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Spirolingzhine compounds as well as pharmaceutical composition and applications thereof

A compound, the technology of Ganoderma lucidum, applied in the field of application of spirocyclic heteroterpene derivatives, medicine or health food, can solve the problem of activity that has no value treatment prospect for diabetic nephropathy or chronic kidney disease

Active Publication Date: 2014-05-28
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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  • Spirolingzhine compounds as well as pharmaceutical composition and applications thereof
  • Spirolingzhine compounds as well as pharmaceutical composition and applications thereof
  • Spirolingzhine compounds as well as pharmaceutical composition and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Separation and purification of compound 1-4:

[0020] Take 80kg of Ganoderma lucidum, pulverize, extract with 95% ethanol under reflux (2×360L×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 Extracted three times with ethyl acetate. The combined extracts were concentrated under reduced pressure to obtain 1.1 kg of ethyl acetate extract. The extract was subjected to silica gel column chromatography (silica gel 200-300 mesh, 7kg), chloroform-methanol system gradient elution (99:1, 98:2, 97:3, 96:4, 95:5, 94:6, 93:7, 92:8, 90:10, 85:15, 80:20, 50:50), each solvent gradient is 1.5 times the column volume, collected according to 500mL each) to obtain 7 combined fractions. Component 7 (36g) was chromatographed on MCI gel CHP20P column, eluted with methanol-water (20–100%) to obtain 9 subcomponents, of which component 7.2 (1.3g) was purified by Sephadex LH-...

Embodiment 2

[0042] Any one of the compounds in Example 1 can be made into an injection after adding water for injection according to the conventional method, finely filtering, potting and sterilizing.

Embodiment 3

[0044] Any one of the compounds in Example 1 was dissolved in sterile water for injection, filtered through a sterile funnel, subpackaged, freeze-dried at low temperature, and aseptically melt-sealed to obtain a powder injection.

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PUM

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Abstract

The invention provides seven spiro heterocyclic terpenoid compounds which adopt novel structures and are obtained from ganoderma lucidum as well as pharmaceutical composition, preparation methods and applications thereof to preparation of drugs for treating diabetic nephropathy or chronic nephropathy or health-care food. The compounds have significant effect on inhibition of production of active oxygen by high-glucose-induced rat mesangial cell strains, and oxidative stress commonly exists in the chronic nephropathy, so that application prospects of the compounds in the drugs for the chronic nephropathy are prompted.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, in particular, it relates to spirocyclic heteroterpene derivatives with novel structures in Ganoderma lucidum, their pharmaceutical compositions, their preparation methods, and their use in the preparation of medicines or health food for treating diabetic nephropathy or chronic kidney disease in the application. Background technique: [0002] The hazards, pathological mechanisms and drug research methods and principles of diabetic nephropathy or chronic kidney disease are clearly described by the applicant in the published patent publication number: CN102153630A. As we all know, changes in modern diet and lifestyle, coupled with environmental pollution, drug abuse and other factors, have led to frequent and high incidences of diabetic complications and chronic kidney diseases such as renal fibrosis worldwide. However, there is still a lack of clinically effective drugs for these diseases. [...

Claims

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Application Information

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IPC IPC(8): C07D307/94A61K31/343A61P13/12A23L1/30A23L31/00
CPCA23L33/10A23V2002/00C07D307/94A23V2200/328A23V2250/208A23V2200/30
Inventor 程永现王心龙方萍吕青
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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