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Dactylicapnos scandens derivative, pharmaceutical composition thereof, preparation method and application

A compound and pharmaceutical technology, which is applied in the field of preparation of drugs for treating pain, can solve problems such as the structure and medicinal activity of compounds that have not been reported

Active Publication Date: 2019-05-28
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And there is no structure and medicinal activity report of the compound involved in the present invention in the prior art

Method used

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  • Dactylicapnos scandens derivative, pharmaceutical composition thereof, preparation method and application
  • Dactylicapnos scandens derivative, pharmaceutical composition thereof, preparation method and application
  • Dactylicapnos scandens derivative, pharmaceutical composition thereof, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Separation and purification of compounds 1 and 2:

[0052] Take 3.9 kg of air-dried Zijinlong plant roots, grind them, heat them with 80% ethanol at 70°C, and extract them under reflux for 3 times, recover the solvent, concentrate to a small volume, add 1% HCl to adjust the pH value to 2, and extract 3 times with ethyl acetate. Once, the aqueous layer was adjusted to pH 9 with 10% ammonia water, then extracted 3 times with ethyl acetate, the ethyl acetate layer (104g) was concentrated, and after the ethyl acetate part was mixed with silica gel, 700g, 200-300 mesh silica gel was carried out. Column chromatography, with chloroform / methanol gradient elution segmented, the distribution ratio is chloroform / methanol 10:0, 20:1, 10:1, 8:1, 5:1, 3:1, 1:1, according to each 300 mL portions were pooled into 7 pooled Frs 1-7. Component Fr3 uses methanol / water 35:65, 50:50, 60:40, 70:30, 80:20, 90:10, 100:0 as the eluent, TLC detects the same component of the merged spot to obtain...

Embodiment 2

[0080] The four compounds in Example 1 can all activate TRPV1 ion channels, and may have better analgesic effects than the positive control drug capsaincin. The experimental methods and results are as follows:

[0081] 1. Materials and methods:

[0082] 1.1 Human embryonic kidney cell (HEK293) cell culture and transfection

[0083] 1.1.1 Cell recovery

[0084] When the cells are thawed, the frozen cells should be thawed quickly, and the frozen tube can be shaken from time to time to make it pass through the most vulnerable temperature range (-5-0°C) as soon as possible to ensure high cell survival rate, good growth and shape. Specific steps are as follows:

[0085] ①Take out the cells from the liquid nitrogen tank, put them into warm water at 37°C to thaw quickly and stir constantly, so that the cells in the cryopreservation tube can be thawed as soon as possible (within one minute), and then take out the cells under sterile conditions.

[0086] ② After aseptically removing ...

Embodiment 3

[0114] Examples of structural modification and modification of compounds 1 and 2:

[0115]

[0116] Tested by the method of Example 2, the modified compound 3-6 has similar activity to compounds 1 and 2.

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PUM

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Abstract

The invention provides a Dactylicapnos scandens derivative and a stereoisomer or a pharmaceutically acceptable salt thereof with analgesic activity, an extract and a pharmaceutical composition containing them, and a preparation method and application of the Dactylicapnos scandens derivative and the stereoisomer or the pharmaceutically acceptable salt thereof to preparation of drugs for treating pain.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, and in particular relates to novel skeleton isoquinoline alkaloid aurinoid derivatives and their stereoisomers, pharmaceutically acceptable salts, and pharmaceutical compositions thereof, their preparation methods and their use in the preparation and treatment of Use in Pain Medicine. Background technique: [0002] Pain is a worldwide problem. The drugs currently used clinically to treat pain are mainly opioids and non-steroidal drugs. Drug resistance and dependence limit the clinical use of opioids, and long-term use of non-steroidal drugs that can easily cause gastrointestinal reactions, coagulation disorders, and allergic reactions has also attracted much attention. Therefore, in order to meet the current clinical needs, it is urgent to develop a drug without addiction, dependence, low side effects and clear analgesic effect. [0003] TRPV1 refers to "transient receptor potential cation ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/18A61K31/473A61P29/00A61P25/00A61P21/00
CPCY02A50/30
Inventor 罗晓东刘亚平王蓓赖仞罗雷赵云丽尚建华
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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