CN107334771A - A kind of pharmaceutical composition with antitumaous effect - Google Patents
A kind of pharmaceutical composition with antitumaous effect Download PDFInfo
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- CN107334771A CN107334771A CN201710553035.1A CN201710553035A CN107334771A CN 107334771 A CN107334771 A CN 107334771A CN 201710553035 A CN201710553035 A CN 201710553035A CN 107334771 A CN107334771 A CN 107334771A
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- cinobufagin
- bufotalien
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
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Abstract
The present invention relates to drug field, specifically discloses a kind of pharmaceutical composition with antitumaous effect.Described pharmaceutical composition includes following active component：Resibufogenin, Cinobufagin and bufotalien；The weight ratio of wherein described resibufogenin, Cinobufagin and bufotalien is 1 ~ 2:1~5:1~3.Embodiment experiment display, the anti-liver cancer and anti-, lung cancer and nasopharyngeal carcinoma after resibufogenin, Cinobufagin and bufotalien three are combined with collaboration act on；Wherein, the weight ratio of resibufogenin, Cinobufagin and bufotalien is 1:1.5~2.5:When 1 ~ 2, the best of breed for cooperateing with anti-liver effect is played for three, its anti-liver cancer and anti-lung cancer effects is suitable with positive control drug cis-platinum, and anti-nasopharyngeal carcinoma effect is better than positive control drug cis-platinum.Therefore, can be used after resibufogenin, Cinobufagin and bufotalien three being combined as a kind of brand-new cancer therapy drug.
Description
Technical field
The present invention relates to drug field, and in particular to a kind of pharmaceutical composition with antitumaous effect.
Background technology
The dried venom of toads is the secretion of toad ear rear gland and epidermal gland, white milky liquid or pale yellow syrup, poisonous.The dried venom of toads
Slurries are extracted, are dried, colouring, can be used as medicine after being sealed.With detoxify, ease pain, have one's ideas straightened out, the multiple functions such as antitumor and by
Extensive use.Toadvenom is used for clinical treatment coronary heart disease by Germany, and Japan is using the dried venom of toads as raw material production " lifesaving is red ".China
There is dried venom of toads composition in the kind Chinese patent drugs of famous Melnikov's method, a toothache killer pill, heart treasured, cinobufagin injection etc. more than 50.
But main still using toad cake extract etc. as active ingredient in the medicine of existing listing, active ingredient therein is also
Non- thoroughly research, be unfavorable for quality control and the drug safety of medicine, therefore, using the dried venom of toads be development of raw materials one kind effectively into
Clear and definite medicine is divided to have great importance.
Now studies have found that, substantial amounts of arenobufagin class material, steroid, alkaloids chemical composition are contained in the dried venom of toads.
Arenobufagin class material is the active material that one kind in the dried venom of toads has antitumor action, according to existing research, in the dried venom of toads
Contain hundreds of such material.And different monomer is also very big for antitumor active difference in such material, equally
Monomer it is also very big for the inhibitory activity difference of different tumours, be also difficult such material monomer or composition conduct at present
The cancer therapy drug of listing.Therefore, rational exploitation and utilization arenobufagin class material developing anti-tumor medicaments, defeated for the mankind various
Cancer has great importance.
The content of the invention
The technical problems to be solved by the invention are, in order to overcome prior art for arenobufagin class material antitumaous effect
Research deficiency, there is provided a kind of pharmaceutical composition with antitumaous effect.
Above-mentioned technical problem to be solved by this invention, is achieved by the following technical programs：
A kind of pharmaceutical composition with antitumaous effect, includes following active component：Resibufogenin, Cinobufagin and toadpoison
Its spirit.
Preferably, the weight ratio of the resibufogenin described in pharmaceutical composition, Cinobufagin and bufotalien be 1 ~
2:1~5:1~3。
It is further preferred that the weight of the resibufogenin, Cinobufagin and bufotalien described in pharmaceutical composition
Than for 1:1~3:1~2.
It is further preferred that the weight of the resibufogenin, Cinobufagin and bufotalien described in pharmaceutical composition
Amount is than being 1:1.5~2.5:1~2.
Inventor shows through lot of experiments, after resibufogenin, Cinobufagin and bufotalien three are combined
Synergistic anti-cancer effect can be played, resibufogenin, Cinobufagin and bufotalien three are mixed according to the above ratio can be as
A kind of novel cancer therapy drug.
Preferably, described cancer includes liver cancer, lung cancer and nasopharyngeal carcinoma.
Preferably, described pharmaceutical composition also includes pharmaceutically acceptable carrier.
Preferably, the formulation of described anticancer pharmaceutical composition is liquid injection agent, powder-injection, tablet, capsule, flexible glue
Capsule, powder, pill, oral liquid, paste, granule or dressing.
The present invention also provides resibufogenin, Cinobufagin and bufotalien combination answering in cancer therapy drug is prepared
With.
Preferably, the weight ratio of resibufogenin, Cinobufagin and bufotalien is 1 ~ 2:1~5:1~3.
It is further preferred that the weight ratio of resibufogenin, Cinobufagin and bufotalien is 1:1~3:1~2.
Still more preferably, the weight ratio of resibufogenin, Cinobufagin and bufotalien is 1:1.5~2.5:1~
2。
Beneficial effect：The invention provides a kind of cancer therapy drug completely newly combined, embodiment experiment display, ester toadpoison is matched somebody with somebody
There is anti-liver cancer and anti-, lung cancer and the nasopharyngeal carcinoma effect of collaboration after base, Cinobufagin and bufotalien three combination；Wherein, ester toad
The weight ratio of malicious aglucon, Cinobufagin and bufotalien is 1:1.5~2.5:When 1 ~ 2, Synergistic anti-cancer effect is played for three
Best of breed, its anti-liver cancer and anti-lung cancer effects is suitable with positive control drug cis-platinum, and anti-nasopharyngeal carcinoma effect is better than positive control drug
Cis-platinum.Therefore, can be as a kind of brand-new cancer therapy drug after resibufogenin, Cinobufagin and bufotalien three being combined
Use.
Embodiment
The present invention is explained further below in conjunction with specific embodiment, but embodiment does not do any type of limit to the present invention
It is fixed.
The pharmaceutical composition resisting liver cancer activity of embodiment 1
Human liver cancer cell BEL-7404 is taken to be placed in culture medium（The culture mediums of RPMI 1640）Middle culture, liver cancer cells BEL-7404 with
10×103Add in 96 orifice plates, sucked after adherent after being cultivated 24 hours in 37 DEG C of incubators containing 5%CO2 original per hole
Culture medium.Then blank group adds the culture mediums of RPMI 1640 containing 10% hyclone；Drug-treated group, which adds, contains 0.01
The culture mediums of RPMI 1640 of ~ 100 μM of medicines to be measured；Positive controls add the RPMI 1640 containing 0.01 ~ 100 μM of cis-platinum and trained
Support base；Continue after cultivating 48 h, add concentration 5mg/mL MTT, continue to cultivate 4 h, suck supernatant, add 100 μ L
DMSO, dark place place 10min, utilize ELIASA（Sunrise companies）Light absorption value is determined under 570nm, and according to light absorption value meter
Cell survival is calculated, each processing sets 6 repeating holes.Cell survival rate (%)=Δ OD drug-treateds group/Δ OD blank groups ×
100.Cell 503nhibiting concentration (IC50) is calculated further according to dose-effect curve, the results are shown in Table 1.
Drug-treated group is respectively：Drug-treated group 1 is resibufogenin；Drug-treated group 2 is Cinobufagin；Medicine
Treatment group 3 is bufotalien；Drug-treated group 4 is that weight ratio is 1:The combination of 2 resibufogenin and Cinobufagin；Medicine
Treatment group 5 is that weight ratio is 2:The combination of 1 Cinobufagin and bufotalien；Drug-treated group 6 is that weight ratio is 1:1 ester
The combination of bufotalin and bufotalien；Drug-treated group 7 is that weight ratio is 1:2:1 resibufogenin, Cinobufagin and
The combination of bufotalien；Drug-treated group 8 is that weight ratio is 1:1.5:1 resibufogenin, Cinobufagin and bufotalien
Combination；Drug-treated group 9 is that weight ratio is 1:2.5:The combination of 1 resibufogenin, Cinobufagin and bufotalien；Medicine
Thing treatment group 10 is that weight ratio is 1:2:The combination of 2 resibufogenin, Cinobufagin and bufotalien；Drug-treated group 11
It is 1 for weight ratio:2.5:The combination of 1.5 resibufogenin, Cinobufagin and bufotalien；Drug-treated group 12 is weight
Than for 1:3:The combination of 2 resibufogenin, Cinobufagin and bufotalien；Drug-treated group 13 is that weight ratio is 1:5:1
Resibufogenin, Cinobufagin and bufotalien combination；Drug-treated group 14 is that weight ratio is 1:5:3 ester toadpoison is matched somebody with somebody
The combination of base, Cinobufagin and bufotalien.
IC50 test result of the pharmaceutical composition of table 1. to liver cancer cells BEL-7404
| Group | Composition | IC50 values（μM） |
| Drug-treated group 1 | Resibufogenin | 41.47 |
| Drug-treated group 2 | Cinobufagin | 36.81 |
| Drug-treated group 3 | Bufotalien | 33.14 |
| Drug-treated group 4 | Resibufogenin：Cinobufagin（1:2） | 39.52 |
| Drug-treated group 5 | Cinobufagin：Bufotalien（2:1） | 35.11 |
| Drug-treated group 6 | Resibufogenin：Bufotalien（1:1） | 38.58 |
| Drug-treated group 7 | Resibufogenin：Cinobufagin：Bufotalien（1:2:1） | 15.71 |
| Drug-treated group 8 | Resibufogenin：Cinobufagin：Bufotalien（1:1.5:1） | 16.22 |
| Drug-treated group 9 | Resibufogenin：Cinobufagin：Bufotalien（1:2.5:1） | 16.35 |
| Drug-treated group 10 | Resibufogenin：Cinobufagin：Bufotalien（1:2:2） | 17.01 |
| Drug-treated group 11 | Resibufogenin：Cinobufagin：Bufotalien（1:2.5:1.5） | 16.92 |
| Drug-treated group 12 | Resibufogenin：Cinobufagin：Bufotalien（1:3:2） | 18.84 |
| Drug-treated group 13 | Resibufogenin：Cinobufagin：Bufotalien（1:5:1） | 21.22 |
| Drug-treated group 14 | Resibufogenin：Cinobufagin：Bufotalien（1:5:3） | 20.98 |
| Positive controls | Cis-platinum | 15.25 |
From the test data of table 1, resibufogenin, Cinobufagin and bufotalien, which are used alone, has certain anti-liver cancer and anti-to make
With, but its IC50 value is far longer than the IC50 values of cis-platinum, this explanation, resibufogenin, Cinobufagin and toadpoison is used alone
Its spirit is used as cancer therapy drug, and its anticancer effect is much not as good as the anticancer effect of cis-platinum.
Also have after can also be seen that resibufogenin, Cinobufagin and bufotalien combination of two from the test data of table 1
There are certain antihepatocarcinoma effect, but its antihepatocarcinoma effect and resibufogenin, Cinobufagin and bufotalien exclusive use
IC50 values are suitable, and this explanation resibufogenin, Cinobufagin and bufotalien combination of two can not lift its anticancer effect.
In addition, as can be seen that working as resibufogenin, Cinobufagin and bufotalien three's group from the test data of table 1
After conjunction, the IC50 values of its anti-liver cancer and anti-and the IC50 values of cis-platinum are close, this illustrate by resibufogenin, Cinobufagin and toadpoison it
After clever three's combination, three has played Synergistic anti-cancer effect, has been obviously improved resibufogenin, Cinobufagin and bufotalien
The anticancer effect of monomer.The antihepatocarcinoma effect of especially experimental group 7 ~ 11 is optimal, this explanation resibufogenin, Cinobufagin and
The weight ratio of bufotalien is 1:1.5~2.5:When 1 ~ 2, the best of breed of collaboration antihepatocarcinoma effect, its anti-liver cancer and anti-are played for three
Effect is suitable with positive control drug cis-platinum.
The pharmaceutical composition anti-lung cancer activity of embodiment 2
Human lung cancer cell A549 is taken to be placed in culture medium（The culture mediums of RPMI 1640）Middle culture, lung cell A549 is with 10 × 103Often
Hole is added in 96 orifice plates, and original culture medium is sucked after adherent after being cultivated 24 hours in 37 DEG C of incubators containing 5%CO2.So
Blank group adds the culture mediums of RPMI 1640 containing 10% hyclone afterwards；Drug-treated group is added and treated containing 0.01 ~ 100 μM
Survey the culture mediums of RPMI 1640 of medicine；Positive controls add the culture mediums of RPMI 1640 containing 0.01 ~ 100 μM of cis-platinum；After
After 48 h of continuous culture, concentration 5mg/mL MTT is added, continues to cultivate 4 h, sucks supernatant, add 100 μ L DMSO, secretly
10min is placed at place, utilizes ELIASA（Sunrise companies）Light absorption value is determined under 570nm, and cell is calculated according to light absorption value and deposited
Situation living, each processing set 6 repeating holes.Cell survival rate (%)=Δ OD drug-treateds group/Δ OD blank group × 100.Root again
Cell 503nhibiting concentration (IC50) is calculated according to dose-effect curve, the results are shown in Table 2.
Drug-treated group is respectively：Drug-treated group 1 is resibufogenin；Drug-treated group 2 is Cinobufagin；Medicine
Treatment group 3 is bufotalien；Drug-treated group 4 is that weight ratio is 1:The combination of 2 resibufogenin and Cinobufagin；Medicine
Treatment group 5 is that weight ratio is 2:The combination of 1 Cinobufagin and bufotalien；Drug-treated group 6 is that weight ratio is 1:1 ester
The combination of bufotalin and bufotalien；Drug-treated group 7 is that weight ratio is 1:2:1 resibufogenin, Cinobufagin and
The combination of bufotalien；Drug-treated group 8 is that weight ratio is 1:1.5:1 resibufogenin, Cinobufagin and bufotalien
Combination；Drug-treated group 9 is that weight ratio is 1:2.5:The combination of 1 resibufogenin, Cinobufagin and bufotalien；Medicine
Thing treatment group 10 is that weight ratio is 1:2:The combination of 2 resibufogenin, Cinobufagin and bufotalien；Drug-treated group 11
It is 1 for weight ratio:2.5:The combination of 1.5 resibufogenin, Cinobufagin and bufotalien；Drug-treated group 12 is weight
Than for 1:3:The combination of 2 resibufogenin, Cinobufagin and bufotalien；Drug-treated group 13 is that weight ratio is 1:5:1
Resibufogenin, Cinobufagin and bufotalien combination；Drug-treated group 14 is that weight ratio is 1:5:3 ester toadpoison is matched somebody with somebody
The combination of base, Cinobufagin and bufotalien.
IC50 test result of the pharmaceutical composition of table 2. to lung cell A549
| Group | Composition | IC50 values（μM） |
| Drug-treated group 1 | Resibufogenin | 35.11 |
| Drug-treated group 2 | Cinobufagin | 40.22 |
| Drug-treated group 3 | Bufotalien | 31.78 |
| Drug-treated group 4 | Resibufogenin：Cinobufagin（1:2） | 37.16 |
| Drug-treated group 5 | Cinobufagin：Bufotalien（2:1） | 35.15 |
| Drug-treated group 6 | Resibufogenin：Bufotalien（1:1） | 32.12 |
| Drug-treated group 7 | Resibufogenin：Cinobufagin：Bufotalien（1:2:1） | 13.64 |
| Drug-treated group 8 | Resibufogenin：Cinobufagin：Bufotalien（1:1.5:1） | 14.39 |
| Drug-treated group 9 | Resibufogenin：Cinobufagin：Bufotalien（1:2.5:1） | 14.52 |
| Drug-treated group 10 | Resibufogenin：Cinobufagin：Bufotalien（1:2:2） | 15.88 |
| Drug-treated group 11 | Resibufogenin：Cinobufagin：Bufotalien（1:2.5:1.5） | 15.54 |
| Drug-treated group 12 | Resibufogenin：Cinobufagin：Bufotalien（1:3:2） | 17.13 |
| Drug-treated group 13 | Resibufogenin：Cinobufagin：Bufotalien（1:5:1） | 19.46 |
| Drug-treated group 14 | Resibufogenin：Cinobufagin：Bufotalien（1:5:3） | 19.99 |
| Positive controls | Cis-platinum | 14.10 |
From the test data of table 2, resibufogenin, Cinobufagin and bufotalien, which are used alone, has certain anti-lung cancer to make
With, but its IC50 value is far longer than the IC50 values of cis-platinum, this explanation, resibufogenin, Cinobufagin and toadpoison is used alone
Its spirit is used as anti-lung-cancer medicament, and its anti-lung cancer effect is much not as good as the anti-lung cancer effect of cis-platinum.
Also have after can also be seen that resibufogenin, Cinobufagin and bufotalien combination of two from the test data of table 2
There are certain effect of anti-lung cancer, but its effect of anti-lung cancer and resibufogenin, Cinobufagin and bufotalien exclusive use
IC50 values are suitable, and this explanation resibufogenin, Cinobufagin and bufotalien combination of two can not lift its lung cancer effect.
In addition, as can be seen that working as resibufogenin, Cinobufagin and bufotalien three's group from the test data of table 2
After conjunction, the IC50 values of its anti-lung cancer and the IC50 values of cis-platinum are close, this illustrate by resibufogenin, Cinobufagin and toadpoison it
After clever three combination, three has played collaboration effect of anti-lung cancer, be obviously improved resibufogenin, Cinobufagin and toadpoison it
The anti-lung cancer effect of clever monomer.The effect of anti-lung cancer of especially experimental group 7 ~ 11 is optimal, this explanation resibufogenin, magnificent dried venom of toads poison
The weight of base and bufotalien ratio is 1:1.5~2.5:When 1 ~ 2, the best of breed of collaboration effect of anti-lung cancer is played for three.
The anti-nasopharyngeal carcinoma activity of the pharmaceutical composition of embodiment 3
KB cell CNE is taken to be placed in culture medium（The culture mediums of RPMI 1640）Middle culture, nasopharyngeal carcinoma cell CNE is with 10 × 103
Added per hole in 96 orifice plates, original culture medium is sucked after adherent after being cultivated 24 hours in 37 DEG C of incubators containing 5%CO2.
Then blank group adds the culture mediums of RPMI 1640 containing 10% hyclone；Drug-treated group, which adds, contains 0.01 ~ 100 μM
The culture mediums of RPMI 1640 of medicine to be measured；Positive controls add the culture mediums of RPMI 1640 containing 0.01 ~ 100 μM of cis-platinum；
Continue after cultivating 48 h, add concentration 5mg/mL MTT, continue to cultivate 4 h, suck supernatant, add 100 μ L DMSO,
10min is placed in dark place, utilizes ELIASA（Sunrise companies）Light absorption value is determined under 570nm, and cell is calculated according to light absorption value
Survival condition, each processing set 6 repeating holes.Cell survival rate (%)=Δ OD drug-treateds group/Δ OD blank group × 100.Again
Cell 503nhibiting concentration (IC50) is calculated according to dose-effect curve, the results are shown in Table 3.
Drug-treated group is respectively：Drug-treated group 1 is resibufogenin；Drug-treated group 2 is Cinobufagin；Medicine
Treatment group 3 is bufotalien；Drug-treated group 4 is that weight ratio is 1:The combination of 2 resibufogenin and Cinobufagin；Medicine
Treatment group 5 is that weight ratio is 2:The combination of 1 Cinobufagin and bufotalien；Drug-treated group 6 is that weight ratio is 1:1 ester
The combination of bufotalin and bufotalien；Drug-treated group 7 is that weight ratio is 1:2:1 resibufogenin, Cinobufagin and
The combination of bufotalien；Drug-treated group 8 is that weight ratio is 1:1.5:1 resibufogenin, Cinobufagin and bufotalien
Combination；Drug-treated group 9 is that weight ratio is 1:2.5:The combination of 1 resibufogenin, Cinobufagin and bufotalien；Medicine
Thing treatment group 10 is that weight ratio is 1:2:The combination of 2 resibufogenin, Cinobufagin and bufotalien；Drug-treated group 11
It is 1 for weight ratio:2.5:The combination of 1.5 resibufogenin, Cinobufagin and bufotalien；Drug-treated group 12 is weight
Than for 1:3:The combination of 2 resibufogenin, Cinobufagin and bufotalien；Drug-treated group 13 is that weight ratio is 1:5:1
Resibufogenin, Cinobufagin and bufotalien combination；Drug-treated group 14 is that weight ratio is 1:5:3 ester toadpoison is matched somebody with somebody
The combination of base, Cinobufagin and bufotalien.
IC50 test result of the pharmaceutical composition of table 3. to nasopharyngeal carcinoma cell CNE
| Group | Composition | IC50 values（μM） |
| Drug-treated group 1 | Resibufogenin | 14.15 |
| Drug-treated group 2 | Cinobufagin | 10.32 |
| Drug-treated group 3 | Bufotalien | 12.10 |
| Drug-treated group 4 | Resibufogenin：Cinobufagin（1:2） | 12.33 |
| Drug-treated group 5 | Cinobufagin：Bufotalien（2:1） | 11.41 |
| Drug-treated group 6 | Resibufogenin：Bufotalien（1:1） | 13.14 |
| Drug-treated group 7 | Resibufogenin：Cinobufagin：Bufotalien（1:2:1） | 3.11 |
| Drug-treated group 8 | Resibufogenin：Cinobufagin：Bufotalien（1:1.5:1） | 3.41 |
| Drug-treated group 9 | Resibufogenin：Cinobufagin：Bufotalien（1:2.5:1） | 3.44 |
| Drug-treated group 10 | Resibufogenin：Cinobufagin：Bufotalien（1:2:2） | 4.01 |
| Drug-treated group 11 | Resibufogenin：Cinobufagin：Bufotalien（1:2.5:1.5） | 4.25 |
| Drug-treated group 12 | Resibufogenin：Cinobufagin：Bufotalien（1:3:2） | 5.72 |
| Drug-treated group 13 | Resibufogenin：Cinobufagin：Bufotalien（1:5:1） | 6.14 |
| Drug-treated group 14 | Resibufogenin：Cinobufagin：Bufotalien（1:5:3） | 6.48 |
| Positive controls | Cis-platinum | 4.37 |
From the test data of table 3, resibufogenin, Cinobufagin and bufotalien, which are used alone, certain anti-nasopharyngeal carcinoma
Effect, but its IC50 value is far longer than the IC50 values of cis-platinum, this explanation, resibufogenin, Cinobufagin and toad is used alone
Its spirit of poison is used as anti-nasopharyngeal carcinoma medicine, and its anticancer effect is much not as good as the anti-nasopharyngeal carcinoma effect of cis-platinum.
Also have after can also be seen that resibufogenin, Cinobufagin and bufotalien combination of two from the test data of table 3
There is certain anti-nasopharyngeal carcinoma effect, but its anti-nasopharyngeal carcinoma effect individually makes with resibufogenin, Cinobufagin and bufotalien
IC50 values are suitable, and this explanation resibufogenin, Cinobufagin and bufotalien combination of two can not lift its anti-nose
Pharynx cancer effect.
In addition, as can be seen that working as resibufogenin, Cinobufagin and bufotalien three's group from the test data of table 3
After conjunction, IC50 value of the IC50 values of its anti-nasopharyngeal carcinoma with the IC50 values of cis-platinum close to even better than cis-platinum, this illustrates ester toadpoison
After aglucon, Cinobufagin and bufotalien three combination, three has played the anti-nasopharyngeal carcinoma effect of collaboration, has been obviously improved ester toad
The anti-nasopharyngeal carcinoma effect of malicious aglucon, Cinobufagin and bufotalien monomer.The especially anti-nasopharyngeal carcinoma effect of experimental group 7 ~ 11
Most preferably, the weight ratio of this explanation resibufogenin, Cinobufagin and bufotalien is 1:1.5~2.5:When 1 ~ 2, sent out for three
The best of breed for cooperateing with anti-nasopharyngeal carcinoma effect is waved, its anti-nasopharyngeal carcinoma effect is better than positive control drug cis-platinum.
The data of consolidated statement 1,2 and 3 understand that the combination of resibufogenin, Cinobufagin and bufotalien three can be sent out
Wave collaboration anti-liver cancer and anti-, lung cancer and nasopharyngeal carcinoma effect.The especially combination of resibufogenin, Cinobufagin and bufotalien three
It is most notable to nasopharyngeal carcinoma antitumaous effect, when the weight ratio of resibufogenin, Cinobufagin and bufotalien is 1:1.5~2.5:1
Its IC50 value to nasopharyngeal carcinoma cell is less than the IC50 values of cis-platinum when ~ 2, and this illustrates that its anti-nasopharyngeal carcinoma effect is better than positive control
Medicine cis-platinum.
Embodiment 4 has the pharmaceutical composition of antitumaous effect
It is 1 by weight by resibufogenin, Cinobufagin and bufotalien:2:1 mixing is used as active ingredient, then by system
Powder-injection is made in the conventional method in medicine field.
Embodiment 5 has the pharmaceutical composition of antitumaous effect
It is 1 by weight by resibufogenin, Cinobufagin and bufotalien:2:2 mixing are used as active ingredient, then by system
Powder-injection is made in the conventional method in medicine field.
Embodiment 6 has the pharmaceutical composition of antitumaous effect
It is 1 by weight by resibufogenin, Cinobufagin and bufotalien:3:1 mixing is used as active ingredient, then by system
Powder-injection is made in the conventional method in medicine field.
Embodiment 7 has the pharmaceutical composition of antitumaous effect
It is 1 by weight by resibufogenin, Cinobufagin and bufotalien:3:2 mixing are used as active ingredient, then by system
Powder-injection is made in the conventional method in medicine field.
Embodiment 8 has the pharmaceutical composition of antitumaous effect
It is 1 by weight by resibufogenin, Cinobufagin and bufotalien:2:1.5 mixing are used as active ingredient, then press
Liquid injection agent is made in the conventional method of pharmaceutical field.
Embodiment 9 has the pharmaceutical composition of antitumaous effect
It is 1 by weight by resibufogenin, Cinobufagin and bufotalien:1.5:1 mixing is used as active ingredient, then presses
Liquid injection agent is made in the conventional method of pharmaceutical field.
Embodiment 10 has the pharmaceutical composition of antitumaous effect
It is 2 by weight by resibufogenin, Cinobufagin and bufotalien:1:1 mixing is used as active ingredient, then by system
Tablet is made in the conventional method in medicine field.
Embodiment 11 has the pharmaceutical composition of antitumaous effect
It is 1 by weight by resibufogenin, Cinobufagin and bufotalien:5:3 mixing are used as active ingredient, then by system
Tablet is made in the conventional method in medicine field.
Embodiment 12 has the pharmaceutical composition of antitumaous effect
It is 1 by weight by resibufogenin, Cinobufagin and bufotalien:1:3 mixing are used as active ingredient, then by system
Capsule is made in the conventional method in medicine field.
Embodiment 13 has the pharmaceutical composition of antitumaous effect
It is 1 by weight by resibufogenin, Cinobufagin and bufotalien:5:3 mixing are used as active ingredient, then by system
Capsule is made in the conventional method in medicine field.
Claims (10)
1. a kind of pharmaceutical composition with antitumaous effect, it is characterised in that include following active component：Resibufogenin, China
Bufalin and bufotalien.
2. pharmaceutical composition according to claim 1, it is characterised in that resibufogenin described in pharmaceutical composition,
The weight of Cinobufagin and bufotalien ratio is 1 ~ 2:1~5:1~3.
3. pharmaceutical composition according to claim 2, it is characterised in that resibufogenin described in pharmaceutical composition,
The weight of Cinobufagin and bufotalien ratio is 1:1~3:1~2.
4. pharmaceutical composition according to claim 3, it is characterised in that resibufogenin described in pharmaceutical composition,
The weight of Cinobufagin and bufotalien ratio is 1:1.5~2.5:1~2.
5. according to the pharmaceutical composition described in any one of claim 1 ~ 4, it is characterised in that described cancer includes liver cancer, lung cancer
And nasopharyngeal carcinoma.
6. according to the pharmaceutical composition described in any one of claim 1 ~ 4, it is characterised in that characterized in that, described medicine
Composition also includes pharmaceutically acceptable carrier.
7. according to the pharmaceutical composition described in any one of claim 1 ~ 4, it is characterised in that described anticancer pharmaceutical composition
Formulation is liquid injection agent, powder-injection, tablet, capsule, soft capsule, powder, pill, oral liquid, paste, granule or applied
Material.
8. resibufogenin, Cinobufagin and bufotalien are combined the application in cancer therapy drug is prepared.
9. application according to claim 8, it is characterised in that the weight of resibufogenin, Cinobufagin and bufotalien
Amount is than being 1 ~ 2:1~5:1~3.
10. application according to claim 9, it is characterised in that the weight of resibufogenin, Cinobufagin and bufotalien
Amount is than being 1:1~3:1~2；Still more preferably, the weight ratio of resibufogenin, Cinobufagin and bufotalien is 1:1.5
~2.5:1~2。
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| CN201710553035.1A CN107334771A (en) | 2017-07-07 | 2017-07-07 | A kind of pharmaceutical composition with antitumaous effect |
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