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Flavonol glycoside derivatives and their use and preparation method

A technology for converting flavonol glycoside derivatives and ethanol, applied in the field of medicine, can solve the problems of long treatment process, severe IC cannot be used for a long time, slow curative effect and the like

Active Publication Date: 2021-07-30
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ursodeoxycholic acid can significantly improve cholestasis, but it is expensive and has a slow effect, and some patients do not respond well to it
Glucocorticoids (such as dexamethasone, etc.) are considered to be one of the traditional drugs for the treatment of acute IC, but they are prone to rebound after taking them, and long-term use of corticosteroids will cause serious adverse reactions, so they cannot be used for severe IC for a long time
Generally speaking, the treatment of IC by Western medicine is mainly to improve symptoms and control related complications. There is no specific drug in clinical practice, and there are not many drugs to choose from. The adverse reactions caused serious physical and mental burden to the patients

Method used

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  • Flavonol glycoside derivatives and their use and preparation method
  • Flavonol glycoside derivatives and their use and preparation method
  • Flavonol glycoside derivatives and their use and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Separation of the main ingredients in the gold waist

[0039] This embodiment is the separation method of the main components in the diaphragm gold waist, including:

[0040] (1) Drying the gold waist and dry the whole steroid. The whole grass is 6.0 kg, properly pulverized, placed in a permeable barrel, add 70% ethanol osmication extraction, combined extract, concentrate the solvent, and soon it. 2.5 kg. Take a small amount of dipper, dissolved in 70% methanol, a 0.45 μm filter, and the resulting filtrate was 10 μl of injection of high-performance liquid chromatograph (HPLC), and the HPLC fingerprint of 70% alcohol of the long stem gold waist ( image 3 ). like figure 1 , figure 2 , image 3 As shown, its main component is Compound 1 and Compound 2.

[0041] (2) Take 2.4 kg of dipping and heat it with 500 ml 10% ethanol, then add 500 mL of distilled water to disperse.

[0042](3) Dispersion liquid HP-20 macroporous adsorption resin column, with distilled water, 10%...

Embodiment 2

[0046] EXAMPLE 2 This example is a structural identification of the compound 1 and Compound 2, including two parts:

[0047] (1) Structure identification of Compound 1

[0048] Compound 1 is a yellow-brown non-forming powder, which is soluble in methanol. HR-ESI-MS gives the alignment molecular ion peak m / z : 553.1545 ([M + H] + , C 25 Hide 29 O 14 The theoretical calculation value is 553.1552), determine its molecular formula C 25 Hide 28 O 14 .

[0049] Nuclear magnetic resonance (NMR) hydrogen spectrum of Compound 1 1 H) figure 2 Distant] and carbon spectrum ( 13 C) image 3 The data shown is very similar to a known fiven oxagleanoside h. With Chrysosplenoside H 1 Compound 1 is more phenolic hydroxyprom signal in the low field region than the H NMR spectrum. δ H 9.00 (1 H, BRS), while a signal of a methoxy group in the high field area δ H 3.93 (3 h, s); with Chrysosplenoside H 13 C NMR spectrum compared to a signal of 1 methoxy group δ C 56.9. This suggests that Compound 1 is ...

Embodiment 3

[0059] This example is about Chrysosplenoside A and Chrysosplenoside I acute toxicity evaluation, the evaluation method is: "Chemical Drug Acute Test Technical Guidelines" and acute toxicity in accordance with China Food and Drug Administration, CFDA The guidelines of the law were carried out as the initial administration of Chrysospleniside I and Chrysosplenoside A, and mice were performed in a mouse acute toxicity test.

[0060] The animal grouping and administration protocol was as follows: randomly selected 40 mice, more than half of female, and labeled 3% bitter acid solution; the experiment was divided into 4 groups, each group of male, female each, respectively, blank control group, mediating control Group, Chrysosplenoside I administration group, Chrysosplenoside A administration group; test drugs were dissolved with 0.5% CMC-NA solution, the dose of 2 g / kg, a single irrigant administration; the mediative control group 0.5% CMC-NA solution, blank control group gave a sol...

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Abstract

The invention belongs to the field of medicine, and specifically relates to two highly methoxylated flavonol glycoside derivatives in the Tibetan medicine Changgan Jinyao and their new application in the preparation of drugs for treating cholestatic liver damage diseases, and disclose their preparation methods at the same time. This derivative has the chemical structure shown below: . The compound has been verified as an active substance against intrahepatic cholestasis liver injury, and provides a basis for the research and development of drugs for treating diseases related to intrahepatic cholestasis liver injury.

Description

Technical field [0001] The invention belongs to the field of medicine, and there is specifically related to 2 high methoxylated flavonol glycoside derivatives in Tibetan Pharmaceuticals and their preparation methods in the preparation of bile sludge liver injury disease drugs. Background technique [0002] Intrahepatic Cholestasis, ICs are a clinical syndrome of bile acid in the liver due to hepatocytes or capillary structures and dysfunction, resulting in clinical syndrome of liver disease. Long-term continued IC will develop into primary biliary cirrhosis, primary cirrhosis cholangitis, liver cancer, liver failure, etc. Modern medicine believes that any factors that cause hepatocytes and biliary cell damage can lead to ICs, common causes including viruses and bacterial infections, drug damage, autoimmune diseases, alcoholism, etc. The epidemiological survey results show that the incidence of IC is rising year by year. Therefore, looking for high-efficiency IC therapeutic drugs ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H15/26C07H1/08A61P1/16
CPCA61P1/16C07H1/08C07H15/26
Inventor 任刚蒋伟蔡紫嫣李文艳龚德梅吴昊芬陈思孙宁喆
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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