Sucrose derivatives, preparation method of same, and application thereof as anti-cancer medicine
A technology of derivatives and anti-tumor drugs, applied in the field of medicine, can solve the problems that have not been found in the research report of the activity of Yunnan rabbit ear wind
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Embodiment 1
[0050] Example 1: Preparation of Ansloside B(2)
[0051] 1 Sample source
[0052] The whole plant of Ainsliaea yunnanensis Franch.
[0053] 2 Extraction, separation and purification methods
[0054] Take the dried whole plant (15.0kg) of Yunnan rabbit ear wind and crush it, heat and reflux it twice with 80L of 95% and 80% ethanol respectively, then combine the extracts; the extracts obtained after concentration under reduced pressure are dispersed in water Then, petroleum ether (15L), chloroform (15L), ethyl acetate (15L), and n-butanol (15L) were used for liquid-liquid extraction of the water-dispersed extract in the order of polarity from small to large. Four extraction parts of petroleum ether, chloroform, ethyl acetate and n-butanol were obtained respectively; the extract (400g) of the ethyl acetate part was obtained, and subjected to 80-100 mesh silica gel column chromatography, with petroleum ether-acetic acid Ethyl ester system 100:1,50:1,30:1,20:1,10:1,5:1,0:1 for elution, a...
Embodiment 2
[0059] Example 2: Determination of glycoglycone and sugar structure in compound 2
[0060] Compound 2 6.0mg dissolved in 5% KOH-H 2 In O (5mL), heat at 95°C and reflux for 3h. The reaction mixture was acidified with hydrochloric acid to pH=4.0, extracted with chloroform and n-butanol three times, and dried under reduced pressure to obtain 2.1 mg of chloroform layer. After being dissolved in deuterated chloroform, the NMR spectrum was measured and it was identified as isovaleric acid.
[0061] Isovaleric acid: 1 H NMR(in CDCl 3 ,500MHz)δ H 2.23(2H,d,J=7.5Hz), 2.12(1H,m), 0.99(6H,d,J=7.0Hz); 13 C NMRδ C 178.8(- C OOH),43.0(CH 2 ),25.5(CH),23.3(CH 3 ),22.3(CH 3 ).
[0062] The n-butanol layer of compound 2 alkaline hydrolyzate, add a small amount of methanol to dissolve in 2M HCl-H 2 In O (5mL), heat to reflux at 95°C for 4h, and extract three times with n-butanol. After the water layer is dried under reduced pressure, it is dissolved in water and analyzed directly by HPLC with ELSD ...
Embodiment 3
[0063] Example 3: Cytotoxicity test
[0064] 1. Experimental materials
[0065] Human lung adenocarcinoma cells (A549) were purchased from the Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences;
[0066] The compound ansloside B(2) was prepared in Example 1.
[0067] 2. Methods of screening for cytotoxic activity and mechanism of action
[0068] (1) MTT method to detect cytotoxic activity
[0069] Collect A549 cells growing in log phase and adjust the cell suspension concentration to 1×10 5 Inoculate each well into 96-well plate, each well volume is 100μL, 37℃, 5% CO 2 Cultivation under conditions, after the cells adhere to the wall, add different concentrations of the test compound to continue the culture for 24 hours. After the culture is terminated, add 10μL of 5mg / mL MTT solution to each well, continue to incubate for 4 hours, centrifuge to discard the culture solution, add 100μL of DMSO to each well to dissolve the f...
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