Application of 2-methoxy-6-acetyl-7-methyljuglone (MAM) for preparing medicine for treating neoplastic diseases

An acetyl and methoxy technology, applied in antineoplastic drugs, drug combinations, pharmaceutical formulations, etc.

Inactive Publication Date: 2013-03-27
UNIVERSITY OF MACAU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the anti-tumor effect of MAM at home and abroad.

Method used

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  • Application of 2-methoxy-6-acetyl-7-methyljuglone (MAM) for preparing medicine for treating neoplastic diseases
  • Application of 2-methoxy-6-acetyl-7-methyljuglone (MAM) for preparing medicine for treating neoplastic diseases
  • Application of 2-methoxy-6-acetyl-7-methyljuglone (MAM) for preparing medicine for treating neoplastic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1 (in vitro antitumor effect of MAM)

[0043] Take the tumor cells in the logarithmic growth phase and inoculate them on 96-well plates according to the size of the cells ((5-10)×10 3 per well), after 24 hours of growth, the supernatant was discarded. Then administer the drug at the following concentration, set up no drug-dosing group (blank control group) and drug-dosing group (concentration 0.1-10 μ M), each group is set up 6 duplicate wells, continue to cultivate for 24 hours, discard the supernatant, add 100 μ l containing 0.5mg / ml of MTT serum-free culture solution was incubated for 4 hours, the supernatant was discarded, 100 μl of dimethyl sulfoxide (DMSO) was added, placed on a micro-oscillator for 10 minutes, and the OD value was detected at 570 nm with a microplate reader. The normal human liver cell line LO2 was used for toxicity evaluation. Each experiment was repeated 3 times. The results are shown in Table 1 and image 3 .

[0044] image ...

Embodiment 2

[0049] Example 2 (Cell Morphological Observation)

[0050] MCF-7 cells were cultured in 96-well plates and divided into blank control group and MAM treatment group. Different concentrations of MAM (1 μM, 2 μM, 3 μM, 5 μM, 8 μM) were added to the MAM treatment group, and the same concentration of vehicle (DMSO) was added to the blank control group. After continuing to culture for 24 hours, the morphological changes of the cells were observed under a microscope.

[0051] Such as Figure 4 As shown, it was found that the cells in the blank control group had normal morphology, and after being treated with different concentrations of MAM, the cells became round, smaller, and shrunken; under the action of high concentrations of MAM, cell fragments appeared, and the cells floated, indicating death. The concentration dependence is obvious.

Embodiment 3

[0052] Example 3 (JC-1 staining to detect changes in mitochondrial membrane potential)

[0053] MCF-7 cells were cultured in 24-well plates and divided into blank control group and MAM treatment group. Different concentrations of MAM (1 μM, 2 μM, 5 μM) were added to the MAM treatment group, and the same concentration of vehicle (DMSO) was added to the blank control group. After continuing to culture for 4 hours, stain with JC-1 dye in the dark (final concentration 2 μg / ml) for 15 minutes, observe and take pictures with a fluorescent microscope.

[0054] Such as Figure 5 As shown, it was found that the cells in the blank control group had red fluorescence and green fluorescence, and after MAM treatment, with the increase of drug concentration, the green fluorescence gradually increased, and the red fluorescence gradually decreased, suggesting that MAM treatment caused a change in the mitochondrial membrane potential of the cells. changes, resulting in a decrease in the mitoc...

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Abstract

The invention discloses application of 2-methoxy-6-acetyl-7-methyljuglone (MAM) for preparing a medicine for treating neoplastic diseases. According to the invention, found from research on the anti-neoplastic activity of MAM, MAM has obvious inhibitory activity on proliferation of a plurality of measured neoplastic cells in vitro; the better cytotoxic effect is shown; the IC50 (50% inhibiting concentration) of MAM is less than or equal to 10 mu M; furthermore, MAM has good dose-effect relationship; simultaneously, when MAM is acted on a normal hepatic cell strain LO2, the cytotoxicity of MAM is lower than the toxic reaction of MAM on a hepatic neoplastic cell HepG2; and furthermore, the research also finds that MAM is capable of obviously reducing mitochondrial membrane potential of neoplastic cells and inducing apoptosis.

Description

technical field [0001] The present invention relates to the field of natural medicines, in particular to 2-methoxy-6-acetyl-7-methyljuglone (2-Methoxy-6-Acetyl-7-Methyljuglone, also known as 2-Methoxystypandrone, hereinafter referred to as MAM) application. Background technique [0002] Polygonum cuspidatum is the dry rhizome and root of Polygonum cuspidatum Sieb.et Zucc. Polygonum cuspidatum is a traditional Chinese medicine, which has the functions of clearing heat and detoxifying, promoting gallbladder and reducing jaundice, dispelling wind and dampness, dispelling blood stasis and relieving pain, relieving cough and reducing phlegm, etc. A variety of chemical components have been found in knotweed, including stilbenes, anthraquinones, flavonoids, tannins, polysaccharides, etc. Among them, resveratrol (Huang et al., Anticancer Agents Med Chem.2011, 11, 479-490.), emodin (Ma et al., Food Chem Toxicol.2012, 50, 1271-1278.) etc. have been confirmed It has obvious antitumo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P35/00A61P35/02
Inventor 王一涛陈修平张庆文鲍娇琳
Owner UNIVERSITY OF MACAU
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