CN105963310A - Radish thioglycoside composition and application thereof - Google Patents

Radish thioglycoside composition and application thereof Download PDF

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CN105963310A
CN105963310A CN201610501285.6A CN201610501285A CN105963310A CN 105963310 A CN105963310 A CN 105963310A CN 201610501285 A CN201610501285 A CN 201610501285A CN 105963310 A CN105963310 A CN 105963310A
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glucorphanin
compositions
food
oligomeric
product
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CN105963310B (en
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李晓龙
朱志鹏
罗永平
李欣
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SHENZHEN FUSHAN BIOTECHNOLOGY CO Ltd
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SHENZHEN FUSHAN BIOTECHNOLOGY CO Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105Plant extracts, their artificial duplicates or their derivatives
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/125Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives containing carbohydrate syrups; containing sugars; containing sugar alcohols; containing starch hydrolysates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/702Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23VINDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00Food compositions, function of food ingredients or processes for food or foodstuffs

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Abstract

The invention provides a composition with radish thioglycoside and functional oligosaccharide and application of the composition to preparing chemical cancer prevention and/or treatment products.

Description

Glucorphanin compositions and application thereof
Technical field
The invention provides a kind of compositions comprising glucorphanin and functional oligose.The invention still further relates to described group Compound purposes in the product that preparation is used for cancer chemoprevention and treatment.
Background technology
According to World Health Organization (WHO) 2014 annual report, cancer is whole world morbidity and main causes of death, to people's people's livelihood Life health causes grave danger, brings heavy financial burden to social development.In the lengthy procedure to anticancer, people Proposed the concept of cancer chemoprevention in 1976, refer to utilize natural or synthesis chemical substance to prevent, slow down Or reverse the strategy that cancer occurs to develop.Sulforaphen (Sulforaphane, SFN), also known as Sulforaphane, chemical entitled 1-is different Hydrogen thiocyanate-4-mesyl butane, belongs to isosulfocyanate, is the strongest anticancer component found in vegetable up to now. Molecular mechanisms of action for sulforaphen studies and cell experiment result shows further, and sulforaphen is lived by regulation and control II phase enzyme Property carries out the number of ways such as metabolism detoxification to I phase enzymes metabolism thing or exotic and plays work same or analogous with cancer chemoprevention With (list of references Myzak MC, Dashwood RH. Cancer Lett., 2006,233:208-18.).
Sulforaphen is as a kind of isosulfocyanate, unstable chemcial property, degradable.Store for convenience, transport and Using, usual sulforaphen carries out product development and utilization with its precursor forms glucorphanin.In multiple crucifer Containing glucorphanin, wherein Brassica genus brassica specie mutation Caulis et Folium Brassicae capitatae (Brassica oleracea L.var.italic Planch.) in sprout glucorphanin content far above other plant and autologous adult tissue (list of references Fahey JW, Zhang Y, Talalay P. Proc Natl Acad Sci U S A., 1997,94:10367-72.), frequently as plant Extract source.In plant, the glucorphanin as precursor forms is present in vacuole, with the β being positioned in specific protein body- Sulfur glycosides enzyme is separated by biofilm system.Plant tissue cell extract or add man-hour destroyed after, glucorphanin contacts with enzyme will Start sulfur glycosides fast hydrolyzing, obtain comprising multiple biological decomposition product (the list of references Latt é of sulforaphen, Radix Raphani sulfur nitrile KP, Appel KE, Lampen A. Food Chem Toxicol., 2011,49:3287-309.).Therefore, in order to prevent Enzymatic degradation loses, and generally in processing technique, the β in plant-sulfur glycosides enzyme is carried out inactivation treatment to reduce Radix Raphani sulfur in prior art The loss of glycosides.
Although the β in plant-sulfur glycosides enzyme being carried out inactivation be conducive to the preservation of glucorphanin in product, but glucorphanin existing Need to be converted into sulforaphen competence exertion in organism and go out cancer-resisting activity.According to the literature, glucorphanin mainly passes through root β-sulfur glycosides enzyme myrosin contained by the beneficial bacteria of intestinal tract such as bulgaricus bacillus, bacillus bifidus group in human body intestinal canal (myrosinase) it is converted into sulforaphen, and then is absorbed by the body and then plays a series of effect.The present inventor is under study for action Having been surprisingly found that, due to individual difference, the conversion in the body efficiency of glucorphanin is unsatisfactory and differs greatly, generally can be About 10%-50% changes, and major part glucorphanin fails to be converted into sulforaphen and absorbed.Therefore, if can improve in intestinal The efficiency that glucorphanin converts to sulforaphen, potentially contributes to preferably play its anticancer and protective effect on cancer risk.
In order to prevent from glucorphanin extraction process in vitro is degraded loss, prior art before Extraction and enrichment often Need to take enzyme denaturing to process;On the other hand, for the glucorphanin product of Extraction and enrichment, require consideration for how again to ensure that it is at body The most effectively play biological activity.China's application 200810210355.8 proposition takes to add exogenous β-sulfur glycosides enzyme and enzyme is lived The means of agent (such as ascorbic acid), directly increase the total amount of β-sulfur glycosides enzyme in intestinal and are aided with activation β-sulfur glycosides enzyme, promoting to produce In product, glucorphanin Efficient Conversion in vivo is sulforaphen.But, enzyme is congenital just has unstability as a kind of for β-sulfur glycosides enzyme, Easily lose activity under room temperature condition.Therefore the condition extracting and storing accordingly traffic requirements of enzyme is the harshest, causes producing containing enzyme Product are relatively costly and accumulating is inconvenient, it is difficult to extensively apply.
Therefore, prior art in the urgent need to provide a kind of can guarantee that the product effectively converting in glucorphanin body and utilizing and Method.
Summary of the invention
The present inventor finds in studying for a long period of time: glucorphanin in intestinal to the transformation efficiency of sulforaphen unsatisfactory and And differ greatly, this can affect effective performance of glucorphanin vivo biodistribution operation, this be before people unwitnessed ask Topic.In order to solve this problem, the present inventor has attempted multiple way, but effect is the most not ideal enough.In an experiment, invention image So find that the glucorphanin being mixed into functional oligose is significantly improved to the conversion of sulforaphen in intestinal.Through repeatedly entering One step experiment and checking, the problems referred to above have had gratifying solution.
To this end, in the first aspect of the invention, it is provided that a kind of compositions, it comprises:
(1) glucorphanin;With
(2) functional oligose.
Inventors have surprisingly discovered that: with the addition of the glucorphanin product after functional oligose after taking in Intestinal can change into sulforaphen expeditiously.
It is low that functional oligose is that those can not be digested and assimilated, can completely enter the Non-digestible of large intestine by human gastrointestinal tract Polysaccharide.The non-limiting example of functional oligose includes but not limited to oligofructose, soybean oligo saccharide, oligomeric galactose, low Xylan, oligomeric isomaltose, oligomeric lactulose, cyclodextrin, oligochitosan, inulin and combinations thereof.
Without being bound by theory, applicant guesses, it is possible to functional oligose is because can not being decomposed by human body and utilizing still By beneficial bacteria of intestinal tract selective use, thus its possibility affecting beneficial bacteria of intestinal tract quantity and vigor may be not excluded for, probiotic bacteria Quantity and the change of vigor and then glucorphanin is converted in indirectly improving human body intestinal canal the ability of sulforaphen.Nonetheless, Above-mentioned imagination is still the supposition afterwards according to experimental result of the present invention.It is true that due to the complexity of internal milieu, merit to be analyzed Can property oligosaccharide be extremely difficult on the impact of beneficial bacteria of intestinal tract.
In the present compositions, described functional oligose is preferably selected from oligofructose, oligomeric xylose, oligomeric gala Sugar, oligomeric lactulose and oligomeric isomaltose.In a more preferred embodiment, described functional oligose be oligomeric xylose or Oligofructose;In a more preferred embodiment, described functional oligose is oligomeric xylose.
In the present compositions, glucorphanin can in the form of a single compound with described functional oligose group Become compositions;Glucorphanin can also be with the form of plant powder or plant extract and the composition combination of described functional oligose Thing.Described plant powder or plant extract are the powder from the plant containing glucorphanin or its extract.Preferably, institute Stating plant is crucifer, particularly Vegetables in Brassica.The example of these plants includes Caulis et Folium Brassicae capitatae, common head cabbage, the garment or robe made of feathers Caulis et Folium Brassicae capitatae, Chinese cabbage, Brassica oleracea L. var. botrytis L., Caulis et Folium Brassicae junceae, kohlrabi, brussels sprout, Radix Brassicae rapae, Radix Cochleariae officinalis etc..It is highly preferred that glucorphanin can to the west of Presented in Cymbidium ensifolium (L.) Sw. sprout extract or Caulis et Folium Brassicae capitatae sprout (powder) in the compositions of the present invention.
The compositions of the present invention can also additionally contain myrosin activator.Described myrosin activator is this area Known, include but not limited to vitamin C (ascorbic acid), zinc ion.Preferably myrosin activator is vitamin C.
In another aspect of the present invention, it is provided that a kind of pharmaceutical composition or food compositions, described compositions except Outside glucorphanin and functional oligose, it is also possible to additionally contain acceptable on pharmaceutically acceptable excipient or carrier or food adding Add agent.
The compositions of the present invention may reside in applicable product form, includes but not limited to medicine, food, functional Food and health food etc..Especially, for food, product form can be selected from following food: food supplement, Health food, beverage, shake drink, baked product, tea, soup, frumentum, salad, sandwich, salad dressing, soy sauce, coffee, Cheese, Yoghurt, energy food, and mixture.
Having it is still another aspect of the present invention to provide a kind of method increasing and converting to sulforaphen in glucorphanin body, bag Include external interpolation functional oligose in glucorphanin product.
Preparing for treatment or the product of prophylaxis of cancer in the compositions that it is still another aspect of the present invention to provide the present invention Purposes in product.Described cancer selected from selected from the brain cancer, breast carcinoma, colon and rectum carcinoma, skin carcinoma, head and neck cancer, cervical cancer, renal carcinoma, Pulmonary carcinoma, hepatocarcinoma, ovarian cancer, cancer of pancreas, carcinoma of prostate, thyroid carcinoma, gastric cancer, leukemia, lymphoma, sarcoma and melanoma.Institute Stating product can be to be the form of medicine or food, and described food includes the form such as health food, functional food.Specifically, Described food can be to be the food selected from form in detail below: food supplement, health food, beverage, shake drink, bakes product Product, tea, soup, frumentum, salad, sandwich, salad dressing, soy sauce, coffee, cheese, Yoghurt, energy food, and mixing Thing.Described medicine or food can be to be following form: soft capsule, hard capsule, drop pill, tablet, granule, pill, injection, mouth Take liquid, powder, medicated wine, hard sugar, soft sweet, medicinal tea.
In the present compositions, described functional oligose relative to the usage ratio of glucorphanin (based on weight Than) can be 1:100 to 100:1, preferably 1:50 to 50:1,1:30 to 30:1, more preferably 1:10 to 10:1,1:5 to 5: 1, particularly preferred 1:3 to 3:1.
In the compositions of present aspect, it can be 0.1% to 90%, 0.5% that glucorphanin accounts for the percentage ratio of composition total weight To 70%, 1% to 50%, preferably 2% to 30%, more preferably 3% to 20%.
The general consumption of the present composition can determine with purpose according to actual needs.For example, it is possible to be agent every day Amount ensures to take in glucorphanin or the Radix Raphani of the glucorphanin of 0.2mg to 200mg, preferably 0.5mg to 100mg of 0.1 mg to 500mg Sulfur glycosides or the glucorphanin of the glucorphanin of 1mg to 50mg, more preferably 1mg to 30mg, the glucorphanin of 1mg to 20mg or 2mg are extremely The glucorphanin of 10mg.
In the present compositions, it is also possible to preferably contain myrosin activator, such as ascorbic acid or zinc from Son.The consumption of activator ascorbic acid or zinc ion can according to it is generally required to and practical situations determine, such as, this In bright compositions, the consumption of ascorbic acid can account for the 0.01% to 5% or 0.02% to 2% of composition total weight, preferably 0.05% to 1%, more preferably 0.05% to 0.5%.
Accompanying drawing explanation
Fig. 1 be show compositions A of the present invention, B, C compared with blank group in sulforaphen level in simulated intestinal fluid Time dependent situation.
Detailed description of the invention
Term " is treated " and is defined as in order to (resist the disease, disease or obstacle are such as referred to as the polytype of " cancer " One in disease) and process that patient is carried out and nursing, it includes that the compositions using the present invention is with prevention symptom or also Send out the outbreak of disease or mitigation symptoms or complication or cure or eliminate a disease, disease or obstacle.
Term " prevents " to refer to that it can be applied to disease by using medicine and stop, slowing down or the generation of reverse disease Any stage before sick generation.
" treatment " in the context of the present invention means to alleviate the symptom relevant to disease or disease, or suppresses these diseases The development further of shape or deterioration, or prevent or prevent described disease or disease.Similarly, of the present inventionization used herein " effective dose " or " therapeutically effective amount " of compound refers to alleviate the symptom relevant to described disease or situation wholly or in part or stop Stop or slow down the development further of these symptoms or deteriorate, or prevention or offer are to described disease or the chemical combination of the prevention of situation The amount of thing.
Term used herein " cancer " refer to any malignant entity tumor, metastatic tumor or wherein cell division uncontrolled System and other disease of cell loss differentiation.
The pharmaceutical composition of the present invention can be prepared by routine techniques, such as at Remington:The Science And Practice of Pharmacy, the 19th edition, the method described in 1995, it is incorporated herein by.Described group Compound can occur with conventionally form, such as capsule, tablet, aerosol, solution, suspensoid or Topical application forms.
Typical compositions comprises the compounds of this invention and excipient or carrier.Such as, reactive compound is generally and carrier Mixing, or loaded body dilution, or to be sealed in can be the carrier of ampoule, capsule, sachet, paper or other vessel form In.When being mixed with carrier by reactive compound, or when carrier serves as diluent, described carrier can be to serve as activation The solid of the carrier of compound, excipient or medium, semisolid or fluent material.Described reactive compound can adsorb in graininess (such as it is contained in sachet) on solid carrier.Suitably some examples of carrier are water, saline solution, alcohol, Polyethylene Glycol, gather Hydroxyl-oxethyl Oleum Ricini, Oleum Arachidis hypogaeae semen, olive oil, gelatin, lactose, hargil, sucrose, dextrin, magnesium carbonate, sugar, cyclodextrin, straight The lower alkyl ether of chain starch, magnesium stearate, Talcum, gelatin, agar, pectin, arabic gum, stearic acid or cellulose, silicic acid, Fatty acid, fatty acid amine, fatty mono glyceride and diglyceride, pentaerythritol fatty ester, polyoxyethylene, hydroxylmethyl cellulose Element and polyvinylpyrrolidone.Similarly, described carrier or diluent can include any sustained release material known in the art Material, such as individually glyceryl monostearate or distearin or its mixture with wax.
Described preparation can mix with the adjuvant of discord active component generation adverse reaction.These additives can include Wetting agent, emulsifying agent and suspending agent, affect the salt of osmotic pressure, buffer agent and/or coloring material, preservative, sweeting agent or seasoning Agent.If desired, it is also described compositions is carried out sterilizing.
Route of administration can be that reactive compound of the present invention is transported to suitable or desired site of action effectively Any approach, such as oral, per nasal, pulmonary, suck, subcutaneous, Intradermal, transdermal or parenteral route, such as rectum, reservoir, skin Under, in intravenous, urethra, intramuscular, intranasal, ophthalmic solution or the approach of ointment, oral route is preferred.
If using solid carrier for Orally administered, then said preparation can be tabletting, puts with powder or pellet form In hard gelatin capsule, or it can be with the form being lozenge or lozenge.If use liquid-carrier, the most described preparation can be Syrup, Emulsion, Perle or the form of sterile injectable liquid, such as aqueous or non-aqueous liquid suspension or solution Agent.
Injectable dosage form generally includes aqueous suspension or Oil suspensions, and it can use suitable dispersant or profit Prepared by humectant and suspending agent.Injectable form can be solution mutually in or the suspendible prepared with solvent or diluent The form of agent.Acceptable solvent or carrier include sterilized water, Ringer's solution or normal isotonic saline solution.Or, nothing can be applied Bacterium oil is as solvent or suspending agent.Preferably, described oil or fatty acid are fixednesies, including natural oil or artificial oil, fat Fat acid, monoglyceride, diglyceride or triglyceride.
For injection, described preparation can also is that the powder be suitable to above-mentioned appropriate solution reconstruct.These reality Example include but not limited to cryodesiccated, Rotary drying or be spray-dried powder, amorphous powder, granule, precipitate or Microgranule.For injection, described preparation can optionally comprise stabilizer, pH adjusting agent, surfactant, biological utilisation Degree regulator and the combination of these reagent.Described compound can be formulated as carrying out parenteral administration, example by injection As by injecting or continuous infusion.Unit dosage forms for injection can be in ampoule or in multi-dose container.
The compositions of the present invention is all effective at wide dosage range.Depend on that purposes used (is such as prevented or controls Treat), the compositions of the present invention can be adjusted in wide in range scope.As it was previously stated, the consumption of compositions can be according to Radix Raphani The daily intaking amount of sulfur glycosides determines, for example, it is possible to determine the consumption of compositions based on following daily ingestion of dosage: 0.1 mg is extremely The glucorphanin of 500mg or the glucorphanin of the glucorphanin of 0.1mg to 200mg, preferably 0.5mg to 100mg or 1mg's to 50mg The glucorphanin of glucorphanin, more preferably 1mg to 30mg, the glucorphanin of 1mg to 20mg or the glucorphanin of 2mg to 10mg.
Generally, can be distributed in unit dosage forms by the present composition, its per unit dosage comprises the Radix Raphani sulfur of effective dose Glycosides and pharmaceutically suitable carrier.
Generally, be suitable to be administered orally, per nasal, the dosage form of pulmonary or transdermal administration include the glucorphanin of effective dose and pharmaceutically acceptable load Body or diluent.
Dosage form can be once a day or once a day above the most such as every day twice or use three times a day.Or, dosage form The most every other day or once in a week can use as required to use less than frequency once a day.
Pharmaceutical composition can be with the form being tablet, capsule, powder, granule, lozenge, liquid or jelly.For oral Tablet and capsule may be adapted to the form of unit dose medication, and the excipient of routine can be contained, these examples have: combine Agent such as syrup, Radix Acaciae senegalis, gel, sorbitol, yellow work glue, polyvinylpyrrolidone (PVP);Filler such as lactose, saccharide, jade Rice flour, calcium phosphate, sorbitol or glycine;Tablet lubricants such as magnesium stearate, silicon dioxide, Talcum, Polyethylene Glycol or dioxy SiClx;Disintegrating agent such as potato starch;Acceptable lubricant such as sodium lauryl sulfate.Tablet can be according to known conventional manner Method in practice is coated.Oral liquid can make watery or oleaginous suspension, solution, Emulsion, syrup or tincture, May be made as a kind of dry, again modulate with water or other suitable carrier the most again.These liquid preparations can contain Having the additive of routine, such as suspending agent is (such as: sorbitol, syrup, methylcellulose, glucose syrup, gelatin, hydrogenated food With oils and fats).Emulsifying agent (such as incubates phospholipid, sorbitol list oleate or Radix Acaciae senegalis), and nonaqueous phase carrier (includes edible oil such as Fructus Pruni Core oil, the Oleum Cocois of rectification, oils and fats such as glycerol, propylene glycol or ethanol), preservative (such as methyl or propyl p-hydroxybenzoate or Sorbic acid), also can be containing conventional flavoring agent or coloring agent if needed.
In pharmaceutical composition of the present invention, the percentage ratio of active substance is variable, because medicaments dispensing must be made to make necessarily The dosage of proper ratio, to obtain preferable curative effect.In a word, pharmaceutical preparation oral administration or the drug administration by injection of the present invention should be by often 70kg body weight 1 to 15 milligram of active substance every day.Following illustrative rather than restrictive be given some implement embodiments.
Below in conjunction with specific embodiment, the present invention is described in further detail, raw materials used as without special theory in following embodiment Bright, it is the most commercially available, described percentage ratio, without specified otherwise, is i.e. weight percentage.
Embodiment 1:
Preparation rich in Caulis et Folium Brassicae capitatae sprout extractive composition (compositions A) of glucorphanin
(1) mixing: 1800 g Caulis et Folium Brassicae capitatae sprout extract (containing glucorphanin 16.0%) are mixed homogeneously with 200 g oligofructoses, Obtaining 2 kg Caulis et Folium Brassicae capitatae sprout extractive compositions, wherein glucorphanin accounts for 14.4%.
(2) pack product: by the above-mentioned Caulis et Folium Brassicae capitatae sprout extractive composition rich in glucorphanin by the weight of every bag of 2 g Subpackage enters in pouch-packaged, obtains powder product.
Embodiment 2:
Preparation rich in Caulis et Folium Brassicae capitatae sprout extractive composition (compositions B) of glucorphanin
(1) mixing: 2 kg Caulis et Folium Brassicae capitatae sprout extract (containing glucorphanin 16.0%) are mixed homogeneously with 1 kg oligomeric xylose, obtains 3 kg are rich in the Caulis et Folium Brassicae capitatae sprout extractive composition of glucorphanin, and wherein glucorphanin accounts for 10.7%.
(2) pack product: by the above-mentioned Caulis et Folium Brassicae capitatae sprout extractive composition rich in glucorphanin by the weight of every bag of 2 g Subpackage enters in pouch-packaged, obtains powder product, and wherein glucorphanin accounts for 10.7%.
Embodiment 3:
Rich in the Caulis et Folium Brassicae capitatae sprout powder of glucorphanin and the preparation of the compositions (compositions C) of Caulis et Folium Brassicae capitatae sprout extract
(1) mixing: by 200 g Caulis et Folium Brassicae capitatae sprout powder extracts (containing glucorphanin 16%), 800 g Caulis et Folium Brassicae capitatae sprout powder (containing Radix Raphani sulfur Glycosides 5%), 250 g oligochitosans, 250 g oligofructoses, 250 g oligomeric xyloses, 250 g oligomeric isomaltoses, 10 g ascorbic acid Mix homogeneously, obtains 2.01 kg rich in the Caulis et Folium Brassicae capitatae sprout powder of glucorphanin and Caulis et Folium Brassicae capitatae sprout extractive composition, wherein Radix Raphani Sulfur glycosides accounts for 3.58%.
(2) pack product: the above-mentioned Caulis et Folium Brassicae capitatae sprout powder rich in glucorphanin and Caulis et Folium Brassicae capitatae sprout extractive composition are pressed The weight subpackage of every bag of 2 g enters in pouch-packaged, obtains powder product, and wherein glucorphanin accounts for 3.58%.
Embodiment 4:
In gut simulation liquid, sulforaphen level of conversion measures
Reagent and test sample:
Gut simulation liquid: by 2015 editions " Chinese Pharmacopoeias " two annex method preparation simulated intestinal fluids, take 40 mL simulated intestinal fluids and add The Lactobacillus bulgaricus of logarithmic (log) phase, elongated bacillus bifidus, Bacillus licheniformis, streptococcus thermophilus and clostridium butyricum each 2 × 107 (each strain 37 DEG C of cultivation 48 h, list of references Cheng DL, Hashimoto in buffering GAM meat soup (pH 7.0) in advance K, Uda Y. Food Chem Toxicol., 2004,42:351-7.), 37 DEG C of insulations are standby.
Blank group: Caulis et Folium Brassicae capitatae sprout extract, wherein glucorphanin content is 16%.
Compositions A group: with Caulis et Folium Brassicae capitatae sprout extract (glucorphanin content is for 16%): oligofructose=9:1 mixes, Wherein glucorphanin content is 14.4%.
Compositions B group: with Caulis et Folium Brassicae capitatae sprout extract (glucorphanin content is for 16%): oligomeric xylose=2:1 mixes, Wherein glucorphanin content is 10.7%.
Compositions C group: with Caulis et Folium Brassicae capitatae sprout mixture (Caulis et Folium Brassicae capitatae sprout extract and Caulis et Folium Brassicae capitatae sprout powder press 1:4 mixing, Its glucorphanin content is 7.2%): oligosaccharide mixture: vitamin C=100:100:1 mixes, wherein glucorphanin content It is 3.58 %.
Oligosaccharide mixture: by oligofructose: oligomeric xylose: oligochitosan: oligomeric isomaltose=1:1:1:1 directly mixes Make.
Operation processes:
(1) blank group: take blank group 0.251 g(and contain glucorphanin 40.1 mg), join in 20 mL gut simulation liquid, in 37 DEG C of insulations, when 0.5 h, 1 h and 2 h, sampling measures wherein sulforaphen content by HPLC, calculates sulforaphen raw One-tenth rate.
(2) compositions A group: take compositions A group 0.278 g(and contain glucorphanin 40.1 mg), join 20 mL intestinal moulds Intending in liquid, in 37 DEG C of insulations, when 0.5 h, 1 h and 2 h, sampling measures wherein sulforaphen content by HPLC, calculates Sulforaphen production rate.
(3) compositions B group: take compositions B group 0.375 g(and contain glucorphanin 40.1 mg), join 20 mL intestinal moulds Intending in liquid, in 37 DEG C of insulations, when 0.5 h, 1 h and 2 h, sampling measures wherein sulforaphen content by HPLC, calculates Sulforaphen production rate.
(4) compositions C group: take compositions C group 1.12 g(and contain glucorphanin 40.1 mg), join 20 mL intestinal moulds Intending in liquid, in 37 DEG C of insulations, when 0.5 h, 1 h and 2 h, sampling measures wherein sulforaphen content by HPLC, calculates Sulforaphen production rate.
The HPLC assay method of sulforaphen: take sample solution, crosses 0.45 μm filter membrane, carries out HPLC analysis.HPLC condition: Chromatographic column: company of HuaPu Unitary C18(4.6 mm × 250 mm, 5 μm);Column temperature: 30 DEG C;Flowing phase: 70% water-30% second Nitrile;Flow velocity: 0.8 mL/min;Sample size: 10 μ L;Ultraviolet detection wavelength: 245 nm.
Experimental result see table 1 and Fig. 1.
The blank group of table 1. and the relative amount (chromatographic peak area) of sulforaphen in compositions A, B, C group sample solution
From experimental result, rich in the blank group of glucorphanin and compositions group microorganism species in simulation intestinal liquid Under help, all create sulforaphen, and the prolongation over time of the growing amount of sulforaphen and increase, after reaction 4 hours, The conversion ratio of blank group has reached 7%, and it is notable to the addition of the conversion ratio of glucorphanin in compositions B of functional oligose and C Increasing, wherein the conversion ratio increase of the glucorphanin in compositions C group is the most notable, has reached 67%, has carried relative to blank group High nearly 9 times.Obviously, after with the addition of functional oligose, glucorphanin in intestinal environment to the conversion ratio of sulforaphen Significantly improve.

Claims (10)

1. a compositions, it comprises:
(1) glucorphanin;With
(2) functional oligose.
Compositions the most according to claim 1, wherein said functional oligose is selected from oligofructose, soybean oligo saccharide, oligomeric Galactose, oligomeric xylose, oligomeric isomaltose, oligomeric lactulose, cyclodextrin, oligochitosan, inulin and combinations thereof.
3., according to the compositions of claim 1 or 2, wherein said functional oligose is selected from oligofructose, oligomeric xylose, oligomeric Galactose, oligomeric lactulose and oligomeric isomaltose.
4., according to the compositions of claim 1 or 2, wherein said functional oligose is oligomeric xylose.
5., according to the compositions any one of Claims 1-4, it is pharmaceutical composition or food compositions, the most additionally contains Acceptable additive on pharmaceutically acceptable excipient or carrier or food.
6. the method converted to sulforaphen in increasing glucorphanin body, including adding functional oligose in glucorphanin.
7. the purposes in the product that preparation is used for treatment or prophylaxis of cancer of the compositions any one of claim 1 to 5.
Purposes the most according to claim 7, wherein said product is medicine or food.
9. according to the purposes of claim 7 or 8, wherein said product is selected from following food: food supplement, health care food Product, beverage, shake drink, baked product, tea, soup, frumentum, salad, sandwich, salad dressing, soy sauce, coffee, cheese, acid Cheese, energy food, and mixture.
10., according to the purposes of claim 7 or 8, wherein said product is selected from following form: soft capsule, hard capsule, drip Ball, tablet, granule, pill, injection, oral liquid, powder, medicated wine, hard sugar, soft sweet, medicinal tea.
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