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Natural antineoplastic compound and preparation method and use thereof

A compound and drug technology, applied in the field of natural anti-tumor compounds and their preparation and use, can solve problems such as unreported anti-tumor activity

Inactive Publication Date: 2015-12-02
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The anti-tumor activity and application of a new diterpenoid compound isolated and prepared from the fermented product of the fungus of the genus Parashieldii related to the present invention has not been reported so far

Method used

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  • Natural antineoplastic compound and preparation method and use thereof
  • Natural antineoplastic compound and preparation method and use thereof
  • Natural antineoplastic compound and preparation method and use 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 P. hawaiiense

[0049] Activation of strain P. hawaiiense. 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 P. hawaiiense. Preparation of rice culture medium (add 1Kg rice and 1500mL purified water to 12 500mL Erlenmeyer flasks in equal portions, soak overnight, sterilize with high pressure steam at 121°C for 30 minutes, 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 a bacterial suspension (spore concentration of 1×10 6 Individuals / mL) 5 mL was inoculated on the rice culture medium, and fermente...

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 is carried out high-resolution mass spectrometry (HRESIMS), infrared spectrum (IR), nuclear magnetic resonance spectrum (NMR), circular dichroism (CD) and rotational spectrum (ORD) analysis, wherein high-resolution mass spectrometry The test is provided by the Mass Spectrometry Testing Center of the Institute of Microbiology, Chinese Academy of Sciences (the test instrument model is AgilentAccurate-Mass-Q-TOFLC / MS6520), the infrared spectrum is provided by the School of Chemistry, Peking University (the test instrument model is NicoletMagna-IR750), and the nuclear magnetic resonance spectrum is provided by The National Drug and Metabolite Analysis and Research Center, Institute of Materia Medica, Chinese Academy of Medical Sciences provides the test (the test instrument model is VarianMercury-400), and the circular dichroism spec...

Embodiment 3

[0073] Embodiment 3, the effect of the compound shown in formula I on tumor cell reproductive growth

[0074] Construction of cell screening models: lung cancer cells (A549), breast cancer cells (MCF-7), colon cancer cells (HCT116), cervical cancer cells (HeLa) and bladder cancer cells (T24) (the above cells were provided by the Institute of Microbiology, Chinese Academy of Sciences Provided by Jiang Xuejun's research group).

[0075] 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 five tumor cells. In order to verify the dose-response of several tumor cells to the compound, the compound shown in formula I prepared in Example 1 and the positive control drug cisplatin were formulated with DMSO (dimethyl sulfoxide, Dimethylsulfoxide, DMSO) as a solvent to form concentrations respectively For the tested solutions of 123.76 μM, 61.88 μM, 30.94 μM, 15.47 M, 7.74 ...

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Abstract

The invention discloses a natural diterpenoid compound as shown in the formula I or pharmaceutically acceptable salt thereof, and a preparation method and a use thereof. The compound can inhibit activity of reproductive growth of cancer cells, and is used for preparing the medication for inhibiting eukaryote tumor cell proliferation or is used for preparing the medication for preventing and / or treating tumor.

Description

technical field [0001] The invention relates to a preparation method and application of a diterpenoid compound in a rice fermented product of a Paraconiothyrium hawaiiense fungus (Paraconiothyrium hawaiiense), and the compound has the effect of inhibiting the reproductive growth of tumor cells. Background technique [0002] Tumors are a serious threat to human health. The latest statistics show that the number of new cancer patients worldwide has reached 14.1 million each year, and the number of deaths from malignant tumors has increased to 8.2 million; there are about 280 cancer patients per 100,000 people in my country. About 180 people died of cancer, and the incidence of cancer is increasing year by year and getting younger. Cancer is becoming the number one killer of human health. Although some new anti-tumor drugs have emerged after years of hard work by scientists from various countries, there has not yet been a drug that can completely cure tumors, and it is the most...

Claims

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Application Information

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IPC IPC(8): C07D305/14A61K31/337A61P35/00C12P17/02C12R1/645
Inventor 车永胜陈申习张杨任凤霞牛树彬
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A