CN107028930A - A kind of antiprostate cancer composition and application thereof - Google Patents

A kind of antiprostate cancer composition and application thereof Download PDF

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Publication number
CN107028930A
CN107028930A CN201710298783.XA CN201710298783A CN107028930A CN 107028930 A CN107028930 A CN 107028930A CN 201710298783 A CN201710298783 A CN 201710298783A CN 107028930 A CN107028930 A CN 107028930A
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China
Prior art keywords
prostate cancer
pharmaceutical composition
inonotus obliquus
edible fungus
polysaccharide
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CN201710298783.XA
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CN107028930B (en
Inventor
田河
张智慧
孟扬
白吉祥
张高坤
周辉华
何春艳
何光梅
邸彦橙
闫本纯
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Mudanjiang Medical University
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Mudanjiang Medical University
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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
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • 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
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to a kind of medical composition and its use for anti-prostate cancer, described pharmaceutical composition includes inonotus obliquus and optional edible fungus polysaccharide, and the edible fungus polysaccharide is selected from:One or more in lentinan, pachymaran, GL-B or flammulina velutipes.Pharmaceutical composition of the present invention can effectively suppress propagation and the migration of prostate gland cancer cell, the immunity of patient itself can not only be strengthened after addition edible fungus polysaccharide, the side effect that patients with prostate cancer chemotherapy is brought is reduced, the activity of inonotus obliquus anti-prostate cancer can also be further enhanced, the effect of collaboration anti-prostate cancer is shown.

Description

A kind of antiprostate cancer composition and application thereof
Technical field
The invention belongs to drug field, in particular it relates to a kind of medical composition and its use of anti-prostate cancer.
Background technology
Prostate cancer is the epithelial malignancy for betiding prostate, multiple to be born in more than 45 years old the elderly, is complete The second largest male malignancy of ball, in recent years the incidence of disease of China's prostate cancer steeply rise, it is strong as China's middle-aging male The significant threat of health.
Inonotus obliquus, also known as Polyporus picipes, CHAGA, are a kind of domestomycetes for being grown in frigid zone, are mainly distributed in China In the big Xiaoxinanlin Mountains and Changbaishan area, the tradition among the people for generally thering is edible Inonotus obliquus to prevent and treat a variety of diseases.Modern study table Bright Inonotus obliquus includes tens kinds of chemical compositions, mainly including steroid compound, aromatic compound, aliphatic compound Thing, triterpene compound, lignan derivatives, alkaloid etc..Modern pharmacology research shows that Inonotus obliquus has a variety of pharmacology Activity, is specifically included:(1) antitumor activity, existing document report Inonotus obliquus has anti-liver cancer and anti-, stomach cancer, lung cancer, cervical carcinoma Activity;(2) antiviral activity, the alcohol composite extract for having document report Inonotus obliquus has anti HIV-1 virus, the work of influenza virus Property;(3) diabetes are treated, the water extract of Inonotus obliquus has hypoglycemic activity;(4) hypotensive, Adjust-blood lipid;(5) enhancing is exempted from Epidemic disease power;(6) it is anti-oxidant;(7) it is anti-ageing to wait for a long time.
The present invention is further screened to its anti-tumor active ingredient, therefrom sieved on the Research foundation of existing Inonotus obliquus Choosing obtained it is a kind of there is the monomeric compound of excellent inhibition to prostate cancer, and pass through its compounding with other compounds Research, thus obtain it is a kind of can effective anti-prostate cancer pharmaceutical composition.
The content of the invention
It is an object of the present invention to provide a kind of pharmaceutical composition of anti-prostate cancer, described pharmaceutical composition includes birch Obliquus and pharmaceutically acceptable carrier.
It is preferred that described pharmaceutical composition using inonotus obliquus as sole active agent.
Further, described pharmaceutical composition also includes edible fungus polysaccharide, it is preferred that the edible fungus polysaccharide choosing From:Lentinan (being purchased from Xi'an Bai Chuan biotechnologies Co., Ltd), pachymaran (have purchased from Xi'an Bai Chuan biotechnologies Limit responsible company), GL-B (be purchased from Xi'an Bai Chuan biotechnologies Co., Ltd) or flammulina velutipes (be purchased from Fu Jianhui Damp bio tech ltd) in one or more.
The weight ratio of inonotus obliquus and edible fungus polysaccharide is in pharmaceutical composition of the present invention:1-3:5-10, Preferably:1-2:6-8, more have choosing for 1:8.
The pharmaceutical composition of anti-prostate cancer of the present invention can be prepared into combination of oral medication according to this area conventional method, The combination of oral medication is selected from capsule, tablet or granule, wherein the pharmaceutically acceptable carrier is selected from:Filling One or more in agent, adhesive, disintegrant or lubricant, it is preferred that the filler be selected from starch, dextrin, lactose or Microcrystalline cellulose, described adhesive is selected from:Cellulose derivative, pregelatinized starch, PVP, the disintegrant are selected from:Carboxylic first Base sodium starch, Ac-Di-Sol, PVPP, the lubricant are selected from:Talcum powder, magnesium stearate or micro mist silicon Glue, it is preferred that the cellulose derivative is selected from:Methylcellulose, hydroxypropyl cellulose, sodium carboxymethylcellulose or ethyl are fine Dimension element.
It is a further object to provide purposes of the inonotus obliquus in antiprostate cancer is prepared.
Anti- prostatitis is being prepared it is also another object of the present invention to provide the composition of inonotus obliquus and edible fungus polysaccharide Purposes in gland cancer medicine, it is preferred that the edible fungus polysaccharide is selected from:Lentinan, pachymaran, GL-B or acupuncture needle One or more in mushroom polysaccharide.
Beneficial effect
Present invention screening in the complicated composition of Inonotus obliquus is obtained substantially suppressing prostate gland cancer cell propagation and migrated Monomeric compound inonotus obliquus, so as to obtain a kind of pharmaceutical composition with clear and definite anti-prostate cancer effect, pass through Show with the composition research of other compounds, after inonotus obliquus with edible fungus polysaccharide by compounding, can not only play food Strengthen immunity of organisms with fungi polysaccharide, reduce the intrinsic effect for the side effect that chemotherapy is brought, birch can also be significantly increased brown The anti-prostate cancer activity of pore fungi element, shows obvious synergistic function, so as to further provide before a kind of resist The more excellent pharmaceutical composition of row gland cancer effect.
Embodiment
The present invention is described below in more detail to contribute to the understanding of the present invention.
It should be appreciated that the term or word that use in the specification and in the claims are not construed as having The implication limited in dictionary, and be interpreted as on the basis of following principle having and its implication one in the context of the present invention The implication of cause:The concept of term can be limited suitably by inventor for the best illustration to the present invention.
Embodiment 1:A kind of tablet of anti-prostate cancer
The tablet of the anti-prostate cancer is prepared according to following steps:
(1) weigh and crushed respectively after each composition by recipe quantity, cross 80 mesh sieves;
(2) inonotus obliquus of recipe quantity, lentinan, GL-B, microcrystalline cellulose, pregelatinized starch are put into height Fast wet granulator, adds suitable quantity of water granulation, crosses 20 mesh sieve whole grains after drying, adds the PVPP and stearic acid of recipe quantity Magnesium, well mixed rear tabletting produces the tablet of anti-prostate cancer of the present invention.
Embodiment 2:A kind of capsule of anti-prostate cancer
The anti-prostate cancer capsule, is prepared in accordance with the following steps:
(1) weigh and crushed respectively after each composition by recipe quantity, cross 100 mesh sieves;
(2) inonotus obliquus of recipe quantity, lentinan, GL-B, microcrystalline cellulose, pregelatinized starch are put into height Fast wet granulator, adds suitable quantity of water granulation, and 20 mesh sieve whole grains are crossed after drying;
(3) step (2) particle in addition recipe quantity magnesium stearate after be well mixed;
(4) anti-prostate cancer capsule of the present invention is produced in gelatine capsule shell by particles filled obtained by step (3).
Effect example 1:The influence bred to prostate gland cancer cell
1.1 Experimental agents
(1) blank group:The culture medium of serum-free 1640;
(2) inonotus obliquus group:The addition culture medium of serum-free 1640 is configured to the suspension that content is 5%;
(3) polysaccharide group:According to GL-B, lentinan according to 1:1 proportional arrangement is trained into 20% serum-free 1640 Support based sols;
(4) Inonotus obliquus extract group:Inonotus obliquus extract is weighed, the culture medium of serum-free 1640 for being configured to 5% is mixed Suspension;
(5) complex group:Weigh inonotus obliquus, GL-B and lentinan, be configured to containing 2% inonotus obliquus, The culture medium of serum-free 1640 of 20% polysaccharide is combined suspension.
1.2 experimental method
Take the logarithm the Human Prostate Cancer Cells (PC-3) in growth period, with 5 × 103The density in/hole is inoculated in 96 orifice plates, per hole 200 μ L, addition is put into 37 DEG C and contains 5%CO after 1640 culture mediums containing 10% hyclone2Incubator in cultivate 24 hours.
96 orifice plates set up blank group, inonotus obliquus group, polysaccharide group, Inonotus obliquus extract group, complex group, every group 10 separately Multiple holes, each group addition relative medicine, wherein the blank group addition culture medium of serum-free 1640, inonotus obliquus group final concentration of 1%, Inonotus obliquus is final concentration of in polysaccharide group final concentration of 10%, Inonotus obliquus extract group final concentration of 2%, complex group 0.5%, final concentration of the 5% of polysaccharide, continue to cultivate after 48h, continue to cultivate after 4h, supernatant discarding after addition MTT solution, per hole Add after DMSO 150 μ L, fully shaking 10min, 570nm absorbances are determined using ELIASA, calculate each group inhibiting rate, tool Body result is referring to table 1.
Inhibiting rate (%)=(control group-sample sets) control group × 100%
The experimental result of table 1 shows complex polysaccharide, inonotus obliquus and the brown hole of birch that GL-B is constituted with lentinan Fungus extract shows the activity of certain suppression prostate cancer cell proliferation, and wherein inonotus obliquus suppresses human prostate Cancer cell multiplication activity highest, hence it is evident that higher than Inonotus obliquus extract group, show that inonotus obliquus has before excellent suppression people Although the activity of row adenocarcinoma cell propagation, polysaccharide group also show the proliferation activity of certain suppression Human Prostate Cancer Cells, but Although inonotus obliquus is reduced with inonotus obliquus consumption after polysaccharide group compounding, propagation of the complex group to Human Prostate Cancer Cells Inhibitory activity is but significantly improved, so as to show that inonotus obliquus has the activity for cooperateing with anti-prostate cancer with edible fungus polysaccharide.
Table 1, the influence bred to PC-3 cells
Effect example 2:Influence to migration of prostate cancer cells.
2.1 Experimental agents
(1) blank group:The culture medium of serum-free 1640;
(2) inonotus obliquus group:The addition culture medium of serum-free 1640 is configured to the suspension that content is 5%;
(3) polysaccharide group:According to GL-B, lentinan according to 1:1 proportional arrangement is trained into 20% serum-free 1640 Support based sols;
(4) Inonotus obliquus extract group:Inonotus obliquus extract is weighed, the culture medium of serum-free 1640 for being configured to 5% is mixed Suspension;
(5) complex group:Weigh inonotus obliquus, GL-B and lentinan, be configured to containing 2% inonotus obliquus, The culture medium of serum-free 1640 of 20% polysaccharide is combined suspension.
2.2 experimental method
Take the logarithm the Human Prostate Cancer Cells (PC-3) in growth period, add 24 orifice plates, contain 5%CO in 37 DEG C2Incubator Middle culture, 1640 culture mediums of the addition containing 10% hyclone, when cell fusion 80%-90%, is replaced by free serum culture Base, continues to cultivate 12 hours, with 100 μ L liquid transfer gun heads along each bore dia cut of 24 orifice plates, washes cell twice using PBS, discard After PBS, add after 1640 culture mediums of the equivalent containing 10% hyclone, cut area relative distance D1 is recorded under mirror.24 orifice plates point If blank group, inonotus obliquus group, polysaccharide group, Inonotus obliquus extract group, complex group, every group of 4 multiple holes, each group addition is corresponding Medicine, wherein blank group add pure water, inonotus obliquus group final concentration of 1%, polysaccharide group final concentration of 10%, Inonotus obliquus Inonotus obliquus final concentration of 0.5% in extract group final concentration of 2%, complex group, final concentration of the 5% of polysaccharide, continue to train Support after 48h, cut area relative distance D2 is measured under mirror, calculate displacement D3 of the cell to region of causing injury.Calculate each group migration Inhibiting rate, concrete outcome is referring to table 2.
Inhibition of metastasis rate (%)=(control group-sample sets) control group × 100%
Table 2, the influence to PC-3 cell migrations
Note:Compared with blank group:*P<0.05,**P<0.01.
The experimental result of table 2 shows that single inonotus obliquus has the effect for suppressing Human Prostate Cancer Cells migration, Although Inonotus obliquus extract group also show the effect of certain suppression Human Prostate Cancer Cells migration, but inhibition is not Substantially, and complex polysaccharide that GL-B and lentinan are constituted does not show the effect for suppressing migration of prostate cancer cells then, Its final cell migration distance is even also longer than blank group.By inonotus obliquus and GL-B and being combined that lentinan is constituted Group, the effect for suppressing Human Prostate Cancer Cells migration is the most excellent, hence it is evident that higher than single inonotus obliquus group, so that show, Can be bright after being compounded without the GL-B, lentinan and inonotus obliquus group that suppress Human Prostate Cancer Cells migration effect The Human Prostate Cancer Cells inhibition of metastasis effect of aobvious enhancing inonotus obliquus.

Claims (10)

1. a kind of pharmaceutical composition for anti-prostate cancer, it is characterised in that including inonotus obliquus and pharmaceutically acceptable Carrier.
2. the pharmaceutical composition of anti-prostate cancer according to claim 1, it is characterised in that described pharmaceutical composition is with birch Obliquus is sole active agent.
3. the pharmaceutical composition of anti-prostate cancer according to claim 1, it is characterised in that described pharmaceutical composition is also wrapped Include edible fungus polysaccharide.
4. the pharmaceutical composition of anti-prostate cancer according to claim 3, it is characterised in that the edible fungus polysaccharide choosing From:One or more in lentinan, pachymaran, GL-B or flammulina velutipes.
5. the pharmaceutical composition of anti-prostate cancer according to claim 4, it is characterised in that the inonotus obliquus and food It is with the weight ratio of fungi polysaccharide:1-3:5-10, preferably:1-2:6-8, more have choosing for 1:8.
6. the pharmaceutical composition of the anti-prostate cancer according to claim 1, any one of 3-5, it is characterised in that the medicine Composition is combination of oral medication.
7. the pharmaceutical composition of anti-prostate cancer according to claim 6, it is characterised in that the combination of oral medication Selected from capsule, tablet or granule.
8. the pharmaceutical composition of the anti-prostate cancer according to claim any one of 1-7, it is characterised in that it is described pharmaceutically Acceptable carrier is selected from:One or more in filler, adhesive, disintegrant or lubricant, it is preferred that the filler Selected from starch, dextrin, lactose or microcrystalline cellulose, described adhesive is selected from:Cellulose derivative, pregelatinized starch, PVP, The disintegrant is selected from:Sodium carboxymethyl starch, Ac-Di-Sol, PVPP, the lubricant are selected from:Talcum Powder, magnesium stearate or superfine silica gel powder, it is preferred that the cellulose derivative is selected from:Methylcellulose, hydroxypropyl cellulose, carboxylic Sodium carboxymethylcellulose pyce or ethyl cellulose.
9. purposes of the inonotus obliquus in antiprostate cancer is prepared.
10. purposes of the composition of inonotus obliquus and edible fungus polysaccharide in antiprostate cancer is prepared, it is preferred that institute Edible fungus polysaccharide is stated to be selected from:One or more in lentinan, pachymaran, GL-B or flammulina velutipes.
CN201710298783.XA 2017-04-27 2017-04-27 A kind of antiprostate cancer composition and application thereof Expired - Fee Related CN107028930B (en)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101391958A (en) * 2008-11-10 2009-03-25 马宏达 Extraction method of medicinal fungus inonotus obliquus component

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101391958A (en) * 2008-11-10 2009-03-25 马宏达 Extraction method of medicinal fungus inonotus obliquus component

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
ZHONG XIU-HONG ET AL: "Progress of Research on Inonotus Obliquus", 《CHIN J INTEGR MED》 *
刘立萍: "灵芝多糖的药理学作用(摘要)", 《第七次临床中药学术研讨会论文集》 *
胡静娜: "噻唑蓝法测定香菇多糖体外对癌细胞毒作用", 《医药导报》 *

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