Application of cedrol in preparation of medicine for treating acute ulcerative colitis
By using cedrol as the active ingredient, the drug formulation has solved the problem of large side effects of existing UC treatment drugs, achieving effective treatment of ulcerative colitis and improving intestinal health and colon structure.
Patent Information
- Application Number
- CN202511314966.7
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-09-15
- Publication Date
- 2025-11-07
AI Technical Summary
Existing UC treatments, such as aminosalicylic acid derivatives, may have short-term or long-term side effects, and there is a lack of highly effective and low-toxicity treatment options.
Using cedrol as the active ingredient, it is prepared into pharmaceutically acceptable dosage forms for the treatment of acute ulcerative colitis, including an effective amount of cedrol and pharmaceutically acceptable excipients, in dosage forms including tablets, drops, injections and capsules.
Cedarol can effectively improve colon damage, reduce inflammation, improve intestinal mucosal barrier function, slow weight loss, reduce disease activity index, alleviate colonic shortening and loose stools, and protect the structural integrity of the colon.
Smart Images
Figure CN120899678A_ABST
Abstract
Description
TECHNICAL FIELD
[0001] The application belongs to the technical field of biological medicine, and particularly relates to application of cedrol in preparation of a drug for treating acute ulcerative colitis. BACKGROUND
[0002] Ulcerative colitis (UC) is a phenotype of inflammatory bowel disease (IBD), which has the characteristics of chronicity, recurrence and non-specificity. The core pathological features are imbalance of intestinal immune homeostasis and destruction of mucosal barrier. Although the exact cause of IBD is still unknown, it is the result of the combined action of genetic, environmental, infection and immune factors and intestinal flora imbalance.
[0003] Traditional UC treatment drugs are mainly amino salicylic acid, which can suppress UC symptoms to a certain extent, but may cause short-term or long-term side effects such as fever, nausea, allergic reactions and high recurrence rate. Therefore, it is particularly important to find new UC treatment drugs with high efficiency and low toxicity and to explore the mechanism thereof.
[0004] Cedrol (CE), molecular formula: C 15 H 26 O, molecular weight: 222.37, CE is found to have the effects of anti-anxiety, anticancer and anti-hair loss as a natural product. Recent studies have shown that CE has an anti-anxiety effect on male mice, and its anti-anxiety effect may be achieved by increasing the level of 5-hydroxytryptamine (5-HT) and reducing the level of dopamine (DA). In terms of anticancer, it is found by using the sulfo-rhodamine B (SRB) assay that CE has a certain inhibitory effect on anaplastic melanoma C32 cells and renal cell adenocarcinoma cells. CE has cytotoxic activity on human lung cancer cells A549, liver cancer cells J5 and oral tumor cells OEC-M1. In terms of anti-hair loss, CE regulates the JAK3 / STAT3 signaling pathway, activates the Wnt3α / β-catenin reproductive center, and reduces the oxidative stress caused by CP, thereby promoting the proliferation of hair follicle cells and reversing AA, indicating that CE can be used as a raw material for promoting hair growth drugs. However, so far, there has been no report on its use for treating ulcerative colitis. SUMMARY
[0005] In view of this, the purpose of the present application is to provide the application of cedrol in preparation of a drug for treating acute ulcerative colitis.
[0006] In order to achieve the above-mentioned purpose, the present application provides the following technical scheme: In a first aspect, the present application provides the application of cedrol in preparation of a drug for treating acute ulcerative colitis.
[0007] Based on the above technical scheme, further, the cedrol is obtained by recrystallization of acetone and cyclohexane, and the structure of the cedrol is as follows: .
[0008] Based on the above technical scheme, further, the drug comprises an effective amount of cedrol and a pharmaceutically acceptable excipient.
[0009] Based on the above technical scheme, further, the pharmaceutically acceptable excipient comprises a filler, a diluent, a binder, a disintegrant and an emulsifier.
[0010] Based on the above technical scheme, further, the drug takes cedrol as the only active ingredient.
[0011] Based on the above technical scheme, further, the drug is prepared into a pharmaceutically permissible dosage form.
[0012] Based on the above technical scheme, further, the dosage form comprises tablets, drops, injection preparations and capsule preparations.
[0013] Based on the above technical scheme, further, the drug is prepared in the form of a single-dose drug.
[0014] Based on the above technical scheme, further, the single-dose drug contains 1-1000 mg of cedrol.
[0015] Based on the above technical scheme, further, the drug can improve colon injury, reduce inflammatory response and improve intestinal mucosal barrier function.
[0016] Based on the above technical scheme, further, the drug can slow down weight loss caused by ulcerative colitis, reduce disease activity index, relieve colon shortening and loose stool phenomenon, and protect the integrity of the colon structure.
[0017] Compared with the prior art, the present application has the following beneficial effects: The present application firstly verifies through experiments that cedrol can effectively improve DSS-induced colon injury, reduce inflammatory response, improve intestinal mucosal barrier function, slow down weight loss caused by ulcerative colitis, reduce disease activity index, relieve colon shortening and loose stool phenomenon, and protect the integrity of the colon structure; the present application provides a theoretical basis for research and development of drugs for treating ulcerative colitis, and has wide clinical application value. BRIEF DESCRIPTION OF DRAWINGS In order to more clearly illustrate the embodiments of the present application, the drawings involved in the embodiments will be briefly introduced below.
[0018] Figure 1Figure for the effect of cedrol CE on DSS-induced UC mice DAI score (A) and body weight (B).
[0019] Figure 2 Figure for the effect of cedrol CE on DSS-induced UC mice colon length.
[0020] Figure 3 Figure for the HE staining sections of cedrol CE on DSS-induced UC mice colon, liver and kidney.
[0021] Figure 4 Figure for the F4 / 80 and +CD86 staining results of cedrol CE on DSS-induced UC mice colon. DETAILED DESCRIPTION
[0022] The application will be described in detail below with examples, but the embodiments of the application are not limited thereto, and it is obvious that the examples described below are only part of the embodiments of the application, and other similar embodiments obtained by those skilled in the art without creative labor fall within the protection scope of the application.
[0023] Example 1 Experimental materials: dextran sulfate sodium salt (DSS), mesalazine (5-ASA), cedrol; Cedrol is a compound extracted from ginger by the team of Shenyang Pharmaceutical University for the first time, which is different from the finished product cedrol on the market. The cedrol used in the application is cedrol recrystallized from acetone and cyclohexane, which has been proved by experiments to have very good anti-inflammatory and analgesic activity. The structure of cedrol is as follows:
[0024] Mice: purchased from Liaoning Changsheng Biotechnology Co., Ltd.
[0025] 1. Establishment of DSS-induced acute ulcerative colitis mouse model and grouping C57BL / 6 mice were randomly divided into Control group, DSS group, DSS+5-ASA group (200 mg / kg per day), DSS+CE low dose group (40 mg / kg per day), and DSS+CE high dose group (80 mg / kg per day), with 6 mice in each group. After one week of adaptation, the drug groups: DSS+5-ASA group, DSS+CE low dose group, and DSS+CE high dose group, were given the corresponding dose of drugs by gavage according to the body weight of the mice for 7 days. The rest of the mice were given the same dose of ddH2O by gavage for 7 days. From the 8th day of modeling, except for the Control group, the rest of the mice were allowed to drink 3% DSS solution freely for 7 days to establish the mouse ulcerative colitis (UC) model. During this period, the drug groups continued to be given the corresponding dose of 5-ASA and CE solution by gavage.
[0026] 2. Animal sample collection and experimental process (1) Record the body weight, mental state, blood in stool and stool character of mice from day 8 to day 15. (2) After anesthesia, the mice were sacrificed, fixed in supine position, the abdomen was alcohol disinfected, the abdominal skin and peritoneum were cut open with sterile surgical scissors, the colon tissue was quickly removed at the pubic symphysis and cecum of the mice, the whole colon length was measured and the picture and sample were reserved for subsequent experiments.
[0027] (3) After the experimental mice were sacrificed, the colon, liver and kidney were collected and divided, a part of the tissue was cut into pieces and fixed in the pre-prepared formaldehyde reagent for histopathological section observation; a part of the tissue was quickly frozen in liquid nitrogen, transported to the laboratory on dry ice and stored in a -80°C refrigerator for subsequent physiological and biochemical index analysis.
[0028] 3. Disease Activity Index (DAI) score determination During the period from day 8 to day 15, the general condition (body weight, bleeding and stool character) of the mice was observed and recorded daily, the disease activity index was calculated, DAI = (body weight index + stool character + bleeding condition) / 3, and the scoring details are shown in Table 1.
[0029] Table 1 Scoring details
[0030] The results are shown in Figure 1 , which show that compared with the Control group, the body weight of the mice in the DSS group has a significant downward trend, and the DAI score is significantly increased, while compared with the DSS group, the DSS+5-ASA group and the DSS+CE high and low dose groups can effectively alleviate the body weight loss of mice caused by DSS, and the increase in DAI score is smaller.
[0031] 4. Measurement of colon length in mice: The colon of UC mice will be significantly shortened, and the severity of the disease is positively correlated with the shortening of the colon. In the UC animal experiment, the inflammation of the ulcerative colitis mice can also be judged by observing the length of the colon of the mice. The experimental results are shown in Figure 2 , which show that the colon length of the mice in the DSS group is significantly shortened, while the administration of 5-ASA and CE high and low dose groups can significantly inhibit the shortening of the colon length of the mice, and the intervention effect of the CE high dose group is the best.
[0032] 5. Observation of pathological tissue sections of mouse colon The HE staining section images of the colon, liver and kidney of DSS-induced UC mice treated with cedrol CE are shown in Figure 3As shown, according to the HE staining results, the colon structure of the DSS group was severely damaged, mainly manifested as destruction of crypt structure, disappearance of glands, and presence of a large number of inflammatory cell infiltration, and the like, and the pathological damage of intestinal barrier structure caused by DSS was significantly improved after administration of CE. The above results show that CE can alleviate the symptoms of DSS-induced UC mouse colon injury. 6. Fluorescence co-localization images of mouse colon tissues: The results of F4 / 80 and +CD86 staining of DSS-induced UC mouse intestine by cedrol CE are shown in FIG. 6. Figure 4 As shown, compared with the blank control group, the F4 / 80, which is a marker of mature mouse macrophages, was significantly increased in the colon tissue of the DSS mouse of the model group, and the mouse colon lamina propria macrophages abnormally aggregated, and the above conditions were significantly alleviated in the high-dose cedrol administration group.
[0033] Finally, it should be noted that: the above examples are only used to illustrate the technical solutions of the present application, and not to limit it; although the present application has been described in detail with reference to the foregoing examples, those skilled in the art should understand that: it can still modify the technical solutions recorded in the foregoing examples, or make equivalent substitution for part or all of the technical features; and these modifications or substitutions do not make the essence of the corresponding technical solution deviate from the scope of the technical solutions of the embodiments of the present application.
Claims
1. Use of cedrol in the preparation of a medicament for treating acute ulcerative colitis.
2. Use according to claim 1, characterized in that, The structure of the cedrol is as follows: 。 3. Use according to claim 1, characterized in that, The medicament comprises an effective amount of cedrol and a pharmaceutically acceptable adjuvant.
4. Use according to claim 3, characterized in that, The pharmaceutically acceptable adjuvant comprises a filler, a diluent, a binder, a disintegrant and an emulsifier.
5. The use according to claim 1, characterized in that, The medicament takes cedrol as the only active ingredient.
6. Use according to claim 1, characterized in that, The medicament is prepared into a pharmaceutically permissible dosage form, which comprises tablets, drops, injection preparations and capsule preparations.
7. The use according to claim 1, characterized in that, The medicament is prepared into a single-dose medicament.
8. The use according to claim 8, characterized in that The single-dose medicament contains 1-1000 mg of cedrol.
9. The use according to claim 1, characterized in that, The medicament can improve colon injury, reduce inflammatory response and improve intestinal mucosal barrier function.
10. The use according to claim 1, characterized in that, The medicament can slow down weight loss caused by ulcerative colitis, reduce disease activity index, relieve colon shortening and loose stool phenomenon and protect colon structural integrity.