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New application of isopentene-based flavonoids compound in drug

A compound and drug technology, applied in the field of preparation of anti-inflammatory bowel disease and/or colorectal cancer drugs, can solve the problem of less than 50% survival rate

Active Publication Date: 2013-01-02
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But in general, even after radical surgery for colorectal cancer, the five-year survival rate is still less than 50%, and even in the advanced stage is less than 30%.
[0005] IAA (Isoangustone A) belongs to the known prenyl isoflavone compounds, and the biological activities reported in the literature include induction of apoptosis and cycle arrest in prostate cancer cells (Seon MR et al., Mol Nutr Food Res. 2010; 54(9) : 1329-39; J Nutr Biochem.2012; 23(1): 85-92), antioxidant (Lee YS et al., J Sep Sci.2010; 33(4-5): 664-71), inhibition of aldose reduction Enzymes (Lee YS et al., Biol Pharm Bull.2010; 33(5):917-21), inhibit mesangial fibrosis and inflammation (Li J et al., Exp Biol Med(Maywood).2011; 236(4):435 -44, Korean Patent Publication No. KR20110060993A), and as a possible active ingredient in the complex to induce NADPH quinone redoxase (Korean Patent Publication No. KR101066457B1, KR20100050767A), etc., but the effect on anti-inflammatory bowel disease and colorectal cancer is completely unknown see the report

Method used

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  • New application of isopentene-based flavonoids compound in drug
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  • New application of isopentene-based flavonoids compound in drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1. Effect of IAA on SW480 and other colon cancer cell viability and related signal transduction pathways

[0039] experimental method:

[0040] (1) Human colon cancer cell lines SW480, SW620, HCT116 and LoVo were purchased from American Type Culture Collection (ATCC). All experiments used cells in the logarithmic growth phase. After seeding in 96-well plates for 24 hours, IAA at specified concentrations were added and cultured for 24 hours or specified time. Add MTT to each well 4 hours before the end of the culture to a final concentration of 0.5 mg / mL, discard the supernatant after the end of the culture, add 150 μL of DMSO to each well, shake for 30 minutes, measure the absorbance of each well at 490 nm with an automatic microplate reader, and analyze its inhibition rate.

[0041] (2) After SW480 cells were treated with IAA for 2 hours or 24 hours, the supernatant was discarded, the cells were lysed with RIPA buffer, and the protein concentration was determ...

Embodiment 2

[0054] Example 2, IAA inhibits colon cancer cell NF-κB signal

[0055] experimental method:

[0056] (1) SW480 cells in logarithmic growth phase were transfected with NF-κB luciferase reporter gene with Lipofectamine 2000 (Life Technologies), and divided into two groups one day later. One group was directly treated with different concentrations of IAA; the other group was pretreated with bacterial lipopolysaccharide for one hour to further activate NF-κB signaling, and then treated with different concentrations of IAA. Cells were lysed after 6 hours, luciferase activity was measured, and the activity was corrected for the protein concentration of the different groups.

[0057] (2) After SW480 cells were treated with IAA for 2 hours, the proteins were extracted by SDS-PAGE and immunoblotting as in Example 1 to detect the protein levels of p-NF-κB p65, p-IKKα / β and p-IκB.

[0058] Experimental results:

[0059] (1) The NF-κB signaling pathway is significantly activated in inf...

Embodiment 3

[0062] Example 3, IAA inhibits DSS-induced inflammatory bowel disease in mice

[0063] Experimental method: Male ICR / CD1 mice with a body weight of 25-30 g were selected and randomly divided into 4 groups, namely blank control group, DSS treatment group, IAA group 1 (15 mg / kg) and IAA group 2 (30 mg / kg) . Except for the blank control group, the other three groups were only given 2% DSS (dextran sodium sulfate) aqueous solution as drinking water for 7 consecutive days, and changed to normal drinking water on the 8th day, and the mice were weighed every other day.

[0064] IAA was made into a suspension with 2% sodium carboxymethylcellulose solution, and the solution was sonicated until the solution was clear. IAA group 1 and group 2 were given 15 mg / kg and 30 mg / kg of IAA by intragastric administration respectively from the 8th day, and the other two groups were given the same amount of 2% carboxymethylcellulose sodium solution by intragastric administration, once every two da...

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PUM

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Abstract

The invention discloses a new application of isopentene-based flavonoids compound IAA (isoangustone A) in a drug. The new application disclosed by the invention is as follows: pharmaceutically acceptable salt, ester, solvolyte, stereoisomers, tautomers, prodrugs and a mixture of the salt, the ester, the solvolyte, the stereoisomers, the tautomers and prodrugs are applied in the following aspects: 1) preparing an anti-inflammatory bowel disease drug; 2) preparing a drug for preventing and / or treating colorectal cancer; 3) preparing an eucaryon colorectal cancer cell apoptosis inducer; and 4) preparing an NF-kB (nuclear factor-kappa B) signal inhibitor. The compound IAA can obviously induce the colon cancer cell apoptosis, and inhibit the activity of colon cancer cell and inflammation signals, and also can obviously alleviate the colon inflammation induced by dextran sulfate.

Description

technical field [0001] The invention relates to a new drug application of prenyl flavonoids, in particular to its application in the preparation of anti-inflammatory bowel disease and / or colorectal cancer drugs. Background technique [0002] Inflammatory bowel disease (IBD) is a kind of digestive system disease with complex etiology, common clinical and serious harm, mainly including Crohn's disease (CD) and ulcerative colitis (UC). In recent years, the incidence of inflammatory bowel disease in my country has shown a significant upward trend. It has become the main intestinal disease in my country. It has a long course of disease, repeated illnesses, often progressive aggravation, and may lead to various serious complications including colorectal cancer. . Colorectal cancer is currently the third most common malignant tumor in men and the second in women in the world; the death rate ranks fourth in men and third in women; in 2008, newly diagnosed colorectal cancer in the wo...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P29/00A61P1/00A61P35/00
Inventor 余四旺叶敏黄维乔雪马婉婉刘春芳
Owner PEKING UNIV
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