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Application of myricanol and/or myricetin to preparation of medicine for preventing and/or treating inflammatory bowel diseases

A technology for inflammatory bowel disease and myricetone, which is applied in the field of medicine, can solve the problems of unmet medical needs, low patient acceptance, and poor curative effect, and achieves the advantages of large-scale production, reduction of production costs, and reduction of ulcer area. Effect

Active Publication Date: 2018-08-24
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 myricanol and/or myricetin to preparation of medicine for preventing and/or treating inflammatory bowel diseases
  • Application of myricanol and/or myricetin to preparation of medicine for preventing and/or treating inflammatory bowel diseases
  • Application of myricanol and/or myricetin to preparation of medicine for preventing and/or treating inflammatory bowel diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0052] The effect of myricetin and myricetin on the expression of 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 The cell suspension was inoculated into a 96-well plate at 20,000 cells / well, 100 μL / well, and placed at 37°C, 5% CO 2 Cultivate overnight in the incubator, discard the original culture medium, add 100 μL of prepared medium with different concentrations of the test drug solution to each well, and add LPS after 1 hour of culture, and 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 solvent) and a blank medium control group (no cells, zero wells) were set...

Embodiment 2

[0057] In this example, an acute toxicity test was carried out on myricetin and myricetin, which are anti-inflammatory bowel disease drugs, to test the safety of myricetin and myricetin

[0058] Thirty SD rats were used, half male and half male. The average body weight of the group was 160-200 g for females and 180-220 g for males, and the individual body weights should be within the range of ±20% of the average body weight. Animals need to adapt to the environment for at least 5 days before the test, and healthy (female must not be pregnant) rats are selected as test animals. The main inspection contents during the adaptation period: whether it is consistent with the quality index required at the time of order; general status inspection; whether the weight reaches the weight range required by the test. Unqualified abnormal animals were not included in this experiment. Rats were intragastrically given a single dose, given low, medium and high doses, respectively 100mg / kg, 300...

Embodiment 3

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

[0065] SPF level C57BL / 6 mice, female, 6-8 weeks old, after 3-7 days of adaptive feeding, were fed with 4% dextran sodium sulfate (DSS) aqueous solution, and fed with free drinking water (day0 ), replace fresh DSS aqueous solution every 2 days, and after drinking DSS aqueous solution freely for 7 days (day7), replace fresh purified water for feeding. After 4 days of modeling, administration began on the 5th day of modeling, and the animals were given 10 mg / kg, 5 mg / kg, and 2.5 mg / kg of drugs for treatment through tail vein administration. The administration was continued for 4 days, followed by observation for 1 day, and the experiment was ended 24 hours after the last administration.

[0066] Detection index: observe and record the weight of animals in each group every day, and collect the f...

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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 myricetin and / or myricetin in the preparation of medicaments 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 whose etiology is not very clear, including ulcerative colitis (ulcerative colitis, UC) and Crohn's disease (Crohn's disease, CD ). The pathogenesis is unknown, but related pathogenic factors have been found to 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, with an incidence rate of 10 / 100,000 to 20 / 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 gradually increased. Although th...

Claims

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Application Information

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Patent Type & Authority Applications(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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