Use of a bauhinia championii extract in the preparation of a drug for treating ulcerative colitis

Abstract

The application provides an application of a Triadica Ludovicana extract in preparation of a medicine for treating ulcerative colitis, and belongs to the technical field of medicines.The application is proved to show that the Triadica Ludovicana extract can reduce the inflammatory response of ulcerative colitis, has a good treatment effect on ulcerative colitis, can effectively improve the pathological damage of colon tissues, has an obvious protective effect on ulcerative colitis, can reduce the symptoms of weight loss and fecal occult blood, has a potential for preparing a medicine preparation for treating ulcerative colitis, provides a new material basis for developing the medicine for ulcerative colitis, and has potential and great social and economic benefits.In addition, the raw material used in the application is Yao medicine, the resource of which is rich, the extraction and preparation method is simple and easy to operate, and the Triadica Ludovicana extract can be prepared in a large quantity.

Description

Technical Field

[0001] This invention relates to the field of pharmaceutical technology, and in particular to the application of an extract of *Xiao Liu Teng* in the preparation of a drug for treating ulcerative colitis. Background Technology

[0002] *Pileostegia tomentella* Hand.-Mazz., a plant belonging to the genus *Pileostegia* in the family Hydrangeaceae, is also known as Tumor Vine, Mountain Loquat, and in Yao ethnicity as Buerng deic wiang. *Pileostegia tomentella* has the effects of resolving phlegm and relieving cough, clearing heat and reducing swelling, dispersing nodules, promoting blood circulation, and anti-cancer properties. Recent studies have shown that *Pileostegia tomentella* mainly contains phenylpropanoids, terpenes, and organic acids (esters), which have anti-tumor and antioxidant biological activities. However, there are currently no methods for using *Pileostegia tomentella* to treat ulcerative colitis.

[0003] Ulcerative colitis (UC), in Traditional Chinese Medicine (TCM), falls under the categories of "dysentery" and "intestinal obstruction." The disease originates in the large intestine and is closely related to the spleen. Spleen dysfunction hinders the transformation and transportation of nutrients, leading to the accumulation of damp-heat toxins and stagnation of qi and blood in the intestines, which is the key pathogenesis of this disease. UC is one of the two main forms of inflammatory bowel disease and a chronic, immune-mediated idiopathic inflammatory bowel disease, primarily affecting the rectum and sigmoid colon. Clinically, it often manifests as diarrhea and abdominal pain, with bloody diarrhea being the most common symptom. UC is usually diagnosed through a combination of symptoms, endoscopic examination, and histological changes. In recent years, due to various environmental factors and changes in dietary habits, the incidence of UC has been steadily increasing. Some severe cases may even lead to complications such as intestinal bleeding, intestinal perforation, or intestinal obstruction. Furthermore, recurrent UC can increase the incidence of colorectal cancer. Therefore, the treatment of UC is crucial.

[0004] Currently, the most common treatment for ulcerative colitis (UC) is drug therapy, including aminosalicylic acids, glucocorticoids, immunosuppressants, and biologics. However, the clinical efficacy of many drugs is unstable, and they may even cause a series of problems such as liver and kidney toxicity, drug dependence, and relapse after drug withdrawal, which limits the clinical application of UC treatment drugs. Traditional Chinese medicine (TCM) has the advantages of multiple pathways and multiple targets in the treatment of UC. Through syndrome differentiation and treatment, it can effectively alleviate patients' symptoms, reduce disease recurrence, and has good application prospects. Summary of the Invention

[0005] The purpose of this invention is to provide an application of *Xiao Liu Teng* extract in the preparation of a drug for treating ulcerative colitis, which can reduce the inflammatory response of ulcerative colitis and effectively improve the pathological damage of colon tissue.

[0006] To achieve the above-mentioned objectives, the present invention provides the following technical solution:

[0007] This invention provides an application of *Xiao Liu Teng* extract in the preparation of a drug for treating ulcerative colitis.

[0008] Furthermore, the preparation method of the extract of *Xiaolu Teng* is as follows:

[0009] After crushing the 'Xiaolu Teng' (a type of herb), ethanol was added and refluxed for extraction and filtration. The filtrates were combined and concentrated to obtain the 'Xiaolu Teng' extract.

[0010] Furthermore, the ethanol is 50% ethanol, and the mass ratio of *Xiaolu Teng* to ethanol is 1:8-10.

[0011] Furthermore, the reflux extraction is performed 1 to 3 times, and the reflux extraction time is 1 to 2 hours.

[0012] Furthermore, the medication for treating ulcerative colitis may be added with a pharmaceutically acceptable carrier.

[0013] Furthermore, the dosage form of the drug for treating ulcerative colitis is one of the following: injection, powder, capsule, granule, tablet, pill, or ointment.

[0014] The beneficial effects of the *Xiaoliu Teng* extract described in this invention in the preparation of drugs for treating ulcerative colitis compared with existing technologies are as follows:

[0015] This invention has verified that the extract of *Xiaolu Teng* (a type of herb) can reduce the inflammatory response of ulcerative colitis, has a good therapeutic effect on ulcerative colitis, can effectively improve the pathological damage of colon tissue, has a significant protective effect against ulcerative colitis, and can also alleviate symptoms such as weight loss and fecal occult blood. It has the potential to prepare a pharmaceutical formulation for the treatment of ulcerative colitis, providing a new material basis for the development of drugs for ulcerative colitis, and has potential and huge social and economic benefits.

[0016] The raw material used in this invention is Yao medicine, which is abundant and has a simple and easy extraction and preparation method that can be used for large-scale production. Attached Figure Description

[0017] To more clearly illustrate the technical solutions in the embodiments of the present invention or the prior art, the drawings used in the embodiments will be briefly introduced below. Obviously, the drawings described below are only some embodiments of the present invention. For those skilled in the art, other drawings can be obtained based on these drawings without creative effort.

[0018] Figure 1 The results show the body weight of the five groups of mice in Example 2;

[0019] Figure 2 The Disease Activity Index (DAI) values ​​of the five groups of mice in Example 2;

[0020] Figure 3 is the colon length of 5 groups of mice in Example 2;

[0021] Figure 4 shows the colonic histopathological conditions of 5 groups of mice in Example 2, where A is the normal control group; B is the model group; C is the low-dose group of the extract of Xiaoliuteng; D is the medium-dose group of the extract of Xiaoliuteng; E is the high-dose group of the extract of Xiaoliuteng. Detailed Description of the Embodiments

[0022] The embodiments of the present invention are described in detail below, and the embodiments are intended to explain the present invention, and shall not be construed as a limitation to the present invention. Where no specific techniques or conditions are specified in the embodiments, the procedures shall be carried out according to the techniques or conditions described in the literature in the art or according to the product specification. Where no manufacturers of reagents or instruments used are indicated, they are all conventional products commercially available.

[0023] The experimental animals used in the following examples are SPF-grade male C57BL / 6 mice, weighing 18-22g, provided by Changsha Tianqin Biotechnology Co., Ltd., with the production license number SCXK(Xiang)2022-0011.

[0024] Instruments used: Leica RM2255 fully automatic rotary microtome, Leica DM2500 microscopic imaging analysis system (Leica Instruments Co., Ltd., Germany).

[0025] Example 1

[0026] Example 1 of the present invention prepares the extract of Xiaoliuteng, and the specific preparation method is as follows:

[0027] Coarse powder of Xiaoliuteng medicinal material is added with 8 times the amount of 50% ethanol for reflux extraction 2 times, 1.5h each time, filtered, the filtrates are combined, and concentrated to obtain an extract equivalent to 5.53g of crude drug per gram of ointment, so as to obtain the extract of Xiaoliuteng.

[0028] Example 2

[0029] Example 2 of the present invention detects the therapeutic effect of the extract of Xiaoliuteng obtained in Example 1 on ulcerative colitis, and the method is as follows:

[0030] (1) Administration and modeling of mice

[0031] C57BL / 6 mice are randomly divided into 5 groups: normal control group, model group, low-dose, medium-dose and high-dose groups of the extract of Xiaoliuteng (25, 50, 100g crude drug / kg), 8 mice in each group.

[0032] Starting from the first day of the experiment, mice in the low, medium and high dose groups of Xiaoru Teng extract were given the corresponding drug solution by gavage to protect them. The gavage volume was 20 mL / kg. The normal control group and the model group were given the same volume of pure water by gavage once a day.

[0033] Starting from day 4 of the experiment, mice in the normal control group drank pure water, while mice in the other four groups drank 3% DSS solution to induce the mouse model. Drug administration continued during model initiation. Mouse weight was recorded daily (see...). Figure 1 The characteristics of the feces and the presence of blood in the stool were observed. Mice were sacrificed on day 10, and the colon was dissected and the length of the colon from the proximal rectum to the ileocecal junction was measured (see...). Figure 3 Distal colon tissue was harvested and fixed with 10% formalin solution.

[0034] (2) DAI scores were calculated based on the recorded mouse weight, fecal characteristics, and fecal blood loss (see [reference]). Figure 2 ), and compared the colon length of mice:

[0035] The scoring method is as follows:

[0036] Weight loss percentage: No weight loss is 0 points. Based on the initial weight, a weight loss of 1-5% is 1 point, 5-10% is 2 points, 10-15% is 3 points, and more than 15% is 4 points.

[0037] Stool viscosity: 0 points for normal stool consistency, 2 points for pasty stool, and 4 points for watery stool.

[0038] Fecal occult blood: 0 points for no visible blood in the stool, 2 points for slight visible blood in the stool, and 4 points for severe blood in the stool.

[0039] The average of the three scores each day is the DAI value.

[0040] Depend on Figure 1 , Figure 2 It was found that after modeling with 3% DSS solution, the mice in the model group experienced a decrease in body weight and an increase in DAI score. Overall, the pre-protected mice in the medium and high dose groups of *Xylaria dichotoma* extract showed a lower rate of body weight loss and a lower DAI score than the model group. Furthermore, compared to the model group, the DAI score of mice in the high dose group of *Xylaria dichotoma* extract was significantly lower on day 6 after modeling (P < 0.01), and the rate of body weight loss and DAI score were significantly reduced on day 7 after modeling (P < 0.01). Therefore, *Xylaria dichotoma* extract has a significant therapeutic effect on ulcerative colitis. Figure 3 It was found that after modeling with 3% DSS solution, the colon length of mice in the medium and high dose groups of *Xiaoruoteng* extract was significantly increased compared with the model group. The results indicate that *Xiaoruoteng* extract has a protective effect against DSS-induced UC in mice.

[0041] (3) Histopathological observation of mouse colon tissue

[0042] Colonic tissue fixed in formalin solution was dehydrated, embedded in paraffin, sectioned, and then subjected to routine hematoxylin and eosin (HE) staining. The pathological condition of the colonic tissue was observed under a microscope. The results are as follows: Figure 4 As shown.

[0043] Depend on Figure 4 It was found that the colonic tissue structure of mice in the normal control group was intact, with neatly arranged epithelial cells, abundant goblet cells in the intestinal crypts, and no inflammatory cell infiltration. In the model group mice, the colonic tissue structure was disordered, with diffuse damage to the crypt structure, loss of goblet cells, and extensive inflammatory cell infiltration. The pathological damage to the colonic tissue of mice treated with medium and high doses of *Xiaolu Teng* extract was improved to varying degrees. In particular, the high-dose group showed relatively intact crypt structure, significantly reduced goblet cell loss, and significantly decreased inflammatory cell infiltration.

[0044] The above description is only a preferred embodiment of the present invention. It should be noted that for those skilled in the art, several improvements and modifications can be made without departing from the principle of the present invention, and these improvements and modifications should also be considered within the scope of protection of the present invention.

Claims

1. The application of an extract of *Xiao Liu Teng* (a type of herb) in the preparation of a drug for treating ulcerative colitis, characterized in that... The preparation method of the extract of *Xiaolu Teng* is as follows: After crushing the 'Xiaolu Teng' (a type of herb), ethanol was added and refluxed for extraction and filtration. The filtrates were combined and concentrated to obtain the 'Xiaolu Teng' extract.

2. The application of the extract of *Xiao Liu Teng* according to claim 1 in the preparation of a drug for treating ulcerative colitis, characterized in that, The ethanol is 50% ethanol, and the mass ratio of *Xiaolu Teng* to ethanol is 1:8~10.

3. The application of the extract of *Xiao Liu Teng* according to claim 1 in the preparation of a drug for treating ulcerative colitis, characterized in that, The reflux extraction is performed 1 to 3 times, and the reflux extraction time is 1 to 2 hours.

4. The application of the extract of *Xiao Liu Teng* according to claim 1 in the preparation of a drug for treating ulcerative colitis, characterized in that, The medication for treating ulcerative colitis may be added with a pharmaceutically acceptable carrier.

5. The application of the extract of *Xiao Liu Teng* according to claim 4 in the preparation of a drug for treating ulcerative colitis, characterized in that, The dosage form of the drug for treating ulcerative colitis is one of the following: injection, powder, capsule, granule, tablet, pill, or ointment.

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