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Flavonol glycoside derivatives and application and preparation method thereof

A technology of flavonol glycoside derivatives and drugs, which is applied in the field of medicine and can solve problems such as poor response, adverse reactions, and slow curative effect

Active Publication Date: 2021-06-15
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 application and preparation method thereof
  • Flavonol glycoside derivatives and application and preparation method thereof
  • Flavonol glycoside derivatives and application and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Separation of Main Components in Long Stem Golden Waist

[0039] The present embodiment is the separation method of the main components in the long stem golden waist, including:

[0040] (1) Take 6.0 kg of dried whole herb of Chrysanthemum long stems, crush it properly, put it in a percolation barrel, add 70% ethanol for percolation extraction, combine the extracts, concentrate under reduced pressure to recover the solvent, and obtain 2.5 kg of extract. A small amount of extract was dissolved in 70% methanol, passed through a 0.45 μM filter membrane, and 10 μL of the resulting filtrate was injected into a high-performance liquid chromatography (HPLC) to obtain the HPLC fingerprint of the 70% alcohol extract of Aurantia chinensis ( image 3 ). Such as figure 1 , figure 2 , image 3 As shown, its main components are compound 1 and compound 2.

[0041] (2) Take 2.4 kg of extract, heat and knead with 500 mL of 10% ethanol to dissolve, then add 500 mL of dist...

Embodiment 2

[0046] Example 2 This example is the structural identification of the above-mentioned compound 1 and compound 2, including two parts:

[0047] (1) Structural identification of compound 1

[0048] Compound 1 is a yellow-brown amorphous powder, which is easily soluble in methanol. HR-ESI-MS gives quasi-molecular ion peaks m / z : 553.1545([M+H] + , C 25 h 29 o 14 , the theoretical calculation value is 553.1552), and its molecular formula is determined to be C 25 h 28 o 14 .

[0049] The nuclear magnetic resonance (NMR) hydrogen spectrum of compound 1 ( 1 H) [such as figure 2 Shown] and carbon spectrum ( 13 C) [such as image 3 The data shown are very similar to that of a known pentamethoxyflavonol glycoside, chrysosplenoside H. with chrysosplenoside H 1 Compared with H NMR spectrum, compound 1 has one more phenolic hydroxyl proton signal in the low field region δ H 9.00 (1 H, brs), and there is one less methoxy signal in the high field region δ H 3.93 (3 H...

Embodiment 3

[0059] This example is about the acute toxicity evaluation of chrysosplenoside A and chrysosplenoside I. The evaluation method is: in accordance with the "Technical Guidelines for Acute Toxicity Test of Chemical Drugs" issued by China Food and Drug Administration (CFDA) and acute toxicity classification According to the guiding principles of the method, 2 g / kg was used as the initial dosage of chrysosplenoside I and chrysosplenoside A, and the mice were orally administered once, and the acute toxicity test in mice was carried out.

[0060] The animal grouping and dosing plan are as follows: randomly select 40 mice, half male and half male, and mark them with 3% picric acid solution; the experiment is divided into 4 groups, with 5 males and 5 females in each group, which are blank control group and vehicle control group respectively. group, chrysosplenoside I administration group, and chrysosplenoside A administration group; the test drug was ultrasonically dissolved with 0.5% C...

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PUM

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Abstract

The invention belongs to the field of medicine, and particularly relates to two highly methoxy flavonol glycoside derivatives in Tibetan medicine chrysosplenium axillare and novel application thereof in preparation of drugs for treating cholestasis type liver injury diseases, and discloses a preparation method of the methoxy flavonol glycoside derivatives at the same time. The highly methoxy flavonol glycoside derivatives have the following chemical structures shown in the specification. The compound is verified to have an active substance for resisting intrahepatic cholestasis type liver injury, and a basis is provided for research and development of medicines for treating intrahepatic cholestasis type liver injury related diseases.

Description

technical field [0001] 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 medicines for treating cholestatic liver damage diseases, and disclose their preparation methods at the same time. Background technique [0002] Intrahepatic cholestasis (IC) is a clinical syndrome in which bile acid accumulates in the liver due to structural and dysfunctional hepatocytes or capillary bile ducts, leading to liver lesions. Long-term persistent IC will develop into primary biliary cirrhosis, primary cirrhotic cholangitis, liver cancer, liver failure and other serious consequences. Modern medicine believes that any factor that causes damage to liver cells and cholangiocytes can lead to IC. Common causes include viral and bacterial infections, drug injuries, autoimmune diseases, and alcoholism. Epidemiological survey result...

Claims

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Application Information

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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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