CN107260734A - A kind of compound medicament composition with effect of anti-lung cancer and application thereof - Google Patents
A kind of compound medicament composition with effect of anti-lung cancer and application thereof Download PDFInfo
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- 230000000694 effects Effects 0.000 title claims abstract description 43
- 206010058467 Lung neoplasm malignant Diseases 0.000 title claims abstract description 31
- 201000005202 lung cancer Diseases 0.000 title claims abstract description 29
- 208000020816 lung neoplasm Diseases 0.000 title claims abstract description 29
- 239000000203 mixture Substances 0.000 title claims abstract description 25
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- 239000010282 Emodin Substances 0.000 claims abstract description 35
- RHMXXJGYXNZAPX-UHFFFAOYSA-N emodin Chemical compound C1=C(O)C=C2C(=O)C3=CC(C)=CC(O)=C3C(=O)C2=C1O RHMXXJGYXNZAPX-UHFFFAOYSA-N 0.000 claims abstract description 35
- VABYUUZNAVQNPG-UHFFFAOYSA-N Piperlongumine Natural products COC1=C(OC)C(OC)=CC(C=CC(=O)N2C(C=CCC2)=O)=C1 VABYUUZNAVQNPG-UHFFFAOYSA-N 0.000 claims abstract description 30
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention belongs to natural medicine field, a kind of compound medicament composition with effect of anti-lung cancer and application thereof is disclosed.The active component of the compound medicament composition be by mol ratio be 1:1~1:10 piperlongumine and rheum emodin composition.Both drug combinations have the purposes of stronger synergistic treatment lung cancer.
Description
Technical field
It is more particularly to a kind of that there is effect of anti-lung cancer containing piperlongumine and rheum emodin the invention belongs to natural medicine field
Compound medicament composition and application thereof.
Background technology
Lung cancer is that morbidity and mortality growth is most fast, to one of population health and the maximum malignant tumour of life threat.
The morbidity and mortality of many countries of immediate and mid-term all report lung cancer substantially increase, and male lung cancer morbidity and mortality are equal
First of all malignant tumours is accounted for, the women incidence of disease accounts for second, the death rate accounts for second.The cause of disease of lung cancer is still endless so far
It is complete clear and definite.At present, the common treatment mode for the treatment of lung cancer has：Operation, radiotherapy, chemotherapy, treatment by Chinese herbs.Wherein perform the operation and radiotherapy is
Most common method, but the risk of operative treatment is big, costly, and radiotherapy side effect is big, greatly adds patients with lung cancer
Pain.In recent years, the medicine of some treatment lung cancer has been engendered on the market, for example：Platinum class, for Buddhist nun's class etc..But it is above-mentioned
Medicine wholistic therapy effect is still pessimistic, and is easy to recurrence.Therefore, research and develop out a kind of therapeutic effect good, be difficult
The lung cancer of recurrence is the problem of current urgent need to resolve.So find safely, effectively, the antineoplastic of low toxicity and study its effect
Mechanism, it is significant.
Piperlongumine (piperlongumine, PLM) is also known as piplartine (piplEDine), belongs to alkaloid compound.
Initial separation from Piperaceae plant Bi roots of grass Piper longum Linn. root, in long handle pepper P.sylvaticum Roxb. and
Also have in the prominent pepper P.tuberculatumJacq. of knurl etc. root and get.With going deep into for studying piperlongumine, the Bi roots of grass is found
Acid amides has a variety of pharmacotoxicological effects, wherein having significant CDCC to tumour cell, can adjust hyperlipidemia ratses
Blood lipid metabolism, and show many pharmacological activity such as anti-platelet aggregation, analgesia, antimycotic.It recent studies have shown that it to many
Planting tumour cell has specific CDCC, and to the very small (Nature.2011Jul 13 of toxicity of normal cell；
475(7355):231-4.；ACS Chem Biol.2013May 17；8(5):923-9.), therefore piperlongumine is a kind of great
Potentiality can selectively kill the traditional Chinese medicine monomer of tumour.
Rheum emodin (Emodin, ED) is one of principle active component of rheum officinale, with the effect such as anti-inflammatory, antibacterial, antiviral,
In recent years, research finds that it has obvious broad-spectrum anti-tumor effect, and toxic side effect is relatively low, and selectivity is relatively strong and receives much concern.Greatly
The research of flavine antitumor action, mainly from suppress tumour growth, suppress migration invasion and attack, drug combination heighten the effect of a treatment, assisting a ruler in governing a country
Treat enhanced sensitivity and be attenuated 4 aspects.ED has positive prevention to kinds cancers such as liver cancer, lung cancer, breast cancer and colorectal cancers and controlled
Treatment acts on (Oncotarget.2017.doi:10.18632/oncotarget.16611.；Biomed
Pharmacother.2017；90:222-228.；Cell Physiol Biochem.2017；41(1):339-357.), this will
It is favorably improved the effect of chemotherapeutics.ED anticancer mechanisms relate generally to remove hydroxyl radical free radical, have selection to tumour cell
Property lethal effect, moreover it is possible to by change nucleus molecular sequences suppress tumour growth, apoptosis and differentiation.
Based on above-mentioned background, by literature survey, combination PLM and ED is used for the preventive and therapeutic action of malignant tumour lung cancer
There is not yet pertinent literature report does not almost have.
The content of the invention
In order to overcome shortcoming and defect present in prior art, primary and foremost purpose of the invention is to provide a kind of with anti-
The compound medicament composition of lung cancer effect；The active component of the compound medicament composition is made up of piperlongumine and rheum emodin.
Another object of the present invention is to provide a kind of purposes of the above-mentioned compound medicament composition with effect of anti-lung cancer；
Pharmacological testing proves that the compound medicament composition has collaboration effect of anti-lung cancer.
The purpose of the present invention is achieved through the following technical solutions：
A kind of compound medicament composition with effect of anti-lung cancer, the active component of the compound medicament composition is by the Bi roots of grass
Acid amides and rheum emodin composition.
It is preferred that, the mol ratio of the piperlongumine and rheum emodin is 1:1~1:10.
More preferred, the mol ratio of the piperlongumine and rheum emodin is 1:1~1:5.
The compound medicament composition also contains pharmaceutically acceptable carrier.
A kind of purposes of the above-mentioned compound medicament composition with effect of anti-lung cancer in anti-pouring lung-cancer medicament is prepared.
The anti-lung-cancer medicament can be used for the treatment of the lung cancer of mammal including people.
The present invention has the advantages that to protrude as follows and beneficial effect compared with prior art：
Inventor has found in the research to piperlongumine (PLM) and rheum emodin (ED) compatibility pharmacological activity, by Bi roots of grass acyls
Amine and rheum emodin combination medicine-feeding, particularly when both mol ratios are 1:1-1:The collaboration with fine inhibiting tumor cell is made during 10 compatibility
With.Inventor is respectively that model carries out external MTT screenings to lung cancer, it is found that it has very strong antiproliferative activity and in good
Timeliness and dose-effect relationship, with reference to classical administering drug combinations analysis principle (Median-effect Principle) and statistical analysis, knot
Fruit shows that it has synergy, and cooperative effect especially can be substantially produced in fa ＜ 0.5 and suppresses three kinds of cancer cell multiplications, this
Illustrate that ED and PLM compositions can produce the biological effect of the mono- medicine high doses of ED or PLM in low dosage compatibility, so as to big
The toxic side effect of big reduction medicine is produced, with good clinical application DEVELOPMENT PROSPECT.Meanwhile, show etc. effect dose evaluation,
Combination drug not yet increases normal liver cell L-O2 toxicity.
Embodiment
With reference to embodiment, the present invention is described in further detail, but the implementation of the present invention is not limited to this.
Embodiment 1：Lung carcinoma cell screening and optimizing piperlongumine (PLM) and rheum emodin (ED) compound medicament composition.
Take the logarithm the lung carcinoma cell in growth period, 3 × 10 are inoculated with respectively4Individual cells/well is on 96 orifice plates, 6 hours to be grown
Afterwards, supernatant is abandoned in centrifugation, is then administered by following packet：Tumour cell sets not dosing group and dosing group, wherein dosing group set ED and
The mono- medicine groups of PLM, ED and PLM drug combinations different mol ratio example group, every group sets 4-6 multiple holes, cultivates 24 hours, abandons supernatant, plus
Enter MTT (tetrazolium) serum-free medium cultures of the 100 μ l containing 0.5mg/ml 4 hours, adding 100 μ l DMSO, (diformazan is sub-
Sulfone), it is positioned on micro-oscillating instrument and vibrates 10min, then is placed on ELIASA detection OD values at 570nm.As a result according to following suppression
Rate formula processed calculates the inhibiting rate of growth of tumour cell under each case, and concrete outcome is shown in Table 1.
Inhibiting rate=(1- dosing groups OD values/control group OD values)
Table 1 is independent and administering drug combinations function cells various concentrations after 24 hours the IC of ED and PLM50Inhibiting rate.
As PLM and ED in molar ratio 1:1 and 1:Suppression situation when 10 compatibilities are combined.When mol ratio changes, PLM and ED
The concentration of compatibility is adjusted increase, and its inhibiting rate is in concentration dependent.
24 hours IC of the mono- medicine/compound actions of the ED of table 1 and PLM50(μM)
Embodiment 2：PLM and ED administering drug combinations effect analysis
It is evaluation base with Median-effect Principle (median-effect principle or Chou-Talalay association indexs method)
Plinth, Combination index curve (the fa-C songs under dose-effect curve and different effect are drawn using CombiDrug statistical softwares
Line), be between the effect shared from two medicines and the medicine of relation quantitative assessment two of Combination index cooperate with, antagonism or addition relation.Tool
Body step is as follows：
Medicine action effect is that (the average OD570 values/tumour cell blank control group of test group is averaged inhibiting rate (fa)=1-
OD570) the efficacious prescriptions formula fa/fu=(D/Dm) inm, take the logarithm logfa/fu=mlogD-mlogDm on both sides, if a=-
Efficacious prescriptions formula obtains y=bx-a in mlogDm, b=m, x=logD, y=logfa/fu, substitution；Wherein fa is medicine action effect,
Fu=1-fa, D are drug concentration, and m is slope, and Dm is middle effect concentration, i.e. drug concentration during 50% effect.According to above-mentioned formula,
Calculate that two kinds of anticarcinogens are alone and respective middle effect concentration Dm (logDm=-a/m) when sharing, then calculate alone and two medicines
When sharing in various effects required drug concentration (D=Dm (fa/f u) 1/m), can calculate when two medicines are shared in various effects
When Combination index (when CI=D1/DX1+D2/DX2+ α (D1D2)/(DX1DX2), D1, D2 are that two medicines produce X effects when sharing
Two medicines each needed for concentration, DX1, DX2 are two medicines respective concentration when producing X effects when two medicines are used alone).α=0 is two kinds of phases
Mutual repellency medicine, α=1 is two kinds of mutual nonexclusion medicines.Because ED is different from PLM mechanism of action, thus taken in this experiment α=
0.Work as CI<1, it is collaboration that two medicines, which share effect,；CI=1, two medicines share effect addition；CI>1, two medicines share effect antagonism.
By software analysis, compound medicament composition of the invention has good synergy, and specific effect is shown in Table 2,
The principle of effect, i.e. CI indexes are evaluated according to Median-effect Principle<With very strong synergy when 0.1
(Very strong synergism)；CI indexes are strong cooperative effect (Strong synergism) when being 0.1-0.3；CI refers to
Number has cooperative effect (Synergism) for 0.3-0.7；CI indexes are 0.7-0.85 with moderate cooperative effect (Moderate
synergism)；CI indexes have weak cooperative effect (Slight synergism) when being 0.85-0.90 interval；CI indexes are
0.90-1.10 has nearly synergistic effect (Nearly additive) when interval；CI indexes>1.10 and there is antagonism effect during the above
Should.Table 2 is visible, ED and PLM compatibilities have cooperative effect；Especially when both mol ratios are 1-1:With good during 10 compatibility
Cooperative effect, when both mol ratios are 1-1:Cooperative effect is most strong when 5.
The PLM of table 2 is different with ED, and compatibility combination is compared the A549 association index CI for acting on 24 hours
Embodiment 3：Tablet is made according to following prescription in piperlongumine (PLM) and rheum emodin (ED) compound medicament composition：
Prescription is as follows：
Preparation technology is as follows：
Medicine and auxiliary material are crossed into 80 mesh sieves respectively, by piperlongumine and 50 grams of microcrystalline celluloses and 12 grams of sodium carboxymethyl starches
It is sufficiently mixed, 10% starch slurry softwood, the granulation of 18 mesh sieves, is dried at 60 DEG C, obtain particle 1.By rheum emodin and 12 grams of crystallite fibres
Dimension element, 15 grams of starch and 8 grams of sodium carboxymethyl starches are sufficiently mixed, 10% starch slurry softwood, the granulation of 18 mesh sieves, are done at 60 DEG C
It is dry, obtain particle 2.By equal increments principle, particle 1 and particle 2 are sufficiently mixed, 16 mesh sieve whole grains, add magnesium stearate, mixed
It is even, tabletting, piece weight 500mg.
Above-described embodiment is preferably embodiment, but embodiments of the present invention are not by above-described embodiment of the invention
Limitation, other any Spirit Essences without departing from the present invention and the change made under principle, modification, replacement, combine, simplification,
Equivalent substitute mode is should be, is included within protection scope of the present invention.
Claims (5)
1. a kind of compound medicament composition with effect of anti-lung cancer, it is characterised in that：The compound medicament composition activity into
Divide and be made up of piperlongumine and rheum emodin.
2. a kind of compound medicament composition with effect of anti-lung cancer according to claim 1, it is characterised in that：The Bi
The mol ratio of roots of grass acid amides and rheum emodin is 1:1~1:10.
3. a kind of compound medicament composition with effect of anti-lung cancer according to claim 1, it is characterised in that：The Bi
The mol ratio of roots of grass acid amides and rheum emodin is 1:1~1:5.
4. a kind of compound medicament composition with effect of anti-lung cancer according to claim 1, it is characterised in that：The compound
Pharmaceutical composition also contains pharmaceutically acceptable carrier.
5. a kind of compound medicament composition with effect of anti-lung cancer according to any one of Claims 1 to 4 is anti-in preparation
The purposes drenched in lung-cancer medicament.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109516926A (en) * | 2018-07-27 | 2019-03-26 | 四川大学 | A kind of preparation of piplartine derivative and anti-tumor activity |
| CN109602744A (en) * | 2018-12-13 | 2019-04-12 | 中国人民解放军总医院 | Piperlongumine is preparing the application in antibacterial-anti-inflammatory drug |
| CN109620836A (en) * | 2018-12-24 | 2019-04-16 | 陕西科技大学 | A kind of compound medicament composition with anti-breast cancer effect and application thereof and the drug based on this composition |
-
2017
- 2017-06-30 CN CN201710523641.9A patent/CN107260734B/en active Active
Non-Patent Citations (2)
| Title |
|---|
| JIE ZHENG等: ""Piperlongumine inhibits lung tumor growth via inhibition of nuclear factor kappa B signaling pathway"", 《SCIENTIFIC REPORTS》 * |
| LISHA ZHANG等: ""Sensitization of HER-2/neu-overexpressing non-small cell lung cancer cells to chemotherapeutic drugs by tyrosine kinase inhibitor emodin"", 《 ONCOGENE》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109516926A (en) * | 2018-07-27 | 2019-03-26 | 四川大学 | A kind of preparation of piplartine derivative and anti-tumor activity |
| CN109516926B (en) * | 2018-07-27 | 2021-09-17 | 四川大学 | Preparation and application of piperlonguminine derivative |
| CN109602744A (en) * | 2018-12-13 | 2019-04-12 | 中国人民解放军总医院 | Piperlongumine is preparing the application in antibacterial-anti-inflammatory drug |
| CN109620836A (en) * | 2018-12-24 | 2019-04-16 | 陕西科技大学 | A kind of compound medicament composition with anti-breast cancer effect and application thereof and the drug based on this composition |
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| CN107260734B (en) | 2020-07-28 |
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