Application of mogrol H9 for preparing antitumor drugs

An anti-tumor drug and tumor technology, applied in the chemical industry, can solve the problems of low content and difficult to separate and purify in large quantities, and achieve the effects of inhibiting proliferation, small side effects, and obvious tumor inhibiting effect.

Inactive Publication Date: 2012-07-04
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] H9 is found in Luo Han Guo, but the content is very low, it is difficult to separate and purify in large quantities

Method used

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  • Application of mogrol H9 for preparing antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 MTS method to determine the growth inhibitory effect of H9 on liver cancer cells

[0041] HepG2 (purchased from ATCC) 3×10 3 Each well was inoculated into a 96-well plate, cultured for 24 hours to allow it to adhere to the wall, and then added H9 (Shanghai Institute of Materia Medica, Chinese Academy of Sciences), with 6 concentration gradients and 3 replicate wells for each concentration. Cells at 37°C, 5% CO 2 After culturing for 72 hours under the same conditions, the culture medium was discarded, and the cell viability was measured with an MTS kit (Promega Company).

[0042]The test method is: wash the cells once with serum-free medium, add the pre-prepared MTS chromogenic solution according to the amount of 100 μl / well (add 2 ml of solution 1 and 100 μl of solution 2 to 10 ml of serum-free medium, mix thoroughly uniform). A well without cells was set as the background well to correct for the background light absorption of the solution. Put the cells ...

Embodiment 2

[0048] Example 2 The growth inhibitory effect of H9 on human pancreatic cancer cells

[0049] Using cck-8 kit (Japan Dojin Chemical Research Institute) detection.

[0050] step:

[0051] 1) The PANC-1 cells (purchased from the Cell Bank of the Chinese Academy of Sciences) were evenly planted in a 96-well plate, and the number of cells per well was 3*10 3 indivual.

[0052] 2) Wait for the wall to adhere, add the drug after overnight, add the drug (the concentrations of H9 are 50, 16.67, 5.56, 1.85, and 0.62 μM), and each concentration has 3 replicate wells.

[0053] 3) After culturing for 48 hours, replace the complete medium with a mixture of serum-free medium and CCK8 (10:1), and incubate in a 37°C incubator for 2 hours.

[0054] 4) Take 450nm as the measurement wavelength and 650nm as the reference wavelength, and measure the reading on a microplate reader.

[0055] Results: The IC50 value of H9 on PANC-1 cells was 283.8 μM.

[0056] The above results indicated that H9...

Embodiment 3

[0057] Example 3 The growth inhibitory effect of H9 on human gastric cancer cells

[0058] The effect of H9 on HGC was tested according to the method in Example 2, and the results showed that the IC50 value of H9 on HGC cells (purchased from ATCC, American Tissue Culture Collection, American Tissue Culture Bank) was 103.69 μM.

[0059] The above results indicated that H9 had a certain inhibitory effect on gastric cancer cell HGC.

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Abstract

The invention belongs to the technical field of chemical and pharmaceutical industry and particularly relates to the application of mogrol H9 for preparing antitumor drugs. The invention provides the application of mogrol H9 for preparing antitumor medicaments. The tumor cell can be liver cancer cell, leukaemia cell, cervical carcinoma cell, lung adenocarcinoma cell, stomach cancer cell, breast cancer cell or pancreatic cancer cell. The compound H9 is a natural product, has less toxic and adverse effects, high bioavailability and stable property, and is significant in clinical use. The small molecule compound is developed as a new antitumor drug or antitumor effective component, has an obvious antitumor effect, is green and environment-friendly, and provides a new approach to treatment and healing of tumors.

Description

technical field [0001] The invention belongs to the fields of chemical engineering and medicine technology, and in particular relates to the application of a cucurbitane-type tetracyclic triterpenoid compound in the preparation of antitumor drugs. Background technique [0002] The structural formula of the cucurbitane-type tetracyclic triterpenes involved in the present invention is as follows: [0003] [0004] Its CAS number is 64675-48-5, which is abbreviated as H9 in the present invention, and is commonly known as mogrosvenol. [0005] H9 is found in Luo Han Guo, but the content is very low, and it is difficult to separate and purify in large quantities. The Chinese invention patent with the application number 200710039126 and the invention title "Purification and Preparation Method of Mogrosanol" discloses a method for the purification and preparation of H9. The method comprises the steps: (1) crushing Luo Han Guo first, adding ethanol to extract to obtain alcoholi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P35/00C12Q1/02
Inventor 余龙刘祖龙唐丽莎胡立宏
Owner FUDAN UNIV
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