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Chikusetsusaponin IVa, derivatives thereof, preparation method thereof and application thereof to preparation of medicines

A technology of bamboo ginseng saponins and derivatives, applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., can solve the problem of not finding the insulin-sensitizing activity of bamboo ginseng saponins and the like

Inactive Publication Date: 2014-01-22
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

So far, no reports and patents have been found on bamboo ginseng saponin IVa or its derivatives that have insulin-sensitizing activity or use it as a raw material to prepare pharmaceutical preparations for type II diabetes

Method used

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  • Chikusetsusaponin IVa, derivatives thereof, preparation method thereof and application thereof to preparation of medicines
  • Chikusetsusaponin IVa, derivatives thereof, preparation method thereof and application thereof to preparation of medicines
  • Chikusetsusaponin IVa, derivatives thereof, preparation method thereof and application thereof to preparation of medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Extraction and separation of bamboo ginseng saponin IVa:

[0045] Fresh bamboo ginseng rhizomes (18kg) were chopped and extracted 3 times with industrial methanol under reflux for 2 hours each time. The extract was concentrated under reduced pressure to obtain crude extract (2.3kg);

[0046] Dissolve 1.8kg of crude extract in an appropriate amount of water, and extract with ethyl acetate and n-butanol in sequence to obtain ethyl acetate layer (25g), n-butanol layer (1.2kg) and water layer (1.6kg);

[0047] The n-butanol layer (1.2kg) was chromatographed on a macroporous resin column D101 (90×8.5cm), eluted successively with 60-100% methanol water, and the methanol eluent was concentrated and combined to obtain total saponins (approx. 600g);

[0048] The total saponins were chromatographed on a 200-mesh silica gel column with CHCl 3 -MeOH-H 2 O (75:25:5 → 70:30:5 → 60:50:5 → 50:50:10) gradient elution, 250mL / part, a total of 10 components were obtained, detected by t...

Embodiment 2

[0062] Preparation of bamboo ginseng saponin IVa derivatives:

[0063] 1. Preparation of bamboo ginseng saponin IVa methyl ester (R is methyl)

[0064] Put 10mg of bamboo ginseng saponin IVa sample in a 20mL round bottom flask, add dissolved 3mg CH 2 N 2 4 mL of diethyl ether solution, reacted at room temperature for 12 hours, removed diethyl ether and CH under reduced pressure 2 N 2 , to obtain bamboo ginseng saponin IVa methyl ester (R=CH 3 ).

[0065] 2. Preparation of bamboo ginseng saponin IVa amides (R is amine group)

[0066] Put 10 mg of bamboo ginseng saponin IVa sample in a 20 mL round bottom flask, add anhydrous pyridine and ammonia, react at room temperature for 18 hours, remove anhydrous pyridine under reduced pressure, and obtain bamboo ginseng saponin IVa amide (R=NH 3 ).

Embodiment 3

[0068] Experiment on insulin-sensitizing activity of bamboo ginseng saponin IVa

[0069] 1. Detection principle:

[0070] There is a linear relationship between different insulin stimulation concentrations and the expression level of GLUT4 on the cell membrane, so detecting the expression level of GLUT4 on the cell membrane is an index for detecting insulin sensitivity.

[0071] HA and GFP tags (HA-GLUT4-GFP) were added to the N-terminal extracellular segment and C-terminal end of GLUT4 by genetic engineering methods, respectively. GLUT4 expression on the cell membrane was achieved by immunofluorescent staining of the HA tag; total GLUT4 expression in cells was achieved by quantification of GFP.

[0072] 2. Experimental method:

[0073] 2.1. Construction of adipocytes overexpressing HA-GLUT4-GFP:

[0074] The plasmid HA-GLUT4-GFP was used to construct a permanent expression 3T3-L1 cell line through a retrovirus packaging system. After the cells were differentiated into ad...

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Abstract

The invention relates to the technical field of medicines and in particular relates to a triterpenoid saponin compound chikusetsusaponin IVa separated from panax japonicus, derivatives and a preparation method thereof, a medicine composition containing the same and new medical application thereof to preparation of medicines for treating diabetes mellitus II. Biological activity tests show that the compound and the derivatives thereof have significant insulin sensitization activity, and can be used for preparing the medicines for treating diabetes mellitus II and complications which are caused by the diabetes mellitus II.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, in particular, it relates to a compound chikusetsusaponin IVa (chikusetsusaponin IVa) and its derivatives isolated from Panax japonicus C.A.Mey., or natural or synthetic , semi-synthetic composition rich in bamboo ginseng saponin IVa or a mixture of any derivatives thereof, their preparation method, and their significant insulin-sensitizing activity shown through biological activity tests, so as to be used for the preparation of treatment of type II diabetes and Other medications for complications arising from this. Background technique: [0002] Diabetes mellitus is a chronic disease of carbohydrate, fat and protein metabolism disorder caused by relative or absolute deficiency of insulin in the body or decreased sensitivity of target cells to insulin, or structural defects of insulin itself. Its main features are hyperglycemia and diabetes. It is clinically manifested as polydipsia, polypha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00C07H15/256C07H1/08A61K31/704A61P3/10
Inventor 张颖君熊文勇许敏胡敬王东朱宏涛杨崇仁
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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