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Application of demethyleneberberine in preparation of drugs for preventing and/or treating ulcerative colitis

A technology for desmethylene berberine and ulcerative colitis, which is used in desmethylene berberine hydrochloride, the application field of preparing medicines for preventing or treating ulcerative colitis

Inactive Publication Date: 2014-08-27
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] So far, there are no records and reports about the preventive and / or therapeutic effects of desmethylene berberine hydrochloride or desmethylene berberine on ulcerative colitis in the prior art

Method used

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  • Application of demethyleneberberine in preparation of drugs for preventing and/or treating ulcerative colitis
  • Application of demethyleneberberine in preparation of drugs for preventing and/or treating ulcerative colitis
  • Application of demethyleneberberine in preparation of drugs for preventing and/or treating ulcerative colitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1. Antioxidative activity of desmethylene berberine hydrochloride (DMB) at cellular level

[0060] Method: Normally, the body has a complete set of antioxidant defense system under physiological conditions, but when the antioxidant system is weakened or ROS is formed excessively, ROS can cause a series of damage to the body. A large number of studies have shown that a large number of inflammatory cells, including macrophages and neutrophils, are infiltrated in the gastrointestinal inflammation of patients with ulcerative colitis. exposure to oxidative stress. RAW264.7 cells are mouse peritoneal mononuclear macrophage leukemia cells, which retain the characteristics of peritoneal macrophages secreting inflammatory factors. After being stimulated with LPS and ATP, they can produce a large amount of ROS, and excessive ROS can induce the level of inflammation. Therefore, it can well simulate the inhibitory effect of drugs on colonic inflammatory factors at the in v...

Embodiment 2

[0063] Example 2. Anti-inflammatory activity of desmethyleneberberine hydrochloride (DMB) at the cellular level

[0064] Methods: Ulcerative colitis is a chronic colitis inflammatory lesion with unknown etiology. The main clinical manifestations are chronic recurrent or persistent lower abdominal pain, diarrhea, mucus and pus and blood in the stool. Studies have suggested that the intestinal epithelial cells and mononuclear macrophages in the lamina propria of UC patients secrete a large number of inflammatory cytokines. The expression changes of these cytokines in the colonic mucosa of UC patients were basically consistent with their expression changes in serum. The anti-inflammatory activity of desmethylene berberine hydrochloride in vitro will provide a theoretical basis for the development of DMB in the treatment of UC.

[0065] In this example, RAW264.7 was taken as the research object, and the anti-inflammatory effect of demethylene berberine hydrochloride was detected ...

Embodiment 3

[0068] Example 3. DMB preventive treatment reduces DSS-induced mortality in mice with ulcerative colitis

[0069] Methods: Female C57BL / 6 mice, weighing 18-22 grams, were randomly divided into five groups, 7 mice in each group, which were normal control group (control), DSS model group (model), DMB low-dose administration group (L -DMB, 75 mg / kg, IG), medium dose administration group (M-DMB, 150 mg / kg, IG) and high dose administration group (H-DMB, 300 mg / kg, IG). The administration group was intragastrically administered DMB, once a day, for 14 days in total, and the other groups were given the same volume of excipients. On the eighth day of administration, except for the normal control group, the model group and the administration group drank 3% DSS water freely for seven days to establish models, and were executed on the fourth day after the end of modeling, and the number of dead mice during the experiment was recorded.

[0070] Results: The mortality rate of the mice in ...

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Abstract

The invention discloses application of demethyleneberberine in preparation of drugs for preventing and / or treating ulcerative colitis. Please see the molecular structural formula (I) of the demethyleneberberine in the specification.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the application of desmethylene berberine hydrochloride in the preparation of drugs for preventing or treating ulcerative colitis. Background technique [0002] Ulcerative colitis (UC) is one of the common intestinal diseases. The lesions mainly invade the colonic mucosa and submucosa, and are characterized by continuity, diffuseness, and protracted healing. The severity of the disease varies greatly with different patients. , and its intractability is widely recognized internationally. If ulcerative colitis is not treated in time, it will lead to repeated attacks of the disease, from mild to severe, and chronic colitis will not be cured for a long time. Chronic colitis is prone to multiple complications, such as a large amount of blood in the stool, which can lead to shock due to excessive blood loss, and enteritis infection can cause intestinal strictures. Intestinal ulcer attacks ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61P1/04A61P29/00
Inventor 张玉彬陈盈盈闫岩张壮伟陈晓茜王永辰姚健李睿岩陈欢
Owner CHINA PHARM UNIV
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