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New application of in-vivo metabolites of paeonol
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A metabolite, paeonol technology, applied in the field of medicine to achieve a strong inhibitory effect
Inactive Publication Date: 2020-10-13
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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[0008] In a large number of literature reports about the metabolism of paeonolin 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 livercancercell Hep-G2 and malignant melanomacell A-375
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Embodiment 1
[0025] Example 1: Separation, preparation and structure confirmation of M1-M6
[0026] 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
[0027] Example 2: M2 and M5 for the proliferation inhibition experiment of Hep-G2
[0028] 1) Test cell line: human livercancer cell Hep-G2, derived from American type culture collection (ATCC, Manassas, VA, USA)
[0029] 2) Experimental materials
[0030] 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).
[0043] Example 3: M2 and M5 for the proliferation inhibition experiment of A375
[0044] 1) Test cell line: human malignant melanoma cell A-375, derived from American type culture collection (ATCC, Manassas, VA, USA)
[0045] 2) Experimental materials
[0046] 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).
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Abstract
The invention discloses new application of in-vivo metabolites of paeonol, and particularly relates to new application of 2-hydroxy-4-methoxyacephenone-5-O-sulfate (M2) and 2, 5-dihydrofroxy-4-methoxyacephenone (M5) in preparation of antitumor drugs, and particularly relates to application in treatment of liver cancer and malignant melanoma. The metabolites M2 and M5 can inhibit growth of human livercancer cells and melanoma cells, especially have an obvious inhibition effect on growth of A375 cells, and also have an obvious inhibition effect on growth of Hep-G2 cells.
Description
technical field [0001] The invention relates to the field of medicine, in particular to the new application of paeonol 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. [000...
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Application Information
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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/12A61K31/255A61P35/00
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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