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Ampelopsin derivative, synthesizing method thereof and application of the same in preparing antineoplastic medicine

A technology for the synthesis of staphylococcus, which can be used in antitumor drugs, drug combinations, medical preparations containing active ingredients, etc., and can solve the problems of low bioavailability and low lipophilicity of 5-fluorouracil, affecting anti-tumor efficacy and the like.

Inactive Publication Date: 2008-05-28
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to significant first-pass metabolism and low lipophilicity, the bioavailability of 5-fluorouracil is low, which affects the anti-tumor efficacy, and its therapeutic dose is close to the toxic dose

Method used

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  • Ampelopsin derivative, synthesizing method thereof and application of the same in preparing antineoplastic medicine
  • Ampelopsin derivative, synthesizing method thereof and application of the same in preparing antineoplastic medicine
  • Ampelopsin derivative, synthesizing method thereof and application of the same in preparing antineoplastic medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation of compound 3,5,3',4',5'-pentahydroxy-7-(5-fluorouracil-1-acetic acid)-2,3-dihydroflavone

[0036] 1 Experimental instruments and materials

[0037] 1.1 Instruments and equipment

[0038] Rotary evaporator: RE-52AA, Shanghai Yarong Biochemical Instrument Factory; circulating water multi-purpose vacuum pump: SHB-III, Zhengzhou Great Wall Technology Industry and Trade Co., Ltd.; collector type constant temperature heating magnetic stirrer: DF-101S, Yingyu, Gongyi City Yuhua Instrument Factory; Vacuum Drying Oven: 876-1, Shanghai Pudong Dongfeng Scientific Instrument Co., Ltd.; Electrothermal Constant Temperature Blast Drying Oven: 101-1, Shanghai Yuejin Medical Instrument Factory; pH ​​Meter: pHS-25, Shanghai Leici Instrument Factory; constant temperature magnetic stirrer: JB-2 type, Shanghai Leici Instrument Factory.

[0039] High performance liquid chromatography: LC-10AT VP, Shimadzu, Japan; UV-visible spectrophotometer: UV4802, Unico Instrument...

Embodiment 2

[0072] Embodiment 2 Antitumor pharmacological experiments of the compound of Example 1

[0073] 1. Experimental Instruments and Materials

[0074] 1.1 Instruments and equipment

[0075] CO 2 Incubator: American Precision Company; Inverted microscope: Chongqing Optical Instrument Factory; Microplate reader: American Bio-TEK Company; Desktop low-speed centrifuge: Type 0412-1, Shanghai Medical Instrument Co., Ltd.; 96-well cell culture plate: American CORNING Company ;Cell culture flask: American CORNING company

[0076] 1.2 Drugs and reagents

[0077] RPMI-1640 medium, newborn bovine serum: GIBCO Company; green chain double antibody: Shanghai Sangong; brominated thiazolyl blue tetrazolium (MTT): SIGMA Company;

[0078] Cell line: K562 sensitive strain, Sun Yat-sen University Cancer Hospital Experimental Center

[0079] 2 Experimental methods

[0080] 2.1 Liquid preparation

Embodiment 1

[0081] The compound of Example 1 was directly dissolved in serum-free culture medium to prepare the concentration required for the experiment, and sterilized by filtration with a 0.22 μm microporous membrane, ready to use.

[0082] 2.2 Cell Culture

[0083] Human leukemia K562 cells contained 10% inactivated newborn bovine serum by volume, 1×10 5 U·L -1 penicillin and 100mg·L -1 Cultured in RPMI-1640 medium of streptomycin, placed at 37°C, CO 2 Cultured in an incubator with a content of 5%. After 2-3 days, replace the medium by centrifugation or subculture, and take the cells in the logarithmic growth phase for experiments.

[0084] 2.3 Determination of tumor cell growth inhibition rate by MTT method

[0085] Dilute the K562 cells in the logarithmic growth phase with fresh culture medium, count them, and inoculate them in 96-well culture plates, so that each well has 5×10 4 about a cell. Dissolve the compound of Example 1 with serum-free culture solution, and configure 3....

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Abstract

The invention relates to a ampelopsin derivative, wherein R1-R5 are represented as formula II or H, and R1-R5 are not all as H. The invention further relates to the synthesis method of the derivative and relative application for preparing anti-cancer drug.

Description

technical field [0001] The present invention relates to a compound, its synthesis method and its application in the preparation of anti-tumor drugs, in particular, it relates to a staphylophyllin derivative, its synthesis method and its application in the preparation of anti-tumor drugs. Background technique [0002] Ampeloptin, also known as dihydromyricetin, chemically named "3,5,7,3',4',5'-hexahydroxy-dihydroflavone", is a plant of the genus Ampeloptin The main component of Ampelopsis cantoniensis (Hook.et Am.) Planch.], or Ampelopsis grossedentata (Hand.-Mazz.) W.T.Wang], belongs to dihydroflavonols. In recent years, it has been found that staphylophyllin is a strong tyrosinase inhibitor [Liu Deyu, Lei Huanqiang. Inhibition of myricetin and staphylophyllin on tyrosinase. Journal of Biochemistry, 1996, 12( 5): 618-620]. Staphylococcus can significantly inhibit the proliferation of human promyelocytic leukemia HL-60 and K562 cells, human nasopharyngeal carcinoma HK-1 cel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12A61K31/506A61P35/00
Inventor 刘德育
Owner SUN YAT SEN UNIV
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