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Application of myricetin and/or myricetin in the preparation of medicines for preventing and/or treating inflammatory bowel disease

A technology for inflammatory bowel disease and myricetin, applied in the field of medicine, can solve problems such as unmet medical needs, low patient acceptance, complex etiology, etc., and achieve the effect of facilitating large-scale production, reducing production costs, and low prices

Active Publication Date: 2020-01-17
SUZHOU PHARMAVAN CANCER RES CENT CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Traditional IBD treatment schemes based on aminosalicylic acid, glucocorticoids, immunosuppressants, and biological agents are still the mainstream. Due to the complex etiology and poor curative effect, many patients who received treatment did not get relief, up to 80% Crohn's disease patients and 30% of UC patients ultimately require surgery, and there is a huge unmet medical need in this area
In recent years, clinical trials and applications of fecal microbiota transplantation are in the ascendant, but the acceptance rate of patients is low, and further exploration is needed

Method used

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  • Application of myricetin and/or myricetin in the preparation of medicines for preventing and/or treating inflammatory bowel disease
  • Application of myricetin and/or myricetin in the preparation of medicines for preventing and/or treating inflammatory bowel disease
  • Application of myricetin and/or myricetin in the preparation of medicines for preventing and/or treating inflammatory bowel disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] In this example, myricetol and myricetone, which are anti-inflammatory bowel disease drugs, were tested for in vitro anti-inflammatory activity

[0052] Effects of myricetol and myricetone on the expression of inflammatory factors such as IL-6, TNF-α, IL-1β and other inflammatory factors secreted by the mouse macrophage cell line RAW264.7 induced by bacterial lipopolysaccharide (hereinafter referred to as LPS) stimulation: take pre-prepared 20,000 cells / well, 100 μL / well were seeded in a 96-well plate, set at 37°C, 5% CO 2 Incubate overnight in the incubator, discard the original culture medium, add 100 μL of the prepared medium of different concentrations of the test liquid to each well, and add LPS after culturing for 1 h. The final concentration of LPS in the culture system is 100 μg / mL. Three parallel wells were set for each concentration, and a cell control group (no drug, no vehicle) and a blank medium control group (no cells, zero-adjusted well) were set at the s...

Embodiment 2

[0057] In this example, acute toxicity tests were performed on myricetol and myricetone, which are anti-inflammatory bowel disease drugs, to test the safety of myricetol and myricetone.

[0058] Thirty SD rats, half male and half male, were used. The average weight of the rats was 160-200 g for females and 180-220 g for males. Before the experiment, the animals should be acclimated to the environment for at least 5 days, and healthy (females must be non-pregnant) rats were selected as the test animals. The main inspection contents during the adaptation period: whether it is consistent with the quality index required at the time of ordering; general state inspection; whether the weight reaches the weight range required by the test. Unqualified abnormal animals were not included in this experiment. The rats were given a single dose of intragastric administration, and the low, medium and high doses were 100 mg / kg, 300 mg / kg, 600 mg / kg and 1000 mg / kg, respectively.

[0059] Obse...

Embodiment 3

[0064] In this example, the pharmacodynamics of myricetol, an anti-inflammatory bowel disease drug, was tested in vivo in a dextran sodium sulfate (DSS)-induced IBD model in mice

[0065] SPF grade C57BL / 6 mice, female, 6-8 weeks old, after adaptive feeding for 3-7 days, were fed with 4% dextran sodium sulfate (DSS) aqueous solution, and fed with free drinking water (day 0 ), replaced with fresh DSS aqueous solution every 2 days, and after drinking DSS aqueous solution freely for 7 days (day 7), replaced with fresh purified water for feeding. After 4 days of modeling, the drug was administered on the fifth day of modeling, and the animals were administered with 10 mg / kg, 5 mg / kg, and 2.5 mg / kg of drugs respectively for treatment. Administration was continued for 4 days, followed by observation for 1 day, and the experiment was terminated 24 hours after the last administration.

[0066] Detection indicators: observe and record the body weight of each group of animals every day...

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Abstract

The invention provides application of myricanol and / or myricetin to preparation of a medicine for preventing and / or treating inflammatory bowel diseases. The inflammatory bowel diseases are treated through the myricanol and / or the myricetin. The myricanol and / or the myricetin have / has an inhibition effect on IL-6, TNF-alpha and IL-1beta inflammatory factors secreted by RAW264.7 cells of mouse macrophage in vitro, and inhibition on expression of inflammatory factors is generated; more particularly, the myricanol and / or the myricetin have / has an inhibition effect on the inflammatory bowel diseases and have no obvious toxic and side effects in a medicinal effect expressing process; the ulcer area is effectively reduced. Compared with existing aminosalicylic acid medicines, the myricanol and / or the myricetin have / has a better curative effect and are / is suitable for large-scale production; the myricanol and / or the myricetin have / has a wide application prospect and relatively high application value.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the application of myricetol and / or myricetone in preparing a medicine for preventing and / or treating inflammatory bowel disease. Background technique [0002] Inflammatory bowel disease (IBD) is a group of chronic non-specific intestinal inflammatory diseases with unclear etiology, including ulcerative colitis (UC) and Crohn's disease (CD) ). The pathogenesis is unknown, but the related pathogenic factors that have been found include: heredity, infection, environmental pollution, diet, intestinal microecology, etc. IBD is a common disease in North America and Europe. The prevalence of ulcerative colitis in Europe and the United States is 240 / 100,000, the incidence rate is 10 / 100,000 to 20 / 100,000, and the prevalence of Crohn's disease is 200 / 100,000. , the incidence rate is 5 / 100,000 to 10 / 100,000. In the past 30 years, the incidence of IBD in Japan has also been gradually increasing. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/05A61K31/122A61P1/00A61P1/04A61P29/00
CPCA61K31/05A61K31/122A61P1/00A61P1/04A61P29/00
Inventor 邓世平曹宇俞云会鱼刚张敏洁陈祥李志袁高纲徐涛
Owner SUZHOU PHARMAVAN CANCER RES CENT CO LTD
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