Application of norwerethrin-7-sulfate in the preparation of anti-pulmonary fibrosis drugs

Abstract

The invention relates to application of demethylwedelolactone-7-sulphate in preparation of an anti-pulmonary fibrosis medicine. The compound demethylwedelolactone-7-sulphate is obtained from a traditional Chinese medicinal material eclipta for the first time, and the structure is determined by virtue of NMR (nuclear magnetic resonance) and other spectrum data; In-vivo and in-vitro pharmacological experiment results prove that the demethylwedelolactone-7-sulphate can be used for remarkably inhibiting proliferation of TGF (transforming growth factor)-beta1 induced human embryonic lung fibroblast and HYP (hydroxyproline) content thereof, and inflammation and fibrosis degree of the lung tissue in a bleomycin induced mouse pulmonary fibrosis model can be improved in the oral gavage dosing range of 5-30mg / kg, the MDA (methylene dioxyamphetamine) content reflecting the lung injury degree in the lung tissue can be influenced, the HYP content reflecting lung tissue collagen deposition can be reduced, and the cytokine TGF-beta1 content causing pulmonary fibrosis can be reduced, so that the pharmacological action of the pulmonary fibrosis degree can be improved. The demethylwedelolactone-7-sulphate has novel application in medicines for treating or improving pulmonary fibrosis diseases.

Description

technical field [0001] The invention relates to a new use of the compound norwedelolide-7-sulfate as a medicine for treating pulmonary fibrosis. Background technique [0002] Pulmonary fibrosis is a progressive disease characterized by fibrosis and lung parenchymal remodeling. Pulmonary fibroblasts hyperproliferate, transdifferentiate into myofibroblasts, secrete a large amount of collagen and deposit matrix. There is no effective treatment. Bleomycin-induced pulmonary fibrosis animal model is the most commonly used. Intratracheal administration of bleomycin causes tissue inflammation and fibrosis within a short period of time, and bleomycin causes upregulation of pro-inflammatory cytokines such as IL-1 and TNF-α, followed by an increase in pro-fibrotic markers such as TGF-β1 , Fibronectin, and α-SMA expression reached the highest value at 14 days. The bleomycin animal model began to show fibrosis symptoms 9 days after modeling, and typical fibrosis symptoms appeared on 2...

AI Technical Summary

Problems solved by technology

The general treatment of emphysema drugs is ineffective or poor in the treatment of pulmonary fibrosis, because the drugs that relax the bronchi cannot finally slow down or stop the excessive deposition of collagen in the lung tissue, and collagen deposition is the main feature of pulmonary fibrosis and etiology

[0006] At present, there is no literature report that norwedelolide and other analogues have pharmacological efficacy in the treatment of pulmonary fibrosis and their application in drugs for the treatment of pulmonary fibrosis

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