CN108815463A - Natural drug, preparation method and application with cancer prevention effect - Google Patents
Natural drug, preparation method and application with cancer prevention effect Download PDFInfo
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- A61K36/88—Liliopsida (monocotyledons)
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Abstract
The present invention relates to a kind of natural drug with cancer prevention effect, preparation method and applications.The natural drug with cancer prevention effect is formulated by the raw material of following parts by weight：The turmeric of 30-70 parts by weight, the broccoli of 5-20 parts by weight, the rainbow conk of 10-50 parts by weight, the yeast beta-dextran of 5-20 parts by weight and 5-20 parts by weight pepper.The Cancer-causing mutation that natural drug of the present invention forms by reducing intracorporal carcinogen, hazardous compound is prevented to induce, forms the primary prevention of cancer；Cancer early stage patient tumour inflammation is reduced by immunocytes such as activated lymphocyte, macrophages, improves the clinical symptoms of tumor patient, forms the secondary prevention of cancer；It is acted synergistically by cancer patient and other chemotherapeutics, inhibits drug resistance of tumor, form the tertiary prevention of cancer, the final incidence and the death rate for reducing cancer achievees the purpose that cancer prevention.
Description
Technical field
The present invention relates to biochemistry field of medicaments, and in particular to natural drug, its preparation with cancer prevention effect
Methods and applications.Natural drug of the present invention is formed by reducing intracorporal carcinogen, hazardous compound is prevented to induce
Cancer-causing mutation forms the primary prevention of cancer；Cancer early stage is reduced by immunocytes such as activated lymphocyte, macrophages to suffer from
Person's tumour inflammation, improves the clinical symptoms of tumor patient, forms the secondary prevention of cancer；Pass through cancer patient and other chemotherapeutics
Object synergistic effect, inhibits drug resistance of tumor, forms the tertiary prevention of cancer, and the final incidence and the death rate for reducing cancer reaches
To the purpose of cancer prevention.
Background technique
Cancer, also known as malignant tumour are a kind of diseases characterized by undesired cell proliferation.Induce expression of proto-oncogenes
Factor mainly has 3 kinds：Energy-ray, chemical substance, virus.Research confirms, contacts and take in the various chemical carcinogenesis in environment
Object, such as BaP, aflatoxins, organochlorine phosphorus pesticide and nitrosamine compound are the main reason for various cancers occur.
After how effectively realizing that these substances are contactd by mistake by human body, the formation of internal carcinogen not will lead to, be pre- anti-cancer hair
Raw the first line of defence.
In general, modern medicine is treated usually based on operation, chemotherapy and radiotherapy after if cancer unfortunately occurs
Tumour, since these means also can largely anti-personnel normal cell while killing tumour, it will give people
Body bring serious toxic side effect and pain sensation by.Therefore the mitigation for how realizing cancer clinical symptom, prevents the expansion of tumour
It is second and the three lines of defence of pre- anti-cancer with transfer.
If certain mode can be taken to reduce or even prevent ever-increasing cancer morbidity, mitigate the pain of cancer sufferer
Hardship extends the period and promotes life quality, while avoiding using some high and strong therapeutic agent, undoubtedly to cancer patient
It is beneficial.
In recent years, the weight that there is the active constituent of cancer chemoprevention effect to become cancer research for screening from natural plants
Want one of direction.
Early stage canceration or in cancer cell forming process, before being inhibited using the lower natural or synthetic chemical substance of toxicity
Body compound forms real carcinogenic substance, and prevent its be in contact with intracellular macromolecular such as DNA, RNA or protein and
Reaction, until being completely exhausted out external；Or it is pernicious to reduce by each stage that reverse, blocking or delay cancer occur
The Critical policies that tumorigenic danger is prevention, inhibits or cancer is reversed to occur.This process, that is, so-called " change of cancer
Learn prevention ".
The process that research discovery for many years promotes body itself to eliminate chemical carcinogen occurs that I phase and II can be divided into liver
Phase.First after I phase metabolic enzyme such as Cytochrome P450 effect, hydroxyl is introduced in hydrophobic chemical carcinogen；Then in liver
Dirty II phase metabolic enzyme such as glutathione transferase (GST), nicotinamide-adenine dinucleotide phosphate (NADP) quinone oxidoreductase
(NQO1), it under the action of uridine diphosphate glucuronatetransferase (UGTPGT) etc., is glycosylated again on the hydroxyl generated,
It further increases the water solubility of compound and it is promoted to excrete.Therefore, inhibit the activity of I phase metabolic enzyme and improve induction II
The activity of phase metabolic enzyme is the committed step of cancer chemoprevention.Find low toxicity, the natural plant extracts of safety become various countries
The research emphasis and difficult point of cancer prevention.The antitumoral compounds sulforaphane (SFN) such as extracted from brassicaceous vegetable, it
It is the strength inducer of II phase metabolic enzyme, it can GST and NQO1 in rat bladder tissue and external bladder cells in significant inductor
Expression (Zhang Y, Munday R, Jobson HE, the et al.Induction of GST and NQO1 in of enzyme
cultured bladder cells and in the urinary bladders of rats by an extract of
Broccoli (Brassica oleracea itallca) sprouts.J Agric Food Chem, 2006,54 (25)：
9370-9376.).In addition, how to adjust cancer starting and develop relevant signaling pathway molecule out of control, to prevent carcinogenic
The starting protection DNA of effect is from being mutated, inhibiting tumor cell proliferation, antitumor infiltration and DISTANT METASTASES IN, and realization cancer
An important factor for prevention.
Summary of the invention
To solve the above-mentioned problems, the present invention provides a kind of natural drugs with cancer prevention effect, its preparation side
Method and application.The natural drug not only itself has good cancer prevention effect, moreover it is possible to be combined reductionization with chemotherapeutics
Treat the toxic side effect of drug.The present composition can be used for preparing any one following product：1) prevent and/or treat tumour
Drug；2) health care product；3) food；Or 4) nutrient prime replenisher.Tumour mentioned in the present invention includes lung cancer, liver cancer, white
Blood disease, breast cancer, cancer of the esophagus, gastric cancer, cervical carcinoma, prostate cancer, the carcinoma of the rectum, Gastric stromal tumors, oophoroma, preferably lung cancer.
The present invention provides a kind of natural drug with cancer prevention effect, by the raw material preparation of following parts by weight
At：
The turmeric of 30-70 parts by weight, the broccoli of 5-20 parts by weight, the rainbow conk of 10-50 parts by weight, 5-20 parts by weight ferment
The pepper of female beta glucan and 5-20 parts by weight.
Further, the natural drug with cancer prevention effect is formulated by the raw material of following parts by weight：
The turmeric of 50 parts by weight, the broccoli of 30 parts by weight, the rainbow conk of 10 parts by weight, 10 parts by weight yeast beta-dextran
With the pepper of 10 parts by weight.
The present invention also provides the preparation methods of the natural drug described in one kind with cancer prevention effect, including following step
Suddenly：
Turmeric, broccoli, rainbow conk and pepper are weighed in parts by weight as extracting to obtain ginger respectively after raw material grind
Yellow extract, Caulis et Folium Brassicae capitatae, Coriolus Versicolor P.E. and Fructus Piperis extract add after yeast beta-dextran mixing and medicine are added
It learns acceptable auxiliary material and is mixed and made into acceptable any dosage form.
Further, the preparation of the Turmeric P.E includes：It takes turmeric to be ground into coarse powder, smashed turmeric 5 is added
Three times, 1.5~2 hours every time, add 2~3 times of amount concentration was the ethyl alcohol and heating extraction that~8 times of amount concentration are 80~85%
80%~85% ethyl alcohol soaked extracting solution, stirring stand 24~48 hours, take supernatant, depressurize and add at 65~75 DEG C
Hot filtrate is concentrated into saturated solution, stands until precipitate crystal, take crystal dry Turmeric P.E is spare；
The preparation of the Caulis et Folium Brassicae capitatae includes：Selecting broccoli seed, sprout and/or bulb is raw material, by raw material
After mechanical crushing, 3-5 times be added after being mechanically pulverized measures water mixing, adds proper amount of acetic acid, pH is adjusted to 5-6, then according to
The parts by weight of broccoli raw material and complex enzyme are 100:The complex enzyme is added in 1 ratio, 25-40 DEG C at a temperature of hydrolyze 2-
8 hours, promote glucosinolate in broccoli to be converted into sulforaphen, hydrolyzate is obtained by filtration, the hydrolyzate is inhaled by macropore
Attached resin (resin can select AB-8, D101, HP850, HP870 etc.) column absorption, after having adsorbed, respectively with three times column volume
The impurity adsorbed in deionized water and 20% ethanol elution resin, then with the work in 80% ethanol elution resin of three times column volume
Property ingredient, the eluent finally obtained at 20-40 DEG C by vacuum concentration, be concentrated into relative density 1.1~1.2 (45 DEG C~
60 DEG C), then be spray-dried and crush, obtain Caulis et Folium Brassicae capitatae；
The preparation of the Coriolus Versicolor P.E. includes：It takes rainbow conk pulverizing medicinal materials at the coarse powder of 80~120 mesh, is added smashed
15~40 times amount water ultrasonic extraction 60~80 minutes, Aqueous extracts obtain filtrate through ultrafiltration membrance filter, add dense after 95% ethyl alcohol
Determining alcohol is reduced to up to 80%, precipitates to obtain polysaccharide, is dried in vacuo, obtains Coriolus Versicolor P.E.；
The preparation of the Fructus Piperis extract includes：Pepper is taken to be ground into the coarse powder of 80~120 mesh, it is added smashed 5~
8 times of amount concentration be 80~85% ethyl alcohol heating extractions three times, 1.5~2 hours every time, combined extract, filtering and standing, filtrate returned
Ethyl alcohol is received, relative density 1.1~1.25 (45 DEG C~60 DEG C) is concentrated into, is dried in vacuo to obtain Fructus Piperis extract.
Further, in the preparation of the Caulis et Folium Brassicae capitatae, the complex enzyme includes with weight ratio 1:1 mixed wood
Melon protease: cellulase.
Further, acceptable any dosage form is tablet, soft capsule, hard capsule, the capsule and pill, drop of oral preparation
Ball, liposome or granule.
Further, the pharmaceutically acceptable auxiliary material include one of bonding agent, filler, lubricant and disintegrating agent or
It is several；Wherein the bonding agent includes in syrup, Arabic gum, gel, D-sorbite, xanthan gum and polyvinylpyrrolidone
It is one or more of；The filler includes one of lactose, carbohydrate, cornstarch, calcium phosphate, D-sorbite and DEXTROSE ANHYDROUS
Or it is several；The lubricant includes one or more of magnesium stearate, talcum powder, polyethylene glycol and silica；It is described to collapse
Solving agent includes one or more of potato starch and sodium carboxymethylcellulose.
The present invention also provides a kind of applications in terms of cancer prevention of natural drug with cancer prevention effect.
Further, the cancer includes lung cancer, liver cancer, leukaemia, breast cancer, cancer of the esophagus, gastric cancer, cervical carcinoma, forefront
Gland cancer, the carcinoma of the rectum, Gastric stromal tumors or oophoroma.
The features of the present invention：
1, the present invention is filtered out from food source plant has natural anti-cancer, anti-cancer active matter, has carried out scientific compatibility group
Cancer chemoprevention natural drug composition made of conjunction has ideal antitumous effect, not will cause internal organs pathologic damage
Evil, it is highly-safe.It is metabolized expression of enzymes by the plant compound activation of safety, II phase of induction and plays cancer chemoprotective effect,
The Cancer-causing mutation for preventing hazardous compound from inducing, the secretion for increasing body itself by protection enzyme system effectively prevent to induce cancer
Injury of the compound to human body, while having stronger inhibiting effect to I phase metablic enzyme of cytochrome P450s, reduce carcinogenic substance
Metabolism activation, ultimate carcinogen generate reduction, to cell DNA generate protective effect.With attenuation, inhibit tumor cell proliferation,
Antitumor infiltration and DISTANT METASTASES IN effect.
2, the present invention select natural plants compound can the immunocytes such as activated lymphocyte, macrophage, and can antagonism
Tumour itself or the decline of caused by chemotherapeutic medicines immune cell function, reduce chemotherapy adverse effect, mitigate tumour inflammation, improve tumour
The clinical symptoms of patient.Chemicotherapy curative effect is improved with other chemotherapy drugs in combination applications, inhibits drug resistance of tumor.
3, the present invention selects natural plants compound by the collaboration or superposition between each natural phytochemicals,
Effect more stronger than single use under same concentrations is obtained, the usage amount of single compound is also reduced, is mitigated that may be present
To the toxicity of host cell.
4, the present invention uses modern plants medicine extractive technique, and ingredient each in prescription is extracted respectively, clean, is refined into standard
Extract, the effective component of each ingredient or position are clear, and content is high, have stringent quality standard, the consistency of analysis method
So that system easy to control the quality, has pharmacodynamic substances basis and specific pharmacological activity, curative effect is stablized, and administration absorbs the target that can go directly
Position.
5, curative effect of the present invention is high, cheap, easy to use simple and direct, and patient compliance is high, can substantially save cancer patient
Treatment cost.
Detailed description of the invention
Fig. 1 is curcumin and derivative prevents the action site schematic diagram that chemical method induces cancer.
Specific embodiment
By studying a large amount of natural drugs, filter out clinical be used for a long time confirms effectively with anti-swollen the present invention
The cancer chemoprevention natural drug of tumor effect, natural drug of the invention are mentioned by Turmeric P.E, Caulis et Folium Brassicae capitatae, pepper
Take object, Coriolus Versicolor P.E. and yeast beta-dextran composition, the effect of each component as follows：
Turmeric is the dry rhizome of zingiberaceous plant turmeric or Radix Curcumae, is removing blood stasis and promoting blood circulation medicine, returns liver, the spleen channel.Turmeric it is main
Effective component is curcumin (Curcumin, Cur).Curcumin is a kind of plant polyphenol, shows that curcumin has through pharmacological research
The effect of anti-inflammatory, anti-oxidant, anticoagulant, reducing blood lipid, antiatherosclerosis, antitumor, anti-mutation etc..
Curcumin can significantly inhibit the transfer and infiltration of tumour cell.Inside and outside is it is demonstrated experimentally that curcumin can inhibit lung cancer
The proliferation of cell.In experiment in vitro, curcumin can promote the table of Nrf2 in kidney epithelia cell in a manner of dosage and Time Dependent
It reaches.From the gene expression path of II phase metabolic enzyme it is found that the number of II phase metabolic enzyme can be increased by activation Nrf2/ARE access
Amount, to reinforce the ability of body degradation carcinogenic compound.By years of researches, curcumin is induced through Nrf2/ARE access
II phase is metabolized expression of enzymes and plays cancer chemoprotective effect.
Further investigations have shown that curcumin has stronger inhibiting effect to I phase metablic enzyme of cytochrome P450s, mainly
It is to inhibit P450IA1/IA2, reduces carcinogenic metabolism activation, ultimate carcinogen generates reduction, generates protection to cell DNA and makees
With.Animal experiments show that continuously giving Swiss mouse containing 5% turmeric food 5 days, it can obviously inhibit liver P450-bsContain
The level of amount and Cytochrome P450.Meanwhile II the activity of phase enzyme GST significantly improve.Mouse curcumin is given by 250mg/kg
15 days, liver GST activity can be made to improve 18 times.Give rat continuously edible food 4 weeks containing turmeric, GST and UDP-glucose
The activity of glucuronyl transferase is obvious to be risen.Induction and activation to I phase enzyme can promote carcinogenic removing toxic substances discharge.
Curcumin, can also directly attack of a variety of chemical factors of antagonism to cell DNA other than the activity for influencing metabolic enzyme.
The enhancing and its facedown of inhibition, function of detoxification that curcumin is metabolized carcinogenic substance act on, then can make carcinogenic substance-DNA addition
The generation of object is reduced.
In test, curcumin and the action site of derivative prevention chemical method induction cancer are as shown in Figure 1.
Turmeric is known as fabulous tumor prevention effect, especially early stage tumour formation.Curcumin and other chemotherapeutics
Object use in conjunction helps to improve chemotherapeutic efficacy.Clinically curcumin can be drawn with adriamycin application with substantially reduced adriamycin
The heart and Toxicity of Kidney served.
Clinical research report curcumin it is oral up to 12g/ days when, there is no any toxicity to people, therefore curcumin has been used as one
It plants less toxic, effective, expense low (most people can be born) anti-tumor drug and is concerned.
(Proceedings of is found from broccoli sprouting by U.S. John-John Hopkins University researcher within 1992
The National Academy of Sciences, USA.1992,89:2399-2403) sulforaphen, also known as sulforaphane
(English name is Sulforaphane).Isothiocyanic acid salt compound contained in broccoli can effectively prevent liver cancer,
The cancers such as lung cancer, prostate cancer, breast cancer, the carcinoma of the rectum, NIH mice.Sulforaphane is presently found anti-oxidant, anti-cancer, anticancer
The most significant isothiocyanic acid salt compound of activity, is that enzyme induction object is effectively protected in one kind, carcinogenic compound can be protected to draw
The injury risen.
Sulforaphane is mainly a kind of inducer of II phase enzyme, can prevent many chemical carcinogens inductions DNA damage and
Generation (Hintze KJ, Keck AS, the Finley JW.Induction of hepatic thioredoxin of kinds of tumors
Reductase activity by sulforaphane, both in Hepa1c1c7 cells and in male Fisher
344 rats[J]. Nutr Biochem 2003 Mar；14(3):173-179).Sulforaphane can completely inhibit I phase enzyme (such as
Cytochrome P450), the expression of mouse macrophage COX-2 can be lowered, to inhibit generation (the Heiss E, Herhaus of tumour
C, Klimo K, et a1.Nuclear factor KB is a molecular target for sulforaphane-
Mediated anti-infannatory mechanisms [J] J BiolChem, 2001,276 (34)：32008-
32015).Due to the lipophilic characteristics of sulforaphane, inhibiting the biosynthesis of phosphatide and other lipid materials is also that sulforaphane lures
Guided cell growth stops and an important mechanisms of apoptosis.Sulforaphane can offset carcinogenic chemicals confrontation by number of mechanisms
The toxic action of gene, thus protect DNA from mutagenic compounds damage (Kuroiwa Y, Nishikawa A,
Kitamura Y, et al.Protective0771Journal of Chinese Medicinal Materials
effects of benzyl isothiocyanate and sulforaphane but not resveratrol against
Initiation of pancreatic carcinogenesis in hamsters [J] .Cancer Lett, 2006,241
(2):275-280.).Sulforaphane can induce apoptosis of tumor cells, cell growth cycle made to stop, inhibiting a variety of chemical carcinogenesis
The metabolism activation and inhibition inflammation of object, it is now recognized that sulforaphane is potential tumor therapeutic agent (Wang Shuran, Xia Wei radish
Sulfane and tumour [J] disease control magazine.2004,8 (5)；452-455).
Rainbow conk is traditional Chinese medicine, belongs to Polyporaceae plant, has effects that strengthen the body resistance to consolidate the constitution, nourishing the essence and strengthening QI.Rainbow conk is extracted
Object polysaccharide-peptide is the high score seed glycopeptide polymer extracted from prepared from coriolus versicolor mycelium.Japanese scholars are reported, in prepared from coriolus versicolor mycelium
Proteoglycan (abbreviation PSK) has apparent tumor suppression and immunologic enhancement, non-evident effect.(dry original Wu youth, tumor suppression are more
Sugar, foreign medical science: traditional Chinese medicine credit volume, 1982,4: 333).Japanese government approved PSK is controlled for clinical tumor within 1997
It treats.
Recent domestic scholar enhances immune function to Coriolus Versicolor P.E. polysaccharide-peptide and anti-tumor activity has been done more
In-depth study, polysaccharide-peptide are applied to clinic as biological regulator at present.Polysaccharide-peptide has apparent righting
Eliminating evil effect, can enhance the immune function of normal body and tumor animal, can inhibit the life of in vitro culture animal and human cancer cell
It is long, the clinical symptoms of tumor patient can be improved, improve Kanofsky score value.
Polysaccharide-peptide is to play antitumor action by enhancing body's immunity, it mainly enhance T lymphocyte,
Macrophage and natural killer cells function (in super polysaccharide-peptide Advances in antitumor activity (J) of Liu Yan, Li Rui at
Medicine, 2001,23 (10)).Research shows that after malignant tumor patient takes polysaccharide-peptide, T3, T4 lymphocyte subgroup and cytometer
Count (the P that is significantly increased<0.01), bone-marrow-derived lymphocyte is without significant changes (P>0.01).Polysaccharide-peptide can increase the function of T lymphocyte
Can, and can antagonism tumour itself or caused by chemotherapeutic medicines T lymphocyte function reduction.
Beta glucan is to be distributed widely in fungi, bacterium and the intracorporal large biological molecule of plant, is to construct a variety of biologies carefully
The material of cell wall has antitumor, increasing leucocyte, anti-complement activity, antiviral, anticoagulation, activating macrophage, promotes cell
The various biologicals activity such as synthesis, the induction NO synthesis of the factor, also show that various lifes during influencing each other between biology
Object activity (such as to the stimulation of animal immune system).Yeast cell wall polysaccharide is reported from Brander in 1958
(Zymosan) since having antitumor action, a large amount of immunization experiments prove that beta glucans can not only activate T/B lymphocyte, huge
The immunocytes such as phagocyte (M), natural killer cells (NK), moreover it is possible to which complement activation promotes the generation of cell factor, to siberian crabapple
System plays various adjustment effects.
Yeast beta-dextran dextran, Glucan are also known as dextran, are a kind of polysaccharide.Yeast β-the Portugal of research at present is poly-
The main target of sugared anti-cancer function is exactly the activity and phagocytosis energy that beta glucan reinforces the macrophage being present in cell tissue
Power.The ability of macrophage can be enhanced in yeast beta-dextran, can improve macrophages phagocytic capacity and reach several times or more.Usually tool
There is the very strong inhibiting rate to mutant, it can further be locked while protecting and enhancing immunocyte fight capability
" the residual tumor cell " for determining dormant period, drug resistance and subclinical lesion, carries out targeting antivirus.
Pepper is the nearly mature or ripening fruits of drying of Piperaceae plant pepper, pungent, heat.Return stomach, large intestine channel, there is middle benefit gas to dissipate
It is cold, the effect of lower gas, dissolving phlegm.Modern medicine study show pepper main pharmacodynamics ingredient piperine have it is antitumor, resist it is insane
Epilepsy, antidepression, it is anti-oxidant, promote drug metabolism the effects of.Piperine can be improved general naphthalene Lip river as bioavilability reinforcing agent
The bioavilability in vivo such as that, choline theophyllinate, curcumin.
Curative effect of the present invention is high, cheap, easy to use simple and direct, has no toxic side effect, and patient compliance is high.It is of the present invention
The Cancer-causing mutation that natural drug forms by reducing intracorporal carcinogen, hazardous compound is prevented to induce, forms the one of cancer
Grade prevention；Cancer early stage patient tumour inflammation is reduced by immunocytes such as activated lymphocyte, macrophages, improves tumour and suffers from
The clinical symptoms of person form the secondary prevention of cancer；It is acted synergistically by cancer patient and other chemotherapeutics, inhibits tumour resistance to
Pharmacological property forms the tertiary prevention of cancer, and the final incidence and the death rate for reducing cancer achievees the purpose that cancer prevention.
Embodiment：Utilize the case study on implementation of drug of the present invention
Embodiment 1 (capsule)
It takes 50 parts by weight turmerics to be ground into coarse powder, the ethyl alcohol that 8 times of smashed turmeric amount concentration are 85% and heating is added
It extracts three times, 1.5 hours every time, adds the ethyl alcohol soaked extracting solution that 2 times of amount concentration are 80%, stirring stands 48 hours, takes
Supernatant, depressurizes and heats filtrate at 70 DEG C and be concentrated into saturated solution, stands until precipitate crystal, take crystal dry turmeric
Extract is spare；
10 parts by weight broccoli sprouts are taken to crush coarse powder, 4 times of amount water being added after being mechanically pulverized mix, and add appropriate vinegar
PH is adjusted to 6 by acid, is 100 then according to the parts by weight of broccoli raw material and complex enzyme:It is (multiple that the complex enzyme is added in 1 ratio
Synthase is with weight ratio 1:1 mixed papain: cellulase), 36 DEG C at a temperature of hydrolyze 6.5 hours, promote west blue
It spends middle glucosinolate to be converted into sulforaphen, hydrolyzate is obtained by filtration, the hydrolyzate is adsorbed by large pore resin absorption column,
After having adsorbed, respectively with the impurity adsorbed in the deionized water of three times column volume and 20% ethanol elution resin, then with three times column
Active constituent in 80% ethanol elution resin of volume, the eluent finally obtained is at 40 DEG C by vacuum concentration, concentration
It to relative density 1.12 (45 DEG C), then is spray-dried and crushes, obtain Caulis et Folium Brassicae capitatae；
It takes 20 parts by weight rainbow conk pulverizing medicinal materials at the coarse powder of 120 mesh, smashed 30 times of amount water ultrasonic extraction 80 is added and divides
Clock, Aqueous extracts obtain filtrate through ultrafiltration membrance filter, are concentrated into determining alcohol up to 80% after adding 95% ethyl alcohol, precipitate to obtain polysaccharide,
Vacuum drying, obtains Coriolus Versicolor P.E.；
10 parts by weight peppers are taken to be ground into the coarse powder of 100 mesh, it is that the heating of 85% ethyl alcohol mentions that smashed 8 times of amount concentration, which is added,
It takes three times, 1.5 hours every time, combined extract, filtering and standing, filtrate recycling ethanol, is concentrated into relative density 1.25 (55 DEG C),
It is dried in vacuo to obtain Fructus Piperis extract.
It extracts according to the method described above and respectively obtains Turmeric P.E, Caulis et Folium Brassicae capitatae, Coriolus Versicolor P.E., Fructus Piperis extract
Afterwards, 10 parts of weight of yeast beta-dextran, 1 parts by weight of magnesium stearate, 1 parts by weight of superfine silica gel powder, dextrin is added and fits 3 weight deal tune
Whole total amount mixes, is filled into capsule after pellet through sieves are made.
Embodiment 2 (tablet)
It takes 40 parts by weight turmerics to be ground into coarse powder, the ethyl alcohol that 6 times of smashed turmeric amount concentration are 82% and heating is added
It extracts three times, 2 hours every time, adds the ethyl alcohol soaked extracting solution that 2 times of amount concentration are 80%, stirring stands 48 hours, takes
Supernatant, depressurizes and heats filtrate at 70 DEG C and be concentrated into saturated solution, stands until precipitate crystal, take crystal dry turmeric
Extract is spare；
15 parts by weight broccoli sprouts are taken to crush coarse powder, 4 times of amount water being added after being mechanically pulverized mix, and add appropriate vinegar
PH is adjusted to 6 by acid, is 100 then according to the parts by weight of broccoli raw material and complex enzyme:It is (multiple that the complex enzyme is added in 1 ratio
Synthase is with weight ratio 1:1 mixed papain: cellulase), 36 DEG C at a temperature of hydrolyze 8 hours, promote broccoli
Middle glucosinolate is converted into sulforaphen, and hydrolyzate is obtained by filtration, and the hydrolyzate is adsorbed by large pore resin absorption column, is inhaled
It is attached it is complete after, respectively with the impurity adsorbed in the deionized water of three times column volume and 20% ethanol elution resin, then with three times cylinder
Active constituent in 80% long-pending ethanol elution resin, the eluent finally obtained, by vacuum concentration, are concentrated at 35 DEG C
Relative density 1.15 (55 DEG C), then be spray-dried and crush, obtain Caulis et Folium Brassicae capitatae；
It takes 25 parts by weight rainbow conk pulverizing medicinal materials at the coarse powder of 100 mesh, smashed 25 times of amount water ultrasonic extraction 60 is added and divides
Clock, Aqueous extracts obtain filtrate through ultrafiltration membrance filter, are concentrated into determining alcohol up to 80% after adding 95% ethyl alcohol, precipitate to obtain polysaccharide,
Vacuum drying, obtains Coriolus Versicolor P.E.；
5 parts by weight peppers are taken to be ground into the coarse powder of 100 mesh, it is that the heating of 80% ethyl alcohol mentions that smashed 6 times of amount concentration, which is added,
It takes three times, 2 hours every time, combined extract, filtering and standing, filtrate recycling ethanol, is concentrated into relative density 1.20 (60 DEG C),
It is dried in vacuo to obtain Fructus Piperis extract.
It extracts according to the method described above and respectively obtains Turmeric P.E, Caulis et Folium Brassicae capitatae, Coriolus Versicolor P.E., Fructus Piperis extract
Afterwards, 15 parts of weight of yeast beta-dextran, 10 parts by weight of lactose, 15 parts by weight of cornstarch are added to be uniformly mixed, lubricant is added
3 parts by weight of magnesium stearate are uniformly mixed, and whole grain, then tablet is made in tabletting.
Embodiment 3 (granule)
It takes 70 parts by weight turmerics to be ground into coarse powder, the ethyl alcohol that 8 times of smashed turmeric amount concentration are 80% and heating is added
It extracts three times, 2 hours every time, adds the ethyl alcohol soaked extracting solution that 4 times of amount concentration are 80%, stirring stands 48 hours, takes
Supernatant, depressurizes and heats filtrate at 75 DEG C and be concentrated into saturated solution, stands until precipitate crystal, take crystal dry turmeric
Extract is spare；
10 parts by weight broccoli sprouts are taken to crush coarse powder, 6 times of amount water being added after being mechanically pulverized mix, and add appropriate vinegar
PH is adjusted to 5.5 by acid, is 100 then according to the parts by weight of broccoli raw material and complex enzyme:The complex enzyme is added in 1 ratio
(complex enzyme is with weight ratio 1:1 mixed papain: cellulase), 40 DEG C at a temperature of hydrolyze 6 hours, promote west blue
It spends middle glucosinolate to be converted into sulforaphen, hydrolyzate is obtained by filtration, the hydrolyzate is adsorbed by large pore resin absorption column,
After having adsorbed, respectively with the impurity adsorbed in the deionized water of three times column volume and 20% ethanol elution resin, then with three times column
Active constituent in 80% ethanol elution resin of volume, the eluent finally obtained is at 40 DEG C by vacuum concentration, concentration
It to relative density 1.10 (55 DEG C), then is spray-dried and crushes, obtain Caulis et Folium Brassicae capitatae；
It takes 10 parts by weight rainbow conk pulverizing medicinal materials at the coarse powder of 100 mesh, smashed 35 times of amount water ultrasonic extraction 80 is added and divides
Clock, Aqueous extracts obtain filtrate through ultrafiltration membrance filter, are concentrated into determining alcohol up to 80% after adding 95% ethyl alcohol, precipitate to obtain polysaccharide,
Vacuum drying, obtains Coriolus Versicolor P.E.；
5 parts by weight peppers are taken to be ground into the coarse powder of 100 mesh, it is that the heating of 80% ethyl alcohol mentions that smashed 6 times of amount concentration, which is added,
It takes three times, 2 hours every time, combined extract, filtering and standing, filtrate recycling ethanol, is concentrated into relative density 1.15 (60 DEG C),
It is dried in vacuo to obtain Fructus Piperis extract.
It extracts according to the method described above and respectively obtains Turmeric P.E, Caulis et Folium Brassicae capitatae, Coriolus Versicolor P.E., Fructus Piperis extract
Afterwards, 5 parts of weight of yeast beta-dextran, 20 parts by weight of lactose, 10 parts by weight of cornstarch are added to be uniformly mixed, whole grain is dry, system
At granule.
Carry out the natural chemical composition that the present invention is further explained below by way of experiment and applies cancer chemoprevention
Effect.
One, the influence that case study on implementation 1 of the present invention grows mice transplanted tumor
1 experimental method
1 experiment purpose：Determine the influence that case study on implementation 1 of the present invention grows mice transplanted tumor
2 materials and method：
2.1 tested materials and model comparison
Tested material title and source：Case study on implementation 1 of the present invention.
Model comparison：Distilled water
2.2.2 experimental animal
4~6 week old BALB/c mouses, 40,18-22g, female, ties up tonneau China experimental animal skill purchased from Beijing by SPF grades
Art Co., Ltd.Conventional base feed was given before on-test to adapt to 5 days~7 days.
2.2.3 feeding environment
It raises in barrier environment, temperature is 26~28 DEG C (78~820F), relative humidity 40~60%.
2.2.4 tumor inoculation, grouping and administration
Every animal inoculates lung cancer A549 cell 5*106It is a, respectively control group (give same amount physiological saline), it is high,
In, low dose group oral administration (200,100,50mg/kg) successive administration observation administration after changes of weight and the time-to-live.Respectively
Group continuous gavage be administered 30 days, 1 times/day, observation administration when and 30 days in animal toxic reaction and death condition, after 30 days take off
Neck puts to death mouse, and dissection tumour, weighing simultaneously calculate tumour inhibiting rate and carry out statistical test.Experimental result difference is as shown in table 1,
In the 2nd, 3,4 group of tumour inhibiting rate be the knurl weight of each group and the ratio of the 1st group of knurl weight respectively.
3 experimental results
Table 1 is as can be seen that high, medium and low dosage can significantly extend the life (p of mice with tumor<0.01), especially with high agent
It measures more significant.
1 native chemical of table prevents influence of the composition to Transplantable Murine A549 lung cancer growth
Note：Compared with model group, * * * P < 0.001
Two, using 153 cancer patients of drug therapy of the present invention, and certain curative effect is obtained.
1 data and method
1.1 general information
Patient 153 are taken, wherein male patient is 103, female patient is 50, patient age 35~81 years old, average year
Age is 63.28 years old, and the course of disease is 1~3 year.It takes own control to test, that is, chooses and be diagnosed as cancer, controlled by chemicotherapy intervention
After treatment or be reluctant to carry out chemicotherapy or can not the patient of operative treatment (being to abandon treating) controlled using drug of the present invention
It treats.
1.2 treatment method
Oral case study on implementation 1 of the present invention 5 tablets each time, or is followed the doctor's advice 3 times a day.Blood routine, liver are checked at medication 3 months
Kidney function, abdominal CT evaluate curative effect.Responder continues to take, and related content was checked at 6 months, evaluates curative effect.Continue later
The person of taking drugs observes life cycle.
1.3 criterion of therapeutical effect
Reference WHO curative effect determinate standard,
Complete incidence graph (CR)：Tumor focus fully absorbs；
Alleviate (PR) in part：Tumor focus constantly reduces, but reduces volume and be greater than 50%；
Stablize (SD)：Tumor focus constantly reduces, but reduces volume less than 50%；
It is in progress (PD)：Tumor focus, which is presented, constantly expands trend, and volume expands 25% or more.
Objective efficient=(alleviating complete incidence graph+part)/evaluable case load × 100% of patient's treatment,
Patient disease control rate=(complete incidence graph+part alleviation+minor responses)/evaluable case load × 100%.
Life cycle index 3 months (people), 6 months (people), 1 year (people), 2 years (people), 3 years (people).
2 results
2.1 clinical efficacy
It treats in 153 patients, complete incidence graph patient is 42, and part reduction of patient is 62, and minor responses patient is
10, refractory patient 39.Objective effective percentage is 81.04%, disease control rate 74.50%.
3 months 8 people of life cycle index, 6 months 28 people, 1 year 65 people, 2 years 34 people, 3 years 18 people.
It is above-mentioned statistics indicate that, the objective efficient and disease control rate of drug therapy of the present invention is higher.
Typical case is only chosen below to be introduced.
Case 1：Mr. Lin, male, 45 years old, cirrhosis merge liver cancer；2014 are after diagnosing cirrhosis merging liver cancer, 2015
The beginning of the year takes orally case study on implementation 1 of the present invention, and daily 14, liver function recovery is normal after half a year, white blood cell from 1084 restore to
Normally, blood platelet, albumin restore normal, adhere to medication 3 years, are repeatedly checked tumour and do not find to spread, CT examination in 2017
It was found that reducing 40% tumor focus.
Case 2：Week, certain was blue, female, 73 years old, lung cancer；Lung cancer is diagnosed as through tumour hospital of Peking University within 2014.Do not carry out into
The treatment of one step, takes case study on implementation 1 of the present invention, and after taking 3 months according to 3-4-3 methods daily, dyspnea symptom disappears,
Cooperation takes Iressa (Gefitinib piece) so far after half a year, and pulmonary lesions disappear.
Case 3：Hao China, female, 82 years old, advanced lung cancer are diagnosed as adenocarcinoma of lung through tumour hospital of Hebei province in November, 2013,
3.5 centimeters of tumor focus, suggest carrying out chemotherapy 1 month through doctor, but patient's age is greatly (being 82 years old at that time), abandoning
It treats.It is changed within 2 months 2014 take case study on implementation 2 of the present invention, after taking the present invention 5 months, knurl is reduced into 2.5 centimeters；Together
December in year, knurl was reduced into 1.4 centimeters.So far ultrasound diagnosis also has no nascent tumor there is no transfer.
Case 4：Mr. Wang friend, male, 59 years old, later period of hepatocarcinoma, clinical diagnosis in 2014 are later period of hepatocarcinoma, concurrently reveal now double lungs
Transfer.Patient is implementing chemical PTCA or and STENTS, takes the present invention always since hospital does not have other suitable treatment methods
Case study on implementation 1.Daily 12, after taking 3 course for the treatment of (6 months), liver knurl reduces 50% (about 0.8 centimeter)；Double Lung metastases
Left tuberculosis stove is eliminated in lesion.
Case 5：Lee ancestral, male, 38 years old, low differentiation adenocarcinoma of lung；Clinical diagnosis in 2016 is low differentiation adenocarcinoma of lung, takes this
Invention case study on implementation 1, main suit feels good, and the common side effect of chemotherapy is unobvious, and 6 kilograms of weight gain, pulmonary lesions do not go out
Now further development diffusion.
Case 6：Poplar, male, 70 years old, 1 phase of prostate cancer；In June, 2014 is 1 phase of prostate cancer through clinical definite,
PSA11.69, prostate have mass tubercle, hard, and size is about 34x36x28mm.Take case study on implementation 2 of the present invention, daily 9
Grain, patient's state of an illness does not occur further to deteriorate after taking 1 year, and inspection has no residual metastasis of cancer, and adenoncus object product in forefront is reduced into
19x28x28mm.Patient main suit's spirit improves, and pain disappears.
The foregoing is merely presently preferred embodiments of the present invention, is not intended to limit the invention, it is all in spirit of the invention and
Within principle, any modification, equivalent replacement, improvement and so on be should all be included in the protection scope of the present invention.
Claims (9)
1. a kind of natural drug with cancer prevention effect, which is characterized in that be formulated by the raw material of following parts by weight：
The turmeric of 30-70 parts by weight, the broccoli of 5-20 parts by weight, the rainbow conk of 10-50 parts by weight, 5-20 parts by weight yeast β-
The pepper of glucan and 5-20 parts by weight.
2. the natural drug according to claim 1 with cancer prevention effect, which is characterized in that by following parts by weight
Raw material be formulated：
The turmeric of 50 parts by weight, the broccoli of 30 parts by weight, the rainbow conk of 10 parts by weight, the yeast beta-dextran of 10 parts by weight and 10
The pepper of parts by weight.
3. a kind of preparation method of the natural drug according to claim 1 or 2 with cancer prevention effect, feature exist
In including the following steps：
Turmeric, broccoli, rainbow conk and pepper are weighed in parts by weight as extracting to obtain turmeric respectively after raw material grind to mention
Object, Caulis et Folium Brassicae capitatae, Coriolus Versicolor P.E. and Fructus Piperis extract are taken, adding after yeast beta-dextran mixing and pharmacy is added can
The auxiliary material of receiving is mixed and made into acceptable any dosage form.
4. the preparation method of the natural drug according to claim 3 with cancer prevention effect, which is characterized in that
The preparation of the Turmeric P.E includes：Turmeric is taken to be ground into coarse powder, 5~8 times of amount concentration of smashed turmeric, which are added, is
Three times, 1.5~2 hours every time, add 2~3 times of amount concentration was 80%~85% to 80~85% ethyl alcohol and heating extraction
Ethyl alcohol soaked extracting solution, stirring stand 24~48 hours, take supernatant, depressurize and heating filtrate is concentrated at 65~75 DEG C
Saturated solution is stood until precipitate crystal, take crystal dry Turmeric P.E is spare；
The preparation of the Caulis et Folium Brassicae capitatae includes：Selecting broccoli seed, sprout and/or bulb is raw material, by raw material machinery
After crushing, 3-5 times be added after being mechanically pulverized measures water mixing, adds proper amount of acetic acid, pH is adjusted to 5-6, then according to western blue
The parts by weight of flower raw material and complex enzyme are 100:The complex enzyme is added in 1 ratio, small in 25-40 DEG C of at a temperature of hydrolysis 2-8
When, promote glucosinolate in broccoli to be converted into sulforaphen, hydrolyzate is obtained by filtration, the hydrolyzate is passed through into macroporous absorption
Resin column absorption, after having adsorbed, respectively with the impurity adsorbed in the deionized water of three times column volume and 20% ethanol elution resin,
Again with the active constituent in 80% ethanol elution resin of three times column volume, the eluent finally obtained passes through at 20-40 DEG C
Vacuum concentration, is concentrated into relative density 1.1~1.2 (45 DEG C~60 DEG C), then be spray-dried and crush, obtains Caulis et Folium Brassicae capitatae；
The preparation of the Coriolus Versicolor P.E. includes：Take rainbow conk pulverizing medicinal materials at the coarse powder of 80~120 mesh, it is added smashed 15~
40 times amount water ultrasonic extraction 60~80 minutes, Aqueous extracts obtain filtrate through ultrafiltration membrance filter, are concentrated into after adding 95% ethyl alcohol
Determining alcohol precipitates to obtain polysaccharide up to 80%, and vacuum drying obtains Coriolus Versicolor P.E.；
The preparation of the Fructus Piperis extract includes：It takes pepper to be ground into the coarse powder of 80~120 mesh, smashed 5~8 times of amounts is added
Concentration be 80~85% ethyl alcohol heating extractions three times, 1.5~2 hours every time, combined extract, filtering and standing, filtrate recycle second
Alcohol is concentrated into relative density 1.1~1.25 (45 DEG C~60 DEG C), is dried in vacuo to obtain Fructus Piperis extract.
5. the preparation method of the natural drug according to claim 1 with cancer prevention effect, which is characterized in that in institute
It states in the preparation of Caulis et Folium Brassicae capitatae, the complex enzyme includes with weight ratio 1:1 mixed papain: cellulase.
6. the preparation method of the natural drug according to claim 1 with cancer prevention effect, which is characterized in that described
Acceptable any dosage form is tablet, soft capsule, hard capsule, capsule and pill, dripping pill, liposome or the granule of oral preparation.
7. the preparation method of the natural drug according to claim 3 with cancer prevention effect, which is characterized in that described
Pharmaceutically acceptable auxiliary material includes one or more of bonding agent, filler, lubricant and disintegrating agent；The wherein bonding agent packet
Include one or more of syrup, Arabic gum, gel, D-sorbite, xanthan gum and polyvinylpyrrolidone；The filler packet
Include one or more of lactose, carbohydrate, cornstarch, calcium phosphate, D-sorbite and DEXTROSE ANHYDROUS；The lubricant includes
One or more of magnesium stearate, talcum powder, polyethylene glycol and silica；The disintegrating agent includes potato starch and carboxylic
One or more of sodium carboxymethylcellulose pyce.
8. the application in terms of cancer prevention of the natural drug according to claim 1 or 2 with cancer prevention effect.
9. application according to claim 8, which is characterized in that the cancer include lung cancer, liver cancer, leukaemia, breast cancer,
Cancer of the esophagus, gastric cancer, cervical carcinoma, prostate cancer, the carcinoma of the rectum, Gastric stromal tumors or oophoroma.
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| CN113575950A (en) * | 2021-08-06 | 2021-11-02 | 徐文红 | A nutritional product with adjuvant rehabilitation effect for radiotherapy and chemotherapy of cancer patients |
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