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Application of hyperforin to preparation of medicine for promoting browning of white fat and improving activity of brown fat

A technology of hypericin and brown fat, applied in the directions of drug combination, organic active ingredients, digestive system, etc., can solve the problem that the application of hypericin has not been reported yet.

Inactive Publication Date: 2018-12-21
SHANGHAI SIXTH PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] At present, the application of hypericin with the mechanism of promoting the browning of white fat and increasing the activity of brown fat in the resistance to obesity-related diseases has not been reported

Method used

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  • Application of hyperforin to preparation of medicine for promoting browning of white fat and improving activity of brown fat
  • Application of hyperforin to preparation of medicine for promoting browning of white fat and improving activity of brown fat
  • Application of hyperforin to preparation of medicine for promoting browning of white fat and improving activity of brown fat

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Hypericin reduces intracellular lipid droplet levels and promotes SVF-induced UCP1 protein expression in mature adipocytes

[0050] C3H10T1 / 2 is a mouse embryo-derived mesenchymal stem cell with multidirectional differentiation potential. It can differentiate into fat, skeletal muscle, bone, cartilage and endothelial cells under different induction conditions in vitro; it differentiates into white under BMP4 orientation Adipocytes differentiate into brown adipocytes under BMP7 directed treatment. In the present invention, the inventors induced differentiation of C3H10T1 / 2 cells into mature adipocytes in vitro, and used this as a cell model for preliminary screening of compounds and studying the mechanism of HPF's effect on fat.

[0051] Cultivation and differentiation of C3H10T1 / 2: Inoculate C3H10T1 / 2 on a six-well cell culture plate, and add BMP4 (final concentration of 10ng / ml) or BMP7 (final concentration of 40ng / ml) to the culture medium the next day. The cells are in c...

Embodiment 2

[0056] Hypericin perforatum promotes the expression of thermogenic genes in adipocytes

[0057] Cultivation and differentiation of C3H10T1 / 2: Inoculate C3H10T1 / 2 on a six-well cell culture plate, and add BMP4 (final concentration of 10ng / ml) or BMP7 (final concentration of 40ng / ml) to the culture medium the next day. The cells are in contact inhibition state. Two days after reaching contact inhibition, use differentiation medium A (0.5mM I BMX, 1μM dexamethasone, 10μg / ml insulin, 100nM indomethacin, 1nM triiodothyronine); 2 days later, change the differentiation medium B (10μg / ml insulin), after two days, change to fresh medium, and form mature adipocytes on the 8th day of differentiation.

[0058] HPF treatment: HPF powder was dissolved in DMSO at a stock solution concentration of 10 mM. HPF was added on the 6-8 days from the start of differentiation to a final concentration of 5 μM. The drug treatment experiment for extracting total RNA was used to collect cells 8 hours after HP...

Embodiment 3

[0064] Hypericin promotes oxygen consumption and respiration of adipocytes and improves mitochondrial production and function

[0065] The inventors conducted a series of experiments to study the effect of Hypericin on the overall respiratory chain of cells, especially the function of mitochondria. Specifically, the inventors used advanced Seahorse XFe cell energy metabolism analysis technology to fully evaluate the mitochondrial respiratory function after hypericin treatment.

[0066] Among them, the Seahorse XF cell mitochondrial stress test can detect the following key parameters of mitochondrial function: basic respiratory level, respiratory value related to ATP synthesis, proton leakage level, maximum respiratory capacity, and respiratory capacity reserve value.

[0067] The detailed steps include:

[0068] Pre-seed cells of the Seahorse experiment: Inoculate the C3H10T1 / 2 cells directed to BMP7 on the second day of differentiation into the Seahorse XF V7 cell culture plate, and ...

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Abstract

The invention relates to the technical field of natural medicine chemicals and in particular relates to application of hyperforin to preparation of a medicine for promoting browning of white fat and improving the activity of brown fat. On the basis of action mechanisms of promoting browning of white fat and improving the activity of brown fat, the hyperforin has an effect of increasing energy consumption of a body to lose weight; in addition, the hyperforin has the effects of reducing blood sugar and blood grease levels, improving sugar resistance, improving insulin sensitivity and maintainingglycometabolism steadiness, and thus can be used as a medicine for relieving diabetes symptoms; in addition, the hyperforin can be also used for relieving or treating non-alcoholic fatty liver diseases. Therefore, the hyperforin, an extract with the hyperforin, or a preparation of the hyperforin has wide clinical application prospects in preventing or treating metabolic syndromes such as obesityand diabetes.

Description

Technical field [0001] The present invention relates to the technical field of natural medicine chemistry, in particular to the use of hypericin perforin in the preparation of a medicine for promoting the browning of white fat and increasing the activity of brown fat, and to the preparation of hypericin perforin in the preparation of a medicine for preventing or treating obesity The use in the invention also relates to the use of hypericin perforatum in the preparation of a medicine for improving the symptoms of diabetes, and a pharmaceutical composition for relieving or treating non-alcoholic fatty liver. Background technique [0002] According to the definition of the World Health Organization, overweight and obesity refer to excessive and / or abnormal accumulation of body fat that may harm human health. As early as 1948, obesity was defined as a disease and added to the International Classification of Diseases. In June 2013, the American Medical Association officially declared...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61P3/04A61P3/10A61P1/16
CPCA61K31/122A61P1/16A61P3/04A61P3/10
Inventor 刘军力刘筱筱陈素贞孙洪林柯蒋风
Owner SHANGHAI SIXTH PEOPLES HOSPITAL
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