CN-121991145-A - Compound extracted from colocynth, pharmaceutical composition thereof and application of compound in liver protection

Abstract

The invention belongs to the field of medicines, and relates to a compound with a novel structure in colocynth, a preparation method thereof and application of the compound in medicines with liver protection activity.

Inventors

• JIANG JIANSHUANG
• GAO CHEN
• SUN HUA
• ZHANG PEICHENG
• YANG YANAN
• ZHANG LINGZHI
• YUAN XIANG
• ZHANG XU
• FENG ZIMING
• LIU SIQI

Assignees

• 中国医学科学院药物研究所

Dates

Publication Date

20260508

Application Date

20241105

Claims (7)

1. 1. A compound or a pharmaceutically acceptable salt thereof, characterized in that the structure of the compound is as follows:
2. 2. The compound or pharmaceutically acceptable salt thereof according to claim 1, wherein the pharmaceutically acceptable salt is selected from the group consisting of salts of the compound with inorganic bases and organic bases.
3. 3. The compound according to claim 2, or a pharmaceutically acceptable salt thereof, wherein the organic base comprises methylamine, ethylamine, diethylamine, triethylamine, propylamine, butylamine, octylamine, hexamethylenediamine, ethylenediamine, propylenediamine, butylenediamine, xylylenediamine, phenethylamine, xylylenediamine, p-xylylenediamine, and the inorganic base comprises sodium hydroxide, potassium hydroxide, calcium hydroxide, aluminum hydroxide, lithium hydroxide, magnesium hydroxide, zinc hydroxide, copper hydroxide, iron hydroxide, ammonium hydroxide, sodium bicarbonate, potassium bicarbonate.
4. 4. The preparation method of the compound of claim 1 is characterized by comprising the steps of extracting a colocynth drug material with 70% ethanol under reflux, concentrating the extract, and separating and purifying the extract by using an organic solvent, macroporous resin column chromatography, gel column chromatography, silica gel column chromatography and preparative HPLC to obtain the compound 1-21.
5. 5. A pharmaceutical composition comprising a compound according to any one of claims 1 to 3, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.
6. 6. The pharmaceutical composition according to claim 5, wherein the dosage form of the pharmaceutical composition comprises a tablet, capsule, pill, granule, oral liquid or suspension.
7. 7. Use of a compound according to any one of claims 1-3 for the manufacture of a medicament having liver protecting function.

Description

Compound extracted from colocynth, pharmaceutical composition thereof and application of compound in liver protection Technical Field The invention belongs to the field of medicines, and particularly relates to a liver protection application of a compound separated from colocynth and an application of the compound in preparation of liver protection medicines. Background Liver disease is a major group of diseases that are serious threatened to human health in the world today, including hepatitis caused by various causes, such as steatohepatitis, alcoholic, viral and autoimmune hepatitis, liver fibrosis and liver cancer. In recent years, with the development of urban, people's life style and diet structure are continuously changed, and the incidence of liver diseases is continuously increased due to factors such as environmental pollution, excessive diet, excessive drinking, food additive abuse and the like, so that diseases such as hepatitis, fatty liver, liver fibrosis, liver cirrhosis and even liver cancer are seriously threatened with human health, therefore, the development of liver protection medicines with high efficiency and no obvious toxic or side effect is widely focused on society, and meanwhile, the liver protection activity research clear of natural medicines shows wide application prospect. Therefore, development of drugs for treating liver diseases with better activity and better therapeutic effect from natural products is a urgent problem for clear people to solve. Colocynthis Citrullus colocynthis (l.) Schrad is a plant of the genus colocynthis of the family cucurbitaceae, which is an external medicinal material native to arid regions in northern africa, and is distributed throughout the saharan desert in morocco, egypt, sudan, iran, india, pakistan and afgham, and transported to singapore via the ancient silk road in the song generation and used until now. The colocynth is currently distributed in northwest, northeast, north China, henan, hubei, xinjiang and other places in China, and is widely planted in Changji, hetian, yecheng and other places to meet clinical requirements. In Uighur medicine theory, the medicinal parts of the colocynth are dry mature fruits, four-grade heat and two-grade dryness, have the effects of dispelling phlegm and fluid and the like, and can be used for treating various headaches, deafness, arthritis, amenorrhea and the like. Modern pharmacological studies show that the pulp Citrulli has anticancer, liver protecting, antioxidant, antidiabetic, and anti-pathogenic microorganism activities. The colocynth contains cucurbitacin, alkaloid, flavone, steroid saponin, phenolic acid, phenylpropanoid and other compounds, wherein the cucurbitacin compound is a main component and a main active component of the colocynth, and has various biological activities of resisting tumor, protecting liver, improving body immunity and the like. Disclosure of Invention The applicant researches show that the compound with novel structure is separated from the colocynth and has the chemical structure as follows, Pharmacological experiments prove that part of the compounds can effectively improve the cell survival rate of the HepG2 cell injury induced by APAP or H 2O2, lighten the cell injury and have good potential of developing liver protection medicines. At present, research reports of using the compounds in liver protection medicines, a preparation method and patent documents are not yet seen. The invention solves the technical problem of providing a preparation method of a compound separated and extracted from colocynth and application of the compound in preparation of liver protection medicines. In order to solve the technical problems of the invention, the invention provides the following technical scheme: According to a first aspect of the technical scheme, the invention provides a compound or pharmaceutically acceptable salt thereof, which is characterized by comprising the following structure: The pharmaceutically acceptable salts are selected from salts of the compounds with inorganic and organic bases. The organic base comprises methylamine, ethylamine, diethylamine, triethylamine, propylamine, butylamine, octylamine, hexamethylenediamine, ethylenediamine, propylenediamine, butylenediamine, phenylmethylamine, phenylethylamine, o-xylylenediamine and p-xylylenediamine, and the inorganic base comprises sodium hydroxide, potassium hydroxide, calcium hydroxide, aluminum hydroxide, lithium hydroxide, magnesium hydroxide, zinc hydroxide, copper hydroxide, ferric hydroxide, ammonium hydroxide, sodium bicarbonate and potassium bicarbonate. According to a second aspect of the present invention, there is provided a process for the preparation of the compound of the first aspect. Reflux-extracting 50kg of dry fruit of Citrullus colocynthis with 70% ethanol for 2 times, each time for 2 hours, concentrating the extractive solution, extracting with petroleum ether, ethyl acetate and n-butanol,