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Compound for preventing cancers and preparation method thereof

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

Active Publication Date: 2015-05-20
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 calyx in the extraction tank, add 5 times the weight of the calyx in the calyx, each time with a 95% ethanol aqueous solution (that is, 5Kg of ethanol), and reflux at 90°C. Each extraction time is 2h, a total of 4 extractions (a total of 20Kg of ethanol aqueous solution), and the extracts are combined;

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

[0059] 3) Concentrate the extract obtained in step 2) to obtain 20 g of the extract through a silica gel column (wet column, dry sample), wherein the filler used for the silica gel column is 100 mesh column chromatography silica gel The weight ratio of the extract to the column chromatography silica gel is 1:15, and then it is eluted with an elution solvent composed of petroleum ether and ethyl acetate with a volume ratio o...

Embodiment 2

[0068] 1) Put 1Kg of the calyx in the extraction tank, each time add 3 times the weight of the calyx in the calyx with ethanol containing 95% ethanol (ie 3Kg of ethanol), reflux and extract at 100℃. The time for each extraction is 3h, a total of 2 extractions (a total of 6Kg of ethanol aqueous solution), and the extracts are combined;

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

[0070] 3) Concentrate the extract obtained in step 2) to obtain 16 g of the extract through a silica gel chromatography column (wet column loading, dry loading), wherein the packing used for the silica gel column is 200 mesh column chromatography silica gel The weight ratio of the extract to the column chromatography silica gel is 1:20, and then it is eluted with an elution solvent consisting of petroleum ...

Embodiment 3

[0073] Example 3 (quinone reductase induction experiment)

[0074] Take log phase mouse liver cancer cells (Hepa1c1c7, purchased from ATCC), 1×10 per well 4 Inoculate on a 96-well plate, add 200μL of DMEM medium to each well, 12h later, discard the supernatant, and then add the compound A (0.106mg) with quinone reductase activity prepared in Example 1 to 3 replicate wells. Choose 3 multiple wells to add compound B with cancer preventive effect, and finally add compound C with cancer preventive effect to the other 3 multiple wells, corresponding to compound dosing group A, compound dosing group B, and compound plus Drug group C; 4'-bromoflavonoids (0.106mg) were added to 3 re-wells, which was the positive control dosing group; dimethyl sulfoxide (0.106mg) was added to 3 re-holes, which was the negative control group; The blank group was 200 μL of DMEM medium without drug. After culturing for 24h, discard the supernatant. Add digitalis saponin (10μg) to the compound dosing group ...

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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 present invention relates to the field of biochemical medicine, in particular to a compound with cancer preventive effect extracted from Mao Kuzhen and a preparation method thereof. Background technique [0002] WITHANOLIDE type compound is a kind of ergostane type steroid compound with 28 carbon atoms. Its main structure is as 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. WITHANOLIDE type compounds are divided into classic type and non-classical type. Classic WITHANOLIDE-type compounds occupies an absolute majority in nature, and these compounds are mainly distributed in several genera of the Solanaceae (Solanaceae) such as physalis. The biological activities of WITHANOLIDE compounds are mainly manifested in anti-tumor, anti-inflammatory, antibacterial, and insect antifeedant for plants. Due to the complex structure of such compounds and many chiral centers, these comp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J17/00A61P35/00
Inventor 马忠俊丁辉胡志娟
Owner ZHEJIANG UNIV
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