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Aspongopus amide A and composition thereof, and application thereof in pharmacy and food

A technology of nonacidamide and its composition, applied in the field of application of nonacidamide A and its pharmaceutical composition, medicine or health food, can solve the problem of diabetic nephropathy or chronic kidney disease that has no value treatment prospect Activity and other issues

Inactive Publication Date: 2014-04-16
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, there are no related reports on the compound of the present invention and its activity with promising therapeutic prospects for diabetic nephropathy or chronic kidney disease

Method used

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  • Aspongopus amide A and composition thereof, and application thereof in pharmacy and food
  • Aspongopus amide A and composition thereof, and application thereof in pharmacy and food
  • Aspongopus amide A and composition thereof, and application thereof in pharmacy and food

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Separation and purification of compound 1 nonapongamide A [(±)-Aspongamide A]:

[0024] Take Aspongopus chinensis Dallas, crush it, and extract it with petroleum ether (60-90°C) (3×80L), acetone (3×80L) and 50% methanol (3×80L) at room temperature, stirring continuously. The 50% methanol extraction fractions were combined, the solvent was recovered under reduced pressure to obtain an extract (1 kg), which was suspended with an appropriate amount of water, and then extracted three times with an equal volume of n-butanol, and the solvent was recovered under reduced pressure to obtain an n-butanol extract (100 g). The n-butanol extract was subjected to MCI gel CHP20P column chromatography, gradient methanol water elution (10%-100%), ferric chloride-potassium ferricyanide (1:1) reagent color tracking, positive spots merged, and LC-MS tracking molecular weight is in the component of 450-600 Dalton interval, obtains component Fr.3 (10.5g), and it is through Sephadex LH-20 fil...

Embodiment 2

[0033] The compound Aspongamide A [(±)-Aspongamide A] obtained in Example 1 can be prepared into an injection after adding water for injection according to a conventional method, finely filtering, potting and sterilizing.

Embodiment 3

[0035] The compound Aspongamide A [(±)-Aspongamide A] obtained in Example 1 was dissolved in sterile water for injection, filtered with a sterile funnel, sub-packaged, freeze-dried at low temperature and sealed aseptically to obtain a powder injection .

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PUM

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Abstract

The invention relates to a novel-structure dopamine tripolymer aspongopus amide A extracted from insect Chinese medicine aspongopus capable of warming the middle-jiao and invigorating yang, a pharmaceutical composition containing the aspongopus amide A, and application thereof in preparing medicines and health food for treating diabetic nephropathy or chronic nephropathy. The clinical application of insect collateral-dredging theory proves that collaterals are related to pathological changes of blood capillaries. The aspongopus amide A has the functions of obviously inhibiting high-saccharide induced kidney mesenteric cell secretory cell epimatrix and inflammatory factor, and is a Smad3 phosphorylation inhibitor capable of obviously inhibiting TGF-beta1-induced Smad3 phosphorylation and Smad3 expression. The signal route of the TGF-beta / Smad3 is the main pathology of mediated organ fibrosis, which indicates that the compound has application value in chronic nephropathy, including diabetic nephropathy, renal fibrosis and the like.

Description

Technical field: [0001] The present invention belongs to the technical field of medicines, and in particular, relates to nonapearamide A, a pharmaceutical composition containing it and its application in preparing medicine or health food for treating diabetic nephropathy or chronic kidney disease. Background technique: [0002] The hazards, pathological mechanisms, and methods and principles of drug research of diabetic nephropathy or chronic kidney disease are clearly described by the applicant in the published patent application (Chinese patent publication number: CN102153630A). In short, chronic kidney disease presents a high incidence and refractory situation in the world. [0003] Modern studies have shown that the TGF-β / Smads signaling pathway is the main pathological mechanism mediating chronic kidney disease, including diabetic nephropathy and renal fibrosis. Smad3 hyperphosphorylation has adverse effects on the kidney, so its effective prevention will be beneficial...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D319/24A61K31/357A61P3/10A61P13/12A23L1/30A23L33/10
CPCC07D319/14
Inventor 程永现晏永明吕青
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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