Application of ferulamide compound in preparation of anticomplementary drugs

A ferulic acid amide and compound technology, applied in the separation/purification of carboxylic acid amide, drug combination, antipyretic, etc., can solve problems such as excessive activation of the autoimmune system

Inactive Publication Date: 2019-06-21
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Studies have shown that the above-mentioned diseases related to the treatment of Huo Tanmu and their pharmacological activities are mostly related to the complement system, and the complement system plays a very important role in maintaining the body's immune balance and eliminating foreign microorganisms. Many pathogenic microorganisms can cause disease in the human body. Excessive activation of the autoimmune system can lead to serious consequences, such as SARS, influenza, rheumatoid arthritis, etc. Therefore, it is particularly important to find low-toxicity and high-efficiency complement inhibitors from traditional Chinese medicines for the treatment of related diseases

Method used

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  • Application of ferulamide compound in preparation of anticomplementary drugs
  • Application of ferulamide compound in preparation of anticomplementary drugs
  • Application of ferulamide compound in preparation of anticomplementary drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1. Preparation of ferulic acid amides compound

[0032] Take Polygonum chinense Linn. 10kg medicinal material, pulverize it, and extract it by cold immersion in 95% ethanol for 3 times. After the extract is concentrated, it is suspended in water, and extracted with petroleum ether, ethyl acetate, and n-butanol respectively to obtain the active part positive Butanol 300g, get the extractant 250g and wet the macroporous resin D101 with H 2 O / EtOH (30,60,95%, v / v) obtained three fractions Fr.B1-Fr.B3; 18 Medium pressure flash preparative column with CH 3 OH-H 2 O (25:75to 100:0) was eluted to obtain 7 Fr.B2fractions (A-G).; all fractions were purified by semi-preparative column, and compound n-tans-feruloyl tyramine (1) and compound lyciumamide were obtained from Fr.B2fraction C D(2) and compound lyciumamide B(3), (CH 3 CN-H 2 O-CH 3 COOH37:63:0.05).

[0033] After further identification, the NMR data of the obtained compound 1-3 are shown in Table 1-3. ...

Embodiment 2

[0034] Example 2. Anti-complement classical pathway experiment in vitro

[0035]Take 0.1 mL of complement (guinea pig serum), add barbiturate buffer solution (BBS) to prepare a 1:10 solution, and double-dilute with BBS to 1:20, 1:40, 1:80, 1:160, 1:10 320, 1:640 and 1:1280 solutions; take 1:1000 hemolysin, each concentration of complement and 2% sheep red blood cell (SRBC) each 0.1mL dissolved in 0.3mL BBS, mix well, 37 ℃ water bath for 30min, put into Centrifuge in a low-temperature high-speed centrifuge at 5000rpm and 4°C for 10min; take 0.2mL of the supernatant from each tube and place it in a 96-well plate, and measure its absorbance at 405nm; set up a complete hemolysis group (0.1mL 2% SRBC dissolved in 0.5mL three distilled water); the absorbance of three-distilled water lysed blood vessels was used as the standard of total hemolysis to calculate the hemolysis rate. Take the complement dilution as the x-axis and the hemolysis percentage as the y-axis to draw a graph; se...

Embodiment 3

[0036] Example 3. Anti-complement alternative pathway experiment in vitro

[0037] Take complement (human serum) 0.2mL, add AP diluent (barbital buffer, pH 7.4, containing 5mM Mg 2+ , 8mMEGTA) was double-diluted into 8 concentration gradients (1:2, 1:4, 1:8, 1:16, 1:32, 1:64, 1:128, 1:256), and then hemolyzed In the reaction system, 0.15mL of various concentrations of complement and 0.2mL of 0.5% RRBC were dissolved in 0.35mL of AP diluent, mixed evenly, placed in a low-temperature high-speed centrifuge at 37°C for 30 minutes, centrifuged at 5000rpm, 4°C for 10 minutes; Put 0.2 mL of the supernatant in a 96-well plate, and measure the absorbance at 405 nm. At the same time, a total hemolysis group (0.5% RRBC 0.2mL dissolved in 0.5mL triple distilled water) was set up in the experiment; the absorbance of triple distilled water lysed blood vessels was used as the standard of total hemolysis, and the hemolysis rate was calculated. Take the dilution factor of complement as the x...

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Abstract

The invention belongs to the technical field of preparation of traditional Chinese medicine and relates to application of a ferulamide compound in the preparation of anticomplementary drugs. the ferulamide compound n-trans-feruloyl tyramine, compound lyciumamide D and compound lyciumamide B shown as formulas below are isolated and extracted from the whole plant of Polygonum chinensis Linn of the family Polygonaceae through activity-oriented separation; anticomplementary activity evaluation tests show that the compounds can well inhibit both typical and alternative pathways of the complementarysystem, wherein the inhibitory action (CH50) on the typical pathway is 0.35-0.92 mM, and the inhibitory action (AP50) on the alternative pathway is 0.40-1.36 mM. The compounds herein can be preparedinto anticomplementary drugs and drugs to treat complement-related diseases.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine, and relates to the use of ferulic acid amide compounds in the preparation of anti-complement drugs, in particular to the use of ferulic acid amide compounds isolated and identified from the traditional Chinese medicine Huo Tanmu in the preparation of anti-complement drugs. Background technique [0002] The prior art discloses that tannin is the dry aerial part of Polygonumchinensis Linn., a plant of the genus Polygonum genus in the family Polygonum chinensis Linn. It is a traditional heat-clearing and detoxifying traditional Chinese medicine in southern my country, and it is also a main component drug of Wanglaoji herbal tea, etc.; its taste is pungent, bitter, and cool in nature. It has the effects of clearing heat and dampness, cooling blood and detoxifying, calming liver and improving eyesight, promoting blood circulation and relaxing tendons. Modern pharmacological studies have show...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61K31/395A61P37/02A61P11/00A61P31/16A61P19/02A61P29/00C07C231/24C07C235/34C07C235/40C07D273/02
Inventor 陈道峰郑昊钏卢燕
Owner FUDAN UNIV
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