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CN-121971417-A - Application of physcion in preparation of medicine for reducing hepatic cell lipid deposition

CN121971417ACN 121971417 ACN121971417 ACN 121971417ACN-121971417-A

Abstract

The invention discloses application of physcion in preparing medicines for reducing hepatic cell lipid deposition, in particular relates to application of physcion in preparing medicines for preventing and treating lipid deposition fatty liver, and the application proves that physcion shows low toxicity and wide safety range in a human normal liver cell line THLE3, a human liver cancer cell line HepG2 and a mouse normal liver cell line AML12, can obviously reduce intracellular triglyceride level induced by oleic acid in a dose-dependent manner, and also intuitively shows that the physcion can effectively reduce intracellular lipid droplet deposition.

Inventors

  • XU QINYI
  • WANG JIANWEI

Assignees

  • 重庆医科大学

Dates

Publication Date
20260505
Application Date
20260319

Claims (8)

  1. 1. An application of physcion in preparing medicine for reducing hepatic cell lipid deposition is provided.
  2. 2. The application of the physcion monomer in preparing the medicine for treating the lipid deposition fatty liver is characterized in that the physcion monomer simultaneously satisfies the following conditions under the condition of 24 hours of administration after molding in an oleic acid-induced hepatocyte lipid deposition model: (a) Cell viability for THLE3, hepG2 and AML12 cell lines is no less than 80%; (b) Compared with the model group, the intracellular triglyceride level is reduced by more than 50 percent.
  3. 3. The use according to claim 2, wherein the oleic acid-induced hepatocyte lipid deposition model is a model established by treatment with 150 μm oleic acid for 24 h.
  4. 4. The use of physcion according to claim 1 for the preparation of a medicament for reducing hepatic cell lipid deposition, wherein said physcion is in monomeric form with a purity of more than 95%.
  5. 5. The use according to claim 2, wherein the administration is for 24 hours after moulding.
  6. 6. The use according to claim 2, wherein the cell viability is not less than 85%.
  7. 7. The use according to claim 2, wherein the triglyceride level is reduced by not less than 60%.
  8. 8. A pharmaceutical composition for the treatment of lipid-deposited fatty liver comprising as the sole active ingredient an physcion monomer, wherein said physcion monomer exhibits low toxicity and significantly reduces lipid deposition in THLE3, hepG2 and AML12 cell lines, and a pharmaceutically acceptable carrier.

Description

Application of physcion in preparation of medicine for reducing hepatic cell lipid deposition Technical Field The invention belongs to the technical field of application of traditional Chinese medicine active ingredients, and particularly relates to application of physcion in preparation of a medicine for reducing hepatic cell lipid deposition. Background The traditional Chinese medicine has no fatty liver disease name, and is classified into the categories of liver turbidity, hypochondriac pain, liver nodules and the like according to the clinical manifestation characteristics. The disease is located in the liver and involves the spleen and stomach. The Chinese medical college Zhang Zhiyuan treats fatty liver by treating liver diseases, and takes the main thought of liver transmission and spleen transmission without spleen transmission as well as the key of disease occurrence such as qi stagnation, dampness accumulation and the like as well as other viscera and viscera concurrent symptoms. The radix et rhizoma Rhei is root and rhizome of Rheum palmatum, rheum tanguticum Maxim or Rheum officinale Maxim of Rheum of Polygonaceae, which is one of the common clinical traditional Chinese medicines, has bitter taste and cold property, and is suitable for spleen, stomach, large intestine, liver and pericardium channel. Has antibacterial, antiinflammatory, antipyretic, analgesic, blood pressure lowering, blood lipid reducing, liver protecting, gallbladder function promoting, immunity regulating, and antitumor effects, and contains anthraquinone as main ingredient. The Chinese pharmacopoeia of the people's republic of China takes 5 anthraquinone compounds of aloe-emodin, rhein, emodin, chrysophanol and physcion as index components for content measurement. Physcion is one of the main active ingredients of rheum officinale. The radix et rhizoma Rhei charcoal is prepared by parching radix et rhizoma Rhei, and has effects in clearing away heat and toxic materials, promoting blood circulation, removing blood stasis, removing necrotic tissue, and promoting tissue regeneration. Fatty liver disease has become the most common chronic liver disease worldwide, and its core pathological feature is steatosis caused by abnormal deposition of lipids such as triglycerides in liver cells, and this disease can further progress to nonalcoholic steatohepatitis, liver fibrosis and even cirrhosis. However, according to the clear records of the guide for preventing and treating metabolic-related (nonalcoholic) fatty liver disease (2024 edition), the current drug treatment for NASH is very limited, the existing drugs such as vitamin E can improve liver steatosis and accompany hemorrhagic stroke risk, the adverse reactions of the famous ester X receptor agonist obeticholic acid are limited due to pruritus and blood lipid disorders, even the drugs such as Resmetirom newly obtained have the defects of single target point, obvious side effect or high price, and the like, and more importantly, the single component drugs capable of simultaneously meeting the dual requirements of high-efficiency lipid lowering and liver safety are not available in the current clinical practice, and the treatment dilemma highlights the urgent need of developing novel safe and effective drugs. Under the background, the traditional Chinese medicines of rhubarb and polygonum multiflorum are taken as traditional polygonaceae medicinal materials, and are paid attention to for long-term use in the clinic of traditional Chinese medicine for protecting liver and reducing lipid. In the prior art, rheum officinale is recorded to have the effects of purging pathogenic accumulation, clearing heat and purging fire, the compound preparation of the rheum officinale is a lipid-lowering and liver-protecting medicament disclosed in a patent CN100356953C and a medicament for treating fatty liver related to a patent CN1229124C, rheum officinale is taken as an integral medicinal material, polygonum multiflorum is used for regulating blood lipid due to the effects of tonifying liver and kidney and replenishing essence and blood, and the preparations such as Danshao Gankang particles disclosed in patents CN104524448A and CN104771702A are in multi-component compound forms. However, the liver protection effect based on the whole medicinal material is not equivalent to the accurate treatment aiming at the specific pathological mechanism of lipid deposition, and more importantly, a technical prejudice exists in the prior art, namely anthraquinone components contained in rheum officinale and polygonum multiflorum are considered as potential hepatotoxic substances, attenuation or synergism must be realized through compound compatibility, and the recognition directly leads to the technical scheme that physcion is used as a single active ingredient for treating the lipid deposition fatty liver never occurs in the prior art. The development of this technical prejudice is not a hole wind but is d