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Novel medical application of isopentenyl isoflavone compounds in licorice roots

A technology of compounds and mixtures, which is applied in the field of new medical applications of a class of prenyl isoflavones in licorice, and can solve the problems that the related activities of the three compounds have not been reported.

Active Publication Date: 2016-05-18
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These targets are closely related to the pharmacological effects of licorice, and it has also been reported that some compounds or extracts derived from licorice can inhibit these targets, but the activities of the three compounds disclosed in the present invention have not been reported

Method used

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  • Novel medical application of isopentenyl isoflavone compounds in licorice roots
  • Novel medical application of isopentenyl isoflavone compounds in licorice roots
  • Novel medical application of isopentenyl isoflavone compounds in licorice roots

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1. Separation and purification of Glycyrrhizidine, angustoneA and crude Liquiritigenin D.

[0029] 1. Experimental materials and methods.

[0030] All chemical reagents mentioned in this method were purchased from Beijing Chemical Plant.

[0031] Get 35kg of licorice medicinal material (Glycyrrhiza branch of Inner Mongolia Yili Science and Technology Industrial Co., Ltd.), pulverize, extract twice with 10 times the amount of 95% ethanol and 70% ethanol, each time for 2 to 3 hours, reclaim the ethanol under reduced pressure, and the obtained The extract (10 L) was suspended in water and extracted 5 times with ethyl acetate to obtain 2500 g of the ethyl acetate fraction. Take 1280g of ethyl acetate, separate it by silica gel column chromatography (200-300 mesh, Qingdao Ocean Chemical Co., Ltd.), and elute with petroleum ether-ethyl acetate gradient (1:0-1:1) to obtain fractions A-J . Fraction E was separated by MCI column chromatography (Chengdu Kepu Biological C...

Embodiment 2

[0034] Example 2, Glycyrrhizidine, angustoneA and pillycyrrhizin D inhibit the viability of various cancer cells.

[0035] 1. Experimental materials and methods.

[0036] HepG2 human liver cancer cells, SW480 human colon cancer cells, A549 human lung cancer cells, and MCF7 human breast cancer cells were purchased from the American Type Culture Collection (ATCC), and all experiments used cells in logarithmic growth phase.

[0037] (1) 12 hours after the cells were seeded in a 96-well plate, add the specified licorice compound to a final concentration of 10 μM, and continue to cultivate for 24 hours, then add MTS solution to each well to a final concentration of 0.5 mg / mL, and continue to cultivate for 2 to 4 hours. Hours, and then use an automatic microplate reader to measure the absorbance of each well at 490nm, and calculate its inhibition rate relative to the control group.

[0038] (2) 12 hours after the cells were seeded in the 96-well plate, add the specified licorice co...

Embodiment 3

[0043] Example 3, Glycyrrhizin and angustoneA inhibit SW480 cell proliferation and induce SW480 cell apoptosis.

[0044] 1. Experimental materials and methods.

[0045] (1) After SW480 cells were seeded in 6-well plates for 12 hours, add Glycyrrhizidine or angustoneA to the specified concentration, continue to culture for 24 hours, collect all floating and adherent cells, add 1 mL of 70% ethanol, and fix overnight at -20°C . Centrifuge the fixed cells at 200 g for 5 minutes, discard the supernatant, add 1 mL of PBS (Zhongke Maichen Technology Co., Ltd.), pipette evenly, and centrifuge again. Then add 5 μg / mL propidium iodide (PI) and 100 μg / mL RNase (Beijing Boya Innovation Technology Development Co., Ltd.), incubate at 37°C for 30 minutes, and use FASCAN flow cytometry (Beckon Dickenson Company, USA) to measure, The excitation wavelength is 488nm and the emission wavelength is 630nm.

[0046] (2) 12 hours after SW480 cells were inoculated in a 6-well plate, licoricedin or ...

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Abstract

The invention discloses novel medical application of isopentenyl isoflavone compounds in licorice roots. Through systematic research on the chemical components and activity screening of the licorice roots, it is discovered that the isopentenyl isoflavone compounds including licoricidin, angustone A and glyasperin D of which the structures are similar have the significant activity on inhibition of cancer cell proliferation and inhibition of protein tyrosine phosphatase 1B (PTP1B), licoricidin and glyasperin D have the significant activity on inhibition of acetylcholine esterase (AChE), and glyasperin D also has the significant activity on inhibition of tyrosinase. On the basis of the discovery, the active compounds or salt, ester and solvent compounds, stereoisomers, tautomer and prodrugs which are acceptable in pharmacy of the active compounds and mixtures of the compounds can be used for preparing anti-cancer drugs, PTP1B inhibitors, antidiabetic drugs, tyrosinase inhibitors, freckle removing and whitening products, AChE inhibitors, anticholinesterase drugs and the like.

Description

technical field [0001] The present invention relates to a new drug application of a class of prenyl isoflavone compounds in licorice, in particular to their preparation of anticancer drugs, PTP1B inhibitors and antidiabetic drugs, tyrosinase inhibitors, and acetylcholinesterase inhibitors Applications. Background technique [0002] Licorice (Glycyrrhizauralensis Fisch.) is one of the most commonly used traditional Chinese medicines. It has been used in China for more than 2,000 years. In addition to the Chinese Pharmacopoeia, it is also included in the Japanese Pharmacopoeia, European Pharmacopoeia and American Pharmacopoeia. Licorice root has various functions such as clearing heat and detoxifying, eliminating phlegm and relieving cough, harmonizing various medicines, invigorating spleen and replenishing qi, etc. Treatment of diseases such as respiratory infections, gastric ulcers, diabetes and viral hepatitis. In addition, licorice is also widely used in the cosmetics in...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61K31/352A61K8/49A61P35/00A61P3/10A61P25/28A61Q19/02
CPCA61K8/498A61K31/352A61K31/353A61Q19/02
Inventor 叶敏余四旺季帅李紫薇王永瑞唐叔南乔雪
Owner PEKING UNIV
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