Sorput extract and ranitidine, the ulcer areas of the administration group are reduced compared with the model group, and the anti-gastric ulcer effects of the Sorput extract and the high-dose group are significantly better than those of the ranitidine group. The result shows that the sauce head extract reduces the damage of absolute ethyl alcohol to the gastric mucosa and plays a role in protecting the gastric mucosa.

TABLE 1 influence of Maotai extract and ranitidine as positive drug on acute gastric ulcer of rats caused by absolute ethyl alcohol

Note: in comparison with the set of models,^*P<0.05，^**P<0.01; compared with the ranitidine group, the method has the advantages that,^△P<0.01

(6) histopathological observation of stomach tissue

After the stomach tissue is fixed in 4% paraformaldehyde, paraffin embedding is carried out, histopathological section is carried out on the ulcer area of the stomach tissue, the thickness is 5 mu m, dewaxing and hematoxylin-eosin (HE) staining are carried out, the morphological change of cells and tissues of the stomach tissue is observed under the condition that the microscope magnifies 20 times, and image acquisition and analysis are carried out.

The observation result of the histopathological morphology of the stomach is shown in fig. 2, the infiltration of the gastric mucosa histiitis cells and the gland destruction in the model group are very serious, the tissue mucosa layer is damaged, and the interstitium can show bleeding. Compared with a model group, the high, medium and low doses of the sauce head extract have the effect of improving the gastric mucosa injury of rats, and particularly, the high dose group hardly has hemorrhagic injury, has no gland injury, has no obvious edema in the submucosa, and is slightly soaked in inflammatory cells. The sauce head extract has obvious improvement effect on the pathological form of the gastric mucosa injury of the rat.

Finally, it should be noted that: the above examples are only used to illustrate the technical solution of the present invention, but not to limit it; although the present invention has been described in detail with reference to the foregoing embodiments, it will be understood by those of ordinary skill in the art that: the technical solutions described in the foregoing embodiments may still be modified, or some technical features may be equivalently replaced; and such modifications or substitutions do not depart from the spirit and scope of the corresponding technical solutions of the embodiments of the present invention.