JPH0522687B2 - - Google Patents

Description

[Detailed description of the invention]

[Object of the Invention] The present invention relates to an active oxygen scavenger, and aims to prevent or treat inflammatory diseases, liver disorders, and allergic diseases by removing active oxygen in living bodies. [Prior art] It has become clear that active oxygen, oxides, and peroxides are involved in the onset and aggravation of many diseases, and compounds that have active oxygen scavenging effects are useful for the prevention and treatment of these diseases. It is expected that For example, sesamol derivatives (Japanese Patent Application Laid-open No. 55
-167288), amino acid derivatives (Japanese Patent Application Laid-open No. 56-58495)
Antioxidants such as quercitrin
In addition to liver damage protective agents such as 140021), various compounds having active oxygen scavenging effects are known. Methods for assaying these effects have not necessarily been established, and various methods have been used, but the present inventor created a mouse inflammation model involving active oxygen by administering PMA (Phorbol Myristate Acetate). However, they discovered that fuisetin is effective in this model, and completed the present invention. [Structure of the Invention] The present invention relates to an active oxygen scavenger containing fuisetin as an active ingredient, and fuisetin is a known compound that is a type of flavonoid having the following structural formula. Inflammatory diseases that can be prevented and treated by removing active oxygen include, for example, chronic rheumatism, liver disorders such as acute and chronic hepatitis, and allergic diseases such as bronchial asthma. The appropriate dosage for adults per day is 10 mg to 10 g, especially 200 mg to 5 g, and 10 mg to 2 g, especially 100 mg to 1.5 g, per day for intravenous injections, and is usually administered in several doses. The dosage should be increased or decreased as appropriate depending on the symptoms and patient's condition. The toxicity of fuisetin is within a range that does not affect its use as a medicine, for example, the LD ₅₀ when intravenously administered to mice.
is 180mg/Kg (Registry of Toxic Effects
of Chemical Substances (1979) US
Department of Health and Human
Services). [Effects of the invention] Example Effect of fuisetin on PMA-induced inflammation 2 ml of sterile air was injected into the back of an ICR mouse (6-8 weeks old, male) using a syringe to create an air bag, and saline containing 5 μg of PMA was added to the bag. Water G (NaCl8.0
KCl0.4 MgSO ₄・7H ₂ O0.154 CaCl ₂・2H ₂ O0.016
Na ₂ HPO ₄・7H ₂ O0.29 KH ₂ PO ₄ 0.15 Glucose
1.10 Phenol Red 0.0012g/) 1ml was injected. Phytisene was dissolved in 0.1 ml of physiological saline G at various concentrations and injected. After 44 to 46 hours, the area of the inflamed area (vasodilation, redness) in the back skin was measured. Two mice were used as a control, and three mice were used in each other group. The results are shown in the table.

【table】

[Table] As a result of this experiment, it was clearly observed that fuisetin had an inhibitory effect on PMA-induced inflammation. Fisetin can be formulated with appropriate accessory ingredients (excipients, binders, disintegrants, solubilizers, etc.) using conventional formulation techniques. For example, it is suitable to administer orally or by injection, depending on the dosage form such as tablets, capsules, powders, granules, syrups, and injections.

Claims (1)

[Claims] 1 Active oxygen scavenger containing fuisetin as an active ingredient.