Application of 7,3'-dimethoxy hesperetin in preparation of anti-inflammatory immune medicaments

A dimethoxy, immune drug technology, used in anti-inflammatory agents, drug combinations, antipyretics, etc., can solve the problems of low activity, difficult absorption, and difficulty of hesperidin, and achieve strong pharmacological effects and good medicinal uses. Prospects, less adverse effects

Active Publication Date: 2009-09-23
ANHUI MEDICAL UNIV
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  • Abstract
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Problems solved by technology

Hesperidin tastes bitter, insoluble in water, slightly soluble in alcohol, easily soluble in lye, it has a wide range of biological activities, such as anti-tumor effect (Koyunku H, et al. Anticancer Res.1999, 19 (4B): 3237 -41), anti-inflammatory effect (Guardia, et al.Farmaco.2001, 56 (9): 683-7), therapeutic effect on CIA rats (KawaguchiK, et al.Planta Med.2006, 72: 477-9 ), antibacterial effect (Bae EA, et al.

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  • Application of 7,3'-dimethoxy hesperetin in preparation of anti-inflammatory immune medicaments
  • Application of 7,3'-dimethoxy hesperetin in preparation of anti-inflammatory immune medicaments
  • Application of 7,3'-dimethoxy hesperetin in preparation of anti-inflammatory immune medicaments

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[0027] In order to better understand the essence of the present invention, specific experimental results and data are used to illustrate its anti-inflammatory activity and its new use in the pharmaceutical field.

[0028] 1 In vitro anti-inflammatory activity screening

[0029] Studies on the mechanism of inflammation have found that inflammation is directly related to the metabolism of arachidonic acid. The body's arachidonic acid is mainly metabolized through two pathways, cyclooxygenase and lipoxygenase, to produce inflammatory mediators such as PGs and LTs, respectively. Prostaglandin PGE 2 And leukotriene LTB 4 They are two important inflammatory mediators of inflammation. The present invention adopts an in vitro administration method to study hesperidin and its derivatives to inhibit the secretion of PGE by peritoneal macrophages (PMφ) in adjuvant arthritis rats (AA rats) 2 And LTB 4 Hesperidin derivatives with high anti-inflammatory activity were selected.

[0030] We have ...

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Abstract

The pharmaceutical application of a hesperetin derivative relates to the application thereof in the preparation of anti-inflammatory immune medicaments, in particular to the application in treatment of autoimmune diseases such as rheumatic, rheumatoid arthritis and osteoarthritis, and the like. The hesperetin derivative is the derivative which is prepared by a non-carbohydrate compound obtained by hydrolyzing hesperidin and removing glycosyl. The pharmacological effect of the hesperetin derivative is significantly higher than that of the parent hesperidin; and compared with traditional non-steroidal anti-inflammatory medicament naproxen and a medicament tripterygium treating rheumatoid arthritis, the hesperetin derivative has equivalent activeness, is safe and non-toxic, not only treats the symptom, but also treats the root, thus having very good medicinal prospect.

Description

Technical field: [0001] The present invention is a divisional application of "Application of Hesperetin Derivatives as Anti-inflammatory and Immunological Drugs", original application number: 200610088016.8, filing date June 15, 2006. [0002] The present invention relates to the medical use of a flavonoid compound, specifically the medical use of hesperetin derivatives, especially the application in the preparation of anti-inflammatory immune drugs. Background technique: [0003] Inflammation is a common pathological process in the body caused by various injury factors, mediated by a variety of inflammatory mediators, mainly including prostaglandins (PGs) and leukotrienes (LTs). Immunity is a specific physiological reaction of the body when it comes into contact with antigenic foreign bodies or foreign components. Its function is to identify and eliminate antigenic foreign bodies to maintain the body's physiological balance. Both immune response and inflammatory response a...

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Application Information

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IPC IPC(8): A61K31/352A61P29/00A61P37/02A61P19/02
Inventor 李俊尤田耙李荣程文明石静波吕雄文
Owner ANHUI MEDICAL UNIV
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