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N-acyl-sphingosine compound, preparation method and application of N-acyl neuro sphingosine compound

A technology of acyl sphingamines and compounds, applied in the application field of preparing drugs for inhibiting the activity of angiotensin I converting enzyme, achieving the effect of easy operation and inhibiting the activity of angiotensin I converting enzyme

Inactive Publication Date: 2015-02-18
DALIAN OCEAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far there is no relevant report about the isolation of N-acylsphingosine compounds from Tamarix multibranches and their use in inhibiting angiotensin I-converting enzymes

Method used

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  • N-acyl-sphingosine compound, preparation method and application of N-acyl neuro sphingosine compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 Extraction and separation of N-acylsphingosine compounds

[0016] a. Take 3.1 kg of tamarisk branches ( Tamarix.ramosissima Ledeb.) The above-ground part is pulverized with a pulverizer, soaked in 24.8L of ethanol with a volume fraction of 100%, and then heated and refluxed for extraction. The extraction time is 2h each time, and the extraction times are 2 times. The extracts are combined and the extracts are recovered under reduced pressure until the alcohol concentration is low. At 5%, the concentration of crude drug contained is 50~100g / ml;

[0017] b. Extract the resulting extract 3 times with petroleum ether, the volume ratio of the extraction solvent to the extract is 2:1, combine the extracts, and recover the solvent to obtain the extract;

[0018] c. Separate 30 g of the obtained extract by silica gel column chromatography, eluting with a mixed solvent of petroleum ether and ethyl acetate, and collect the eluted fractions with a volume ratio of petroleum e...

Embodiment 2

[0021] a. Take 4 kg of tamarisk branches ( Tamarix.ramosissima Ledeb.) The above-ground part is pulverized with a pulverizer, soaked in 24 volume fraction of 80% methanol, and then heated and refluxed for extraction. The extraction time is 2 hours each time, and the extraction times are 2 times. The extracts are combined and the extract is recovered under reduced pressure until the alcohol concentration is lower than 5%, the concentration of crude drug contained is 50~100g / ml;

[0022] b. Extract the resulting extract twice with n-hexane, the volume ratio of the extraction solvent to the extract is 1:2, combine the extracts, and recover the solvent to obtain the extract;

[0023] c. Separate 30 g of the obtained extract by silica gel column chromatography, eluting with a mixed solvent of petroleum ether and ethyl acetate, and collect the eluted fractions with a volume ratio of petroleum ether and ethyl acetate of 100:0~2, The solvent was volatilized at room temperature, and a wh...

Embodiment 3

[0026] a. Take 1 kg of tamarisk branches ( Tamarix.ramosissima Ledeb.) The above-ground part is pulverized with a pulverizer, soaked in 20L of methanol with a volume fraction of 50%, and then heated and refluxed for extraction. Each extraction time is 3h, and the extraction times are 3 times. The extracts are combined, and the extracts are recovered under reduced pressure until the alcohol concentration is lower than 5%, the concentration of crude drug contained is 50~100g / ml;

[0027] b. Extract the resulting extract 4 times with n-hexane, and the volume ratio of the extraction solvent to the extract is 1:1. Combine the extracts and recover the solvent to obtain the extract;

[0028] c. Separate 30 g of the obtained extract by silica gel column chromatography, eluting with a mixed solvent of petroleum ether and ethyl acetate, and collect the eluted fractions with a volume ratio of petroleum ether and ethyl acetate of 100:0~2, The solvent was volatilized at room temperature, and...

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Abstract

The invention discloses an N-acyl-sphingosine compound capable of restraining activity of angiotensin I-converting enzyme. A preparation method comprises the following steps in sequence: pulverized tamarix ramosissima is taken, soaked in ethanol or methanol with a volume fraction of 50-100%, and then subjected to heating backflow extraction for 2-3 times; each extraction time is 2-3h; extracting solutions are mixed; the obtained extracting solution is extracted by petroleum ether, normal hexane or cyclohexane for 2-4 times; a volume ratio of an extracting solvent to the extracting solution is (1-2):(1-2); extracting solutions are mixed; the extracting solvent is recovered, and an extractant is obtained; the obtained extractant is separated by silicagel column chromatography, and subjected to gradient elution by a petroleum ether and ethyl acetate mixed solvent; and elution distillment of petroleum ether and ethyl acetate at the volume ratio of 100:(0-2) is collected.

Description

Technical field [0001] The invention relates to an N-acylsphingosine compound, a preparation method and its application in the preparation of a medicine for inhibiting the activity of angiotensin I converting enzyme. Background technique [0002] Hypertension is the most common cardiovascular disease and a major factor threatening the health of adults. In the human body, Angiotensin I-converting enzyme (ACE) is the most important regulatory hub of the hypertensive protease-angiotensin system (Renin-angiotension system, RAS). On the one hand, ACE can cut off Angiotensin I secreted from the liver and convert it into Angiotensin II. Angiotensin II promotes vasoconstriction and causes high blood pressure; on the other hand, kinin in plasma Relase cuts off the kininogen protein to produce bradykinin (Bradykinin), bradykinin promotes vasodilation and lowers blood pressure, but ACE decomposes bradykinin and inactivates bradykinin; ACE in the human body these two All aspects have cause...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C231/24C07C233/18A61K31/164A61P9/12A23L1/30
Inventor 谭成玉孔亮李伟李倩孟繁桐
Owner DALIAN OCEAN UNIV
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