Use of 5,7-methoxy-3,4'-flavonol in resisting of respiratory tract inflammatory diseases

A technology for inflammatory diseases and hydroxyflavonoids, applied in the field of medicine, can solve the problems of unseen, low content, and low distribution.

Inactive Publication Date: 2018-11-30
杭州勃锐思莫生物医药科技有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 5,7-methoxy 3,4'hydroxyflavone is a kind of flavonoids, but its distribution in natural products is less and the content is very small, no relevant 5,7-methoxy 3,4'hydroxyflavone Biological activity reports

Method used

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  • Use of 5,7-methoxy-3,4'-flavonol in resisting of respiratory tract inflammatory diseases
  • Use of 5,7-methoxy-3,4'-flavonol in resisting of respiratory tract inflammatory diseases
  • Use of 5,7-methoxy-3,4'-flavonol in resisting of respiratory tract inflammatory diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Rat peritoneal mast cell degranulation test

[0019] Method: Sensitized rats: Take SD rats and subcutaneously inject 0.1ml of 2.5mg / ml refined trichosanthemi powder (suspended in 4% AL(OH) 3 In the gel, after 14 days of sensitization, the femoral artery was exsanguinated to death, and 10ml of Hank's solution was injected into the abdominal cavity, and the abdominal cavity was opened gently for 2-3 minutes after the injection. Push the contents of the abdominal cavity to one side, use a dropper to absorb the peritoneal fluid into a test tube, put it in an ice bath, centrifuge at 500×g for 5 minutes, remove the supernatant, and gently shake the precipitate with 2ml of Hank solution, take 1ml of the suspension , Hank solution 1ml, antigen (10 μg / ml) 1ml, test drug 0.1ml, mix well and place in a 37°C water bath for 5 minutes, take out 1-2 drops of mast cells at the bottom of the test tube with a dropper, drop on the wave plate, and mix with l After mixing with 0....

Embodiment 2

[0021] Example 2 Histamine release test of rat peritoneal mast cells:

[0022] Method: Rats were sensitized in the same way as above, and peritoneal mast cells (MC) were collected after 14-21 days. Collect MCs: Rats were bled to death from the carotid artery, and buffered at 37°C (mM) with Nac1 150, Kc1 0.7, Cacl 0.9, Na 2 HPO 4 4.3, KH 2 PO 4 3.5, Glucose 5.6, pH 7.2 flush the peritoneal cavity, 15m1×2. The peritoneal washings were collected and placed in siliconized test tubes in an ice bath (the above experimental steps were all carried out at 4°C). Centrifuge at 500×g for 5 minutes, and remove the supernatant. Shake the precipitate with an appropriate amount of buffer solution to obtain the rat peritoneal MC suspension.

[0023] Antigen induced MC to release histamine: draw 0.4ml of MC suspension of sensitized rats, add phosphatidylserine 10μg / ml, add various concentrations of test drugs (37°C, warm bath for 5min), add refined trichosanthin antigen 10μg / ml, make T...

Embodiment 3

[0030] Example 3 Rat peritoneal neutrophil β-glucuronidase release test:

[0031] Method: collection of neutrophils (NP) in rat peritoneal cavity: rats were anesthetized with ether, and 25ml of 0.7% glycogen saline was injected intraperitoneally. After 4 hours, the rats were killed by carotid artery bleeding, the abdominal cavity was opened, and the peritoneal fluid was carefully sucked (do not touch the intestinal tube), and HBSS (mM, NaCl 138.0, KC1 5.4, CaC1 21.8, HEPES 20, Clucose 5.6, 0.1% BSA, pH 7.4) at 4°C Equally dilute, centrifuge at 250×g for 5min, discard the supernatant, add 2ml of ice water to the precipitate, add 2ml of 1.8% NaCl solution after 2sec, centrifuge, remove the supernatant, resuspend in HBSS, centrifuge to remove the supernatant to prepare NP suspension . After smear, Wright staining inspection, NP purity> 95%, trypan blue inspection cell viability> 95%. fMLP induces NP release: NP suspension lml (5×10 6 ml / NP) into a siliconized glass test tube, ...

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Abstract

The invention provides use of 5,7-methoxy-3,4'-flavonol in resisting of respiratory tract inflammatory diseases and relates to application of the 5,7-methoxy-3,4'-flavonol in preparation of drugs forresisting the respiratory tract inflammatory diseases. According to the use, proven by a series of experiments, 7-methoxy-3,4'-flavonol has obvious inflammation resisting, oxidation resisting, tracheacontraction reaction resisting activity; absorption can be achieved through oral drug administration, a relatively high drug effect is displayed, the bioavailability is 10% to 25%, and the 7-methoxy-3,4'-flavonol can be prepared into oral application preparations, injections and inhalants. The 5,7-methoxy-3,4'-flavonol can replace glucocorticoid preparations and is applicable to various respiratory tract inflammatory diseases such as bronchial asthma, acute bronchitis, chronic obstructive pulmonary disease, acute / chronic lung injury and respiratory distress and pulmonary fibrosis.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of 5,7-methoxy 3,4'hydroxyflavone in the preparation of medicines for resisting respiratory inflammation diseases. Background technique [0002] Bronchial asthma and chronic obstructive pulmonary disease have a high incidence and are common respiratory inflammatory diseases, mainly due to air pollution and environmental changes. Viral and bacterial infections of the lungs caused by environmental changes often induce acute bronchitis, acute / chronic lung injury, and respiratory distress. However, severe stages of bronchial asthma, chronic obstructive pulmonary disease, acute / chronic lung injury, and respiratory distress can all produce difficult-to-treat pulmonary fibrosis. The common clinical symptoms of these diseases are asthma, dyspnea, and chest tightness, which affect the quality of life of patients and are life-threatening in severe cases. It is very imp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K9/72A61K9/16A61K9/20A61K9/48A61K47/06A61K47/26A61P11/00A61P11/06
CPCA61K9/0073A61K9/1652A61K9/2054A61K9/4866A61K31/352A61K47/06A61K47/26A61P11/00A61P11/06
Inventor 谢诒诚董新威贾永良沈剑金亚超谢强敏
Owner 杭州勃锐思莫生物医药科技有限责任公司
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