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A kind of compound extracted and separated from Rhododendron chinensis and the application of the compound in the preparation of antidiabetic drugs

A compound and diabetes technology, applied in the application field of the preparation of anti-diabetic drugs, can solve the problems of unclear mechanism of action, complex components and the like

Active Publication Date: 2021-06-01
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, scholars at home and abroad are mainly studying the biological activity of the traditional Chinese medicine Hongmaoqi. There are few studies on the specific pharmacological activities of the chemical components contained in it. It is mostly used in combination with other medicinal materials. The components are complex and its mechanism of action is still unclear. There are no relevant literatures about the anti-diabetic effects of triterpenoid saponins, and the structure of the triterpenoids has strong specificity. Therefore, starting from the isolation and identification of the monomeric compounds, find the active ingredients that exert various medicinal effects , in order to conduct in-depth research, development and utilization, it is of great significance

Method used

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  • A kind of compound extracted and separated from Rhododendron chinensis and the application of the compound in the preparation of antidiabetic drugs
  • A kind of compound extracted and separated from Rhododendron chinensis and the application of the compound in the preparation of antidiabetic drugs
  • A kind of compound extracted and separated from Rhododendron chinensis and the application of the compound in the preparation of antidiabetic drugs

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Embodiment 1

[0023] The preparation of embodiment 1 formula (1) compound

[0024] Step 1, get the root and rhizome 30.0kg of dry Caulophyllum robustum Maxim., after pulverizing through a 20 mesh sieve, use 95v / v% ethanol (120L) and 60v / v% ethanol (120L) successively Extract by rolling, combine the extracts, and concentrate to obtain 6.3kg of total extract;

[0025] Step 2, after suspending the total extract obtained in step 1 with water, extract with petroleum ether and ethyl acetate in sequence to obtain petroleum ether part extract (200.0g) and ethyl acetate part extract (410.0g);

[0026] Step 3, the ethyl acetate part extract (410.0g) obtained in step 2 is used for silica gel column chromatography, and gradient elution is carried out with petroleum ether: ethyl acetate system, and the volume ratios are: 10:1, 8:1, 6:1, 4:1, 2:1, 1:1, 0:1), collect petroleum ether: ethyl acetate volume ratio 2:1-1:1 eluate, numbered as Fr.C, after subtraction Compress and concentrate to dryness, set a...

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Abstract

The present invention relates to the technical field of medicinal compounds, and specifically discloses a new compound 3 extracted and separated from Rhododendron chinensis β , 23‑dihydroxy‑28‑norolean‑12‑ene‑16‑one, and the application of the new compound in the preparation of antidiabetic drugs. The present invention uses modern spectrum techniques such as 1D-NMR, 2D-NMR, high-resolution mass spectrometry, etc. to identify the structure of the isolated monomer compound, and deduce the molecular structure of the compound. The results of enzyme activity experiments showed that the new compound has a good inhibitory effect on protein tyrosine phosphatase 1B (PTP1B), α ‑Glucosidase activity. The results of molecular docking showed that the new compound had good binding activity with the target protein, and the interaction force was mainly hydrogen bond and hydrophobic force. The new compound has a good hypoglycemic effect and has a good application prospect in the treatment of diabetes.

Description

technical field [0001] The invention relates to the technical field of medicinal compounds, in particular to a new compound 3β,23-dihydroxy-28-norolean-12-ene-16-one (3β,23-dihydroxy-28-one (3β,23-dihydroxy-28- Norcarb-olean-12-en-16-one) and the application of the new compound in the preparation of antidiabetic drugs. Background technique [0002] Caulophyllum robustum Maxim. is the root and rhizome of Berberidaceae plant Caulophyllum robustum Maxim. It is also known as Caulophyllum robustum Maxim. Hongmaoqi is mainly produced in Heilongjiang, Shaanxi, Liaoning, Gansu, Hubei and other places. It grows in the shade and damp places of ravines at an altitude of about 950-3500 meters, under forests or under bamboo forests. It is used as a Tujia national medicine in Hubei Province. Its roots and rhizomes are used as medicines. It has the functions of expelling wind and dampness, clearing away heat and detoxification, promoting blood circulation and removing blood stasis, loweri...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61P3/10A23L33/105
CPCA23V2002/00A23L33/105A61P3/10C07J63/008A23V2200/328A23V2250/21A23V2300/14A23V2300/31A23V2300/38
Inventor 刘新桥王静覃彬华
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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