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A kind of natural small molecular compound and its application in the preparation of antitumor drugs

A technology of compounds and extracts, which is applied in the field of natural small molecule compounds, can solve the problems of cell tumor growth and so on

Inactive Publication Date: 2011-12-21
CENT SOUTH UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, once the function or expression of the genes controlling apoptosis is altered, this precise balance may be disturbed, which may lead to the neoplastic expansion of cells

Method used

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  • A kind of natural small molecular compound and its application in the preparation of antitumor drugs
  • A kind of natural small molecular compound and its application in the preparation of antitumor drugs
  • A kind of natural small molecular compound and its application in the preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1. Isolation and identification of Neoalbaconol.

[0051] Collect complete and fresh fruiting bodies of Albatrellus confluens and soak them in 95% ethanol. After standing at room temperature for 7 days, take the ethanol solution and evaporate to dryness to obtain ethanol extract; weigh the extract residue (0.715kg) and Pulverize, soak for one day at room temperature through dichloromethane / methanol (volume ratio 1: 1), get dichloromethane / methanol solution and evaporate to dryness, obtain extract, repeat extraction like this 6 times; Merge the extract that each extraction obtains, use Chloroform / ethyl acetate mixed solvent (volume ratio 8: 2) was dissolved and separated by 50mm×100cm silica gel column chromatography, the eluent was chloroform / ethyl acetate mixture (volume ratio 8: 2), and the elution speed It is 1 ml per minute; from the first minute, the eluent collected by the chromatography column every 10 minutes is a fraction, wherein fractions 1-4 are evap...

Embodiment 2

[0059] Example 2. Neoalbaconol inhibits the proliferation of various tumor cell lines.

[0060] The inhibitory effect of the compound Neoalbaconol on tumor cell proliferation was observed by Am-Blue method, and the 50% inhibitory concentration (IC50 value) of its proliferation activity was determined. Am-Blue (SUNBIO Company) is a redox indicator used for detection of cell proliferation and toxicity. It is purple-blue and non-fluorescent in the oxidized state, and turns into a pink or red fluorescent reduction product in the reduced state. Its absorption peak is It is 530-560nm, and the scattering peak is 590nm.

[0061] During the process of cell proliferation, the ratios of NADPH / NADP, FADH / FAD, FMNH / FMN and NADH / NAD in cells increase, and they are in a reducing environment. After the Am-Blue reagent is taken into the cell, the oxidized blue indicator is reduced by the mitochondria of the cell and released outside the cell, making the medium turn fluorescent pink or red. U...

Embodiment 3

[0070] Example 3. Neoalbaconol induces apoptosis in tumor cell lines.

[0071] In order to observe the apoptosis-inducing effect of the compound Neoalbaconol on tumor cells, the C666-1 nasopharyngeal carcinoma cell line was treated with different concentrations of the compound, the nuclei were stained with ethidium bromide (PI), and the stained cells were detected by flow cytometry. Ratio, from which the ratio of late apoptotic cells can be judged.

[0072] The operation steps are as follows: the C666-1 cell line was treated with 0 μM, 5 μM, 10 μM, and 20 μM Neoalbaconol for 24 hours and 48 hours respectively; the treated cells were collected by trypsinization without EDTA, and the cells were washed twice with PBS (centrifugation 2000rpm, 5min) to collect 1~5×10 5 Cells were fixed in pre-cooled 70% ethanol; 5 μL PI was added and mixed; protected from light and reacted at room temperature for 5 minutes; flow cytometry (Ex=488nm; Em=530nm) was used to detect PI-positive cells. ...

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Abstract

The invention discloses a natural small molecular compound and its application in the preparation of antitumor drugs. The small molecular compound is isolated from the fruiting body of Albatrellus confluens, and has a new type of C-skeleton composed of a pyrane-type sesquiterpene-like structure as a side chain connected with resorcinol, named Neoalbaconol. A series of studies have found that Neoalbaconol inhibits tumor cell proliferation and induces tumor cell apoptosis by inhibiting NF-κB, E2F-1 and PI3K / AKT / TSC2 / mTOR signaling pathways. It has significant broad-spectrum anti-tumor activity and can be used to prepare antineoplastic drugs.

Description

technical field [0001] The invention relates to a natural small molecule compound and its medical use, in particular to a natural small molecule compound Neoalbaconol isolated from fungi and its application in antitumor drugs. Background technique [0002] Tumor is a general term for diseases caused by uncontrolled growth of some cells in the body and abnormal accumulation of homologous cells. There are currently more than 100 types. These out-of-control cells have the ability to proliferate indefinitely and can escape apoptosis, leading to their abnormal accumulation in the body, infiltration to surrounding tissues and distant metastasis, which eventually lead to the occurrence and development of tumors. At present, the goal of most tumor treatments is to reduce the number of cells and prevent their further aggregation. Inhibiting the proliferation of tumor cells is a common feature of anti-tumor chemical drugs. [0003] Apoptosis plays a key role in many physiological pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C39/17C07C37/70A61K31/05A61P35/00A61P35/02
Inventor 曹亚刘吉开邓启盼丁智慧于新芳冯涛
Owner CENT SOUTH UNIV
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