Application of sodium houttuyfonate in preparation of medicine for preventing and treating nervous system diseases taking Kv7/M channel as target spot

A neurological disease, a technology for sodium houttuyniacin, which is applied in the field of drugs for neurological diseases, and can solve the problems of undiscovered antiepileptic activity, analgesia, and changing neuronal excitability of houttuynia sodium or any derivative thereof. , to achieve the effects of good toxicological safety, small side effects and stable metabolism

Active Publication Date: 2021-06-11
HEBEI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Before the present invention, it was not found that houttuyfonate sodium or any of its derivatives can affect Kv7 / M current and significantly change the mechanism of action of neuron excitability reports and patents, There is also no report that houttuyfonate sodium or any derivative thereof has antiepileptic activity and analgesia, or that it is used as a raw material to prepare pharmaceutical preparations for the treatment of neuropsychiatric diseases such as epilepsy and pain.

Method used

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  • Application of sodium houttuyfonate in preparation of medicine for preventing and treating nervous system diseases taking Kv7/M channel as target spot
  • Application of sodium houttuyfonate in preparation of medicine for preventing and treating nervous system diseases taking Kv7/M channel as target spot
  • Application of sodium houttuyfonate in preparation of medicine for preventing and treating nervous system diseases taking Kv7/M channel as target spot

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Electrophilic tester

[0025] (1) Test compound: sodium fish

[0026] (2) Test method: Culture of Chinese hamster ovary cells (CHO): CHO cells in KCNQ2 / Q3 channels are cultured in 10% fetal bovine serum, 500 ug / ml hygromycin and g418, 100 u / ml penicillin and chain DMEM culture fluid, pancreatic enzyme digestion. Cells were laid in a 12 mm round cover glass, 24-well plate culture.

[0027] The film wrench technology records the cell membrane current: the diaphragm pliers amplifier adopts HEKA-EPC10. Both mymium B (final concentration 0.1 to 0.2 mg / ml) is used in the electrode. After the microelectrode polishes, the inner liquid in which the electrode is applied, and the resistance value is controlled at 2 to 4 MΩ. Electrode induced by (mm): KCl 160, HEPES 5, MGCL 2 3, CACL 2 1, EGTA 3, use KOH to adjust pH to 7.4; extracellular fluid components (mm): NaCl 160, KCl 2.5, HEPES 10, Glucose8, MGCL 2 1, CACL 2 5. After the microelectrode is sealed with the cell membrane, ...

Embodiment 2

[0031] Pharmacodynamics experiment of houtu saffin sodium

[0032] Pentylphenazole PTZ induces seizures:

[0033]Experimental medication: 2% Tween 20 suspension of Sodium Houttuyfonate, the control group used 2% Tween 20 mixer of Ruckill Plus. Experimental method: Each group of male mice induced epilepsy by intraperitoneal injection of glutarazole, observed that epilepsy latency during 90 minutes, seizures, seizures, and epilepsy level. The peritoneal injection of napper sodium is 12.5 mg / kg, 25 mg / kg, 50 mg / kg, and the control group is 15 mg / kg. The experimental results are shown in Table 1, and sodium fish, sodium can significantly reduce the duration of epilepsy, and seizures and seizures. In summary, the sodium of hookuemen is significantly anti-epilepsy.

[0034] Table 1: The sodium of Houttuynia is significantly reduced the continuous episode of epileptic seizures, the number of epilepsy, the level of epilepsy, and mortality.

[0035]

[0036] Note: * The significa...

Embodiment 3

[0039] The tablet is prepared according to the method known in the art, and each piece contains the following ingredients:

[0040] 50 mg of sodium fish, 70 mg of lactose, 3 mg of stearate, and 130 mg of polyvinylpyrrolidone.

[0041] Capsules are prepared according to methods known in the art, and each capsule contains the following ingredients:

[0042] Hydae is 50 mg, lactose 70 mg, corn starch 25 mg, stearate 1 mg, polyvinylpyrrolidone 130 mg.

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Abstract

The invention provides an application of sodium houttuyfonate in preparation of a medicine for preventing and treating nervous system diseases taking a Kv7/M channel as a target spot, sodium houttuyfonate or any derivative of sodium houttuyfonate, or a natural, synthetic or semi-synthetic sodium houttuyfonate-containing mixture or a sodium houttuyfonate-containing composition of sodium houttuyfonate, and the sodium houttuyfonate or any derivative of sodium houttuyfonate has the effects of increasing the Kv7/M current, and changing the action mechanism of cell excitability obviously, the Kv7/M current can be used for preparing medicines for preventing, treating and assisting in treating nervous system diseases and symptoms, the action mechanism of obviously changing the cell excitability by increasing the Kv7/M current is never reported, and the action mechanism is completely different from the action mechanism of the existing medicine application of sodium houttuyfonate.

Description

Technical field [0001] The present invention relates to the field of neurological disease drug technology, in particular to use of a nervous system disease drug in preparing prevention and treatment of KV7 / M channels with kv7 / m channels as a target. Background technique [0002] Neurist system disease is one of the most popular diseases in the future, affecting more than half of the population. Neurismal system disease is very lack of effective treatment, in recent years, innovative drugs listed at home and abroad can be in number. At the same time, the existing drug adverse reactions are large, and multiple long-term uses create addiction, damage memory, sensitivity, and mutual movement. In addition, the domestic treatment of neuropsychiatric disease market is occupied by imported drugs, high prices, and long-term economic problems. Many neuroplastic system diseases (such as epilepsy, pain, depression, anxiety, stroke, insomnia, mania, schizophrenia, spasm, Parkinson's disea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/185A61P25/08A61P25/00A61P29/00A61P25/24A61P25/22A61P9/10A61P25/20A61P25/18A61P25/16A61P25/28A61P25/14A61P21/02
CPCA61K31/185A61P25/08A61P25/00A61P29/00A61P25/24A61P25/22A61P9/10A61P25/20A61P25/18A61P25/16A61P25/28A61P25/14A61P21/02
Inventor 张凡曹鹏程子豪王玉悦耿丹丹王润萌郑荣李亚宁
Owner HEBEI MEDICAL UNIVERSITY
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