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Ganolactone D, pharmaceutical composition thereof and application of ganolactone D in pharmacy and foods

A kind of ganoderma lactone, medicine technology, applied in medicine technology and food field

Inactive Publication Date: 2016-12-14
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the research on the fruiting bodies of Chizhi (Ganoderma lucidum), ganoderma lucidum D and its anti-chronic kidney disease or anti-organ fibrosis effects have been found, but there are no relevant reports on the compounds involved in the present invention and their functions in the prior art

Method used

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  • Ganolactone D, pharmaceutical composition thereof and application of ganolactone D in pharmacy and foods
  • Ganolactone D, pharmaceutical composition thereof and application of ganolactone D in pharmacy and foods
  • Ganolactone D, pharmaceutical composition thereof and application of ganolactone D in pharmacy and foods

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Separation and purification of compound 1:

[0018] Take Chizhi (80kg), pulverize, extract with 95% ethanol under reflux (2x 360L x 2h), combine the extracts and recover the solvent under reduced pressure to obtain a crude extract, suspend the crude extract in water, and then use an equal volume of ethyl acetate Extracted three times, combined extracts, and concentrated under reduced pressure to obtain ethyl acetate extract, which was subjected to silica gel (200-300 mesh) column chromatography, chloroform-methanol system gradient (99:1, 98:2, 97:3, 96:4, 95:5, 94:6, 93:7, 92:8, 90:10, 85:15, 80:20, 50:50) elution, each solvent gradient is 1.5 times the column volume, according to Seven pooled fractions were collected in 500 mL fractions. Among them, component 3 was eluted by MCI gel CHP 20P column chromatography with methanol-water (45%-100%, gradient change program of 5%) to obtain component 3.1-3.11. Among them, component 3.2 (8.4g) was eluted by Sephadex LH‐20 (me...

Embodiment 2

[0032] The compound (+)-ganodelide D in Example 1 can be made into an injection after adding injection solvent according to the conventional method, finely filtering, potting and sterilizing.

Embodiment 3

[0034] The compound (+)-ganodelide D in Example 1 was dissolved in sterile water for injection, filtered with a sterile funnel, subpackaged, freeze-dried at low temperature, and then aseptically melted and sealed to obtain a powder injection.

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PUM

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Abstract

The invention provides Ganolactone D (1), a pharmaceutical composition thereof and application of the ganolactone D in pharmacy and foods. The novel compound Ganolactone D is separated from ganoderma lucidum. Researches show that the Ganolactone D can restrain the expression of TGF-beta1 mediated renal tubular epithelial cell alpha-SMA, fibronectin and I-form collagen, thereby indicating that the Ganolactone D can obviously restrain the fibrosis of kidney tissues; and the researches also find that the Ganolactone D can selectively restrain the phosphorylation of TGF-beta1 mediated renal tubular epithelial cell Smad3, but has no obvious influence on the phosphorylation of Smad2, PI3K, ERK and p-38 and the protein expression of Smad4 and Smad7, and the phosphorylation of Smad3 is a common signal path mediating the fibrosis of multiple organs, thereby indicating the treatment effect of the Ganolactone D on the fibrosis of the organs including kidneys.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical technology and food, and in particular relates to ganoderma lactone D and its pharmaceutical composition, and its application in preparing medicine or food for treating renal fibrosis or chronic kidney disease or organ fibrosis. Background technique: [0002] Prolonged illness (chronic disease) can easily lead to organ fibrosis. Kidney fibrosis is similar to lung and liver fibrosis, and is an inevitable process leading to organ failure. Unfortunately, due to various factors such as self-aging, drug misuse, and environmental pollution, organ fibrosis has increased significantly. Taking kidney disease as an example, the incidence of chronic kidney disease in my country has exceeded 10%. Chronic kidney disease progresses through renal fibrosis to end-stage renal failure. At present, the number of uremia patients in my country has also increased significantly, and its medical expenses are astonishing. ...

Claims

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Application Information

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IPC IPC(8): C07D493/10A61K31/365A61P13/12A23L33/105
CPCC07D493/10A23V2002/00C07B2200/07
Inventor 程永现侯凡凡晏永明艾军
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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