Application of demethylwedelolactone-7-sulfate in preparation of anti-pulmonary fibrosis drug

Abstract

The invention relates to application of demethylwedelolactone-7-sulfate in preparation of an anti-pulmonary fibrosis drug. The compound demethylwedelolactone-7-sulfate is obtained from traditional Chinese medicine herba ecliptae for the first time and the structure of demethylwedelolactone-7-sulfate is determined through NMR (Nuclear Magnetic Resonance) and other wave spectrum data, the in-vivo and in-vitro pharmacological experiments prove that the demethylwedelolactone-7-sulfate can obviously inhibit the proliferation of TGF-beta1 induced human embryo lung fibroblasts and the HYP (hydroxyproline) content, the inflammation and fibrosis degree of lung tissue in bleomycin induced mice pulmonary fibrosis model can be reduced after the anti-pulmonary fibrosis drug is orally taken at a dosage of the 5-30mg / kg, the content of MDA (methylene dioxyamphetamine) reflecting the lung injury degree in lung tissues is influenced, the content of HYP reflecting the collagen deposition of lung tissue can be reduced, the content of cell factor TGF-beta1 causing pulmonary fibrosis can be reduced, and the like, so that the pharmacological action for improving the pulmonary fibrosis degree can be achieved. The demethylwedelolactone-7-sulfate has new applications as a drug for treating or improving pulmonary fibrosis disease.

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...

Examples

Embodiment Construction

[0017] 1. Preparation and structure confirmation of norwedelide 7-sulfate

[0018] Herba Ecliptae (Herba Ecliptae) is the dry aerial part of Eclipta prostrate L., a plant of Compositae, purchased from Bozhou, Anhui. Reagents such as ethanol and petroleum ether were of analytical grade. Dry the aboveground part of Eclipta chinensis, extract 3 times with 80% ethanol 10 times the volume of crude drug, 2 hours each time, filter, combine the extracts, remove ethanol under reduced pressure to obtain 903g of total extract, petroleum ether, ethyl acetate in turn , n-butanol equivalent extraction, and the n-butanol extract was concentrated under reduced pressure by silica gel (150-200 mesh) column chromatography, eluted with chloroform-methanol-water (5:3:0.1), Sephadex LH-20 chromatographic column Purified, and eluted with chloroform-methanol (1:1) to obtain the compound demethylwedelolactone-7-sulfate (Demethylwedelolctone-7-sulfate).

[0019] Spectral data and its structure are as...

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...

Examples

Embodiment Construction

[0017] 1. Preparation and structure confirmation of norwedelide 7-sulfate

[0018] Herba Ecliptae (Herba Ecliptae) is the dry aerial part of Eclipta prostrate L., a plant of Compositae, purchased from Bozhou, Anhui. Reagents such as ethanol and petroleum ether were of analytical grade. Dry the aboveground part of Eclipta chinensis, extract 3 times with 80% ethanol 10 times the volume of crude drug, 2 hours each time, filter, combine the extracts, remove ethanol under reduced pressure to obtain 903g of total extract, petroleum ether, ethyl acetate in turn , n-butanol equivalent extraction, and the n-butanol extract was concentrated under reduced pressure by silica gel (150-200 mesh) column chromatography, eluted with chloroform-methanol-water (5:3:0.1), Sephadex LH-20 chromatographic column Purified, and eluted with chloroform-methanol (1:1) to obtain the compound demethylwedelolactone-7-sulfate (Demethylwedelolctone-7-sulfate).

[0019] Spectral data and its structure are as...

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