Application of Hyperforcinol K in preparation of medicine for preventing and treating non-alcoholic fatty liver disease

A fatty liver disease, non-alcoholic technology, applied in the field of medicine, can solve the problems that have not been reported in the literature, and achieve the effect of reducing the accumulation of lipid droplets and reducing the number of lipid droplets

Pending Publication Date: 2022-03-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Surface active ingredient) derivatives, all found in a variety of Hypericum medicinal plants, whether it has the effect of preventing and treating NASH, has not been reported in the literature

Method used

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  • Application of Hyperforcinol K in preparation of medicine for preventing and treating non-alcoholic fatty liver disease
  • Application of Hyperforcinol K in preparation of medicine for preventing and treating non-alcoholic fatty liver disease
  • Application of Hyperforcinol K in preparation of medicine for preventing and treating non-alcoholic fatty liver disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The extraction process of embodiment 1 Hyperforcinol K

[0037] 1. Experimental method

[0038]The Hyperforcinol K used in the present invention is extracted and separated from the traditional Chinese medicine Hypericum beanii, specifically: use 20 kg of Hypericum beanii as raw material, grind and extract 3 times with 70 L of 95% ethanol cold soaking, and combine 3 times The extract was concentrated to dryness under reduced pressure to obtain 1.8 kg of extract. The extract was suspended in 1.5 L of water and then extracted with petroleum ether for 5 extractions with a solvent volume of 4 L each time to obtain the petroleum ether fraction extract (506.0 g). After dissolving the petroleum ether part extract and mixing the sample, load the sample at a ratio of 3:1 (weight of silica gel filler: weight of concentrate), and separate by normal pressure normal phase silica gel column chromatography, with volume ratios of 100:1 and 10:1, respectively. 1, 5:2, 1:1, 1:5 mixed so...

Embodiment 2

[0041] Example 2 Protective effect of HK on HepG2 cell injury induced by palmitic acid (PA)

[0042] 1. Experimental method

[0043] 1.1 Lipid medium preparation

[0044] Use PBS to prepare 20% d-BSA (fatty acid-free BSA) solution; use 0.1M NaOH solution to prepare 20mM PA solution, dissolve it in a water bath at 70-75°C, and fully saponify; take an equal volume of d-BSA solution and quickly add it to keep warm In the PA solution, it can be placed in a 50-55°C water bath to help dissolve, and a clear 10mM PA+10%d-BSA solution can be obtained, which can be filtered and sterilized in an ultra-clean bench to become palmitic acid lipid medium (PA stock solution) , Store at 4°C after aliquoting. The control solution is a solution obtained by mixing 20% ​​d-BSA solution and an equal volume of 0.1M NaOH solution (BSA stock solution) after filter sterilization.

[0045] 1.2 Construction of PA-induced HepG2 cell injury model

[0046] Take PA and BSA stock solutions and add them to ...

Embodiment 3

[0053] Effect of Example 3 HK on the NASH mouse model induced by high-fat diet (HFD)

[0054] 1. Experimental method

[0055] 1.1 Construction method of NASH mouse model

[0056] Twenty-one C57BL / 6J male mice aged 6-8 weeks were randomly divided into three groups, namely the model group (HFD+solvent), the positive drug group (HFD+OCA) and the administration group (HFD+HK). 7 only. The mice in the three groups were all fed HFD at the age of 8 weeks, for a total of 12 weeks; at the age of 16 weeks, the mice were given intragastric administration, the model group was given intragastric administration of solvent olive oil, and the positive drug group was given intragastric administration of 10 mg / kg of OCA. The drug group was given 20 mg / kg of HK by intragastric administration for 4 weeks in total.

[0057] 1.2 Sample collection

[0058] After the model expired, the mice were fasted for 6 hours, and the whole blood of the mice was taken by picking the eyeballs. The blood colle...

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Abstract

The invention belongs to the field of medicines and health-care products, and particularly relates to application of an acyl phloroglucinol mixed-source terpenoid Hyperformcinol K (HK) derived from hypericum medicinal plants in preparation of medicines or health-care products for preventing and treating non-alcoholic fatty liver diseases. In a PA-induced HepG2 cell injury model, HK can reduce intracellular lipid accumulation and can inhibit activation of an mTOR signal channel in a dose-dependent manner. In a high-fat diet induced NASH mouse model, the HK can reduce liver fatty degeneration, reduce the contents of TG and TC in plasma and liver and improve expression of lipid metabolism pathway related genes, which shows that the HK has a good effect of relieving NASH. The compound Hyperforcinol K disclosed by the invention has the advantages of good effect and relatively high safety, and is expected to be developed into an effective medicine or a health-care product for preventing and treating the non-alcoholic fatty liver disease.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to the application of Hyperforcinol K (HK), an acylphloroglucinol mixed-source terpenoid compound derived from Hypericum medicinal plants, in the preparation of medicines or health care products for preventing and treating nonalcoholic fatty liver disease. Background technique [0002] Nonalcoholic steatohepatitis (NASH) is an advanced stage of nonalcoholic fatty liver disease (NAFLD), which can induce liver fibrosis, cirrhosis and even liver cancer. The overall prevalence of NAFLD in my country is close to 30% , about 25% of which are NASH, and there is no effective means to treat NASH clinically. At present, the anti-NASH drugs in the research and development pipeline mainly include FASN inhibitors (ASC40 and FT-4101), ACC inhibitors (PF-05221304 and firsocostat) , SCD-1 inhibitor (aramchol), PPARα / δ dual agonist (elafibranor), farnesoid X receptor (FXR) agonist (odeoxycholic acid), chemokine ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P1/16A61K36/185A61K36/38
CPCA61K31/365A61P1/16A61K36/185A61K36/38
Inventor 孔令义张浩徐文军罗俊张艳秋卢炜佳叶圣陶
Owner CHINA PHARM UNIV
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