CN105596889A - Antitumor composition containing resveratrol and preparation method of antitumor composition - Google Patents
Antitumor composition containing resveratrol and preparation method of antitumor composition Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/82—Theaceae (Tea family), e.g. camellia
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/88—Liliopsida (monocotyledons)
- A61K36/899—Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane
- A61K36/8994—Coix (Job's tears)
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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Abstract
The invention relates to an antitumor composition containing resveratrol and a preparation method of the antitumor composition. The antitumor composition comprises, by weight, 60-200 parts of resveratrol, 30-150 parts of pterostilbene, 50-220 parts of green tea extract and 100-280 parts of semen coicis extract. The antitumor composition has the advantages that the defect that the resveratrol or pterostilbene is short in in-vivo action time when the resveratrol or pterostilbene is used independently is overcome, the green tea extract and the semen coicis extract are added, the antitumor composition is good in stability, the synergic effect of the components are brought into full play at the same time, the in-vivo action time is prolonged, the action efficiency is increased, and the antitumor composition is good in treatment assisting and preventing effects on tumor patients and people with potential morbidity, safe and free of toxic and side effects.
Description
Technical field
The invention belongs to the field of Chinese medicines, be specifically related to a kind of anti-tumor compositions and preparation method containing resveratrol.
Background technology
Tumour is common, the most serious a kind of disease that the world today directly jeopardizes human life. According to incompletely statistics, the whole world approximately has the new cancer stricken of 1,000 ten thousand people every year, approximately has more than 700 ten thousand people to die from cancer, accounts for 1/4 of total death toll. In China, annual number of the infected is about 2,000,000 people, and death toll is about 1,300,000.
At present, the treatment means of tumour mainly comprise operative treatment, chemotherapy, radiotherapy, treatment by Chinese herbs, natural plant treatment etc. Chemicals treatment, namely chemotherapy, it is the fastest methods for the treatment of of oncotherapy progress, but chemotherapeutics is all failed to differentiate between the enemy and ourselves conventionally, in killing tumor cell, human normal cell is also had to very large damage, cause blood platelet and leukocytic decline, cause local tissue necrosis and angiitis obliterans, to the toxic effect of cardiovascular system, severe patient also can cause heart failure, infringement liver cell, cause patient's alopecia, dermoreaction, the toxic and side effects such as disease such as appearance is felt sick, vomiting, poor appetite, diarrhoea, stomachache. Aspect natural plant treatment tumour, its characteristic and Chinese medicine are very close, equally for the diagnosis and treatment based on an overall analysis of the illness and the patient's condition of tumour illness, focus on strengthening function and the resistance against diseases in tumor patient health, thereby reach mark and this double object of controlling. Therefore, utilize natural medicinal plants composition to the diagnosis and treatment based on an overall analysis of the illness and the patient's condition of tumour pathogenic characteristic day by day by people are paid close attention to. Compared with chemicals, natural plant result for the treatment of is not worse than chemicals, and has no side effect. Simultaneously, can also improve because of various symptoms such as weak, appetite decline, vomiting, blood platelet and leucocyte decline that chemicotherapy causes, heart failure, liver injury, alopecias, but also can solve still more insurmountable chemicotherapy complication problems of current modern medicine.
Show according to version country base medicine catalogue in 2012, antineoplastic has 27 kinds, and wherein chemicals is 26 kinds, and natural plant is only a kind. Therefore, the exploitation of natural plant kind has wide market prospects.
Resveratrol, is the natural polyphenol compounds that a kind of biologically active is very strong, is mainly derived from the plants such as grape (claret), giant knotweed, peanut, mulberry fruit. Being the chemopreventive agent of tumour, is also to reducing platelet aggregation, the chemopreventive agent of prevention and treatment atherosclerotic, cardiovascular and cerebrovascular disease. In January, 1997, the professor JohnPezzuto leader's of Chicago,U.S illinois university pharmaceutical college research group is on the famous U.S. " science " magazine, deliver the paper that is entitled as " active anticancer of the natural product resveratrol of grape ", caused the sensation of medical science circle. Paper proves that resveratrol can effectively suppress the cellular activity relevant to the each process of cancer.
Pterostilbene (or being called pterostilbene), chemical name is: 3,5-dimethoxy-4 ' '-hydroxy diphenyl ethylene, (E)-3,5-dimethoxy-4 ' '-hydroxy styrenes, (E)-4-[2-(3,5-Dimethoxyphenyl)-vinyl]-phenol, 4-[(1E)-2-(3, 5-Dimethoxyphenyl)-vinyl]-phenol, it is the Verakanol derivative that is subject to extensive concern, it is extensively present in Guangxi Sanguis Draxonis (CHINA JOURNAL OF CHINESE MATERIA MEDICA, 1998, 23(10): 616 ~ 618), grape (J.AgrieFoodChem, 2000, 48 (12): 6103 ~ 6105), propolis (Experientia, 1978, 157 ~ 159) etc. 34 (2): in, have anti-oxidant, antiproliferative, reducing blood lipid, moderate strength suppresses the activity of COX-1 and COX-2, HL-60 cells Apoptosis, the canceration that prevention DMBA brings out, hypoglycemic activity and antifungal activity (J.AgricFoodChem, 2002, 50 (12): 3453 ~ 3457, J.NatProd, 1997,60 (6): 609 ~ 610, J.AgricFoodChem, 2005,53 (9): 3403 ~ 3407, J.OregChem, 2004,69 (21): 7101 ~ 7107). itself and resveratrol all belong to stilbenes compound, and on resveratrol phenyl ring 3, the hydrogen atom of 5-hydroxyl is replaced and become Pterostilbene by methyl. Pterostilbene also has powerful antiproliferative effect, strong and selectively strong compared with resveratrol effect, can suppress α-and λ-archaeal dna polymerase, also can suppress copying of SV40DNA, its suppress active and α-, δ-close with the triple AG14361 aphidocolins of ξ-DNA (Aphidicolin). to malignant melanoma cell B16M-F10, process and have significant inhibitory action in 60 minutes every day with the Pterostilbene of 40 μ M, and inhibiting rate reaches 56%(Neoplasia, and 2005,7 (1): 37 ~ 47). (IntJBiochemCellBiol, 2005,37 (8): 1709 ~ 1726) report Pterostilbene can be induced the remarkable apoptosis of the sick cell of mouth blood of multiple medicines and BCR-ABL expression, and normal cell is not almost affected such as TolomeoM.
Green-tea extract is the active component extracting from green tea blade, mainly comprises Tea Polyphenols (catechin), Epigallo-catechin gallate (EGCG) (EGCG) etc. Epigallo-catechin gallate (EGCG) (EGCG) is the main activity of green tea and water-soluble components, it is the highest component of content in catechin, account for the 9%-13% of green tea gross weight, because there is special stereochemical structure, EGCG has very strong antioxidation activity, is taking on important role aspect anticancer and angiocardiopathy. In addition, it is also as the reversal agent of multi-drug resistance of the tumor, can improve the sensitiveness of cancer cell to chemotherapy and alleviate the toxicity to heart.
Semen Coicis extract extracts from the kind benevolence of Job's tears drying and ripening, and main active comprises ester class, unsaturated fatty acids, carbohydrate and lactams etc., has invigorating spleen to remove dampness, removes effect of numbness antidiarrheal, clearing away heat and eliminating pus. Wherein, ester class is the first found composition with antitumor activity, is also report chemical composition of greatest concern at most. Analyze by TLC method, GC and GC-MS method, think in coix seed anticancer active constituent that oleaginous composition is triglycerides, and to record average molecular mass be 870.97, fatty acid residue is hexadecanoic acid, octadecanoic acid, 18 carbon monoenoic acids, octadecadienoic acid. The acetone extract of coix seed has inhibitory action to mice-transplanted tumor, and active component is wherein some acid fragments. Utilize gas-liquid phase chromatography analysis, confirm that these active components are palmitic acid, stearic acid, oleic acid and linoleic acid. In Japan, coix seed is mainly used in the production of health food, as seed of Jobs tears tea etc. The effects such as modern pharmacology research shows, that coix seed and chemical active ingredient thereof have is antitumor, improve immunity, hypoglycemic.
Resveratrol is by promoting apoptosis of tumor cells, induced tumor Cell Differentiation, retardance cell cycle, disturb Signal Transduction path, suppressing performance prevention and the antitumor actions such as tumor vessel generation, but because its structural stability is poor, and in blood the holdup time shorter, therefore its separately application be restricted.
Summary of the invention
The object of the invention is to overcome the deficiencies in the prior art, a kind of anti-tumor compositions that contains resveratrol is provided.
Second object of the present invention is to provide a kind of preparation method of the anti-tumor compositions containing resveratrol.
Containing an anti-tumor compositions for resveratrol, comprise by weight following component: resveratrol 60-200 part, Pterostilbene 30-150 part, green-tea extract 50-220 part, Semen Coicis extract 100-280 part.
Preferred: resveratrol 80-160 part, Pterostilbene 50-120 part, green-tea extract 80-180 part, Semen Coicis extract 120-240 part.
A preparation method for the anti-tumor compositions that contains resveratrol, comprises the steps:
(1) take by weight: resveratrol 60-200 part, Pterostilbene 30-150 part, green-tea extract 50-220 part, Semen Coicis extract 100-280 part
(2) mix, add the acceptable auxiliary material of pharmacy, make capsule, granule or tablet.
Preferred: resveratrol 80-160 part, Pterostilbene 50-120 part, green-tea extract 80-180 part, Semen Coicis extract 120-240 part.
Advantage of the present invention:
When the present invention has overcome independent use resveratrol, in vivo action time short shortcoming, Pterostilbene, green-tea extract and Semen Coicis extract are added, give full play to the synergy between component, the good stability of composition, long action time, has improved curative effect, there is antitumor action, and safe without toxic side effect.
Detailed description of the invention
Raw material of the present invention:
Resveratrol (content 90%-98%), Pterostilbene (content 90%-98%), green-tea extract (EGCG content is greater than 30%), Semen Coicis extract (content 10:1).
Resveratrol, Pterostilbene, green-tea extract, Semen Coicis extract are purchased from Tianjin Ubasichealth Nutrition Co., Ltd..
Disclosing of the source of above-mentioned raw materials, only in order to be that those skilled in the art can understand the present invention better, but the present invention is not done to any restriction, the above-mentioned raw materials that meets other sources of resveratrol, Pterostilbene, green-tea extract, Semen Coicis extract content requirement may be used to the present invention.
Resveratrol in each embodiment and pharmacodynamics test (content 98%), Pterostilbene (content 99%), green-tea extract (EGCG content 50%), Semen Coicis extract (content 10:1)
Embodiment 1
A preparation method who contains jervic alcohol for antineoplastic medicine composition, comprises the steps:
(1) take: resveratrol 60g; Pterostilbene 30g; Green-tea extract 50g; Semen Coicis extract 100g;
(2) mix, add lactose 100g, dextrin 180g, dolomol 20g, the ethanol water that volumetric concentration is 60% is particle processed in right amount, is pressed into 1000, tablet.
Embodiment 2
A preparation method who contains jervic alcohol for antineoplastic medicine composition, comprises the steps:
(1) take: resveratrol 80g; Pterostilbene 50g; Green-tea extract 80g; Semen Coicis extract 120g;
(2) mix, add starch 270g, dolomol 30g, mixes, and makes 1000 of capsules.
Embodiment 3
A preparation method for the anti-tumor compositions that contains resveratrol, comprises the steps:
(1) take: resveratrol 100g, Pterostilbene 60g, green-tea extract 100g, Semen Coicis extract 140g;
(2) mix, add starch 100g, dextrin 180g, dolomol 20g, evenly, the ethanol water that is 60% by volumetric concentration is particle processed in right amount.
Embodiment 4
A preparation method for the anti-tumor compositions that contains resveratrol, comprises the steps:
(1) take: resveratrol 140g; Pterostilbene 90g; Green-tea extract 140g; Semen Coicis extract 180g;
(2) mix, add lactose 100g, dextrin 170g, dolomol 30g, mixes, the ethanol water academic title granule that is 60% by volumetric concentration.
Embodiment 5
A preparation method for the anti-tumor compositions that contains resveratrol, comprises the steps:
(1) take: resveratrol 160g; Pterostilbene 120g; Green-tea extract 180g; Semen Coicis extract 240g;
(2) mix, add lactose 120g, dextrin 150g, dolomol 30g, mixes, the ethanol water granulation agent that is 60% by volumetric concentration.
Embodiment 6
A preparation method for the anti-tumor compositions that contains resveratrol, comprises the steps:
(1) take: resveratrol 200g; Pterostilbene 150g; Green-tea extract 220g; Semen Coicis extract 280g;
(2) mix, add lactose 100g, dextrin 180g, dolomol 20g, mixes, the ethanol water granulation agent that is 60% by volumetric concentration.
Pharmacodynamics test:
1, material and method
1.1 experiment product: active compound part in resveratrol raw material, Pterostilbene raw material, green-tea extract, Semen Coicis extract and various embodiments of the present invention (6 embodiment are and comprise auxiliary material part)
1.2 animals used as test and experimental cell: C57 mouse and B16 mouse melanoma cell line F1
1.3 experiment grouping and medications
Experiment grouping:
Blank group (group 1)
Resveratrol folk prescription group (group 2)
Pterostilbene folk prescription group group (group 3)
Green-tea extract folk prescription group (group 4)
Semen Coicis extract folk prescription group (group 5)
The active compound group (being followed successively by group 6, group 7, group 8, group 9, group 10 and group 11) of embodiment 1-6
Medication:
Blank group does not give any medicine; The dosage of resveratrol folk prescription group, Pterostilbene folk prescription group, green-tea extract folk prescription group, Semen Coicis extract folk prescription group is 10mg/kg; Test group 5-10 group is 10mg/kg by the dosage of the active compound of embodiment 1-6 (composition that step (1) obtains mixes) respectively
2, experimental technique:
Taking C57 mouse as experimental subjects, get the go down to posterity tumor-bearing mice of inoculated tumour about 30 days, de-neck mortar is put to death mouse, dorsal position is fixed on dissection plate, and routine disinfection skin is cut off skin gently in tumor locus, peel off knurl body, reject coating, avoid location of necrosis, cut well-grown flesh of fish shape pale pink tumor tissue, after be cut into 2mm3 size chunky shape, mechanical milling method continues digestion, SPSS is made homogenate, 200 order cell mesh screens filter, and obtain oncocyte suspension. The cell suspension that takes a morsel, 4% tongue is expected blue dyeing, under microscope, counts oncocyte. Physiological saline regulates 1 × 107/ml of cell concentration. This cell suspension inoculation is subcutaneous in C57 mouse right lower extremity veutro, only go down to posterity inoculation 3-5 at every turn. Only select the 3-5 of each inoculation, amount to 330, then be divided at random 11 groups, wherein feed and give resveratrol, Pterostilbene, green-tea extract, Semen Coicis extract respectively for four groups, feed successively respectively the active compound (not comprising auxiliary material) that gives embodiment 1-6, remain one group and do not carry out as a control group administration for other six groups, within after administration 7 days, start to observe, put to death animal every 4 days, strip knurl body and observe the growing state of tumour, and carry out the measurement of tumorous size
3, experimental result: table 1
Table 1: resveratrol composition check melanin tumour result of the test
Result shows, resveratrol folk prescription, Pterostilbene folk prescription, green-tea extract folk prescription, Semen Coicis extract folk prescription and composition of the present invention all have the effect of the growth that suppresses pernicious melanin tumour transplatation thing, four folk prescriptions are approximately 50% to the inhibiting rate of melanin tumor growth, and composition of the present invention is approximately 80% to the inhibiting rate of melanin tumor growth.
Although, above use general explanation, detailed description of the invention and test, the present invention is described in detail, on basis of the present invention, can make some modifications or improvements it, and this will be apparent to those skilled in the art. Therefore, these modifications or improvements without departing from theon the basis of the spirit of the present invention, all belong to the scope of protection of present invention.
Claims (4)
1. containing an anti-tumor compositions for resveratrol, it is characterized in that, in described composition, composition is by weight: resveratrol 60-200 part, Pterostilbene 30-150 part, green-tea extract 50-220 part, Semen Coicis extract 100-280 part; Described anti-tumor compositions is for antitumor colon cancer, lung cancer, black cancer, prostate cancer, liver cancer, kidney, cancer of the stomach, sarcoma, neuroglia cancer, cancer of pancreas, oophoroma, the breast cancer of including but not limited to.
2. composition according to claim 1, is characterized in that, resveratrol 80-160 part, Pterostilbene 50-120 part, green-tea extract 80-180 part, Semen Coicis extract 120-240 part in described composition.
3. a preparation method who contains the anti-apolexis composition of resveratrol, is characterized in that comprising the steps:
(1) take by weight: resveratrol 60-300 part; Pterostilbene 30-150 part; Green-tea extract 50-220 part; Semen Coicis extract 100-280 part;
(2) mix, add the acceptable auxiliary material of pharmacy, make capsule, granule or tablet.
4. the preparation method of a kind of anti-tumor compositions that contains resveratrol according to claim 3, is characterized in that described resveratrol 80-160 part, Pterostilbene 50-120 part, green-tea extract 80-180 part, Semen Coicis extract 120-240 part.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2018210224A1 (en) * | 2017-05-15 | 2018-11-22 | 王晓辉 | Applications of triptolide and derivative thereof in preparing medicament for treating and/or preventing lung-damaging diseases |
| CN110604763A (en) * | 2018-06-14 | 2019-12-24 | 香港科技大学深圳研究院 | Pharmaceutical application of total extract of polygonum cuspidatum, polydatin or resveratrol |
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| CN103349711A (en) * | 2013-07-29 | 2013-10-16 | 天津尖峰弗兰德医药科技发展有限公司 | Anti-aging combination with resveratrol and preparation method thereof |
| CN103462944A (en) * | 2013-09-13 | 2013-12-25 | 天津市益倍建生物技术有限公司 | Composition containing resveratrol and pterostilbene and preparation containing composition |
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| CN101804175A (en) * | 2010-03-10 | 2010-08-18 | 滕树财 | Anti-cancer Chinese medicinal powder and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018210224A1 (en) * | 2017-05-15 | 2018-11-22 | 王晓辉 | Applications of triptolide and derivative thereof in preparing medicament for treating and/or preventing lung-damaging diseases |
| CN110604763A (en) * | 2018-06-14 | 2019-12-24 | 香港科技大学深圳研究院 | Pharmaceutical application of total extract of polygonum cuspidatum, polydatin or resveratrol |
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