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Polycyclic polyisopentenyl acyl phloroglucinol compound and its preparation method and application

A technology for polycyclic polyprenyl acyl phloroglucinol and prenyl acyl phloroglucinol, applied in the field of medicine, can solve problems such as toxic and side effects, and achieve the effects of simple extraction and separation methods and easy raw materials

Active Publication Date: 2021-03-05
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the reported synthetic ligands of RXRα have severe toxic side effects

Method used

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  • Polycyclic polyisopentenyl acyl phloroglucinol compound and its preparation method and application
  • Polycyclic polyisopentenyl acyl phloroglucinol compound and its preparation method and application
  • Polycyclic polyisopentenyl acyl phloroglucinol compound and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Preparation and structural identification of polycyclic polyisopentenyl acylphloroglucinol compounds involved in the present invention

[0046] 1. Preparation of compound:

[0047] Step 1: Mince the whole plant of the material A. spp. (12.9 kg), and extract it by cold soaking with ethanol-water solution with a volume fraction of 60% to 99% for 2 to 4 times, each time for 12 to 24 hours. Preferably, the volume fraction is 70% to 95% ethanol-water solution for cold soaking and extraction for 2 to 3 times, each time for 18 to 24 hours. The soaking liquid was recovered and concentrated under reduced pressure to obtain 949.68 g of crude ethanol extract, which was extracted with an equal volume of petroleum ether and then concentrated under reduced pressure to obtain crude extract.

[0048] Step 2: Pass 150.7 g of the petroleum ether crude extract in step 1 through silica gel column chromatography, using cyclohexane and ethyl acetate as mobile phases (1:0, 50:1, 25:1, 10:1, ...

Embodiment 2

[0066] Example 2: Anti-breast cancer and cervical cancer effects of the compounds involved in the present invention targeting the nuclear receptor RXRα

[0067] 1 Materials and Instruments

[0068] 1.1 Experimental cells: human breast cancer MCF-7 and cervical cancer HeLa cells

[0069] 1.2 Experimental Instruments

[0070] Inverted Microscope Japan Olympus Leica Company

[0071] Cell incubator American Thermo company

[0072] Millipore Ultrapure Water Meter Millipore, USA

[0073] High-speed refrigerated centrifuge American beckMan Coulter Co., Ltd.

[0074] Micropipette Eppendorf, USA

[0075] Protein vertical electrophoresis instrument Bio-Rad, USA

[0076] Wet transfer tank American Bio-Rad company

[0077] Disposable petri dish Belgium Orange Scientific company

[0078] 48-well culture plate, Orange Scientific, Belgium

[0079] 96-well culture plate, Orange Scientific, Belgium

[0080] Vertical Automatic Electric Pressure Steam Sterilizer Shanghai Shenan Medical...

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Abstract

The polycyclic polyisopentenyl acylphloroglucinol compound and its preparation method and application relate to the technical field of medicine. It is obtained from the whole stem of the plant. The extraction and separation method is simple and the raw materials are easy to obtain. The polycyclic polyisopentenyl acylphloroglucinol compound is used in the preparation of antitumor drugs, and can be used as an anticancer drug targeting nuclear receptor RXRα. It can target the nuclear receptor RXRα to inhibit the proliferation of human breast cancer cell line (MCF‑7) and cervical cancer cell line (HeLa). Therefore, the compound is expected to be developed as an anti-tumor drug targeting the nuclear receptor RXRα or as a lead compound for the development of an anti-tumor drug.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to polycyclic polyisopentenyl acylphloroglucinol compounds and their preparation methods and applications. Background technique [0002] Cancer, namely malignant tumor, is one of the main diseases that endanger human health. Breast cancer and cervical cancer are malignant tumors that often occur in women and seriously threaten the health of women all over the world. According to the World Health Organization's International Agency for Research on Cancer's report on cancer research in 184 countries and regions around the world, in 2018 there were about 100 cases of breast cancer worldwide. 2.1 million cases, or 11.6% of all 18.1 million new cancer cases. Breast cancer accounts for 24.2% of the 8.6 million new cancer cases in women, and accounts for 15.0% of the 4.2 million women's cancer deaths, both ranking first (Ma Dandan. 2018 Global Cancer Statistics: Breast Cancer Incidence ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/80A61P35/00
CPCA61P35/00C07D311/80
Inventor 田文静陈海峰王光辉林挺邱大任周宓
Owner XIAMEN UNIV
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