Application of forskolin and derivatives thereof in preparing anti-pulmonary fibrosis drug

A technology for forskolin and pulmonary fibrosis, applied in the application of medicines or health products, in the field of diterpenoids, to achieve a good effect of intervention

Active Publication Date: 2019-06-14
KUNMING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no literature report that FSK and its derivatives have the effect of pre...

Method used

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  • Application of forskolin and derivatives thereof in preparing anti-pulmonary fibrosis drug
  • Application of forskolin and derivatives thereof in preparing anti-pulmonary fibrosis drug
  • Application of forskolin and derivatives thereof in preparing anti-pulmonary fibrosis drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The preparation of embodiment 1FSK and derivative thereof

[0020] The preparation of FSK and its derivatives was carried out by the extraction and separation method of the chemical components of Coleus forskohlii in the reference literature (Wang Yaqin. Determination of the chemical components of Coleus forskohlii and its extracts [D]. Fudan University, 2009.) . In addition, ISOF can also be obtained by chemical synthesis from FSK (Patent Publication No. CN105693684A).

[0021] (1) Take 10kg of Yunnan-produced Coleus forskohlii dry product, extract 3 times with 50 liters of 95% ethanol (ethanol) at room temperature, and the extract is concentrated under reduced pressure to obtain ethanol extract, and the extract is added with a small amount of After mixing well with water, extract with ethyl acetate and n-butanol in turn, and concentrate under reduced pressure to obtain the respective extracts.

[0022] (2) Put the ethyl acetate extract on a silica gel column, elute ...

Embodiment 2

[0024] Example 2 Experimental Research on the Prevention and Treatment of Pulmonary Fibrosis by FSK and DFSK on Paraquat-Induced Mouse Pulmonary Fibrosis Model

[0025] 1. Experimental method

[0026] (1) Establishment of animal model of pulmonary fibrosis

[0027] The experiment was divided into normal control group, model control group, dexamethasone (DXMS, 5mg / kg) positive control group, FSK (2.5, 5mg / kg) group, DFSK (5, 10mg / kg) group (n=10). The normal control group and the model group were given the same volume of normal saline, and the other groups were given the corresponding test drugs by intragastric administration. Except for the normal control group, the other groups were intraperitoneally injected with 20 mg / kg of paraquat (15 mg / kg) 1 hour after administration to prepare a pulmonary fibrosis model. Animals were sacrificed after 28 days of continuous administration.

[0028] (2) Pulmonary function evaluation of conscious animals

[0029] During the administrat...

Embodiment 3

[0048] Example 3 Experimental Research on the Prevention and Treatment of Pulmonary Fibrosis by ISOF on the Bleomycin-Induced Pulmonary Fibrosis Model

[0049] 1. Experimental method

[0050] (1) Establishment of animal model of pulmonary fibrosis

[0051] The experiment was divided into sham operation group, model group, dexamethasone (DXMS, 2.5 mg / kg) positive control group, ISOF (2.5, 5, 10 mg / kg) group (n=30). After the experimental mice were anesthetized with chloral hydrate, they were fixed in a supine position. Under aseptic conditions, the skin of the neck was incised in the middle of the neck to expose the trachea, and 5 mg / kg of bleomycin (BLM) was injected through the space between the cartilage rings of the trachea with a sterile syringe ( In the sham operation group, normal saline was instilled into the trachea), the mice were shaken upright and rotated to make the BLM evenly distributed in the lung, and the incision was sutured. The sham operation group and the...

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Abstract

The invention discloses use of forskolin (FSK) and derivatives thereof, including isoforskolin (ISOF) and deacetylforskolin (DFSK), in preparing a drug or a health care product for preventing and treating pulmonary fibrosis. FSK, ISOF and DFSK are a diterpenoid compound isolated from a medicinal plant coleus forskohlii. The FSK and the DFSK can significantly reduce lung inflammation and fibrosis in mice induced by paraquat, reduce hydroxyproline content in lung tissues and improve the lung function in mice. The ISOF can significantly reduce the hydroxyproline content in the mice lung tissues of bleomycin-induced pulmonary fibrosis, reduce the deposition of collagen fibers in the lung tissues, down regulate the expression of fibrogenic factors and decrease the level of inflammatory cytokines in the bronchoalveolar lavage fluid. Experimental results prove that the FSK and the derivatives ISOF and DFSK have the new use as the drug for preventing and treating the pulmonary fibrosis.

Description

technical field [0001] The invention belongs to the field of drugs for treating lung diseases, and in particular relates to the application of a diterpene compound-forskolin and its derivatives in the preparation of anti-pulmonary fibrosis drugs or health care products. Background technique [0002] Pulmonary fibrosis is a progressive disease characterized by fibrosis and pulmonary parenchymal remodeling, and its incidence is on the rise. Restrictive ventilatory disorder, the condition generally continued to deteriorate, and eventually died of respiratory failure. Excessive proliferation and transdifferentiation of pulmonary fibroblasts into myofibroblasts, secretion of a large amount of collagen and matrix deposition are important features of pulmonary fibrosis. Currently, there is no effective treatment. [0003] Forskolin (FSK) and its derivatives isoforskolin (ISOF) and deacetylforskolin (DFSK) are obtained from the medicinal plant Coleus forskolin The diterpenoid comp...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P11/00
Inventor 杨为民张旋肖创邹澄李鲜王应霞陈骋王永艳龙淑英彭琦琪翁稚颖陈晨
Owner KUNMING MEDICAL UNIVERSITY
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