CN103800341A - Combined medicine for preventing and treating tumors - Google Patents
Combined medicine for preventing and treating tumors Download PDFInfo
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- CN103800341A CN103800341A CN201210455705.3A CN201210455705A CN103800341A CN 103800341 A CN103800341 A CN 103800341A CN 201210455705 A CN201210455705 A CN 201210455705A CN 103800341 A CN103800341 A CN 103800341A
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Abstract
The invention provides a combined medicine for preventing and treating tumors, which has the effects of reducing side effects of chemotherapy and radiotherapy. The combined medicine for preventing and treating tumors comprises cucurbitacine and at least one of coenzyme Q10 and taurine, wherein the weight ratio of cucurbitacine to coenzyme Q10 is 1:(0.1-10000); the weight ratio of cucurbitacine to taurine is 1:(0.1-10000). When the medicine is formed by cucurbitacine, coenzyme Q10 and taurine, the weight ratio of cucurbitacine to coenzyme Q10 to taurine is 1:(0.1-10000):(0.1-10000). The dosage is also provided. The combined medicine can be processed into tablets, capsules, granules, powder, patches, ointment, suspension, syrup, sustained-release preparations, nano-particles or emulsion and other preparations with pharmaceutically acceptable carriers commonly or respectively. The combined medicine can be used in chronic hepatitis treatment and prevention and treatment of cancers in clinical application.
Description
Technical field
The invention belongs to medical technical field, relate to the combination medicine for anti-curing oncoma, relate in particular to the combination medicine for anti-curing oncoma containing cucurbitacin.
Background technology
[0002]in recent years, cancer has exceeded cardiovascular and cerebrovascular disease becomes the No.1 killer who threatens human health.Show approximately have every year at present more than 700 ten thousand people to die from cancer in the whole world according to World Health Organization's statistical data, in average every 8 deaths in the whole world, just have 1 people to die from cancer.This tissue expects the annual cancer mortality number in the year two thousand thirty whole world may be doubled on present basis, reach 1,700 ten thousand.Therefore, seek effectively to prevent and treat the strategy of tumorigenesis, transfer and recurrence extremely urgent.
Chemotherapy is as existing more than the 60 year history of conventional means of clinical anticancer.Although chemotherapy in cure diseases, improve Resection Rate and survival rate, improve aspect life quality and brought into play larger effect, the problem of its existence also can not be ignored.Most of chemotherapeutics lack desirable selectivity, cause " right and wrong are unclear ", " failing to differentiate between the enemy and ourselves ", in killing tumor cell, also killed and wounded human normal cell's (as cardiac toxicity of the inhibition of medulla hematopoietic system, liver cell infringement, the irreversible and property accumulated etc.), cause patient body function to be subject to infringement in various degree and make patient's endurable, force interrupted the normal course for the treatment of, greatly reduce the curative effect of medicine; In addition, chemotherapeutics exists and very easily produces drug resistance and also make its application have certain limitation.
Therefore, how in keeping and improving antitumor drug curative effect, reduce its treatment cost, expansion is suitable for crowd, reduces toxicity, improves compliance and toleration etc. is the emphasis that antitumor drug is researched and developed.
Cucurbitacine composition is the highly oxidized tetracyclic triterpenoid of a class extracting from plant, has found so far kind more than 40.This constituents majority is present in cucurbitaceous plant, in the higher plants such as Cruciferae, Scrophulariaceae, Begoniaceae, Elaeocarpaceae, Datiscaceceae and some macro fungis, is also found.At present, the cucurbitacin that China's approval is produced is again Cucurbitacine, for Chinese medicine muskmelon pedicel (another name: Pedicellus Melo) extract, mainly containing compositions such as Cucurbitacin B, E, in existing extract, Cucurbitacin B content is more than 60%, and its quality standard records in China's ministry standard.
Domestic cucurbitacin is mainly used in chronic hepatitis and primary liver cancer, each 0.1～0.3 mg that is grown up, and 3 times on the 1st, dosage must not arbitrarily strengthen, and maximum dose is 0.6 mg/ time.The cucurbitacin pharmacological action of foreign literature report mainly contains: cell in vitro poison and antitumor, improve immunity, anti-hepatitis, anti-environmental chemical carcinogen, affect the transduction of cell ask signal, stimulating gastrointestinal moves, strengthens capillary permeability, improves microcirculation etc.
Coenzyme Q compounds is extensive in distributed in nature, is present in many animals, plant and microorganism, and the coenzyme Q kind of having found at present comprises that CoQ1 is to CoQ1 3.Maximum in human body is coenzyme Q10, and nineteen fifty-seven, Britain Morton professor separates and obtains coenzyme Q10 from suffer from the rat liver of hypovitaminosis A, and is referred to as ubiquinone.
The iso-amylene structure of the quinoid structure of coenzyme Q10 and side chain, has determined its critical function in organism.It is the important hydrogen carrier in respiratory chain, is biological cell energy forming element; It also has antioxidation and controls the function of flow of oxygen in cell; Cellular metabolism activator and nonspecific immunity strengthening agent; It can be the essential energy of cells survival food conversion, makes cell keep optimum state, protection biofilm structure integrity; Improve organic immunity.Aspect medicinal: be mainly used at present the adjuvant drug of cardiovascular disease, acute, chronic hepatitis and cancer, the neurodegenerative diseases such as acquired immune deficiency syndrome (AIDS), diabetes, Parkinson's disease and mitochondrial disease are had to significant auxiliary treatment.
Taurine, claims again 2-aminoethyl sulfonic acid, the earliest by separating in Calculus Bovis, therefore gain the name.It is a kind of nonprotein amino acid, does not participate in the biosynthesis of body internal protein, but closely related with the metabolism of cystine, cysteine.Its physiological function is extensive, mainly contain promote infant brain tissue and intelligent development, raising nerve conduction and visual function, inhibition platelet aggregation, reduce blood fat, keep human normal blood pressure, prevent arteriosclerosis, arrhythmia, reduction Blood Cholesterol content, treatment heart failure, affect lipid absorption, improve endocrinosity, strengthen human body specificity and non-specific immunity, do not rely on the function that increases the hypoglycemic activity of insulin, suppress cataractous and develop, improve to remember, the effect such as calmness, analgesia, antiinflammatory.
Summary of the invention
The object of this invention is to provide a kind of combination medicine for anti-curing oncoma and medical usage thereof.
A kind of combination medicine for anti-curing oncoma provided by the present invention is made up of cucurbitacin and coenzyme Q10 and/or taurine.
In the time that a kind of combination medicine for anti-curing oncoma provided by the present invention is made up of cucurbitacin and coenzyme Q10, the weight ratio of cucurbitacin and coenzyme Q10 is 1:0.1-1000, as preferably, the weight ratio of cucurbitacin and coenzyme Q10 is 1:1-1000, as more preferably, the weight ratio of cucurbitacin and coenzyme Q10 is 1:5-100.
In the time that a kind of combination medicine for anti-curing oncoma provided by the present invention is made up of cucurbitacin and taurine; the weight ratio of cucurbitacin and taurine is 1:0.1-1000; as preferably; the weight ratio of cucurbitacin and taurine is 1:1-1000; as more preferably, the weight ratio of cucurbitacin and taurine is 1:5-100.
In the time that a kind of combination medicine for anti-curing oncoma provided by the present invention is made up of cucurbitacin, coenzyme Q10 and taurine; the weight ratio of cucurbitacin, coenzyme Q10 and taurine is 1:0.1-1000:0.1-1000; as preferably; the weight ratio of cucurbitacin, coenzyme Q10 and taurine is 1:1-1000: 1-1000; as more preferably, the weight ratio of cucurbitacin, coenzyme Q10 and taurine is 1:5-100: 5-100.
A kind of combination medicine for anti-curing oncoma provided by the present invention, wherein cucurbitacin comprises cucurbitacin A, B, C, D, E, I, Q, S, two hydrogen cucurbitacin A, B, C, D, E, I, Q, S and isocucurbitacin A, B, C, D, E, I, Q, S, a kind of or two or more in glucoside material corresponding to various cucurbitacins.
The medical usage of a kind of combination medicine for anti-curing oncoma provided by the present invention, the described combination medicine for anti-curing oncoma can be made tablet, capsule, granule, powder, patch, ointment, suspensoid, syrup, oral liquid, patch, aerosol, suppository, nasal drop or injection jointly or respectively with acceptable carrier pharmaceutically, and corresponding controlled release agent; Also can make clathrate, liposome, microsphere, nanoparticle or Emulsion, for cavity/canal drug administration, external, oral, injection.
The medical usage of a kind of combination medicine for anti-curing oncoma provided by the present invention, it is characterized in that, the amount of the described each component of combination medicine for anti-curing oncoma, take mice oral administration Rapid Dose Calculation: cucurbitacin is as 0.001-15 mg/kg, as preferably, cucurbitacin is 0.01-10 mg/kg, and as more preferably, cucurbitacin is 0.1-5 mg/kg; Coenzyme Q10 is 1-15 000 mg/kg, and as preferably, coenzyme Q10 is 5-10000 mg/kg, and as more preferably, coenzyme Q10 is 50-1 000 mg/kg; Taurine is 1-2000 mg/kg, and as preferably, taurine is 10-1000mg/kg, and as more preferably, taurine is 50-1000 mg/kg, point 1-4 administration.
The medical usage of a kind of combination medicine for anti-curing oncoma provided by the present invention, it is characterized in that, the amount of the described each component of combination medicine for anti-curing oncoma, take health adult's Rapid Dose Calculation: cucurbitacin is as 0.01-10mg/d, as preferably, cucurbitacin is 0.1-8mg/kg, and as more preferably, cucurbitacin is 0.3-3mg/kg; Coenzyme Q10 is 1-3000 mg/d, and as preferably, coenzyme Q10 is 10-2000 mg/kg, and as more preferably, coenzyme Q10 is 30-1500 mg/kg; Taurine is 1-3000 mg/d, and as preferably, taurine is 10-2000 mg/kg, and as more preferably, taurine is 50-1500 mg/kg; Divide 1-4 administration.
The use that should be appreciated that a kind of combination medicine for anti-curing oncoma of the present invention comprises following two kinds of modes:
The one, a kind of combination medicine for anti-curing oncoma of the present invention is made respectively to independent preparation, the dosage form of two kinds of preparations can be identical, also can be different, can use successively in use, also can take simultaneously.Successively when administration, while giving n kind component before n-1 kind (n=3) component should also not lose its useful effect in vivo.
The 2nd, a kind of combination medicine for anti-curing oncoma of the present invention is made to single compound preparation, when use, take simultaneously.
Advantage of the present invention is: the present invention has good curative effect for the treatment of tumor, also can be used for the prevention of tumor, can be used for the treatment of chronic hepatitis.In keeping and improving antitumor drug curative effect, reduce treatment cost, expanded applicable crowd, toxicity is little, improved compliance and toleration.
Curative effect is better, there is no chemotherapy and radiocurable toxic and side effects.
The specific embodiment
For the present invention that understands who more removes, the present invention is described in further detail for the embodiment completing according to technical scheme of the present invention providing below in conjunction with inventor.
Be below the embodiment that the inventor provides, the present invention is not limited to these embodiment, and any pro forma accommodation that the present invention is made and/or change all will fall into protection domain of the present invention.
In the present invention, if not refer in particular to, described cucurbitacin comprises cucurbitacin A, B, C, D, E, I, Q, S, two hydrogen cucurbitacin A, B, C, D, E, I, Q, S and isocucurbitacin A, B, C, D, E, I, Q, S, a kind of or two or more in glucoside material corresponding to various cucurbitacins.All equipment and raw materials etc. all can be buied from market or the industry is conventional.
embodiment 1:cucurbitacin B (CuB) is combined anti-S180 function of tumor research with coenzyme Q10 (Q10)
Experimental program:
Get Kunming kind white mice, 18～22 grams of body weight, male, right fore oxter inoculation S180 tumor, treats that tumor piece grows into and is greater than 50 mm
2time, be divided at random 3 groups, 10 every group, each group gastric infusion respectively, scheme is as follows:
Dosage: CuB:B (5 mg/kg)
Q10: Q ( 50 mg/kg)
Administering mode: CuB Emulsion, B+Q multiple emulsion
Matched group: normal saline group
Experimental group: CuB group, CuB+Q10 group
Successive administration 14 days, in 24 hours, puts to death animal after last administration, gets tumor and weighs, and calculates tumour inhibiting rate.
Result: the tumour inhibiting rate of CuB group, CuB+Q10 group is respectively 48.6%, 56.8%.
Compared with CuB group, administering drug combinations group tumour inhibiting rate is higher, and mice is in good condition, does not show obvious toxic and side effects.
embodiment 2:cucurbitacin B (CuB) is combined anti-S180 function of tumor research with taurine (T)
Experimental program:
Get Kunming kind white mice, 18～22 grams of body weight, male, right fore oxter inoculation S180 tumor, treats that tumor piece grows into and is greater than 50 mm
2time, be divided at random 3 groups, 10 every group, each group gastric infusion respectively, scheme is as follows:
Dosage: CuB:5 mg/kg
T： 300 mg/kg
Administering mode: CuB Emulsion, CuB+T multiple emulsion
Matched group: normal saline group
Experimental group: CuB Emulsion group, CuB+T multiple emulsion group
Successive administration 14 days, in 24 hours, puts to death animal after last administration, gets tumor and weighs, and calculates tumour inhibiting rate.
Result: the tumour inhibiting rate of CuB Emulsion group and CuB+T multiple emulsion group is respectively 48.6% and 54.5%.
Compared with CuB Emulsion group, administering drug combinations group tumour inhibiting rate is higher, and mice is in good condition, does not show obvious toxic and side effects.
embodiment 3:cucurbitacin B (CuB) is combined anti-H22 function of tumor research with coenzyme Q10 (Q10)
Experimental program:
Get Kunming kind white mice, 18～22 grams of body weight, male, right fore oxter inoculation H22 tumor, treats that tumor piece grows into and is greater than 50 mm
2time, be divided at random 3 groups, 10 every group, each group gastric infusion respectively, scheme is as follows:
Dosage: CuB:B (5 mg/kg)
Q10: Q ( 50 mg/kg)
Administering mode: CuB Emulsion, B+Q multiple emulsion
Matched group: normal saline group
Experimental group: CuB group, CuB+Q10 group
Successive administration 14 days, in 24 hours, puts to death animal after last administration, gets tumor and weighs, and calculates tumour inhibiting rate.
Result: the tumour inhibiting rate of CuB group, CuB+Q10 group is respectively 43.5%, 53.6%.
Compared with CuB group, administering drug combinations group tumour inhibiting rate is higher, and mice is in good condition, does not show obvious toxic and side effects.
embodiment 4:cucurbitacin B (CuB) is combined anti-H22 function of tumor research with taurine (T)
Experimental program:
Get Kunming kind white mice, 18～22 grams of body weight, male, right fore oxter inoculation H22 tumor, treats that tumor piece grows into and is greater than 50 mm
2time, be divided at random 3 groups, 10 every group, each group gastric infusion respectively, scheme is as follows:
Dosage: CuB:5 mg/kg
T： 300 mg/kg
Administering mode: CuB Emulsion, CuB+T multiple emulsion
Matched group: normal saline group
Experimental group: CuB Emulsion group, CuB+T multiple emulsion group
Successive administration 14 days, in 24 hours, puts to death animal after last administration, gets tumor and weighs, and calculates tumour inhibiting rate.
Result: the tumour inhibiting rate of CuB Emulsion group and CuB+T multiple emulsion group is respectively 43.5% and 55.2%.
Compared with CuB Emulsion group, administering drug combinations group tumour inhibiting rate is higher, and mice is in good condition, does not show obvious toxic and side effects.
embodiment 5:cucurbatacin E (CuE) is combined anti-S180 function of tumor research with coenzyme Q10 (Q10)
Experimental program:
Get Kunming kind white mice, 18～22 grams of body weight, male, right fore oxter inoculation S180 tumor, treats that tumor piece grows into and is greater than 50 mm
2time, be divided at random 3 groups, 10 every group, each group gastric infusion respectively, scheme is as follows:
Dosage: CuE:E (5 mg/kg)
Q10: Q ( 50 mg/kg)
Administering mode: CuE Emulsion, E+Q multiple emulsion
Matched group: normal saline group
Experimental group: CuE group, CuE+Q10 group
Successive administration 14 days, in 24 hours, puts to death animal after last administration, gets tumor and weighs, and calculates tumour inhibiting rate.
Result: the tumour inhibiting rate of CuE group, CuE+Q10 group is respectively 44.5%, 53.6%.
Compared with CuE group, administering drug combinations group tumour inhibiting rate is higher, and mice is in good condition, does not show obvious toxic and side effects.
embodiment 6:cucurbatacin E (CuE) is combined anti-S180 function of tumor research with taurine (T)
Experimental program:
Get Kunming kind white mice, 18～22 grams of body weight, male, right fore oxter inoculation S180 tumor, treats that tumor piece grows into and is greater than 50 mm
2time, be divided at random 3 groups, 10 every group, each group gastric infusion respectively, scheme is as follows:
Dosage: CuE:5 mg/kg
T： 300 mg/kg
Administering mode: CuE Emulsion, CuE+T multiple emulsion
Matched group: normal saline group
Experimental group: CuE Emulsion group, CuE+T multiple emulsion group
Successive administration 14 days, in 24 hours, puts to death animal after last administration, gets tumor and weighs, and calculates tumour inhibiting rate.
Result: the tumour inhibiting rate of CuE Emulsion group and CuE+T multiple emulsion group is respectively 44.5% and 54.1%.
Compared with CuE Emulsion group, administering drug combinations group tumour inhibiting rate is higher, and mice is in good condition, does not show obvious toxic and side effects.
embodiment 7:cucurbitacin I (CuI) combines anti-H22 function of tumor research with coenzyme Q10 (Q10)
Experimental program:
Get Kunming kind white mice, 18～22 grams of body weight, male, right fore oxter inoculation H22 tumor, treats that tumor piece grows into and is greater than 50 mm
2time, be divided at random 3 groups, 10 every group, each group gastric infusion respectively, scheme is as follows:
Dosage: CuI:I (5 mg/kg)
Q10: Q ( 50 mg/kg)
Administering mode: CuI Emulsion, B+Q multiple emulsion
Matched group: normal saline group
Experimental group: CuI group, CuI+Q10 group
Successive administration 14 days, in 24 hours, puts to death animal after last administration, gets tumor and weighs, and calculates tumour inhibiting rate.
Result: the tumour inhibiting rate of CuI group, CuI+Q10 group is respectively 42.9%, 51.8%.
Compared with CuI group, administering drug combinations group tumour inhibiting rate is higher, and mice is in good condition, does not show obvious toxic and side effects.
embodiment 8:cucurbitacin D (CuD) combines anti-H22 function of tumor research with taurine (T)
Experimental program:
Get Kunming kind white mice, 18～22 grams of body weight, male, right fore oxter inoculation H22 tumor, treats that tumor piece grows into and is greater than 50 mm
2time, be divided at random 3 groups, 10 every group, each group gastric infusion respectively, scheme is as follows:
Dosage: CuD:5 mg/kg
T： 300 mg/kg
Administering mode: CuD Emulsion, CuD+T multiple emulsion
Matched group: normal saline group
Experimental group: CuD Emulsion group, CuD+T multiple emulsion group
Successive administration 14 days, in 24 hours, puts to death animal after last administration, gets tumor and weighs, and calculates tumour inhibiting rate.
Result: the tumour inhibiting rate of CuD Emulsion group and CuD+T multiple emulsion group is respectively 45.7% and 56.4%.
Compared with CuD Emulsion group, administering drug combinations group tumour inhibiting rate is higher, and mice is in good condition, does not show obvious toxic and side effects.
embodiment 9:cucurbitacin B (CuB) and the research of coenzyme Q10 Bio-prevention S180 function of tumor
Experimental program:
Get Kunming kind white mice, 12～16 grams of body weight, male, be divided at random 2 groups, 10 every group, each group gastric infusion respectively, continuous 14 days, after in right fore oxter inoculation S180 tumor, normally raise afterwards observed and recorded tumor situation of change.
Dosage regimen is as follows:
Dosage: CuB:B (5 mg/kg)
Q10: Q ( 50 mg/kg)
Administering mode: B+Q multiple emulsion
Matched group: normal saline group
Experimental group: B+Q group
Result: normal saline group tumor growth is rapid, connects after tumor 14 days, and average tumor volume has reached 14.0cm
2left and right, anatomic observation after putting to death, finds densely covered speckle on mouse liver, the large area diffusion of visible tumor.The tumor growth of B+Q multiple emulsion group is slow, and average tumor volume reaches 1.0cm
2time, tumor starts necrosis, while connecing after tumor 21 days, and complete tumor necrosis, about 30 days, " neoplasm necrosis tissue " comes off, and presents " without hair " newborn skin, newborn tissue after similar wound heals completely.As can be seen here, Cucurbitacin B (CuB) and coenzyme Q10 administering drug combinations, can obviously suppress generation and the growth of S180 tumor.
embodiment 10:cucurbitacin B (CuB) and the research of taurine (T) Bio-prevention S180 function of tumor
Experimental program:
Get Kunming kind white mice, 12～16 grams of body weight, male, be divided at random 2 groups, 10 every group, each group gastric infusion respectively, continuous 14 days, after in right fore oxter inoculation S180 tumor, normally raise afterwards observed and recorded tumor situation of change.
Dosage regimen is as follows:
Dosage: CuB:B (5 mg/kg)
Taurine: T(300 mg/kg)
Administering mode: B+T multiple emulsion
Matched group: normal saline group
Experimental group: B+T group
Result: normal saline group tumor growth is rapid, connects after tumor 14 days, and average tumor volume has reached 14.0cm
2left and right, anatomic observation after putting to death, finds densely covered speckle on mouse liver, the large area diffusion of visible tumor.The tumor growth of B+T multiple emulsion group is slow, and average tumor volume reaches 1.0cm
2time, tumor starts necrosis, while connecing after tumor 21 days, and complete tumor necrosis, about 30 days, " neoplasm necrosis tissue " comes off, and presents " without hair " newborn skin, newborn tissue after similar wound heals completely.As can be seen here, Cucurbitacin B (CuB) and taurine administering drug combinations, can obviously suppress generation and the growth of S180 tumor.
embodiment 11:cucurbitacin B (CuB) and the research of coenzyme Q10 Bio-prevention H22 function of tumor
Experimental program:
Get Kunming kind white mice, 12～16 grams of body weight, male, be divided at random 2 groups, 10 every group, each group gastric infusion respectively, continuous 14 days, after in right fore oxter inoculation H22 tumor, normally raise afterwards observed and recorded tumor situation of change.
Dosage regimen is as follows:
Dosage: CuB:B (5 mg/kg)
Q10: Q ( 50 mg/kg)
Administering mode: B+Q multiple emulsion
Matched group: normal saline group
Experimental group: B+Q group
Result: normal saline group tumor growth is rapid, connects after tumor 14 days, and average tumor volume has reached 12.5cm
2left and right, anatomic observation after putting to death, finds densely covered speckle on mouse liver, the large area diffusion of visible tumor.The tumor growth of B+Q multiple emulsion group is slow, and average tumor volume reaches 1.5cm
2time, tumor starts necrosis, while connecing after tumor 21 days, and complete tumor necrosis, about 30 days, " neoplasm necrosis tissue " comes off, and presents " without hair " newborn skin, newborn tissue after similar wound heals completely.As can be seen here, Cucurbitacin B (CuB) and coenzyme Q10 administering drug combinations, can obviously suppress generation and the growth of H22 tumor.
embodiment 12:cucurbitacin B (CuB) and the research of taurine (T) Bio-prevention H22 function of tumor
Experimental program:
Get Kunming kind white mice, 12～16 grams of body weight, male, be divided at random 2 groups, 10 every group, each group gastric infusion respectively, continuous 14 days, after in right fore oxter inoculation H22 tumor, normally raise afterwards observed and recorded tumor situation of change.
Dosage regimen is as follows:
Dosage: CuB:B (5 mg/kg)
Taurine: T(300 mg/kg)
Administering mode: B+T multiple emulsion
Matched group: normal saline group
Experimental group: B+T group
Result: normal saline group tumor growth is rapid, connects after tumor 14 days, and average tumor volume has reached 12.5cm
2left and right, anatomic observation after putting to death, finds densely covered speckle on mouse liver, the large area diffusion of visible tumor.The tumor growth of B+T multiple emulsion group is slow, and average tumor volume reaches 1.0cm
2time, tumor starts necrosis, while connecing after tumor 21 days, and complete tumor necrosis, about 30 days, " neoplasm necrosis tissue " comes off, and presents " without hair " newborn skin, newborn tissue after similar wound heals completely.As can be seen here, Cucurbitacin B (CuB) and taurine administering drug combinations, can obviously suppress generation and the growth of H22 tumor.
embodiment 13:cucurbatacin E (CuE) and the research of coenzyme Q10 Bio-prevention S180 function of tumor
Experimental program:
Get Kunming kind white mice, 12～16 grams of body weight, male, be divided at random 2 groups, 10 every group, each group gastric infusion respectively, continuous 14 days, after in right fore oxter inoculation S180 tumor, normally raise afterwards observed and recorded tumor situation of change.
Dosage regimen is as follows:
Dosage: CuE:E (5 mg/kg)
Q10: Q ( 50 mg/kg)
Administering mode: E+Q multiple emulsion
Matched group: normal saline group
Experimental group: E+Q group
Result: normal saline group tumor growth is rapid, connects after tumor 14 days, and average tumor volume has reached 12.0cm
2left and right, anatomic observation after putting to death, finds densely covered speckle on mouse liver, the large area diffusion of visible tumor.The tumor growth of E+Q multiple emulsion group is slow, and average tumor volume reaches 1.0cm
2time, tumor starts necrosis, while connecing after tumor 21 days, and complete tumor necrosis, about 30 days, " neoplasm necrosis tissue " comes off, and presents " without hair " newborn skin, newborn tissue after similar wound heals completely.As can be seen here, cucurbatacin E (CuE) and coenzyme Q10 administering drug combinations, can obviously suppress generation and the growth of S180 tumor.
embodiment 14:cucurbitacin I (CuI) and the research of taurine (T) Bio-prevention S180 function of tumor
Experimental program:
Get Kunming kind white mice, 12～16 grams of body weight, male, be divided at random 2 groups, 10 every group, each group gastric infusion respectively, continuous 14 days, after in right fore oxter inoculation S180 tumor, normally raise afterwards observed and recorded tumor situation of change.
Dosage regimen is as follows:
Dosage: CuI:I (5 mg/kg)
Taurine: T(300 mg/kg)
Administering mode: I+T multiple emulsion
Matched group: normal saline group
Experimental group: I+T group
Result: normal saline group tumor growth is rapid, connects after tumor 14 days, and average tumor volume has reached 13.0cm
2left and right, anatomic observation after putting to death, finds densely covered speckle on mouse liver, the large area diffusion of visible tumor.The tumor growth of I+T multiple emulsion group is slow, and average tumor volume reaches 1.0cm
2time, tumor starts necrosis, while connecing after tumor 21 days, and complete tumor necrosis, about 30 days, " neoplasm necrosis tissue " comes off, and presents " without hair " newborn skin, newborn tissue after similar wound heals completely.As can be seen here, cucurbitacin I (CuI) and taurine administering drug combinations, can obviously suppress generation and the growth of S180 tumor.
embodiment 15:cucurbitacin D (CuD) and the research of coenzyme Q10 Bio-prevention H22 function of tumor
Experimental program:
Get Kunming kind white mice, 12～16 grams of body weight, male, be divided at random 2 groups, 10 every group, each group gastric infusion respectively, continuous 14 days, after in right fore oxter inoculation H22 tumor, normally raise afterwards observed and recorded tumor situation of change.
Dosage regimen is as follows:
Dosage: CuD:D (5 mg/kg)
Q10: Q ( 50 mg/kg)
Administering mode: D+Q multiple emulsion
Matched group: normal saline group
Experimental group: D+Q group
Result: normal saline group tumor growth is rapid, connects after tumor 14 days, and average tumor volume has reached 13.5cm
2left and right, anatomic observation after putting to death, finds densely covered speckle on mouse liver, the large area diffusion of visible tumor.The tumor growth of D+Q multiple emulsion group is slow, and average tumor volume reaches 1.5cm
2time, tumor starts necrosis, while connecing after tumor 21 days, and complete tumor necrosis, about 30 days, " neoplasm necrosis tissue " comes off, and presents " without hair " newborn skin, newborn tissue after similar wound heals completely.As can be seen here, cucurbitacin D (CuD) and coenzyme Q10 administering drug combinations, can obviously suppress generation and the growth of H22 tumor.
embodiment 16:cucurbitacin D (CuD) and the research of taurine (T) Bio-prevention H22 function of tumor
Experimental program:
Get Kunming kind white mice, 12～16 grams of body weight, male, be divided at random 2 groups, 10 every group, each group gastric infusion respectively, continuous 14 days, after in right fore oxter inoculation H22 tumor, normally raise afterwards observed and recorded tumor situation of change.
Dosage regimen is as follows:
Dosage: CuD:D (5 mg/kg)
Taurine: T(300 mg/kg)
Administering mode: D+T multiple emulsion
Matched group: normal saline group
Experimental group: D+T group
Result: normal saline group tumor growth is rapid, connects after tumor 14 days, and average tumor volume has reached 13.5cm
2left and right, anatomic observation after putting to death, finds densely covered speckle on mouse liver, the large area diffusion of visible tumor.The tumor growth of D+T multiple emulsion group is slow, and average tumor volume reaches 1.0cm
2time, tumor starts necrosis, while connecing after tumor 21 days, and complete tumor necrosis, about 30 days, " neoplasm necrosis tissue " comes off, and presents " without hair " newborn skin, newborn tissue after similar wound heals completely.As can be seen here, cucurbitacin D (CuD) and taurine administering drug combinations, can obviously suppress generation and the growth of H22 tumor.
embodiment 17:the preparation of cucurbitacin, coenzyme Q10 capsule
Write out a prescription as follows:
Cucurbitacin 100 mg
Coenzyme Q10 50 g
F68 50 g
Microcrystalline Cellulose 400 g
1000
Technique:
Take each component by prescription, after fully mixing, 1000 of No. 1 capsules of fill.
embodiment 18:the preparation of cucurbitacin, coenzyme Q10 tablet
Write out a prescription as follows:
Cucurbitacin 100 mg
Coenzyme Q10 50 g
Lactose 100 g
Starch 110 g
PVP 10 g
Magnesium stearate 10 g
1000
Technique:
Take cucurbitacin, coenzyme Q10, the lactose of recipe quantity, after mix homogeneously, 10% starch slurry that adds 110g starch to make, spray granulation.After adding again PVP 10g magnesium stearate 10g mix homogeneously, be pressed into 1000.
embodiment 19:the preparation of cucurbitacin, taurine capsule
Write out a prescription as follows:
Cucurbitacin 100 mg
Taurine 50 g
F68 50 g
Microcrystalline Cellulose 400 g
1000
Technique:
Take each component by prescription, after fully mixing, 1000 of No. 1 capsules of fill.
embodiment 20:the preparation of cucurbitacin, taurine tablet
Write out a prescription as follows:
Cucurbitacin 100 mg
Taurine 50 g
Lactose 100 g
Starch 110 g
PVP 20 g
Pulvis Talci 20 g
1000
Technique:
Take cucurbitacin, taurine, the lactose of recipe quantity, after mix homogeneously, 10% starch slurry that adds 110 g starch to make, spray granulation.After adding again PVP 20 g magnesium stearate 20 g mix homogeneously, be pressed into 1000.
embodiment 21:the preparation of cucurbitacin, coenzyme Q10, taurine capsule
Write out a prescription as follows:
Cucurbitacin 100 mg
Coenzyme Q10 50 g
Taurine 50 g
F68 50 g
Microcrystalline Cellulose 350 g
1000
Technique:
Take each component by prescription, after fully mixing, 1000 of No. 1 capsules of fill.
embodiment 22:the preparation of cucurbitacin, coenzyme Q10, taurine tablet
Write out a prescription as follows:
Cucurbitacin 100 mg
Coenzyme Q10 50 g
Taurine 50 g
Lactose 100 g
Starch 110 g
PVP 10 g
Magnesium stearate 10 g
1000
Technique:
Take cucurbitacin, coenzyme Q10, taurine, the lactose of recipe quantity, after mix homogeneously, 10% starch slurry that adds 110 g starch to make, spray granulation.Add PVP 10 g, magnesium stearate 10 g, are pressed into 1000 after mix homogeneously again.
embodiment 23:the preparation of cucurbitacin, coenzyme Q10 multiple emulsion
Write out a prescription as follows:
Cucurbitacin 15 mg
Coenzyme Q10 150 mg
SPC 300 mg
RH40 600 mg
MCT 3000 mg
Glycerol 300 mg
Distilled water is appropriate
30 mL
Technique: take recipe quantity cucurbitacin, coenzyme Q10, MCT, SPC, RH40 and form oil phase; Take in recipe quantity glycerol, distilled water and form water, be heated to respectively 50 ~ 55 ℃ by biphase.After material in oil phase dissolves completely, under the condition of magnetic agitation, water is slowly joined in oil phase, continue to stir 20 min, make colostrum.By colostrum with microjet instrument at 14000 psi, after homogenizing 5 times, with distilled water diluting its to 30 ml, cross 0.22 μ m microporous filter membrane, be sub-packed in cillin bottle, inflated with nitrogen, jumps a queue, and adds aluminium lid sealing, 100 ℃ of flowing steam sterilization 30 min, cold water spray makes emulsion be down to rapidly room temperature, gets product.
embodiment 24:the preparation of cucurbitacin, taurine multiple emulsion
Write out a prescription as follows:
Cucurbitacin 9 mg
Taurine 300 mg
SPC 300 mg
RH40 600 mg
MCT 3000 mg
Glycerol 300 mg
Distilled water is appropriate
30 mL
Technique: take recipe quantity cucurbitacin, MCT, SPC, RH40 and form oil phase; Take in recipe quantity glycerol, taurine, distilled water and form water, be heated to respectively 50 ~ 55 ℃ by biphase.After in oil phase, water, material dissolves completely, under the condition of magnetic agitation, water is slowly joined in oil phase, continue to stir 20 min, make colostrum.By colostrum with microjet instrument at 14000 psi, after homogenizing 5 times, with distilled water diluting its to 30 ml, cross 0.22 μ m microporous filter membrane, be sub-packed in cillin bottle, inflated with nitrogen, jumps a queue, and adds aluminium lid sealing, 100 ℃ of flowing steam sterilization 30 min, cold water spray makes emulsion be down to rapidly room temperature, gets product.
embodiment 25:the preparation of cucurbitacin, coenzyme Q10, taurine multiple emulsion
Write out a prescription as follows:
Cucurbitacin 9 mg
Coenzyme Q10 150 mg
Taurine 300 mg
SPC 300 mg
RH40 600 mg
MCT 3000 mg
Glycerol 300 mg
Distilled water is appropriate
30 mL
Technique: take recipe quantity cucurbitacin, coenzyme Q10, MCT, SPC, RH40 and form oil phase; Take in recipe quantity glycerol, taurine, distilled water and form water, be heated to respectively 50 ~ 55 ℃ by biphase.After biphase middle material dissolves completely, under the condition of magnetic agitation, water is slowly joined in oil phase, continue to stir 20 min, make colostrum.By colostrum with microjet instrument at 14000 psi, after homogenizing 5 times, with distilled water diluting its to 30 ml, cross 0.22 μ m microporous filter membrane, be sub-packed in cillin bottle, inflated with nitrogen, jumps a queue, and adds aluminium lid sealing, 100 ℃ of flowing steam sterilization 30 min, cold water spray makes emulsion be down to rapidly room temperature, gets product.
Below further prove beneficial effect of the present invention by pharmacodynamics embodiment.
Below, by clinical patients use-case, further prove beneficial effect of the present invention.
embodiment 26:primary hepatocarcinoma
Open xx, man, 43 years old, check and be diagnosed as primary hepatocarcinoma in Affiliated Hospital of Xxx medical university in May, 2010, (CT examination result shows: multiple occupy-place in liver, left and right page is shown in multiple low echo occupy-places of differing in size, the maximum occupy-place 4.7*3.8cm of lobus dexter, gallbladder enlargement), take conventional chemotherapy medicine May, without positive effect, 10 the end of month in 2010 start to take cucurbitacin liquid capsule (production of Jin Hai pharmaceutical factory of Macao) simultaneously, coenzyme Q10 capsule (Shanghai Pharmaceutical Group company limited letter friendship pharmacy head factory is produced), adhering to taking March checks once, to be careful in one's diet simultaneously, after half a year, check for the third time at local hospital, CT reports demonstration: liver is little, form is normal, leaf low echo occupy-place in left and right reduces, wherein maximum 4.5*3.4cm, gallbladder enlargement.Find by CT report contrast before, before the maximum occupy-place of right lobe of liver, have obviously and dwindle, little occupy-place also reduces to some extent, take afterwards cucurbitacin liquid capsule and coenzyme Q10 capsule always, up to the present, weight in patients has also increased by 8 jin, and the mental status is good, and the unit of returning to has gone to work.
Claims (8)
1. the combination medicine of anti-curing oncoma, by cucurbitacin and coenzyme Q10 or be prepared into taurine the combination medicine being used for the treatment of with prophylaxis of tumours, or is prepared into by cucurbitacin, coenzyme Q10 and taurine the combination medicine being used for the treatment of with prophylaxis of tumours.
2. the combination medicine of anti-curing oncoma as claimed in claim 1, is characterized in that: the combination medicine of anti-curing oncoma is made up of cucurbitacin and coenzyme Q10, and the weight ratio of cucurbitacin and coenzyme Q10 is 1:0.1-10000.
3. the combination medicine of anti-curing oncoma as claimed in claim 1, is characterized in that: the weight ratio of cucurbitacin and taurine is 1:0.1-10000.
4. the combination medicine of anti-curing oncoma as claimed in claim 1, is characterized in that: medicine cucurbitacin, coenzyme Q10 and taurine composition, the weight ratio of cucurbitacin, coenzyme Q10 and taurine is 1:0.1-10000:0.1-10000.
5. the combination medicine of anti-curing oncoma claimed in claim 1, it is characterized in that: the combination medicine of described anti-curing oncoma can be made tablet, capsule, granule, powder, patch, ointment, suspensoid, syrup, oral liquid, patch, aerosol, suppository, nasal drop or injection jointly or respectively with acceptable carrier pharmaceutically, and corresponding controlled release agent; Also can make clathrate, liposome, microsphere, nanoparticle or Emulsion, for cavity/canal drug administration, external, oral, injection.
6. the combination medicine of described anti-curing oncoma as claimed in claim 1, it is characterized in that: the amount of each component in the combination medicine of described anti-curing oncoma, take mice oral administration Rapid Dose Calculation: cucurbitacin is as 0.001-15 mg/kg, coenzyme Q10 is 5-15 000 mg/kg, taurine is 5-20 000 mg/kg, point 1-4 administration; Take health adult's Rapid Dose Calculation: cucurbitacin is as 0.1-10 mg/d, and coenzyme Q10 is 10-300 mg/d, and taurine is 10-1 000 mg/d, point 1-4 administration.
7. the combination medicine of anti-curing oncoma as claimed in claim 1, is characterized in that: for the preparation of the medicine for the treatment of chronic hepatitis.
As described in claim 1-7 as described in the combination medicine of anti-curing oncoma, it is characterized in that: wherein cucurbitacin comprises cucurbitacin A, B, C, D, E, I, Q, S, two hydrogen cucurbitacin A, B, C, D, E, I, Q, S and isocucurbitacin A, B, C, D, E, I, Q, S, a kind of or two or more in glucoside material corresponding to various cucurbitacins.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN106983758A (en) * | 2017-06-02 | 2017-07-28 | 上海华堇生物技术有限责任公司 | Cucurbitacin S medicinal usage |
| CN111514290A (en) * | 2020-04-27 | 2020-08-11 | 德立唯（北京）生物科技有限公司 | Cucurbitacin composition and application thereof |
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| CN1528282A (en) * | 2003-09-29 | 2004-09-15 | 济南开发区保法药物研究所 | Use of tauring for preparine medicine enhancing leucocyte function |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1528282A (en) * | 2003-09-29 | 2004-09-15 | 济南开发区保法药物研究所 | Use of tauring for preparine medicine enhancing leucocyte function |
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| 么焕开 等: "葫芦素的研究概况", 《齐鲁药事》 * |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106983758A (en) * | 2017-06-02 | 2017-07-28 | 上海华堇生物技术有限责任公司 | Cucurbitacin S medicinal usage |
| CN111514290A (en) * | 2020-04-27 | 2020-08-11 | 德立唯（北京）生物科技有限公司 | Cucurbitacin composition and application thereof |
| CN111514290B (en) * | 2020-04-27 | 2023-03-28 | 德立唯（北京）生物科技有限公司 | Cucurbitacin composition and application thereof |
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| CN103800341B (en) | 2016-08-03 |
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