CN102119953A - Application of euphorbia humifusa wild extract - Google Patents
Application of euphorbia humifusa wild extract Download PDFInfo
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- CN102119953A CN102119953A CN 201010546101 CN201010546101A CN102119953A CN 102119953 A CN102119953 A CN 102119953A CN 201010546101 CN201010546101 CN 201010546101 CN 201010546101 A CN201010546101 A CN 201010546101A CN 102119953 A CN102119953 A CN 102119953A
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Abstract
The invention relates to the application of a euphorbia humifusa wild extract and discloses a fatty acid synthase inhibitor and a preparation method and application thereof, which aims to provide the fatty acid synthase inhibitor and the preparation method thereof and the application of the inhibitor in prevention of related fatty acid synthase targeted diseases and adjuvant therapy. The fatty acid synthase inhibitor is obtained by leaching euphorbia humifusa wild serving as a raw material by using an acetone-water or ethanol-water mixed solvent. The fatty acid synthase inhibitor which is provided by the invention and prepared by taking the euphorbia humifusa wild as the raw material has higher fatty acid synthase inhibition activity and can play a great role in the aspects of the prevention of the related fatty acid synthase targeted diseases and the adjuvant therapy, particularly the preparation of a medicament for preventing and treating cancers and the like.
Description
Technical field
The present invention relates to a kind of fatty acid synthetase inhibitor and application thereof.
Background technology
The former title fatty acid synthetase of fatty acid synthase, (EC 2.3.1.85, fatty acid synthase is abbreviated as FAS), the intravital fatty acid synthase of animal is called I type FAS, and the fatty acid synthase in prokaryote and the plant is called II type FAS.Basic research both at home and abroad shows that fatty acid synthase is the potential target position that can be used for the treatment of purpose.
The Loftus of U.S. John Hopkins University etc. prove the result of study of mice fatty acid synthetase, suppress the accumulation that fatty acid synthetase can cause malonyl coenzyme A, and the latter suppresses the expression with the relevant hypothalamic neuropeptide Y that takes food, appetite is descended, and body weight reduces.T.Loftus etc. point out that fatty acid synthetase can be used as the potential treatment target position of controlling body weight (Loftus.T.M.et al., 2000.Science, 288 (5475): 2379-2381).Above result shows, suppresses the activity of fatty acid synthetase, can suppress the synthetic of body fat, and can also suppress the appetite of animal, and the fat mass that restriction is taken in also consumes body fat.Therefore, the inhibitor of development and exploitation fatty acid synthetase has the potentiality of great Weight-reducing and lipid-lowering fat.
So far, the fatty acid synthase inhibitor of having reported is less, has only synthetic C75 (Kuhajda F.P., PizerE.S., Li J.N., et al.Proc.Natl.Acad.Sci.USA., 97,3450-3454 (2000)), natural product cerulenin (cerulenin) (Vance D., the Goldberg I. that early finds, Mitsuhashi O.et al.Biochem BiophysRes Commun.48,649-656 (1972)) and the ester catechin EGCG in the green tea (Wang X., Tian W.X.Biochem.Biophys.Res.Commun, 288 (5): 1200-1206 (2001)) and ECG (Wang X., SongK.S., Guo Q.X., et al.Biochem Pharmacol, 66:2039-2047 (2003)).The common drawback that these inhibitor had is to suppress active not high enough, and using value is limited to, and therefore searches out the active high fatty acid synthase inhibitor of inhibition and has important application value.The invention describes the inhibitory action of Herba Euphorbiae Humifusae extract to FAS.
Herba Euphorbiae Humifusae (Euphorbia humifusa Wild.), different title Radix seu Caulis Parthenocissi tricuspidatae, milk flowers and plants, Herba Euphorbiae Humifusae, floor file are red, Herba pteridis vittatae, red filament grass, Coriaria sinica, red sand-grass, summer hat grass, purslane speedwell Herba, Herba Lysimachiae Lobelioidis, lobe grass etc., dry herb for euphorbia plant Radix seu Caulis Parthenocissi tricuspidatae Euphorbia hum ifusa Willd or Herba Euphorbiae supinae Euphorbia maculata, annual herb, contain white milk, be born in field, roadside, all there is distribution China various places.
Summary of the invention
The purpose of this invention is to provide a kind of fatty acid synthetase inhibitor and preparation method thereof.
Fatty acid synthase inhibitor provided by the present invention is to be raw material with the Herba Euphorbiae Humifusae, obtains with acetone-water, alcohol-water leaching; Or obtain through the reflow treatment extraction with acetone-sour water or ethanol-sour water mixed solvent.
The percentage by volume of acetone can be 50-70% in the wherein said acetone-water mixed solvent; Alcoholic acid percentage by volume can be 50-70% in the described ethanol-water mixed solvent; The ratio of weight and number of described mixed solvent and Herba Euphorbiae Humifusae can be 8-30: 1; Described sour water is a mineral acid, and the concentration of described acid is 1mol/L.
The method of described leaching can be at 25-70 ℃ and stirs down, or 80-100 ℃ of following reflux; It is described that the time of stirring leaching can be 3-24 hour down at 25-70 ℃; The time of described 80-100 ℃ following reflux can be 2-12 hour.
In order to improve the purity of described extract, also filter and concentrate after the described leaching; Described spissated method is the acetone or alcohol of removing in the filtrate, extracts from aqueous phase with ethyl acetate then, collects acetic acid ethyl acetate extract, removes the ethyl acetate in the described acetic acid ethyl acetate extract again, obtains Herba Euphorbiae Humifusae extract.
Another object of the present invention provides the purposes of described fatty acid synthetase inhibitor.
The application that the purposes of the fatty acid synthetase inhibitor that provides of the present invention is a fatty acid synthetase inhibitor in the preparation appetrol, and prevent and/or treat application in the cancer drug in preparation.
The fatty acid synthetase inhibitor that provides of the present invention can also be used widely as food additive, household chemicals additive and products and health products additive agent etc.
With fatty acid synthetase inhibitor provided by the present invention is that the medicine that active component prepares slimming medicine and prevents and/or treats cancer also belongs to protection scope of the present invention.
When needing, in said medicine, can also add one or more pharmaceutically acceptable carriers.Described carrier comprises diluent, excipient, filler, binding agent, wetting agent, disintegrating agent, absorption enhancer, surfactant, absorption carrier, lubricant of pharmaceutical field routine etc., can also add flavouring agent, sweeting agent and coloring agent etc. in case of necessity.
Slimming medicine with the Herba Euphorbiae Humifusae extract preparation can be made various ways such as injection, tablet, powder, granule, capsule, oral liquid, unguentum, cream.The medicine of above-mentioned various dosage forms all can be according to the conventional method preparation of pharmaceutical field.
Fatty acid synthase inhibitor of the present invention will be aspect the prevention and auxiliary treatment of relevant disease of target spot with the fatty acid synthase, preparing controlling body weight, preventing and treating the medicine of the aspects such as disease relevant, particularly in the medicine of aspects such as the anti-curing cancers of preparation, play a great role with obesity.Simultaneously, fatty acid synthase inhibitor of the present invention also has bigger using value in health product and the production of cosmetic virtue.
Description of drawings
Fig. 1 is the selection figure of Herba Euphorbiae Humifusae optimum solvent; Figure 1A is Herba Euphorbiae Humifusae relatively (ethanol system), Figure 1B are the suppression ratio of different proportion acetone extraction Herba Euphorbiae Humifusae to FAS to the suppression ratio of fatty acid synthase among Fig. 1;
Fig. 2 is Herba Euphorbiae Humifusae extract IC
50The mensuration curve chart; Fig. 2 A is 70% acetone extraction Herba Euphorbiae Humifusae IC
50Mensuration;
Fig. 2 B is Herba Euphorbiae Humifusae ethanolic extract IC
50Mensuration.
The specific embodiment
Among the following embodiment, used fatty acid synthase is with conventional method (W.X.Tian et al., 1985.J.Biol.Chem., 260 (20): 11375-11387; Tian Weixi etc., body lipid level of 1996. different growing stages laying hens and the active relation of liver fatty acid synthetase. journal of biological chemistry, 12 (2): 234-236) in fresh duck liver, separate to purify, and detect through polyacrylamide gel electrophoresis and to be single band.
Active S-acetyl-coenzyme-A, malonyl CoA, the NADPH of adopting of fatty acid synthase is standard measuring method for activity mensuration (W.X.Tian et al., 1985.J.Biol.Chem., 260 (20): 11375-11387 of substrate; Tian Weixi etc., body lipid level of 1996. different growing stages laying hens and the active relation of liver fatty acid synthetase. journal of biological chemistry, 12 (2): 234-236).
The preparation of embodiment 1, fatty acid synthase inhibitor Herba Euphorbiae Humifusae active substance
Herba Euphorbiae Humifusae is pulverized, extract working substance with following method.
Mixed in 8: 1 by ratio of weight and the number of copies with the Herba Euphorbiae Humifusae of above-mentioned pulverizing with ethanol-water mixed solvent (alcoholic acid percentage by volume is 50%), room temperature stirs leaching 12 hours down for 25 ℃, uses common filter paper filtering; Re-leaching is 12 hours under similarity condition, uses common filter paper filtering then, and twice filtrate is merged.At 0.09MPa, 40 ℃ of (decompression) low-temperature evaporations are removed ethanol, obtain containing the water of active substance, slough wherein lipid material, reuse equal-volume ethyl acetate extraction 3 times, combined ethyl acetate layer with isopyknic petroleum ether, the low-temperature evaporation that as above reduces pressure is removed organic solvent, obtain extractum, this extractum (vacuum) dry (50 ℃) is obtained solid-state Herba Euphorbiae Humifusae extract, should be called Herba Euphorbiae Humifusae extract A by solid-state Herba Euphorbiae Humifusae extract.
The preparation of embodiment 2, fatty acid synthase inhibitor Herba Euphorbiae Humifusae active substance
Herba Euphorbiae Humifusae is pulverized, extract working substance with following method.
With the acetone-water mixed solvent (percentage by volume of acetone is 70%) and the Herba Euphorbiae Humifusae of above-mentioned pulverizing is to mix at 15: 1 by ratio of weight and the number of copies, and 80 ℃ of reflux 3 hours are carried out the filtration of common filter paper; Reheat refluxed 2 hours under similarity condition, carried out the filtration of common filter paper, and twice filtrate is merged.At 0.09MPa, 35 ℃ of (decompression) low-temperature evaporations concentrate, and remove organic solvent wherein, obtain the active substance water, working substance to aqueous phase further concentrates, concrete grammar is: divide with isopyknic petroleum ether earlier to extract for 3-4 time, remove lipid material wherein, the reuse ethyl acetate extracts, with acetic acid ethyl acetate extract at 0.09MPa, 40 ℃ of (decompression) low-temperature evaporations concentrate, and remove organic solvent and obtain through spissated working substance extractum, i.e. Herba Euphorbiae Humifusae extract.This extractum is further obtained solid-state Herba Euphorbiae Humifusae extract 40-50 ℃ of (vacuum) drying, should be called Herba Euphorbiae Humifusae extract B by solid-state Herba Euphorbiae Humifusae extract.
The preparation of embodiment 3, fatty acid synthase inhibitor Herba Euphorbiae Humifusae active substance
Herba Euphorbiae Humifusae is pulverized, extract working substance with following method.
With the ethanol-water mixed solvent (ethanol is 70: 30 with the volume parts ratio of water) and the Herba Euphorbiae Humifusae of above-mentioned pulverizing is to mix at 20: 1 by ratio of weight and the number of copies, 100 ℃ of reflux 3 hours, carry out the filtration of common filter paper then, reheat refluxed 2 hours under similarity condition, carry out the filtration of common filter paper then, twice filtrate is merged.At 0.09MPa, 40 ℃ of (decompression) low-temperature evaporations concentrate, and remove organic solvent wherein, obtain containing the water of active substance, i.e. Herba Euphorbiae Humifusae extract.Working substance to aqueous phase further concentrates, concrete grammar is: extract with ethyl acetate, with acetic acid ethyl acetate extract at 0.09MPa, 40 ℃ of (decompression) low-temperature evaporations concentrate, removing organic solvent obtains through spissated working substance extractum, this extractum is obtained solid-state Herba Euphorbiae Humifusae extract 40 ℃ of further (vacuum) dryings, should be called Herba Euphorbiae Humifusae extract C by solid-state Herba Euphorbiae Humifusae extract.
The preparation of embodiment 4, fatty acid synthase inhibitor Herba Euphorbiae Humifusae active substance
Herba Euphorbiae Humifusae is pulverized, extract working substance with following method.
With the acetone-sour water mixed solvent (percentage by volume of acetone is 70%, and the concentration of acid is 1mol/L) and the Herba Euphorbiae Humifusae of above-mentioned pulverizing is to mix at 15: 1 by ratio of weight and the number of copies, and 100 ℃ of reflux 3 hours are carried out the filtration of common filter paper; Reheat refluxed 2 hours under similarity condition, carried out the filtration of common filter paper, and twice filtrate is merged.At 0.09MPa, 35 ℃ of (decompression) low-temperature evaporations concentrate, and remove organic solvent wherein, obtain the active substance water, working substance to aqueous phase further concentrates, concrete grammar is: divide with isopyknic petroleum ether earlier to extract for 3-4 time, remove lipid material wherein, the reuse ethyl acetate extracts, with acetic acid ethyl acetate extract at 0.09MPa, 40 ℃ of (decompression) low-temperature evaporations concentrate, and remove organic solvent and obtain through spissated working substance extractum, i.e. Herba Euphorbiae Humifusae extract.This extractum is further obtained solid-state Herba Euphorbiae Humifusae extract 40-50 ℃ of (vacuum) drying, should be called Herba Euphorbiae Humifusae extract D by solid-state Herba Euphorbiae Humifusae extract.
The preparation of embodiment 5, fatty acid synthase inhibitor Herba Euphorbiae Humifusae active substance
Herba Euphorbiae Humifusae is pulverized, extract working substance with following method.
(ethanol is 70: 30 with the volume parts ratio of water with ethanol-sour water mixed solvent, the concentration of acid is 1mol/L) be to mix at 20: 1 by ratio of weight and the number of copies with the Herba Euphorbiae Humifusae of above-mentioned pulverizing, 100 ℃ of reflux 3 hours, carry out the filtration of common filter paper then, reheat refluxed 2 hours under similarity condition, carry out the filtration of common filter paper then, twice filtrate is merged.At 0.09MPa, 40 ℃ of (decompression) low-temperature evaporations concentrate, and remove organic solvent wherein, obtain containing the water of active substance, i.e. Herba Euphorbiae Humifusae extract.Working substance to aqueous phase further concentrates, concrete grammar is: extract with ethyl acetate, with acetic acid ethyl acetate extract at 0.09MPa, 40 ℃ of (decompression) low-temperature evaporations concentrate, removing organic solvent obtains through spissated working substance extractum, this extractum is obtained solid-state Herba Euphorbiae Humifusae extract 40 ℃ of further (vacuum) dryings, should be called Herba Euphorbiae Humifusae extract E by solid-state Herba Euphorbiae Humifusae extract.
Embodiment 6, to the detection of fatty acid synthase restraining activity:
Under 37 ℃, in 2 milliliters of quartz colorimetric utensils, add this zymolyte: 0.2mM S-acetyl-coenzyme-A solution 25 microlitres, 0.4mM, malonyl CoA solution 50 microlitres and 1.3mM NADPH solution 50 microlitres, add 0.1M again, pH 7.0 phosphate buffer 1 .85 milliliters and FAS solution 30 microlitre mixings start enzymatic reaction.With the variation of spectrophotometer light absorption value A of 340nm wavelength place in the monitoring unit interval, represent the vigor of FAS with (Δ A/min).The Herba Euphorbiae Humifusae pulverizing medicinal materials is crossed 40 mesh sieves, adds solvent (1: 20), and stirring at room is after 4 hours, the centrifugalize supernatant, dilute ten times after the mensuration extracting solution to the suppression ratio of FAS.In the presence of the finite concentration Herba Euphorbiae Humifusae extract, the vigor of FAS holoenzyme reaction descends the concentration IC of required mapler leaf extract when its vigor drop by half
50Value, with the inhibition ability of this numeric representation Herba Euphorbiae Humifusae extract to FAS, above-mentioned survey live body be in the final concentration of FAS be 7 mcg/ml.
Measurement result shows: under condition was lived in above-mentioned survey, Herba Euphorbiae Humifusae 70% acetone soln extracting solution was the highest to the suppression ratio of FAS, reaches 59.01%, surveyed live body and was the Central Plains concentration and be 37.5 (μ g/ml) and (see Figure 1A-B).The IC of Herba Euphorbiae Humifusae extract
50Be respectively 11-23 mcg/ml (seeing Fig. 2 A-B).
Embodiment 7, tumor cell experiment
Cell culture: hepatocarcinoma BEL-7402, breast carcinoma MCF-7, carcinoma of prostate PC-3M, cervical cancer Hela, five kinds of JEG-3 of esophageal carcinoma CAES-17 (all available from medical courses in general institute institute of materia medica) are incubated in the RPMI-1640 culture fluid that contains 10% calf serum, penicillin (100 μ g/ml) and streptomycin (100 μ g/ml), in suitable humidity, contain 5%CO
2Incubator in the cultivation of going down to posterity of 37 ℃ of monolayer adherences.
Collect five kinds of tumor cells of exponential phase, be inoculated in 96 orifice plates 2 * 10 respectively
4Individual/hole, adhere-wall culture changed the culture fluid that contains the Herba Euphorbiae Humifusae extract that obtains according to embodiment 1, embodiment 2 and embodiment 3 methods respectively in 24 hours into, be divided into 7 groups by different Herba Euphorbiae Humifusae extract concentrations and (establish 0,5,10,20,40,60,80 μ g/ml totally 7 experimental grouies, each concentration is established 3 multiple holes, and experimental result is averaged).
Continue to cultivate 24 hours, change the culture fluid that does not contain extract into, (tetramethyl azo azoles indigo plant 5mg/ml) continues to cultivate 4 hours to add 20 μ l MTT simultaneously.Abandon supernatant, every hole adds 200 μ l dimethyl sulfoxide (DMSO) (matched group adds equivalent culture fluid and dimethyl sulfoxide), and level concussion 10 minutes is fully dissolved crystal.Measure light absorption value (A) with microplate reader, wavelength 570nm, and calculate the inhibitory action of extract to growth of cancer cells by following formula, the result shown in table 1, table 2, table 3, table 4, table 5,
Inhibitory rate of cell growth (%)=(1-experimental group A
570/ control group A
570) * 100%
Table 1 variable concentrations Herba Euphorbiae Humifusae maple extract (acting on 24 hours) is to the suppression ratio (%) of growth of tumour cell
Annotate: above-mentioned press down cancer test used Herba Euphorbiae Humifusae extract the ethyl acetate step concentrate.
Claims (9)
1. the application of Herba Euphorbiae Humifusae extract in the preparation fatty acid synthetase inhibitor, described fatty acid synthetase inhibitor is to be raw material with the Herba Euphorbiae Humifusae, obtains with acetone-water, alcohol-water leaching; Or obtain through the reflow treatment extraction with acetone-sour water or ethanol-sour water mixed solvent;
The percentage by volume of acetone can be 50-70% in the wherein said acetone-water mixed solvent; Alcoholic acid percentage by volume can be 50-70% in the described ethanol-water mixed solvent; The ratio of weight and number of described mixed solvent and Herba Euphorbiae Humifusae can be 8-30: 1; Described sour water is a mineral acid, and the concentration of described acid is 1mol/L.
2. application according to claim 1 is characterized in that: the method for described leaching can be at 25-70 ℃ and stirs down, or 80-100 ℃ of following reflux; It is described that the time of stirring leaching can be 3-24 hour down at 25-70 ℃; The time of described 80-100 ℃ following reflux can be 2-12 hour.
3. application according to claim 2, it is characterized in that: described spissated method is the acetone or alcohol of removing in the filtrate, extracts from aqueous phase with ethyl acetate then, collects acetic acid ethyl acetate extract, remove the ethyl acetate in the described acetic acid ethyl acetate extract again, obtain Herba Euphorbiae Humifusae extract.
4. the application of the described fatty acid synthetase inhibitor of claim 1 in the preparation appetrol.
5. the described fatty acid synthetase inhibitor of claim 1 is as the application in the food additive.
6. the described fatty acid synthetase inhibitor of claim 1 is as the application in the products and health products additive agent.
7. the application of the described fatty acid synthetase inhibitor of claim 1 in the household chemicals additive.
8. medicine that prevents and/or treats cancer, its active component is the described fatty acid synthetase inhibitor of claim 1.
9. appetrol, its active component is the described fatty acid synthetase inhibitor of claim 1.
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| CN109276495A (en) * | 2018-10-16 | 2019-01-29 | 拉芳家化股份有限公司 | The preparation of Euphorbia maculata extract and its application in lotion |
| JP2021500023A (en) * | 2017-10-19 | 2021-01-07 | イェール ユニバーシティーＹａｌｅ Ｕｎｉｖｅｒｓｉｔｙ | Inhibition of androgen receptors by herbal extracts and the composition of the extracts |
| WO2021233681A1 (en) * | 2020-05-18 | 2021-11-25 | Cellbitec, S.L. | Drug delivery system based on calcium phosphate nanoparticles functionalized with bioactive compounds from euphorbia extract and the uses thereof |
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| CN101768081A (en) * | 2009-01-06 | 2010-07-07 | 首都医科大学 | Inhibitor of fatty acid synthase and application thereof |
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| CN101525357A (en) * | 2008-03-07 | 2009-09-09 | 首都医科大学 | Method for separating and preparing penta-galloyl glucose from Chinese medicament |
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| JP2021500023A (en) * | 2017-10-19 | 2021-01-07 | イェール ユニバーシティーＹａｌｅ Ｕｎｉｖｅｒｓｉｔｙ | Inhibition of androgen receptors by herbal extracts and the composition of the extracts |
| JP7303558B2 (en) | 2017-10-19 | 2023-07-05 | イェール ユニバーシティー | Inhibition of androgen receptors by herbal extracts and compositions of said extracts |
| CN109276495A (en) * | 2018-10-16 | 2019-01-29 | 拉芳家化股份有限公司 | The preparation of Euphorbia maculata extract and its application in lotion |
| WO2021233681A1 (en) * | 2020-05-18 | 2021-11-25 | Cellbitec, S.L. | Drug delivery system based on calcium phosphate nanoparticles functionalized with bioactive compounds from euphorbia extract and the uses thereof |
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