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Compound for preventing cancers and preparation method thereof

A cancer prevention and compound technology, applied in the fields of steroids, organic chemistry, drug combination, etc., can solve the problems of few reports and no artificial citation and cultivation.

Active Publication Date: 2013-10-09
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Physalis angulata L.var.villosa Bonati is a variety of Physalis angulata L.var.villosa Bonati, which is mostly distributed in Vietnam and Zhejiang, Jiangxi, Hubei, Yunnan and other provinces in mainland China. It generally grows in grass. Currently Not yet cultivated artificially
Mao Kulu, bitter and cold in nature, belongs to the lung meridian. It has the effects of clearing away heat and detoxification, relieving pharynx, reducing phlegm, and diuresis. There are very few reports on Mao Kumi

Method used

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  • Compound for preventing cancers and preparation method thereof
  • Compound for preventing cancers and preparation method thereof
  • Compound for preventing cancers and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] 1) Put 1Kg of the persistent calyx into the extraction tank, add an ethanol aqueous solution containing 95% ethanol by volume (that is, 5Kg of the ethanol aqueous solution) that is 5 times the weight of the persistent calyx, and extract under reflux at 90°C. The time of each extraction is 2h, and the total extraction is 4 times (a total of 20Kg in ethanol aqueous solution), and the extraction liquid is combined;

[0058] 2) Concentrate the extract obtained in step 1) (recover ethanol) to nearly dryness to obtain 130 g of thick extract, dilute with 1 L of water, extract with 1 L of ethyl acetate each time, extract 3 times in total, and combine the extracts;

[0059] 3) 20 g of the extract obtained by concentrating the extract obtained in step 2) is passed through a silica gel chromatographic column (wet column packing, dry loading), wherein the filler used in the silica gel chromatographic column is 100 mesh column chromatography silica gel , the weight ratio of extract ...

Embodiment 2

[0068] 1) Put 1Kg of the persistent calyx into the extraction tank, add an ethanol aqueous solution containing 95% ethanol by volume (that is, 3Kg of the ethanol aqueous solution) which is 3 times the weight of the persistent calyx, and extract under reflux at 100°C. The time of each extraction is 3h, and the total extraction is 2 times (the ethanol aqueous solution is 6Kg in total), and the extracts are combined;

[0069] 2) Concentrate the extract obtained in step 1) (recover ethanol) to nearly dryness to obtain 110 g of thick extract, dilute with 1 L of water, extract with 1 L of ethyl acetate each time, extract 3 times in total, and combine the extracts;

[0070] 3) 16g of extract obtained by concentrating the extract obtained in step 2) is passed through a silica gel chromatography column (wet column packing, dry loading), wherein the filler used in the silica gel chromatography column is 200 mesh column chromatography silica gel , the weight ratio of extract to column ch...

Embodiment 3

[0073] Embodiment 3 (quinone reductase induction experiment)

[0074] Take logarithmic phase mouse liver cancer cells (Hepa1c1c7, purchased from ATCC), 1×10 per well 4Inoculate on a 96-well plate, add 200 μL of DMEM medium to each well, discard the supernatant after 12 hours, and then add compound A (0.106 mg) with quinone reductase activity prepared in Example 1 to three duplicate wells, and another Select 3 multiple wells to add compound B with cancer prevention effect, and finally add compound C with cancer prevention effect to the other 3 multiple wells, corresponding to compound dosing group A, compound dosing group B and compound dosing group Drug group C: add 4′-bromoflavone (0.106 mg) to 3 duplicate wells, which is the positive control drug group; add dimethyl sulfoxide (0.106 mg) to 3 duplicate wells, which is the negative control group; The blank group was 200 μL DMEM medium without drug addition. After culturing for 24 h, the supernatant was discarded. Digitonin ...

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Abstract

The invention discloses a compound for preventing cancers. The structure of the compound is shown in the formula II, wherein R represents Alpha-OH or Beta-OH. The compound has the quinone reductase inducing activity and can be used for preventing cancers. The invention further discloses a preparation method of the compound for preventing cancers. The method is simple, reliable, easy to implement, strong in operability and good in controllability.

Description

technical field [0001] The invention relates to the field of biochemistry and medicine, in particular to a compound with cancer prevention effect extracted from kulan fennel and a preparation method thereof. Background technique [0002] Withanolide-type compounds are a class of ergostane-type steroidal compounds with 28 carbon atoms, and their main structure is shown in the structure of formula III, wherein the T part in the structure of formula III may be a, b, c, d , one of e, f, g, h. WITHHANOLIDE-type compounds are divided into classic and non-classical. The classic WITHHANOLIDE type compounds occupy the absolute majority in nature, and these compounds are mainly distributed in several genera of Solanaceae such as physalis. The biological activities of WITHANOLIDE compounds are mainly manifested in anti-tumor, anti-inflammation, anti-bacterial, insect repellant as plant and so on. Due to the complex structure of such compounds and many chiral centers, such compounds ...

Claims

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Application Information

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IPC IPC(8): C07J17/00A61P35/00
Inventor 马忠俊丁辉胡志娟
Owner ZHEJIANG UNIV
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