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Compound having quinone reductase induced activity and preparation method thereof

A technology for inducing activity and reductase, applied in the fields of steroids, organic chemistry, drug combination, etc., which can solve the problems of no artificial citation cultivation and 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 having quinone reductase induced activity and preparation method thereof
  • Compound having quinone reductase induced activity and preparation method thereof
  • Compound having quinone reductase induced activity and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] 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;

[0057] 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;

[0058] 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

[0067] 1) Put 1Kg of the persistent calyx in the extracting tank, add 3 times the weight of the persistent calyx in each time an ethanol aqueous solution containing 95% ethanol by volume (that is, 3Kg of the ethanol aqueous solution), and reflux extraction 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;

[0068] 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;

[0069] 3) 16g of 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 200 mesh column chromatography silica gel , the weight ratio of extract to column c...

Embodiment 3

[0072] Embodiment 3 (quinone reductase induction experiment)

[0073] 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 prepared in Example 1, and finally add compound C with cancer prevention effect prepared in Example 1 to the other 3 multiple wells, corresponding to the compound dosing group A. Compound dosing group B and compound dosing group C; add 4′-bromoflavone (0.106 mg) to 3 duplicate wells, which is the positive control dosing group; add dimethyl sulfoxide to 3 duplicate wells (0.106mg), which is the negative control group; the blank group is 200μL DMEM medium without adding drugs. After culturing for 24 h, the sup...

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Abstract

The invention discloses a compound having quinone reductase induced activity, which has a structure shown in Formula I. The compound has quinone reductase induced activity and can be used for preventing cancer. The invention also discloses a preparation method of the compound having quinone reductase induced activity, which is simple, reliable, easy to implement, high in operability and favorable in controllability. Formula I is shown in the specification.

Description

technical field [0001] The invention relates to the field of biochemistry and medicine, in particular to a compound with quinone reductase inducing activity extracted from Sophora chinensis 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,...

Claims

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Application Information

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