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Application of alkaloid in preparing pharmaceutical compositions for preventing and treating pulmonary fibrosis

A pulmonary fibrosis and compound technology, which is applied in the field of alkaloids to achieve the effects of reducing the degree of pulmonary fibrosis, easy availability of materials and low price

Active Publication Date: 2014-12-10
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no literature report on the efficacy of phyllonine in the prevention or treatment of pulmonary fibrosis or its application in drugs for the treatment of pulmonary fibrosis.

Method used

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  • Application of alkaloid in preparing pharmaceutical compositions for preventing and treating pulmonary fibrosis
  • Application of alkaloid in preparing pharmaceutical compositions for preventing and treating pulmonary fibrosis
  • Application of alkaloid in preparing pharmaceutical compositions for preventing and treating pulmonary fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1 Preparation and structure identification of alkaloids

[0059] 1. Medicinal materials and reagents

[0060] The medicinal material is the dried root of Stemona tuberosa Lour., purchased from Hebei Anguo Medicinal Materials Market. Reagents such as ethanol, dichloromethane, and methanol were all analytically pure.

[0061] 2. Extraction and separation

[0062] Use 90% ethanol percolation to extract the medicinal material of Phyllostachys chinensis, until the percolation liquid is concentrated and TLC detects that there is basically no bismuth iodide potassium reaction. Add 5% dilute hydrochloric acid to the percolation concentrated solution to acidify to pH 1-2, filter, alkalinize the filtrate to pH 10 with concentrated ammonia water, extract with chloroform, and recover the chloroform to obtain the total alkaloid fraction. The total alkaloids were eluted by silica gel column chromatography, dichloromethane-methanol gradient (100:0~1:5), and the same fractio...

Embodiment 2

[0080] Example 2 Preparation of an animal model of pulmonary fibrosis

[0081] 1. Main reagents and experimental animals

[0082] The bleomycin used in the experiment was purchased from Nippon Kayaku Co., Ltd., batch number 730342.

[0083] The SPF grade C57BL / 6 mice (female, 8 weeks old) used in the experiment were purchased from the Comparative Medicine Center of Yangzhou University.

[0084] 2. Model Preparation

[0085] Bleomycin-induced pulmonary fibrosis in mice is an internationally recognized animal model for screening anti-pulmonary fibrosis drugs. Acute lung injury caused by bleomycin modeling, mainly manifested as inflammation at the initial stage, fibrosis began to appear in about 10 days, and a large amount of collagen concentrated in the lungs, these pathological changes are very similar to those of idiopathic pulmonary fibrosis in clinical practice resemblance. Although the pathogenesis and mechanism of idiopathic pulmonary fibrosis are not clear, both bleom...

Embodiment 3

[0087] Example 3 Identification of Eight Alkaloids and Kebiqing Anti-pulmonary Fibrosis Activity in Mice

[0088] This example aims to study the anti-pulmonary fibrosis activity of the alkaloids obtained in Example 1 to identify whether they have an anti-pulmonary fibrosis effect. Since these alkaloids are the active components of cough suppressant in Baibu, a traditional Chinese medicine, in order to know whether the cough suppressant can resist pulmonary fibrosis, this example chooses the commonly used cough suppressant——pentoxyverine, pentoxyverine citrate tablet, cough suppressant Positive control drugs commonly used in pharmacological experiments) were simultaneously screened for anti-pulmonary fibrosis activity.

[0089] 1. Main reagents and experimental animals

[0090] Compounds I-VIII were obtained according to Example 1, and the purity was >98%. Kebiqing was purchased from Sinopharm Rongsheng Pharmaceutical Co., Ltd., batch number 13110221. The bleomycin used in t...

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Abstract

The invention discloses a new application of a compound shown in a structural formula I in preparing medicaments for preventing and / or treating pulmonary fibrosis. The invention has a compound shown in the structural formula I, which can significantly reduce the inflammation indexes of pathologically changed pulmonary tissues, reduce the content of fibrosis-promoting factors TGF-beta 1 in pathologically changed pulmonary tissues, reduce the excessive deposition of collagens in pathologically changed pulmonary tissues, and has a significant prevention and treatment effect on pulmonary fibrosis.

Description

technical field [0001] The present invention relates to a class of alkaloids with anti-pulmonary fibrosis activity, in particular to the application of the alkaloids represented by structural formula I in the preparation of pharmaceutical compositions for preventing or treating pulmonary fibrosis. Background technique [0002] Pulmonary fibrosis (PF) is a type of disease in which the persistent alveolar damage caused by lung inflammation leads to excessive repair of cells and excessive deposition of extracellular matrix, resulting in changes in the structure of normal lung tissue and loss of function. The clinical manifestations are progressive Difficulty breathing, shortness of breath, and fatigue, and the condition was persistent. In layman's terms, pulmonary fibrosis is the scarring of lung tissue. As the alveoli are gradually replaced by fibrous substances, the lung tissue hardens and thickens, and the ability to exchange oxygen is gradually lost. Patients suffer from va...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/553A61P11/00C07D491/16
CPCA61K31/55A61K31/553A61P11/00C07D491/16
Inventor 张勉许翔鸿向娟张朝凤贺艳慧吴艳
Owner CHINA PHARM UNIV
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