Application of C21 steroid glycoside in pharmacy

A technology of glycosides and steroids, applied in the field of C21 steroid glycosides, can solve problems such as large side effects, application limitations, toxic side effects, etc., and achieve the effects of less toxic side effects, low price, and antidepressant effect.

Active Publication Date: 2005-07-06
YUNNAN BAIYAO GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the 1950s, there were tricyclic antidepressants (TCA) that were effective for depressive symptoms, but they had serious side effects due to lack of selectivity, and the monoamine oxidase inhibitors (MAO1) that appeared later were also irreversible and non-selective. limited in application
Although the antidepressant chemical drugs currently used clinically have been greatly improved compared with the original tricyclic antidepressant drugs, they still have the disadvantage of relatively large side effects.

Method used

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  • Application of C21 steroid glycoside in pharmacy
  • Application of C21 steroid glycoside in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Take 10kg of the rhizome of Qingyangshen, crush it, extract it three times with 80% ethanol, combine the extracts, concentrate and recover the solvent. The concentrated solution was diluted with water, extracted three times with petroleum ether, the aqueous layer was extracted three times with chloroform, and the chloroform fractions were combined. Chloroform was recovered to obtain 300 g of light yellow powder, with a yield of 3.0%. Gained light yellow powder is the total glycosides of Qingyangshen, taking Qingyangshen aglycon as reference substance, referring to the drug standard (WS 3 -B-2343-97) method, the measured total glycoside content is 72.5%. The content of main aglycones in total glycosides was determined by HPLC method, and the results were: Qingyangshen aglycone content was 5.1%, and Kodatin content was 10.5%.

Embodiment 2

[0038] Take 10 kg of rhizomes of Kunming vine crown, crush them, extract three times with 80% ethanol, combine the extracts, concentrate and recover the solvent. The concentrated solution was diluted with water, extracted three times with petroleum ether, the aqueous layer was extracted three times with chloroform, and the chloroform fractions were combined. Chloroform was recovered to obtain 310 g of light yellow powder, with a yield of 3.1%. The obtained light yellow powder is the total glucosides of Kunming cuprosides. With Qingyang ginseng aglycone as the reference substance, refer to the drug standard (WS 3 -B-2343-97) method, the measured total glycoside content is 80.4%. The content of main aglycones in the total glycosides was determined by HPLC, and the results were: the content of Qingyangshen aglycone in the total glycosides was 6.0%, and the content of kudatingin was 15.2%.

Embodiment 3

[0040]Take 50g of total glycosides of Qingyangshen, dissolve it in 200ml of methanol, add 200g of silica gel with a particle size of 100 mesh, stir evenly, and evaporate the methanol to dryness. Take 1000 g of silica gel with a particle size of 300-400 mesh, and perform column chromatography according to a conventional method, and the elution system is chloroform-methanol (20:1-5:1), gradient elution. The eluate was collected to obtain 5 fractions, and the third fraction was subjected to repeated column chromatography on reversed-phase silica gel, eluting with methanol: water (60:40), to obtain 1.2 g of compound 1, which was qingyang shenside A. White powder, molecular formula: C 56 h 86 o 16 , Molecular weight: 932. Soluble in ethanol, methanol, ethyl acetate, chloroform.

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Abstract

The invention discloses the use of C21 steroid glycoside in pharmacy, wherein the systematic test shows that C21 steroid glycocide has low toxic and side effect, but has unique effect for treating psychogenia diseases with depression state, in particular for depression.

Description

technical field [0001] The present invention relates to the new application of C21 steroidal glycoside, especially the application in the field of pharmacy. Background technique [0002] Depression is an affective mental disorder. In 1999, the World Health Organization (WHO) estimated that the incidence rate accounted for 3% to 5% of the world's total population. Research on antidepressants has been very active in recent years. In the 1950s, there were tricyclic antidepressants (TCA) that were effective for depressive symptoms, but they had serious side effects due to lack of selectivity, and the monoamine oxidase inhibitors (MAO1) that appeared later were also irreversible and non-selective. limited in application. In 1988, Eli Lilly and Company of the United States launched the selective 5-hydroxytryptamine (5-HT) reuptake inhibitor (SSR1) fluoxetine (Prozac), which made progress in the treatment of depression. [0003] With the leap in cell mole...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61P25/24
Inventor 杨庆雄金和锴杨崇仁
Owner YUNNAN BAIYAO GROUP
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