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Application of valeriana jatamansi Jones part in preparation of N-type calcium channel inhibitor

A technology of calcium channel inhibitor and aromatic ether, which is applied to the application field of spider iridoid part in the preparation of N-type calcium channel inhibitor, can solve the problem that spider incense research is still not carried out, and achieve a broad The effect of the application foreground

Active Publication Date: 2015-06-24
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these previous research results have not carried out research on the specific mechanism of action of spider fragrance and related diseases, and there are fewer reports on the hydrolysis reaction of the active part of spider fragrance and the active part.

Method used

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  • Application of valeriana jatamansi Jones part in preparation of N-type calcium channel inhibitor
  • Application of valeriana jatamansi Jones part in preparation of N-type calcium channel inhibitor
  • Application of valeriana jatamansi Jones part in preparation of N-type calcium channel inhibitor

Examples

Experimental program
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Effect test

Embodiment 1

[0026] This embodiment provides a method for preparing the iridoid part of spider fragrance, the steps are as follows:

[0027] Take 1000 grams of spider incense medicinal material powder, add 3500 ml of 95% ethanol and put it in the reflux device for reflux for 3 hours, filter out the ethanol liquid after cooling, add 3000 ml of ethanol to the residue and reflux for 2 hours again, filter out the ethanol extract and merge it into the first ethanol filtrate to obtain The ethanol extract is about 6000ml, the ethanol extract is concentrated to the water suspension, and ethyl acetate is added to extract the spider iridoid part, which can effectively inhibit the Ntype calcium channel. The iridoid part of the spider fragrance is added with appropriate excipients, binders, and disintegrants and compressed into tablets to obtain 1000 tablets.

Embodiment 2

[0029] This embodiment provides a method for obtaining the hydrolyzate of the iridoid part, and the specific steps are as follows:

[0030] Add 1000ml of 0.01M hydrochloric acid aqueous solution to the part of the spider iridoid obtained in the above Example 1 to mix, rotate and stir for 1 hour, and neutralize it with 0.01M NAOH to PH = 7 after the reaction is stopped, and then dissolve it with ethyl acetate Extract and concentrate to obtain the hydrolyzate of the iridoid part, which can effectively inhibit the N type calcium channel.

Embodiment 3

[0032] Identification and verification of the active substance of the iridoid part of spider fragrance in Example 1

[0033] The spider iridoid part obtained in the above-mentioned embodiment 1, get 50g and use 100g silica gel (200-300 mesh) to mix the sample, put 10 times the amount of silica gel column (0.5kg, 200-300 mesh), mobile phase is petroleum ether: Acetone=50:1~0:1, 7 components were eluted (Fr 1-7). Fraction 4 (Fr.4, 2.8g) was further subjected to silica gel column chromatography (petroleum ether: acetone = 20:1~1:1 gradient elution) to obtain 4 fractions (sub Fr.4.1~4.4). Wherein the second subcomponent (sub Fr.4.2, 0.8 g) is subjected to MCI gel (60%~90% methanol gradient elution), gel sephadex LH-20 (methanol), reverse phase ODS (methanol: water=50 :50~90:10) was purified to obtain compound valeriandoid J (compound 1, as shown in formula II, 5 mg). Component 6 (Fr.6, 5.3 g) was obtained by an approximate method to obtain valtrate hydrine B8 (compound 2, repres...

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Abstract

The invention discloses an application of a valeriana jatamansi Jones part in preparation of an N-type calcium channel inhibitor and belongs to the field of medicine. The effect of the valeriana jatamansi Jones part in the N-type calcium channel inhibition is provided and two iridoid components of the valeriana jatamansi Jones part for playing a role in the N-type calcium channel inhibition are verified. The inhibition effect of the acidic hydrolysis product of the iridoid in the N-type calcium channel is firstly found. The valeriana jatamansi Jones part provided by the invention taken as a novel N-type calcium channel inhibitor has a wide application prospect and can be applied to the healthcare and treatment of the related diseases such as pain.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to the application of a spider iridoid part in the preparation of N-type calcium channel inhibitors. Background technique [0002] N-type voltage-dependent calcium channels are mainly distributed in neuronal synaptic terminals of pain transmission and regulation pathways, participate in the release and regulation of pain mediators (such as glutamate and substance P), and play an important role in the process of pain transmission and regulation (Foreign Medicine and Pharmacy Volume, 34(2), 93-98). Therefore, blockade of N-type calcium channels can produce analgesic effects, especially in chronic pain and neuropathic pain. Although the use of opioids can relieve pain, there are side effects such as respiratory depression, constipation and addiction. Therefore, finding new analgesic drugs with high analgesic activity and few side effects has increasingly become a topic of concern...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P29/00A61P25/04A23L1/30A23L33/10
Inventor 胡江苗杨建年寅董发武姜河海周俊杨柳
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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