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Dendrobium officinale analogue and preparation method and application thereof

A technology of dendrobium officin and its analogues, which is applied in the field of dendrobium officin analogues and their preparation, and can solve the problems of low bioavailability, expensive source of raw materials and the like

Pending Publication Date: 2021-01-26
YUNNAN AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dendrobium officinale is a natural bibenzyl compound derived from Dendrobium officinale. It has anti-inflammatory effects, but its bioavailability is low and the source of raw materials is expensive.

Method used

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  • Dendrobium officinale analogue and preparation method and application thereof
  • Dendrobium officinale analogue and preparation method and application thereof
  • Dendrobium officinale analogue and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: the synthesis of Dendrobium officinale analogue Compound 1

[0031] The synthesis of Dendrobium officinale analogue Compound 1 is as follows: image 3 shown.

[0032] Synthesis of compound 7: Add 3,5-dimethoxy-4-hydroxybenzaldehyde (9.1 g, 50 mmol), N,N-Diisopropylethylamine (14.0 mL, 80 mmol) into a 250 mL round-bottomed flask replaced with nitrogen and 4-dimethylaminopyridine (61 mg, 0.5 mmol) were added to 100 mL of dichloromethane to fully dissolve, and chloromethyl ether (4.6 mL, 60 mmol) was added dropwise at 0ºC, and the temperature was raised after the addition was completed After reacting at room temperature for 6 h, TLC showed that the reaction was complete. The reaction solution was diluted with water, added with cold HCl aqueous solution (50 mL, 0.1 M), and extracted to obtain an organic layer, which was extracted twice with 50 mL of dichloromethane, and the organic phases were combined. The organic phase was washed with water, washed with s...

Embodiment 2

[0038] Embodiment 2: In vitro inhibitory effect of dendrobium officinale analogues on cancer cells

[0039] 1. Experimental materials

[0040] Cell lines: human lung cancer cell line A549, human breast cancer cell line MCF-7, human leukemia cell line HL-60, human colon cancer cell line SW480, human liver cancer cell line HepG2, human skin squamous cell line A431

[0041] Detection principle: MTT method to detect cell viability

[0042] 2. Test method

[0043] 1) Cell inoculation: Use RMP1640 or DMEM medium containing 10% fetal bovine serum to prepare a single cell suspension, and inoculate 10,000-20,000 cells per well into a 96-well plate with a volume of 100 µL per well.

[0044] 2) After 12 hours, the cells were replaced with 1% penicillin-streptomycin DMEM or RMP1640 medium, and the compound solution to be tested was added (fixed concentration 40µM for primary screening, at which concentration the compound that inhibited tumor cell growth at around 50% was entered at 5 co...

Embodiment 3

[0050] Example 3: In vitro inhibitory effect of dendrobium officinale analogs on colon cancer SW480 cells

[0051] Take the cells in the logarithmic growth phase to adjust the concentration of the cell suspension, and the seeding volume of the cells is 1000 / well. Set blank wells and positive control wells at the same time. Incubate for 24 h at 37°C in an incubator with 5% carbon dioxide. Add the compound to be tested in 1640 medium with 1% penicillin and streptomycin, after 24 hours of treatment, change back to 10% fetal bovine serum medium, and continue to culture for 14 days.

[0052] The result is as Figure 5 As shown, Dendrobium officinale analogs can significantly inhibit the growth of colon cancer SW480 cells in a concentration-dependent manner.

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Abstract

The invention discloses a dendrobium officinale analogue and pharmaceutically acceptable salt and hydrate thereof, and the analogue has anti-tumor activity, especially significantly inhibits the growth of colon cancer SW480 cells, and is a potential new chemical entity for treating colon cancer. The invention further discloses a simple and efficient preparation method of the dendrobium officinaleanalogue and application of the dendrobium officinale analogue in preparation of anti-cancer, anti-tumor and colorectal cancer treatment pharmaceutical compositions, and the dendrobium officinale analogue has important significance in research and development of anti-cancer or anti-colorectal cancer drugs.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a dendrobium officinale analogue and a preparation method and use thereof. Background technique [0002] Colon cancer is a common gastrointestinal malignancy and the fourth leading cause of cancer-related death. In recent decades, although great progress has been made in diagnosis and treatment, its morbidity, mortality, and disability rates have not improved significantly, causing a great burden to society and families. Early colon cancer can be cured by surgery, but colon cancer that has metastasized to the liver or other parts is usually difficult to cure, and the five-year survival rate is low. Chemotherapy is the main method for the treatment of advanced colon cancer. DDP and 5-FU are common drugs, but their side effects are relatively large, which seriously affects the quality of life of patients. Because of the high incidence and poor prognosis of colon cancer, col...

Claims

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Application Information

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IPC IPC(8): C07D319/20A61K31/357A61P35/00A61P35/04
CPCC07D319/20A61P35/00A61P35/04Y02P20/55
Inventor 字成庭盛军王宣军燕静云杨豪男张帮磊胡月杨宁张宁吴以龙
Owner YUNNAN AGRICULTURAL UNIVERSITY
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