Natural compound and preparation method and application thereof

A compound and drug technology, applied in the field of natural compounds and their preparation, can solve the problems of delay in the research and development of anti-tumor drugs

Active Publication Date: 2013-04-24
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, the research and development of anti-tumor drugs is relatively lagging behind, and a drug that can completely cure tumors has not yet appeared

Method used

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  • Natural compound and preparation method and application thereof
  • Natural compound and preparation method and application thereof
  • Natural compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation of compound shown in embodiment 1, formula I

[0048] a. Solid fermentation of strain Doratomyces sp.

[0049] Activation of the strain Doratomyces.sp. PDA medium: 200g of potatoes, 20g of glucose, 15g of agar, 1000mL of purified water, sterilized by high-pressure steam at 121°C for 30 minutes, made into a test tube slant, picked mycelium and inoculated it on the test tube slant, and cultured at 25°C for 10 days.

[0050] Solid state fermentation of strain Doratomyces sp. Preparation of rice culture medium (add 800g rice and 1200mL purified water into ten 500mL Erlenmeyer flasks, soak overnight, sterilize by high-pressure steam at 121°C for 30 minutes, and cool for later use); pick mycelium from the inclined surface of the test tube in Prepare a bacterial suspension in a test tube filled with sterile water, and prepare the prepared bacterial suspension (spore concentration of 1×10 6 Individuals / mL) 5 mL was inoculated on the rice medium, and fermented...

Embodiment 2

[0062] The structural characterization of the compound shown in embodiment 2, formula I

[0063] The compound shown in formula I prepared in Example 1 was analyzed by high-resolution mass spectrometry (HRESIMS), infrared spectrum (IR), nuclear magnetic resonance spectrum (NMR), circular dichroism (CD) and rotational spectroscopy (ORD), wherein high-resolution mass spectrometry The test was provided by the Mass Spectrometry Test Center of the Institute of Microbiology, Chinese Academy of Sciences (the test instrument model is Agilent Accurate-Mass-Q-TOF LC / MS 6520), and the infrared spectrum was tested by the School of Chemistry, Peking University (the test instrument model is NicoletMagna-IR 750), The NMR spectrum was tested by the Instrument Analysis and Test Center of the Academy of Military Medical Sciences (the test instrument model is Varian UNTTY INOVA 600), the circular dichroism spectrum is tested by the Institute of Toxicology and Drugs of the Academy of Military Medi...

Embodiment 3

[0074] Embodiment 3, the effect of the compound shown in formula I on tumor cell reproductive growth

[0075] Construction of cell screening models: lung cancer cells (A549), breast cancer cells (MCF-7), colon cancer cells (SW480, HCT116), cervical cancer cells (HeLa) and bladder cancer cells (T24) (the above cells were provided by the Chinese Academy of Sciences Microbiology Provided by Jiang Xuejun's research group of the Institute).

[0076] MTT method (MTT colorimetric method) was used to test the effect of the compound represented by formula I prepared in Example 1 on the reproductive growth of the above six tumor cells. In order to verify the dosage effect of several tumor cells on the compound, the compound shown in formula I prepared in Example 1 and the positive control drug cisplatin were prepared with DMSO (Dimethyl sulfoxide, DMSO) as a solvent to a concentration of The solutions to be tested were 123.76 μM, 61.88 μM, 30.94 μM, 15.47 μM, 7.74 μM, 3.87 μM, 1.93 μM ...

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Abstract

The invention discloses a natural compound shown in the formula I or pharmaceutically acceptable salts thereof and a preparation method and application thereof. The compound has the activity of inhibiting reproductive growth of tumor cells and can be used for preparing drugs for inhibiting proliferation of tumor cells of eukaryotes or used for preparing drugs for preventing and / or treating tumors. The Formula I is shown in the specification.

Description

technical field [0001] The invention relates to a natural compound and its preparation method and application. The compound has the function of inhibiting the reproductive growth of tumor cells. Background technique [0002] Tumors are a serious threat to human health, and the morbidity and mortality rates of tumors in my country are high. According to the report of the World Health Organization at the 18th International Union Against Cancer Congress, the number of new cancer patients will increase from 10 million to 15 million in the next 20 years, and the number of deaths from malignant tumors will also increase from 6 million to 10 million. million, accounting for 12% of the world's total deaths. Cancer is becoming the number one killer of human beings in the new century. At present, the research and development of anti-tumor drugs is relatively lagging behind, and a drug that can completely cure tumors has not yet appeared. Although my country has developed some anti-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D309/32C12P17/06A61K31/366A61P35/00
Inventor 车永胜李彦
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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