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Natural antiepileptic active compounds and their use in pharmaceutical preparations

An anti-epileptic and compound technology, applied in the field of natural anti-epileptic active compounds and their pharmaceutical preparations, can solve problems such as difficulty in quality control, unknown targets, and complex components of Qingyang ginseng tablets

Active Publication Date: 2018-03-30
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the composition of Qingyangshen Tablets is complex, which brings certain difficulties to quality control, and the target of action is unknown. Clinically, it is mainly used in combination with antiepileptic drugs such as phenytoin or phenobarbital.

Method used

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  • Natural antiepileptic active compounds and their use in pharmaceutical preparations
  • Natural antiepileptic active compounds and their use in pharmaceutical preparations
  • Natural antiepileptic active compounds and their use in pharmaceutical preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0170] Evaluation of antiepileptic effect of compound cynawilfoside A (formula VI) in vivo:

[0171] The preparation method of the compound cynawilfoside A: 10kg of fresh Geshanxiao roots, peeled and sliced ​​to obtain 2.7kg of dry product, crushed and extracted three times with 95% ethanol percolation, each time for 2-3 days, combined extracts, concentrated under reduced pressure to obtain Geshan Disinfected alcoholic extract, suspend the extract in water, extract with ethyl acetate to obtain ethyl acetate extract, mix the sample with 100 mesh silica gel, separate with silica gel column chromatography (200-300 mesh silica gel), and use chloroform- Gradient elution with methanol (10:1→5:1) yielded components Fr1-Fr9. Fr6 was further purified repeatedly with petroleum ether-acetone and preparative HPLC to obtain pure compound cynawilfoside A (1.4 g).

[0172]

[0173] The physical and chemical data of the compound cynawilfoside A are as follows: white amorphous powder, easi...

Embodiment 2

[0178] Evaluation of antiepileptic effect of compound wilfoside C1N (formula IV) in vivo:

[0179] The preparation method of Wilfoside C1N: a. 10kg of fresh Auricularia saponis root tuber, sliced ​​and dried to obtain 3Kg dry product, pulverized and extracted three times with 95% ethanol, the extracts were combined, concentrated under reduced pressure to obtain ethanol extract, mixed with silica gel, passed 200-300 mesh silica gel, gradient elution with petroleum ether-acetone (3:1→2:1), and then gradient elution with chloroform-methanol (10:1→5:1) to obtain components Fr1-Fr6. Fr3 was further purified repeatedly by petroleum ether-acetone silica gel column chromatography to obtain pure compound wilfoside C1N (1.5g); b. 10kg of fresh Geshanxiao root, peeled, sliced ​​and dried to obtain 2.7kg dry product, pulverized and diafiltered with 95% ethanol Extract three times, each time for 2-3 days, combine the extracts, concentrate under reduced pressure to obtain the alcohol extrac...

Embodiment 3

[0185] Evaluation of compound wilfoside K1N (formula V) antiepileptic effect in vivo:

[0186] The preparation method of Wilfoside K1N: a. 10kg of fresh cowhide tuber, sliced ​​and dried to obtain 3kg of dry product, pulverized and extracted three times with 95% ethanol, the extracts were combined, concentrated under reduced pressure to obtain ethanol extract, mixed with silica gel, passed 200- 300 mesh silica gel, gradient elution with petroleum ether-acetone (3:1→2:1), and then gradient elution with chloroform-methanol (10:1→5:1) to obtain fractions Fr1-Fr6. Fr3 was further purified repeatedly by petroleum ether-acetone silica gel column chromatography to obtain pure compound wilfoside K1N (2.5g); b. 10kg of fresh Geshanxiao root, peeled and sliced ​​to obtain 2.7kg of dry product, crushed and percolated with 95% ethanol Extract three times, each time for 2-3 days, combine the extracts, concentrate under reduced pressure to obtain the alcohol extract of Geshanxiao, suspend t...

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Abstract

The present invention relates to a natural anti-epilepsy activity compound and uses of the natural anti-epilepsy activity compound in pharmaceutical preparations. The present invention discloses different monomer compounds having diametrically opposed effects such as epilepsy promoting and epilepsy resistance in Cynanchum otophyllum. According to the present invention, particularly the single component is respectively extracted from Cynanchum, C.auriculatum Royle exWight and C.wilfordii Hemsl, and experiment results prove that each compound has anti-epilepsy activity.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular, the invention relates to natural antiepileptic active compounds and their application in pharmaceutical preparations. Background technique [0002] Epilepsy, also known as cerebral epilepsy or sheep epilepsy, is a syndrome of chronic recurrent transient brain dysfunction. According to statistics, the incidence of epilepsy in my country is about 23 / 100,000 per year, and the prevalence rate is 3.5‰-4.8‰. Seizures can cause a series of symptoms, and convulsions are one of the typical symptoms of epilepsy, including repetitive movements of limbs, abnormal behavior, and general convulsions with loss of consciousness, etc., and even cause body damage or death. The treatment of epilepsy includes various methods such as drug therapy, surgical therapy, physical therapy and psychotherapy, among which drug therapy is the most commonly used and most important means at present. Currently clinically...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J17/00A61K31/704A61P25/08G01N33/15
Inventor 赵维民周娟李金龙李春启陈振华张勇高召兵郭胜亚
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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