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

Glaucocalyxin B, derivative, preparation method and application thereof

A technology of cyanine B and its derivatives, which can be applied in the direction of drug combinations, pharmaceutical formulas, medical preparations containing active ingredients, etc., and can solve the problems of unreported pharmacological effects

Inactive Publication Date: 2010-10-06
SUZHOU JINHAO MEDICINE DEV
View PDF0 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its pharmacological effects have not been reported

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
  • Glaucocalyxin B, derivative, preparation method and application thereof
  • Glaucocalyxin B, derivative, preparation method and application thereof
  • Glaucocalyxin B, derivative, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] The preparation of embodiment 1 cyanine B (GLB) derivative:

[0080] The chemical reagents used in the following preparation process are analytically pure unless otherwise specified.

[0081] A method for preparing gliphyllin (GLB) derivatives by using fragrant tea herbs (aerial parts) as a raw material, purifying gliphyllin (GLB), and modifying its structure with a polypeptide cNGQGEQc, specifically comprising the following steps:

[0082] Step 1: Crush

[0083] Take fragrant tea and vegetable medicinal materials (aerial parts) and pulverize to 20 mesh to 50 mesh.

[0084] Step 2: Extract

[0085] Step 2.1: Mix the pulverized product obtained in step 1 with 95% ethanol (A.R.) at a volume ratio of 1:6 to 1:10, heat, reflux at 80°C to 90°C for 1 to 2 hours, extract and filter, An extract and a residue are obtained.

[0086] Step 2.2: Mix the residue obtained in step 2.1 with 95% ethanol (A.R.) at a volume ratio of 1:6 to 1:10, heat, reflux at 80°C to 90°C for 1 to 2 ...

Embodiment 2

[0131] The preparation of embodiment two cyanine B (GLB) derivatives:

[0132] Adopt the following technical parameters to improve the preparation method of embodiment one:

[0133] In the step 2.1, the pulverized product is mixed with 95% ethanol (A.R.) in a volume ratio of 1:6.5, heated, refluxed at 82° C. for 1.8 hours, and then extracted and filtered.

[0134] In the step 2.2, the residue is mixed with 95% ethanol (A.R.) at a volume ratio of 1:9.5, heated, refluxed at 88° C. for 1.2 hours, extracted and filtered, and this step is repeated once.

[0135] In the step 3.1, the extract is heated and concentrated under reduced pressure at a temperature of 57°C.

[0136] In the step 3.2, the primary concentrate and water were mixed in a volume ratio of 1:8.5, stirred at room temperature and then left to stand for 11 hours before the supernatant and solid were separated.

[0137] In the step 3.3, the solid was mixed with ethyl acetate (A.R.) at a volume ratio of 1:5.5, stirred ...

Embodiment 3

[0161] The preparation of embodiment three cyanine B (GLB) derivatives:

[0162] Adopt the following technical parameters to improve the preparation method of embodiment one:

[0163] In the step 2.1, the pulverized product is mixed with 95% ethanol (A.R.) in a volume ratio of 1:7.5, heated, refluxed at 84° C. for 1.6 hours, and then extracted and filtered.

[0164] In the step 2.2, the residue is mixed with 95% ethanol (A.R.) at a volume ratio of 1:8.5, heated, refluxed at 86° C. for 1.4 hours, extracted and filtered, and this step is repeated once.

[0165] In the step 3.1, the extract is heated and concentrated under reduced pressure at a temperature of 59°C.

[0166] In the step 3.2, the primary concentrate and water were mixed at a volume ratio of 1:8.5, stirred at room temperature and then left to stand for 10 hours before the supernatant and solid were separated.

[0167] In the step 3.3, the solid was mixed with ethyl acetate (A.R.) at a volume ratio of 1:5.5, stirre...

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 a glaucocalyxin B derivative, a preparation method and application thereof. The glaucocalyxin B (GLB) is used as a main body of the glaucocalyxin B (GLB) derivative which is a diterpenes substance and has an ent-kaurane structure, carbonyl, polypeptide cNGQGEQc and / or hydroxyl. In the invention, rabdosia amethystoides medicinal material (part on the above-ground) is used as a raw material, and the preparation method of the derivative is as follows: crashing the raw material, extracting, treating solution, passing through a column, recrystallizing and carrying out other steps to obtain the glaucocalyxin B (GLB), and further carrying out acetylation on the glaucocalyxin B (GLB) and the polypeptide cNGQGEQc to obtain the glaucocalyxin B (GLB) derivative. The glaucocalyxin B (GLB) derivative has high anticancer activity, can significantly inhibit a plurality of tumor cells such as cells in lung cancer, liver cancer, nasopharyngeal carcinoma, lymphoma, melanoma and myelomatosis, especially has a targeting effect on the lung caner and can pertinently treat the lung caner.

Description

technical field [0001] The present invention relates to a cyanine B (GLB) derivative, in particular to a cyanine B (GLB) derivative containing a polypeptide. [0002] The present invention also relates to the preparation method of the glycocalyxin (GLB) derivative containing the polypeptide and its application in treating cancer. Background technique [0003] Fragrant tea is a plant belonging to the family Lamiaceae, which is widely distributed in Henan, Hubei, Sichuan, Guizhou, Shaanxi, Shanxi, Hebei and other provinces. The whole herb has antibacterial and anti-inflammatory effects, and is used in the folk to treat acute jaundice hepatitis, acute cholecystitis, bruises, snake bites, impetigo, etc. Its pharmacological effects have not been reported. The pharmacological effect of the crude preparation of Hubei Xiangchacai was studied, and the results showed that it had obvious inhibitory effect on Ehrlich ascites carcinoma tumor cells in vivo and in vitro. [0004] Plants...

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
IPC IPC(8): C07K7/06C07K7/08C07C69/16A61K38/08A61K38/10A61K31/22A61P35/00A61P35/02
Inventor 李云森陈子珺檀爱民程萍雷启福
Owner SUZHOU JINHAO MEDICINE DEV
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