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Novel use of paeonol and metabolites thereof

A metabolite, paeonol technology, applied in the field of medicine, can solve the problem of increasing glucose consumption in 3T3-L1 adipocytes, and achieve the effect of increasing glucose consumption and strong inhibitory effect

Inactive Publication Date: 2019-05-28
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In a large number of literature reports about the metabolism of paeonol in vivo, there is no metabolite 2-hydroxy-4-methoxyacetophenone-5-O-sulfate (M2) produced after the metabolism of paeonol involved in the present invention in vivo, 2, Related reports of 5-dihyfroxy-4-methoxyacetophenone(M5) inhibiting the growth of human liver cancer cell Hep-G2 and malignant melanoma cell A-375
At the same time, there is no paeonol involved in the present invention and its in vivo metabolite resacetophenone (M1), 2-hydroxy-4-methoxyacetophenone-5-O-sulfate (M2), 2-hydroxy-4-methoxyacetophenone-5 -O-glucopyranuronosid(M3), 2-hydroxyacetophenone-4-O-glucopyranuronoside(M4), 2,5-dihyfroxy-4-methoxyacetophenone(M5), 2,4,5-trihydroxyacetophenone(M6) on 3T3-L1 adipocytes It has no obvious inhibitory effect on the growth of 3T3-L1 adipocytes, but it can significantly increase the glucose consumption of 3T3-L1 adipocytes.

Method used

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  • Novel use of paeonol and metabolites thereof
  • Novel use of paeonol and metabolites thereof
  • Novel use of paeonol and metabolites thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Separation, preparation and structure confirmation of M1-M6

[0033] The preparation method of M1-M6 was the same as that reported in the literature (Isolation and identification of the metabolites of paeonol in human urine, Xenobiotica, 2012, 42(12): 1206-1212). The structures of M1-M6 compounds are consistent with those reported in the literature.

Embodiment 2

[0034] Example 2: M2 and M5 for the proliferation inhibition experiment of Hep-G2

[0035] 1) Test cell line: human liver cancer cell Hep-G2, derived from American type culture collection (ATCC, Manassas, VA, USA)

[0036] 2) Experimental materials

[0037]DMEM medium was purchased from Gibco Company, fetal bovine serum was purchased from Biological Industries Company, trypsin was purchased from Biosharp Company, penicillin was purchased from Shenyang No. (dimethyl sulfoxide), MTT (3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide: tetramethylazozulene blue).

[0038] 3) Instruments and equipment

[0039] Carbon dioxide incubator (Shanghai Lishen Co., Ltd.), biological safety cabinet (China Haier Co., Ltd.), inverted microscope (Nikon, Japan), Milli-Q ultrapure water machine (Merck Millipore, USA), multifunctional enzyme Standard instrument (Shanghai Gene Co., Ltd.), micro oscillator (Jintan Fuhua Instrument Co., Ltd.)

[0040] 4) Cell culture

[0041] Human live...

Embodiment 3

[0051] Example 3: M2 and M5 for the proliferation inhibition experiment of A375

[0052] 1) Test cell line: human malignant melanoma cell A-375, derived from American type culture collection (ATCC, Manassas, VA, USA)

[0053] 2) Experimental materials

[0054] DMEM medium was purchased from Gibco Company, fetal bovine serum was purchased from Biological Industries Company, trypsin was purchased from Biosharp Company, penicillin was purchased from Shenyang No. (dimethyl sulfoxide), MTT (3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide: tetramethylazozulene blue).

[0055] 3) Instruments and equipment

[0056] Carbon dioxide incubator (Shanghai Lishen Co., Ltd.), biological safety cabinet (China Haier Co., Ltd.), inverted microscope (Nikon, Japan), Milli-Q ultrapure water machine (Merck Millipore, USA), multifunctional enzyme Standard instrument (Shanghai Gene Co., Ltd.), micro oscillator (Jintan Fuhua Instrument Co., Ltd.)

[0057] 4) Cell culture

[0058] Human ...

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Abstract

The invention discloses a new use of paeonol and metabolites thereof, particularly relates to a new use of the paeonol metabolites including 2-hydroxy-4-methoxyacetophenone-5-O-sulfate(M2) and 2,5-dihyfroxy-4-methoxyacetophenone(M5) in preparation of anti-tumor drugs, especially in the treatment of liver cancer and malignant melanoma, and further specifically relates to a new use of the paeonol and metabolites M1-M6 thereof in preparation of drugs for treating diabetes. The metabolites M2 and M5 can inhibit the growth of human hepatoma cells and melanoma cells, and especially have an obvious inhibition effect on the growth of A375 cells and Hep-G2 cells; 10 micrometers of the paeonol and the metabolites M1-M6 thereof are not toxic to 3T3-L1 cells; at the dose, the paeonol and the metabolites M1-M6 thereof can significantly increase glucose uptake, and the effect is similar to that of positive drugs; the metabolites M1-M6 of the paeonol can be applied to prepare the drugs for treating the diabetes.

Description

technical field [0001] The invention relates to the field of medicine, in particular to two new uses of paeonol and its metabolites. Background technique [0002] Traditional Chinese medicine is mainly administered orally. After the drug enters the body, it is absorbed, distributed, metabolized, and excreted. The metabolic transformation runs through the entire process in the body. In recent years, more and more studies have shown that after some chemical components of traditional Chinese medicine undergo metabolic transformation in the body, the metabolites formed also have certain biological activities. Obtaining active metabolites by means of enrichment, separation and synthesis, and research on metabolites can not only provide evidence for the metabolism rules and mechanism of action of single drugs or even compound prescriptions in vivo, but also discover lead compounds, which is the basis for the research and development of new drugs. one of the important ways. [00...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/12A61K31/7034A61P35/00A61P3/10
CPCA61K31/12A61K31/255A61P35/00
Inventor 丁丽琴邱峰曹世杰李巍胡欣彤姜本科程丽娜
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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