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Application of derivative of hesperetin as anti-inflammatory and immune medicine

An immune drug, the technology of hesperetin, which is applied in the field of medical application of flavonoids, can solve the problems of low activity, difficult absorption and difficulty of hesperidin, and achieve good medicinal prospects, strong pharmacological effects and small adverse reactions Effect

Active Publication Date: 2006-11-15
ANHUI MEDICAL UNIV
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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 (Kawaguchi K, et al.Planta Med.2006, 72:477- 9), antibacterial effect (Bae EA, et al.Planta Med.1999, 65(5): 442-3), antioxidant effect (Garg A, et al. Phytother Research, 2001, 15(8): 655-69 ), but the activity of hesperidin itself is low, and it can only be effective in large doses. At the same time, hesperidin itself has poor water solubility, is difficult to absorb after oral administration, and has low bioavailability.

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  • Application of derivative of hesperetin as anti-inflammatory and immune medicine
  • Application of derivative of hesperetin as anti-inflammatory and immune medicine

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Embodiment Construction

[0026] In order to better understand the essence of the present invention, its anti-inflammatory activity and its new application in the field of pharmacy will be described below through specific experimental results and data.

[0027] 1 In vitro anti-inflammatory activity screening

[0028] Studies on the mechanism of inflammation have found that the generation of inflammation is directly related to the metabolism of arachidonic acid. Arachidonic acid in the body is mainly metabolized by cyclooxygenase and lipoxygenase, which produce inflammatory mediators such as PGs and LTs, respectively. Prostaglandin PGE 2 and leukotrienes LTB 4 They are two important inflammatory mediators of inflammatory response. The present invention adopts an in vitro administration method to study that hesperidin and its derivatives inhibit the secretion of PGE from peritoneal macrophages (PMφ) of adjuvant arthritis rats (AA rats) 2 and LTB 4 activity, and screen out hesperidin derivatives with...

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Abstract

An application of the hesperetin derivative, which is prepared from hesperidin through hydrolysis to remove glycosyl, in preparing the anti-inflammatory immune medicines for treating rheumatic or rheumatoid arthritis and osteoarthritis is disclosed.

Description

technical field [0001] 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 [0002] 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 are protective defense responses of the body, but excessive immunity and inflammation are harmful to the human body. Immunity and inflammation are two different reactions of the body to foreign bodies, but in essence, immun...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/7048A61P19/02A61P29/00
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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