Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Application of 8-alkylberberine salt in the preparation of drugs for the prevention and treatment of lung cancer

A technology of berberine salt and berberine, which is applied in the field of medicine, can solve problems such as long-chain 8-alkyl berberine salts that have not yet been reported, and achieve good anti-lung cancer effect

Inactive Publication Date: 2020-06-05
SOUTHWEST UNIV
View PDF9 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there is no report on long-chain 8-alkylberberine salts in anti-lung cancer

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of 8-alkylberberine salt in the preparation of drugs for the prevention and treatment of lung cancer
  • Application of 8-alkylberberine salt in the preparation of drugs for the prevention and treatment of lung cancer
  • Application of 8-alkylberberine salt in the preparation of drugs for the prevention and treatment of lung cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: 8-dodecyl berberine hydrochloride

[0035]

[0036] It is prepared as follows:

[0037] ①. Dry all reaction glass instruments, weigh 0.12mol of dried magnesium chips and place in a 250mL three-necked flask, use 60mL of anhydrous tetrahydrofuran as the reaction solvent, add 0.1mol of n-dodecane chloride under nitrogen protection, Prepare the corresponding Grignard reagents.

[0038] ②. Weigh 0.05mol of dry berberine hydrochloride and place it in a 500mL three-necked flask, add 25mL of anhydrous tetrahydrofuran to form a suspension of berberine hydrochloride, and then place it in an ice bath to 10°C under nitrogen protection.

[0039] ③. Slowly add the prepared Grignard reagent to the berberine hydrochloride salt suspension under nitrogen protection and ice bath, and stir at the same time. After the addition, remove the ice bath, return to room temperature, and heat to reflux for 2 hours to complete the reaction.

[0040] ④, centrifuge the reaction solu...

Embodiment 2

[0043] Example 2: 8-tetradecylberberine bromate

[0044]

[0045] Its preparation process is as follows:

[0046] ①. Dry all reaction glass instruments, weigh 0.12mol of dried magnesium chips and place in a 250mL three-neck flask, use 60mL of anhydrous ether as the reaction solvent, add 0.1mol of n-tetradecane bromide under nitrogen protection, Prepare the corresponding Grignard reagents.

[0047] ②. Weigh 0.05mol of dry berberine hydrochloride and place it in a 500mL three-neck flask, add 25mL of anhydrous ether to form a suspension of berberine hydrochloride, and then place it in an ice bath to 0°C under nitrogen protection.

[0048] ③. Slowly add the prepared Grignard reagent to the berberine hydrochloride salt suspension under nitrogen protection and ice bath, and stir at the same time. After the addition, remove the ice bath, return to room temperature, and heat to reflux for 2 hours to complete the reaction.

[0049] ④, centrifuge the reaction solution, take the sup...

Embodiment 3

[0052] Embodiment 3: 8-hexadecyl berberine iodate

[0053]

[0054] Its preparation process is as follows:

[0055] ①. Dry all the reaction glass instruments, weigh 0.12mol of dried magnesium chips and place them in a 250mL three-neck flask, use 60mL of dioxane as the reaction solvent, add 0.1mol of n-hexadecane bromide under nitrogen protection , to prepare the corresponding Grignard reagents.

[0056] ②. Weigh 0.05 mol of dry berberine hydrochloride salt into a 500mL three-neck flask, add 25mL of dioxane to form a suspension of berberine hydrochloride salt, and then ice-bath to 0°C under nitrogen protection.

[0057] ③. Slowly add the prepared Grignard reagent to the berberine hydrochloride salt suspension under nitrogen protection and ice bath, and stir at the same time. After the addition, remove the ice bath, return to room temperature, and heat to reflux for 2 hours to complete the reaction.

[0058] ④, centrifuge the reaction solution, take the supernatant, then ad...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses the application of 8-alkyl berberine salt to the preparation of a medicine for preventing and treating lung cancer. The 8-alkyl berberine salt adopts a molecular structural formula as shown in the specification, wherein X is F-, Cl-, Br- or I-, R1 is CnH2n+1, and n is 12-22. The compound 8-alkyl berberine salt has a relatively good anti-lung cancer effect, and especially when the carbon number of an alkyl chain is 16-22, the anti-lung cancer effect thereof is obviously superior to that of berberine salt; the 8-alkyl berberine salt can be applied to the preparation of the medicine for preventing and treating the lung cancer.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of 8-alkyl berberine salt in the preparation of drugs for preventing and treating lung cancer. Background technique [0002] Berberine, also known as berberine, is one of the main active ingredients of Coptis chinensis, a quaternary ammonium ion-type isoquinoline alkaloid. Berberine has pharmacological effects such as antibacterial, anti-inflammatory, antipyretic, hypoglycemic, hypolipidemic, and anticancer. It is most commonly used clinically to treat bacillary dysentery and gastroenteritis. Studies have found that berberine hydrochloride and some of its structural derivatives have various pharmacological activities such as antibacterial, anti-inflammatory, anti-tumor, hypoglycemic and hypolipidemic. Therefore, research on the pharmacological effects and structural modifications of berberine hydrochloride has become a research topic hotspot. [0003] For exa...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4375A61P35/00
CPCA61K31/4375
Inventor 李学刚叶小利
Owner SOUTHWEST UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com