Application of 2í», 5, 6í», 7-tetrahydroxy dihydroflavonol and its derivative for treating sepsis

A technology of tetrahydroxydihydroflavonol and derivatives, applied in the 2' field, can solve problems such as no sepsis drugs

Inactive Publication Date: 2008-09-17
THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] So far, there are no reports of THF and its derivatives and analogs neutralizing LPS and preparing drugs for treating sepsis

Method used

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  • Application of 2í», 5, 6í», 7-tetrahydroxy dihydroflavonol and its derivative for treating sepsis
  • Application of 2í», 5, 6í», 7-tetrahydroxy dihydroflavonol and its derivative for treating sepsis
  • Application of 2í», 5, 6í», 7-tetrahydroxy dihydroflavonol and its derivative for treating sepsis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1: 12 kinds of Chinese medicinal decoctions and Lipid A binding reaction measurement results

[0048] 1.1 Experimental method:

[0049] (1) Using biosensor technology, lipid A (Lipid A) is coated on the sample pool of affinity-type specific and selective biosensor IAsys Plus (Affinity-sensor IAsys plus) as a stationary phase ligand; A) The anionic group that plays an important biological role in the structure is exposed, and it is used as a target for binding with active substances for treating diseases in traditional Chinese medicine;

[0050] (2) Prepare 12 kinds of traditional Chinese medicine water decoctions, take 5 μL samples respectively, and measure their binding reaction with Lipid A. The specific operation steps are as follows:

[0051] ① Binding reaction: add 45 μL of pH 6.0 and 20mM PBS, then add 5 μL of the sample to be tested, and aspirate after the binding reaction is balanced;

[0052] ②Dissociation reaction: wash with pH 6.0, 20mM PBS 50μL×3,...

Embodiment 2

[0056] Example 2: Extraction and separation of THF, the active ingredient of Scutellaria baicalensis anti-LPS

[0057] 2.1 Separation of macroporous adsorption resin and screening of active sites

[0058] 2.1.1 Experimental method: add about 500g of Scutellaria baicalensis, soak in 5.0L of distilled water for 24h, decoct at 100°C for 1h, filter through coarse filter paper, centrifuge at 9000rpm / min for 35min, collect the supernatant and concentrate it to about 1.0L under reduced pressure; then load the sample in AB-8 macroporous adsorption resin was eluted sequentially with distilled water and 10%, 20%, 40%, and 60% ethanol, and the eluents were collected, concentrated under reduced pressure, and then freeze-dried to obtain 5 groups. The fractions were named as SbG-1-5 according to the order of elution. The components of SbG were dissolved in PBS to 2.0 g / L, and 5 μL was loaded as the sample. The binding activity to Lipid A was detected according to the method in 1.1.

[0059...

Embodiment 3

[0070] Example 3: THF neutralizes the activity of LPS in vitro

[0071] 3.1 Experimental method: Incubate corresponding concentrations of THF and PMB (both 1.0, 2.0, 4.0, and 8.0 mg / L) with LPS at a final concentration of 0.2 ng / mL at 37°C for 30 min, and add an equal amount of pyrogen-free water to the LPS control group , the LPS value after incubation was detected by the dynamic turbidimetric limulus test, and the detection was repeated 4 times for each concentration. The specific operation was carried out according to the instructions of the EDS-99 bacterial endotoxin determination system.

[0072] 3.2 Experimental results: THF has the activity of neutralizing LPS, and its neutralizing effect is weaker than that of PMB. Statistical analysis shows that THF has a significant neutralization effect on 0.2ng / ml LPS at 2.0mg / L level (P Figure 6 shown.

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Abstract

The invention relates to the usage of a 2',5',6',7'-tetrahydroxyflavanonol and the derivative in treating pyohemia, belonging to flavanonol compound THF, which is extracted and separated from baikal skullcap root of Chinese herbal medicine. Through experiment showing, the THF has the advantages that: the THF has direct neutralization effect and reveals better dose effect relationship; the THF also reveals better dose effect relationship upon inhibition of RAW 264.7 cells activation LPS stimulation; the THF can lower LPS level in blood of LPS blood symptom model animal in vivo; the THF also has obvious protection effect upon bacterial sepsis model mouse caused by heat-inactivation escherichia coli with lethal dose; the THF has good application prospect under the condition of lacking effective means treating pyohemia in prior study.

Description

technical field [0001] The invention relates to the use of 2', 5, 6', 7-tetrahydroxy dihydroflavonol and derivatives thereof for treating sepsis. Background technique [0002] Sepsis is an infectious agent-mediated systemic inflammatory response syndrome (systemic inflammatory response syndrome, SIRS), which is a common complication in patients with burns, trauma and infectious diseases. Epidemiological data show that there are more than 18 million sepsis cases worldwide every year, and the number of patients is increasing at a rate of 1.0% every year. Severe sepsis and septic shock are the leading causes of death in intensive care units (ICU), with a mortality rate as high as 50%-60%. [0003] LPS is the main component of the outer membrane of G-bacteria, and is an important pathogen-associated molecular pattern (pathogen-associated molecular patterns, PAMPs) mediating bacterial sepsis. After LPS enters the body, it first binds to lipopolysaccharide-binding protein (LBP)....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P17/02A61P29/00
CPCY02A50/30
Inventor 郑江伏建峰周红郑新川刘鑫曹红卫王宁鲁永玲
Owner THE FIRST AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIVERSITY OF PLA
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