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Application of an azazulene alkaloid in the preparation of drugs for preventing or treating pulmonary fibrosis

A technique for pulmonary fibrosis and drugs, applied in drug combinations, active ingredients of heterocyclic compounds, organic chemistry, etc., can solve problems such as azazune-type alkaloids that have not yet been retrieved, and achieve the reduction of pulmonary fibrosis, low price, The effect of easy access to materials

Active Publication Date: 2017-02-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, no patent has been retrieved for the azazune-type alkaloids shown in structural formula I, and there have been no literature reports that this type of alkaloids has the effect of preventing or treating pulmonary fibrosis or its role in drugs for the treatment of pulmonary fibrosis. application

Method used

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  • Application of an azazulene alkaloid in the preparation of drugs for preventing or treating pulmonary fibrosis
  • Application of an azazulene alkaloid in the preparation of drugs for preventing or treating pulmonary fibrosis
  • Application of an azazulene alkaloid in the preparation of drugs for preventing or treating pulmonary fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Example 1 Preparation and structure identification of alkaloids

[0069] 1. Medicinal materials and reagents

[0070] The medicinal material is the dried root of Stemona sessilifolia (Miq.) Miq., which was purchased from Bozhou Medicinal Materials Market in Anhui. Reagents such as ethanol, dichloromethane, and methanol were all analytically pure.

[0071] 2. Extraction and separation

[0072] 3 times of reflux extraction with 95% ethanol, concentrated under reduced pressure until there is no alcohol smell, acidified with 5% dilute hydrochloric acid to pH 1-2, filtered, the filtrate was alkalized with concentrated ammonia water to pH 10, extracted with chloroform, recovered chloroform to obtain the total biological base site. The total alkaloids were eluted by silica gel column chromatography, dichloromethane-methanol gradient (100:0~100:5), and the same fractions were combined according to the TLC results, and then subjected to repeated silica gel column chromatograp...

Embodiment 2

[0082] Example 2 Preparation of an animal model of pulmonary fibrosis

[0083] 1. Main reagents and experimental animals

[0084] The bleomycin used in the experiment was purchased from Nippon Kayaku Co., Ltd., batch number 730342.

[0085] The SPF grade C57BL / 6 mice (female, 8 weeks old) used in the experiment were purchased from the Comparative Medicine Center of Yangzhou University.

[0086] 2. Model Preparation

[0087] 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

[0089] Example 3 Identification of four alkaloids and Kebiqing anti-pulmonary fibrosis activity in mice

[0090] 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 a commonly used cough suppressant in clinical practice——pentoxyverine, pentoxyverine citrate tablet, cough suppressant Positive control drugs commonly used in pharmacological experiments) were simultaneously screened for anti-pulmonary fibrosis activity.

[0091] 1. Main reagents and experimental animals

[0092] Compounds I-IV were obtained according to Example 1, and the purity was >98%. Kebiqing was purchased from Sinopharm Rongsheng Pharmaceutical Co., Ltd., batch number 13110221. The ble...

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Abstract

The invention discloses application of alkaloids shown in the structural formula I to preparing medicines for preventing and / or treating pulmonary fibrosis. According to the alkaloids shown in the structural formula I, the inflammation degree of the lesion pulmonary tissue can be obviously reduced, the content of fibrosis prompting factors TGF-beta1 in the lesion pulmonary tissue can be reduced, excessive deposition of collagen in the lesion pulmonary tissue can be reduced, and obvious preventing and treating effects on the pulmonary fibrosis are achieved.

Description

technical field [0001] The present invention relates to an azazulene alkaloid with anti-pulmonary fibrosis activity, in particular to the application of the alkaloid represented by structural formula I in the preparation of a pharmaceutical composition for preventing or treating pulmonary fibrosis. Background technique [0002] Idiopathic pulmonary fibrosis (IPF) is a diffuse lung disease of unknown etiology, characterized by rapidly progressive lung parenchymal damage and fibrosis, which eventually diffuses to the entire lung, resulting in severe damage to lung structure and function. The clinical manifestations are progressive dyspnea, dry cough, progressive reduction of lung function, hypoxemia, and eventually respiratory failure and death. The typical pathological changes of IPF are fibroblastic focal lesions composed of fibroblasts and myofibroblasts. In active fibrous foci, myofibroblasts occupy a dominant position and are important effector cells in the process of fi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/55A61P11/00C07D491/147
CPCA61K31/55C07D491/147
Inventor 许翔鸿张朝凤贺艳慧张勉吴艳向娟
Owner CHINA PHARM UNIV
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