Pentacyclic triterpenes compound with ACC1 protein regulation effect and use of pentacyclic triterpenes compound

A technology of compound and application, applied in the field of pharmacy, can solve the problems such as the anti-proliferation effect of boswellic acid needs to be improved

Active Publication Date: 2017-05-17
SUZHOU BOTANY BIOMEDICALS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the antiproliferative effect of the existing boswellic acid still needs to be improved

Method used

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  • Pentacyclic triterpenes compound with ACC1 protein regulation effect and use of pentacyclic triterpenes compound
  • Pentacyclic triterpenes compound with ACC1 protein regulation effect and use of pentacyclic triterpenes compound
  • Pentacyclic triterpenes compound with ACC1 protein regulation effect and use of pentacyclic triterpenes compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Embodiment 1: preparation and identification of formula (II) compound (CKBA)

[0092] Add 8 g of acetyl-11-keto-β-boswellic acid (AKBA for short) and 2.63 g of potassium hydroxide (KOH) into a 100 ml two-necked bottle, and add 50 ml of isopropanol as a solvent under nitrogen protection. Heated to reflux for about 6 hours. After the reaction system was cooled to room temperature, the solvent was spin-dried using a rotary evaporator to obtain a white solid. After adding 30 ml of dichloromethane, dilute hydrochloric acid was added to adjust the pH of the mixed system to acidic. Extract the aqueous phase with dichloromethane for 3 times (3*15 ml), collect the dichloromethane solvent, dry with anhydrous magnesium sulfate, spin the solvent to obtain a brown oily product, use petroleum ether:ethyl acetate (90:10) as The eluent was purified by column chromatography to obtain 5.8 g of white solid KBA with a yield of about 78%. Dissolve 1 g of KBA in 10 ml of dichloromethane (co...

Embodiment 2

[0094] Embodiment 2: the preparation of the sodium carboxymethylcellulose suspension of the compound of formula (II)

[0095] (1) Suspension 1

[0096] A certain amount of sodium carboxymethylcellulose (CMC-Na for short) was dissolved in double distilled water overnight to prepare a 0.3% (g / ml) CMC-Na solution. Add a certain amount of CKBA powder to this solution to prepare a 5 mg / ml suspension, and CKBA can be disperse with simple ultrasonic assistance.

[0097] (2) Blank suspension

[0098] A certain amount of sodium carboxymethylcellulose (CMC-Na for short) was dissolved overnight in double distilled water to prepare a 0.3% (g / ml) CMC-Na solution as a blank suspension. The blank suspension was used as a control in animal experiments.

Embodiment 3

[0099] Embodiment 3: Experiment of inhibiting the growth of human colon cancer cells in vitro

[0100] Take human colon cancer cell lines HCT116, Lovo, HT29 and SW480 (purchased from ATCC) in logarithmic growth phase in 96-well plates, 1.5×10 per well 4 Each cell was added with CKBA and AKBA in gradient concentrations (1, 5, 10, 20, 25, 30, 35, 50, 100 μM) respectively, and the total volume was 100 μl. The control group was added with DMSO at a final concentration of 0.5%. Only 100 microliters of culture medium was added to the blank control wells, and three replicate wells were set up in each group. After 24 hours of culture in the cell incubator, add 10 microliters of CCK-8 solution to each well, and place the culture plate in the incubator (37°C, 5% CO 2 conditions) and incubate in the dark for 4 hours before taking out. The O.D. value at the wavelength of 450nm was measured by a microplate reader. Calculation of inhibition rate: inhibition rate = [1-(O.D. value of exper...

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Abstract

The invention relates to a pentacyclic triterpenes compound with an ACC1 protein regulation effect and a use of the pentacyclic triterpenes compound. The compound can directly act on ACC1 proteins to play an effect of inhibiting the tumor growth, and the inhibition effect is significant.

Description

technical field [0001] The present invention belongs to the field of pharmacy; more specifically, the present invention relates to a pentacyclic triterpenoid compound with ACC1 protein regulation function and its use and its use in the preparation of anti-tumor drugs. Background technique [0002] In the past 20 years, the incidence of colorectal cancer (mainly colon cancer) in most countries in the world is on the rise. With the improvement of people's living standards, changes in eating habits and structure, coupled with the impact of population aging, the incidence and death of colorectal cancer in my country are also increasing. According to statistics, there are more than 170,000 new cases each year in my country, and it is the fourth most common malignant tumor disease in China. The median age of onset of colorectal cancer in China is about ten years earlier than in Europe and the United States, and young patients are more common than in Europe and the United States. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61K31/56A61P35/00
Inventor 王宏林白晶
Owner SUZHOU BOTANY BIOMEDICALS
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