Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Amide alkaloid and preparation method thereof

A technology of alkaloids and amides, which is applied in the field of medicine, can solve the problems of easy recurrence after drug withdrawal, influence on serotonin, and large side effects, and achieve the effect of shortening the immobility time of forced swimming

Inactive Publication Date: 2011-05-25
GUANGXI UNIV
View PDF0 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the antidepressant synthetic drugs widely used in the market only affect the content of individual monoamine neurotransmitters. For example, fluoxetine only affects the content of 5-hydroxytryptamine. It is difficult to obtain satisfactory curative effect for a single link of the drug, and the synthetic Most antidepressants have defects such as narrow antidepressant spectrum, large side effects, high drug price and easy relapse after drug withdrawal

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
  • Amide alkaloid and preparation method thereof
  • Amide alkaloid and preparation method thereof
  • Amide alkaloid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Take 6.3kg of the whole plant of Betelgeus chinensis, dry, pulverize, pass through a 40-mesh sieve, and use 6 times the amount of medicinal materials in 95% ethanol (mL / g) to reflux extract twice for 2 hours each time, filter while hot, and combine The filtrate was concentrated under reduced pressure to obtain 200 g of ethanol extract. The extract was suspended in 700mL of deionized water, extracted five times with equal volumes of petroleum ether and ethyl acetate successively, the extracts were combined, concentrated under reduced pressure and evaporated to remove the solvent to obtain 54g of petroleum ether extract and 62g of ethyl acetate extract , Water extract 84g.

[0022] After dissolving 25g of ethyl acetate extract with solvent, mix the sample with an equivalent amount of 100-200 mesh silica gel, evaporate the solvent, weigh 450g of 100-200 mesh silica gel wet packing column (6 × 50cm), and press petroleum ether: acetic acid Ethyl ester = 9:1, 8:2, 6:4, 4:6, ...

Embodiment 2

[0025] Using the preparation method of the present invention, the amide alkaloid N-(2'-hydroxyl-ethyl)-N-methyl-3,4-methylenedioxy Base-phenyl, its structure is identified, test method and result are as follows:

[0026] Physical properties: white powder, easily soluble in ethyl acetate, acetone, methanol and other organic solvents, hardly soluble in water.

[0027] EI / MS (m / z): 224 (M+1, 9.75), 223 (M + , 5.27), 178 (4.28), 165 (61.49), 149 (3.99), 121 (12.63), 77 (57.33), 74 (5.34), 45 (100.00).

[0028] IR (KBr): 3448.08cm -1 、2925.84cm -1 、2848.00cm -1 、1439.15cm -1 、1711.57cm -1 、1633.73cm -1 、1267.89cm -1 、1230-1030cm -1 、1044.02cm -1 .

[0029] 1 H-NMR and 13 See Table 1 for C-NMR data.

[0030] The NMR data comparison table (CDCl 3 )

[0031]

[0032]

Embodiment 3

[0034] Antidepressant activity test

[0035] 1. Administration method and animal grouping

[0036] Petroleum ether extract, ethyl acetate extract and compound of the present invention are dispersed in 0.2% CMC-Na aqueous solution and are prepared into suspension; Positive control medicine clomipramine hydrochloride is dispersed in water and is prepared into suspension; Water extract Make a solution with distilled water.

[0037] The doses for intragastric administration of mice are: petroleum ether extract, ethyl acetate extract and water extract 50mg·kg each -1 , 100mg·kg -1 ; Clomipramine hydrochloride 30mg·kg -1 0.2% CMC-Na aqueous solution of equal volume of the blank control group; compound of the present invention 5mg·kg -1 , 10mg·kg -1 . The volume of animal administration was 0.2mL / 10g.

[0038] Take 96 male Kunming mice with a body weight of (20±2) g, raise them in a room at (25±1)°C, drink water and eat freely, and adapt for 1 week. They were randomly divided...

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 an amide alkaloid and a preparation method thereof. The name of the amide alkaloid is N-(2'-hydroxyl-ethyl)-N-methyl-3,4-methylenedioxy-benzene. The extraction method comprises the following steps: grinding dry herb of tonkin pepper, performing refluxing extraction with solvent, concentrating the extraction solution to obtain extractum; performing extraction to extractum with petroleum ether, ethyl acetate and water to obtain different polar parts; separating the ethyl acetate part through the silica gel column chromatography, performing gradient elution with petroleum ether-ethyl acetate to obtain each part; and combining the parts with the target compound, separating through the silica gel column chromatography, repeatedly eluting with the eluent consisting of petroleum ether-ethyl acetate, and recrystallizing with petroleum ether-acetone to refine and obtain the compound of the invention. The compound of the invention can be used to prepare medicines for curing the depression.

Description

technical field [0001] The invention belongs to the field of medicine, and specifically relates to an amide alkaloid isolated from a betel plant, a preparation method and application thereof. Background technique [0002] Depression is a mental illness characterized by persistent mood disorders. Statistics show that the lifetime prevalence of depression is 6.1-9.5%, about 13-20% of people have experienced depression once or more in their lives, and 15% of patients with severe depression die due to suicide. With the development of society, depression has a growing trend. [0003] The disorder of monoamine neurotransmitter metabolism in the central nervous system is the main biochemical feature of depression, and increasing the content of monoamine neurotransmitters in the brain can achieve the purpose of antidepressant. However, the antidepressant synthetic drugs widely used in the market only affect the content of individual monoamine neurotransmitters. For example, fluoxe...

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): C07D317/68A61K31/36A61P25/24
Inventor 杨克迪葛利王丽君彭盼文衍宣龙云飞
Owner GUANGXI UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
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