Application of dehydrocorydaline and scoulerine to medicament production

A technology of cordydine and stersonine, which is applied in the field of medicine, can solve problems such as no research reports on anti-hepatitis B virus activity, and achieve significant anti-hepatitis B virus activity and excellent effect

Inactive Publication Date: 2012-02-01
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have been no research reports on the anti-hepatitis B virus activity of the original berberine-type alkaloid components - dehydroclindrine and cordyline sternerine, nor have there been reports on their use in the treatment of hepatitis

Method used

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  • Application of dehydrocorydaline and scoulerine to medicament production
  • Application of dehydrocorydaline and scoulerine to medicament production
  • Application of dehydrocorydaline and scoulerine to medicament production

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Extraction, Separation and Structural Identification of Dehydroclindine and Steiner's Corydine

[0028] After crushing 9kg of dry whole herb of Litectin chinensis, ultrasonically extract 3 times with ethanol, each time with 75L solvent. After reclaiming solvent under reduced pressure, the obtained liquid extract is uniformly dispersed in an appropriate amount of aqueous solution, after sherwood oil, ethyl acetate extraction, with equal volume water-saturated n-butanol extraction, obtains n-butanol extract (224.22g ). The extract was subjected to ODS reverse phase silica gel column chromatography (methanol-water) to obtain 20 fractions (Bu.1-Bu.20). Among them, Bu.5 was separated by silica gel column (chloroform-methanol) to obtain 5 fractions (Bu.5-1~Bu.5-5), and fraction Bu.5-1 was subjected to silica gel column chromatography (n-hexane-acetic acid Ethyl ester-ethanol) to obtain the alkaloid - cordydine (78 mg); Fraction Bu.6 was recrystallized from methano...

Embodiment 2

[0032] Embodiment 2 Preparation of anti-hepatitis B virus pharmaceutical composition injection of the present invention

[0033] In parts by weight, weigh 1 part of dehydrocorydine, 25 parts of polysorbate 80, and 20 parts of sodium chloride, dissolve and dilute to 2500 times the volume with water for injection, stir evenly, filter, pot, Sterilize to obtain dehydroclindine injection (specification: 0.8mg / 2mL).

Embodiment 3

[0034] Embodiment 3 Preparation of anti-hepatitis B virus pharmaceutical composition freeze-dried powder injection of the present invention

[0035] In parts by weight, take 1 part of cordidine, dissolve it with 400 parts of water for injection at 50-60 ° C, add 40 parts of lyophilized excipient mannitol, mix well, filter and sterilize, and test the drug Freeze-drying after the content is obtained, and the freeze-dried powder injection of cordydine sternerine is prepared.

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Abstract

The invention discloses application of dehydrocorydaline and scoulerine to medicament production. In the invention, a diagnostic kit for hepatitis B virus surface antigen and a diagnostic kit for hepatitis B virus e antigen are adopted to perform tests of resisting hepatitis B surface antigen and hepatitis B e antigen on protoberberine alkaloids scoulerine and dehydrocorydaline respectively. Results prove that the dehydrocorydaline and the scoulerine have remarkable hepatitis B virus resisting activity, and can be used for preparing hepatitis B virus resistant medicament.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular, the invention relates to the application of two kinds of proberberine-type alkaloids, dehydroclindine and cordydine styrenine, in pharmacy. Background technique [0002] Hepatitis B virus is caused by hepatitis B virus (HBV), a worldwide disease with high incidence, long course of disease, refractory cure and easy recurrence. According to the statistics of the World Health Organization, about 350 million people in the world are chronic hepatitis patients or asymptomatic virus carriers (HBsAg carriers). These patients with chronic hepatitis have a high risk of turning to liver cirrhosis and liver cancer, and more than 1 million people die from diseases related to hepatitis, liver cirrhosis and liver cancer every year. my country is one of the areas with high incidence of hepatitis, and there are currently about 30 million hepatitis B patients. According to statistics, 80% of live...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4375A61P31/20
Inventor 王冬梅王一飞杨得坡曾凡力程轩轩梁镇然蒋林朱龙平
Owner SUN YAT SEN UNIV
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