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Pseudolarix triterpene lactone, and preparation method, pharmaceutical composition and application thereof

A composition and drug technology, applied in the field of medicine, can solve the problems of repeated symptoms and aggravation, and achieve the effect of good therapeutic effect

Pending Publication Date: 2021-08-06
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But after long-term use, once the drug is stopped or the dosage is reduced, the symptoms will recur or even aggravate soon

Method used

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  • Pseudolarix triterpene lactone, and preparation method, pharmaceutical composition and application thereof
  • Pseudolarix triterpene lactone, and preparation method, pharmaceutical composition and application thereof
  • Pseudolarix triterpene lactone, and preparation method, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: Separation and structural characterization of compound 1-6

[0041] 100kg of pine seeds, pulverized, extracted 3 times by cold soaking with 95% ethanol, the first 12 hours and then twice for 2 hours each time. The extract was concentrated under reduced pressure to obtain 8.87 kg of extract, which was suspended in 20 L of water, extracted successively with petroleum ether, dichloromethane, ethyl acetate and n-butanol (each extracted 3 times), combined the extracts and recovered the solvent to obtain dichloromethane Part 3.97kg. The dichloromethane part was adsorbed on a silica gel (160-200 mesh) chromatographic column, and eluted with petroleum ether to ethyl acetate 30:1, 20:1, 10:1, 5:1, 1:1 and ethyl acetate in sequence, Six fractions of G1-G6 were obtained respectively. Among them, the G3 fraction (480g) was adsorbed on a silica gel (200-300 mesh) chromatographic column, and then eluted with petroleum ether to acetone 10:1, 8:1, 5:1, 3:1, and 1:1 to o...

experiment example 1

[0065] Experimental example 1 isolates and obtains all triterpene compounds (containing active best compound 1-6) anti-inflammatory activity test

[0066] 1. In vitro NF-κB pathway inhibition experiment

[0067] (1) Experimental principle

[0068] NF-κB is a nuclear transcription factor that plays an important role in immune and inflammatory responses by regulating the expression of inflammatory cytokines. In the resting state, the subunits p50 and p65 of NF-κB usually exist in the cytoplasm in the form of heterodimer. When pro-inflammatory stimuli (such as TNF-α) act on cells, they will activate NF-κB through the degradation and phosphorylation of IκBα, and the activated NF-κB p65 enters the nucleus and binds to DNA, and up-regulates inflammatory genes COX-2, Transcription of iNOS. NF-κB is activated and starts the transcription and expression of pro-inflammatory genes, leading to the excessive secretion of TNF-α, IL-6, IL-1β and other pro-inflammatory factors, thus aggrav...

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PUM

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Abstract

The invention discloses pseudolarix triterpene lactone, and a preparation method, a pharmaceutical composition and application thereof, belongs to the technical field of medicines, and particularly relates to an anti-inflammatory effective component separated from pseudolarix amabilis (Nelson) Rehd, including two new triterpenoids (1-2) and four known triterpenoids (3-6), pharmacodynamically acceptable salts of the triterpenoids (1-2) and a preparation method of the inflammatory effective component, the composition containing the compounds and the application of the compounds in the preparation of anti-inflammatory drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to triterpene lactone compounds (1-6) of chrysanthemum pine, including new compounds (1-2) and known compounds (3-6), and pharmacodynamically acceptable salts thereof , a preparation method thereof, a pharmaceutical composition containing this type of compound, and the use of this type of compound in the preparation of drugs for preventing, relieving and / or treating inflammation. Background technique [0002] Natural products have always been an important source of anti-inflammatory drugs, and finding anti-inflammatory components from natural products is an important way to develop new drugs. Aspirin, a non-steroidal anti-inflammatory drug commonly used in the market, is derived from natural products. Pine is an endemic species of Pine genus in the family Pinaceae, and it is also endemic to my country. It grows scattered in coniferous trees and broad-leaved forests at an altitude of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J73/00C07J71/00A61K31/585A61P29/00
CPCC07J73/003C07J71/0005A61P29/00
Inventor 李勇吴练秋张海婧朱裕勋王雨菲
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI