CN109045050A - Polygonin paclitaxel composition and purposes - Google Patents
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- CN109045050A CN109045050A CN201811049845.4A CN201811049845A CN109045050A CN 109045050 A CN109045050 A CN 109045050A CN 201811049845 A CN201811049845 A CN 201811049845A CN 109045050 A CN109045050 A CN 109045050A
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- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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Abstract
The invention discloses polygonin paclitaxel composition and purposes, polygonin paclitaxel composition is made of polygonin and taxol that mass ratio is 440.17-510.00:1.Experiments have shown that: polygonin is combined within the scope of mass ratio 440.17-510.00:1 to compatibility utilization with taxol, can preferably cooperate with and inhibit human lung cancer, breast cancer, the activity of ovarian cancer cell；The therapeutic effect of attenuation synergistic can be also preferably played at the same time.Therefore, polygonin and Paclitaxel combinations can be prepared into prevention and treatment human lung cancer drug, prevention and treatment human breast carcinoma drug or prevention and treatment human ovarian cancer drug as effective component at composition.
Description
Technical field
The invention belongs to medical applications field, be related to polygonin paclitaxel composition preparation prevention and treatment human lung cancer, breast cancer,
The purposes of Ovarian Cancer tumour medicine.
Background technique
Currently, malignant tumour has become the disease for seriously threatening human health and life.Since population increases, aging mistake
Fast and people's bad life habits etc. influence, on the disease incidence of malignant tumour continues in worldwide in recent years
It rises[1].Lung cancer is as one of most common malignant tumour, and the morbidity and mortality of whole world lung cancer are in rising situation at present, especially
It is in the Economic Development in China man such as China.In China, as commercial speeds are accelerated, environmental pollution exacerbation, aging of population add
Play increasingly aggravates so as to cause the cancer burden of lung cancer[2-3].The breast cancer malignant tumour one of common as women, morbidity
Rate is high, and invasion is strong, easily occurs recurring and shifting；And its disease incidence is rising year by year, and the trend with rejuvenation[4].And
The oophoroma malignant tumour common as female reproductive system second, according to ASSOCIATE STATISTICS, the result shows that, the whole world is annual about
225000 new cases, survival rate only about 30%[5].However, clinic is directed to some biographies of above three cancer kind patient at present
System chemotherapy regimen, it is not good enough for the existence and outcome of progressive stage；At the same time, related targeted drug is treated often again
It can not be suitble to every patient.Therefore, it continues deeper into and seeks screening novel clinical anticancer drug, for finding human lung cancer, breast cancer
With the new method of oophoroma prevention and treatment, the breakthrough for seeking the treatment of its broad spectrum activity is of great significance.
Occupy in the chemotherapy field of malignant tumour from the related effective component extracted in natural plants extremely important
Status.It is reported that nearly 47% is natural in 155 kinds of small molecule anti-malignant tumor medicines of exploitation in 1940 to 2006
Plant extracts or derivatives thereof[6], among these just include the taxol (Taxol) from Chinese yew.Taxol is a kind of multiple
Miscellaneous tetracyclic diterpene compound, 1971 for the first time by Wani etc. from the tree of yewtree Taxus brevifolia Nutt.
It is extracted in skin and determines its structure[7].Currently, taxol is clinically widely used for lung cancer, breast cancer, oophoroma
With the treatment of part H/N tumors and malignant tumor of digestive tract, but it still can generate some toxicities, such as: alopecia, marrow
Transplanting, flush, muscle arthrosis are ached.
Polygonin (Polydatin, PD) is the drying from polygonaceae arsesmart polygonum cuspidate (Polygonum Cuspidatum)
The 4th kind of monomer extracted in rhizome, it is also known as polygonum cuspidatum crystal 4, while also known as polydatin, in grape and grape wine
Largely exist.In recent years, both at home and abroad related scholar to some of polygonin research shows that: polygonin is in anti-platelet aggregation/anti-
Microcirculation etc. of vital tissue organ has after thrombosis, reinforcement mycardial contractility and diastolic function, improvement shock
Remarkable effect[8-14]；At the same time, polygonin also has to mitigate chronic ache caused by endometriosis and improve and tie
The effects of enteritis[15,16].Derivative of the polygonin as resveratrol, before relevant some basic research are the results show that white
Veratryl alcohol has preferable effect for the prevention and treatment of malignant tumour[17-20]。
Chinese Patent Application No. 2018101759652 discloses a kind of polygonin paclitaxel composition and prevents and treats stomach in preparation
The purposes of portion's malignant tumor medicine, disclosing polygonin and paclitaxel composition mass ratio in the publication is 22.65-33.77:
There is inhibiting effect to gastric carcinoma cells under 1 proportion.But the composition of polygonin and taxol is for preventing and treating human lung cancer, mammary gland
The effect of cancer, Ovarian Cancer tumour yet there are no report.
Summary of the invention
The purpose of the present invention is overcome the deficiencies of the prior art and provide a kind of polygonin paclitaxel composition.
A second object of the present invention is to provide a kind of polygonin paclitaxel compositions to prepare prevention and treatment human lung cancer medicine in preparation
Object, prevention and treatment human breast carcinoma drug or the purposes for preventing and treating human ovarian cancer drug.
Technical solution of the present invention is summarized as follows:
Polygonin paclitaxel composition is made of polygonin and taxol that mass ratio is 440.17-510.00:1.
The molecular formula of the polygonin is C20H22O8；Shown in structural formula formula (I):
The molecular formula of the taxol is C47H51NO14；Shown in structural formula Formula II:
Above-mentioned polygonin paclitaxel composition prepares prevention and treatment human lung cancer drug, prevention and treatment human breast carcinoma drug or prevention and treatment in preparation
The purposes of human ovarian cancer drug.
The present invention is mainly proved with cell biological functional experiment: by polygonin and taxol in mass ratio 440.17-
Combine compatibility within the scope of 510.00:1 to use, can preferably cooperate with and inhibit human lung cancer, breast cancer, the activity of ovarian cancer cell；With
This can also preferably play the therapeutic effect of attenuation synergistic simultaneously.It therefore, can be by polygonin and Paclitaxel combinations at composition
Preparation prevention and treatment human lung cancer drug, prevention and treatment human breast carcinoma drug or prevention and treatment human ovarian cancer drug are prepared as effective component.
Detailed description of the invention
Fig. 1 polygonin paclitaxel composition acts on human lung carcinoma cell LTEP-A-2 in different quality ratio range, observation
Concrete condition of the two in terms of collaboration (action time is for 24 hours).Note: Fig. 1 (I) A: blank group；B:PD IC50 group；C:Taxol
IC50 group；D:Taxol IC50+PD IC50 group.Fig. 1 (II) A: blank group；B:PD IC50 group；C:Taxol 0.5IC50 group；
D:Taxol 0.5IC50+PD IC50 group.Fig. 1 (III) A: blank group；B:PD IC50 group；C:Taxol 0.25IC50 group；D:
Taxol 0.25IC50+PD IC50 group.Fig. 1 (IV) A: blank group；B:PD IC50 group；C:Taxol 0.1IC50 group；D:
Taxol 0.1IC50+PD IC50 group.
Fig. 2 polygonin paclitaxel composition acts on human lung carcinoma cell GLC-82, observation two in different quality ratio range
Concrete condition of the person in terms of collaboration (action time is for 24 hours).Note: Fig. 2 (I) A: blank group；B:PD IC50 group；C:Taxol
IC50 group；D:Taxol IC50+PD IC50 group.Fig. 2 (II) A: blank group；B:PD IC50 group；C:Taxol 0.5IC50 group；
D:Taxol 0.5IC50+PD IC50 group.Fig. 2 (III) A: blank group；B:PD IC50 group；C:Taxol 0.25IC50 group； D:
Taxol 0.25IC50+PD IC50 group.Fig. 2 (IV) A: blank group；B:PD IC50 group；C:Taxol 0.1IC50 group； D:
Taxol 0.1IC50+PD IC50 group.
Fig. 3 polygonin paclitaxel composition acts on human lung carcinoma cell LTEP-A-2 in different quality ratio range, observation
Concrete condition of the two in terms of attenuation synergistic (action time is for 24 hours).Note: Fig. 3 (I) A: blank group；B:Taxol IC50 group；
C:Taxol 0.5IC50 group；D:Taxol 0.5IC50+PD IC50 group.Fig. 3 (II) A: blank group；B:Taxol IC50 group；C:
Taxol 0.25IC50 group；D:Taxol 0.25IC50+PD IC50 group.Fig. 3 (III) A: blank group；B:Taxol IC50 group；
C:Taxol 0.1IC50 group；D:Taxol 0.1IC50+PD IC50 group.
Fig. 4 polygonin paclitaxel composition acts on human lung carcinoma cell GLC-82, observation two in different quality ratio range
Concrete condition of the person in terms of attenuation synergistic (action time is for 24 hours).Note: Fig. 4 (I) A: blank group；B:Taxol IC50 group；C:
Taxol 0.5IC50 group；D:Taxol 0.5IC50+PD IC50 group.Fig. 4 (II) A: blank group；B:Taxol IC50 group； C:
Taxol 0.25IC50 group；D:Taxol 0.25IC50+PD IC50 group.Fig. 4 (III) A: blank group；B:Taxol IC50 group；
C:Taxol 0.1IC50 group；D:Taxol 0.1IC50+PD IC50 group.
Fig. 5 polygonin paclitaxel composition acts on human breast cancer cell MDA-MB-231 in different quality ratio range,
Concrete condition of both observations in terms of collaboration (action time is for 24 hours).Note: Fig. 5 (I) A: blank group；B:PD IC50 group； C:
Taxol IC50 group；D:Taxol IC50+PD IC50 group.Fig. 5 (II) A: blank group；B:PD IC50 group；C:Taxol
0.5IC50 group；D:Taxol 0.5IC50+PD IC50 group.
Fig. 6 polygonin paclitaxel composition acts on human breast cancer cell line MDA-MB-453 in different quality ratio range,
Concrete condition of both observations in terms of collaboration (action time is for 24 hours).Note: Fig. 6 (I) A: blank group；B:PD IC50 group； C:
Taxol IC50 group；D:Taxol IC50+PD IC50 group.Fig. 6 (II) A: blank group；B:PD IC50 group；C:Taxol
0.5IC50 group；D:Taxol 0.5IC50+PD IC50 group.
Fig. 7 polygonin paclitaxel composition acts on human breast cancer cell MDA-MB-231 in different quality ratio range,
Concrete condition of both observations in terms of attenuation synergistic (action time is for 24 hours).Note: Fig. 7 A: blank group；B:Taxol IC50 group；
C:Taxol 0.5IC50 group；D:Taxol 0.5IC50+PD IC50 group.
Fig. 8 polygonin paclitaxel composition acts on human breast cancer cell line MDA-MB-453 in different quality ratio range,
Concrete condition of both observations in terms of attenuation synergistic (action time is for 24 hours).Note: Fig. 8 A: blank group；B:Taxol IC50 group；
C:Taxol 0.5IC50 group；D:Taxol 0.5IC50+PD IC50 group.
Fig. 9 polygonin paclitaxel composition acts on Proliferation of Human Ovarian Cell SKOV-3 in different quality ratio range, observation
Concrete condition of the two in terms of collaboration (action time is for 24 hours).Note: Fig. 9 (I) A: blank group；B:PD IC50 group；C:Taxol
IC50 group；D:Taxol IC50+PD IC50 group.Fig. 9 (II) A: blank group；B:PD IC50 group；C:Taxol 0.5IC50 group；
D:Taxol 0.5IC50+PD IC50 group.Fig. 9 (III) A: blank group；B:PD IC50 group；C:Taxol 0.25IC50 group；D:
Taxol 0.25IC50+PD IC50 group.Fig. 9 (IV) A: blank group；B:PD IC50 group；C:Taxol 0.1IC50 group；D:
Taxol 0.1IC50+PD IC50 group.
Figure 10 polygonin paclitaxel composition acts on Proliferation of Human Ovarian Cell 3AO, observation two in different quality ratio range
Concrete condition of the person in terms of collaboration (action time is for 24 hours).Note: Figure 10 (I) A: blank group；B:PD IC50 group；C:Taxol
IC50 group；D:Taxol IC50+PD IC50 group.Figure 10 (II) A: blank group；B:PD IC50 group；C:Taxol 0.5IC50
Group；D:Taxol 0.5IC50+PD IC50 group.
Figure 11 polygonin paclitaxel composition acts on Proliferation of Human Ovarian Cell SKOV-3 in different quality ratio range, observation
Concrete condition of the two in terms of attenuation synergistic (action time is for 24 hours).Note: Figure 11 (I) A: blank group；B:Taxol IC50 group；
C:Taxol 0.5IC50 group；D:Taxol 0.5IC50+PD IC50 group.Figure 11 (II) A: blank group；B:Taxol IC50 group；
C:Taxol 0.25IC50 group；D:Taxol 0.25IC50+PD IC50 group.Figure 11 (III) A: blank group；B:Taxol IC50
Group；C:Taxol 0.1IC50 group；D:Taxol 0.1IC50+PD IC50 group.
Figure 12 polygonin paclitaxel composition acts on Proliferation of Human Ovarian Cell 3AO, observation two in different quality ratio range
Concrete condition of the person in terms of attenuation synergistic (action time is for 24 hours).Note: Figure 12 A: blank group；B:Taxol IC50 group；C:
Taxol 0.5IC50 group；D:Taxol 0.5IC50+PD IC50 group.
Specific embodiment
Experiment is provided with humanized's lung carcinoma cell LTEP-A-2 from Shanghai Inst. of Life Science, CAS cell
Source center, humanized's lung carcinoma cell GLC-82 is in Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences's preclinical medicine cell
The heart, humanized's breast cancer cell MDA-MB-231 (HTB-26TM) and MDA-MB-453 (HTB-131TM) come
Derived from U.S.'s ATCC collection, humanized's ovarian cancer cell SKOV-3 (HTB-77TM) protected from U.S. ATCC
Hiding center, humanized's ovarian cancer cell 3AO from Shanghai after and Biotechnology Co., Ltd.
Below with reference to specific example, the present invention is further illustrated.
Embodiment 1
The molecular formula of polygonin is C20H22O8；Shown in structural formula Formulas I:
The molecular formula of the taxol is C47H51NO14；Structural formula is shown in Formula II:
Using polygonin paclitaxel composition as active constituent, the auxiliary material that pharmaceutical acceptable is added can be made into respectively according to a conventional method
The liquid injection agent of kind specification.
The administration route of polygonin paclitaxel composition includes a variety of administration routes, such as drug administration by injection, intracavitary administration etc..
Embodiment 2
Polygonin paclitaxel composition is made of polygonin and taxol that mass ratio is 440.17:1.
Embodiment 3
Polygonin paclitaxel composition is made of polygonin and taxol that mass ratio is 475.09:1.
Embodiment 4
Polygonin paclitaxel composition is made of polygonin and taxol that mass ratio is 510.00:1.
Embodiment 5
Select human lung cancer cell line LTEP-A-2 and GLC-82, human breast cancer cell line MDA-MB-231 and MDA-MB-
453, abortion syndrome SKOV-3 and 3AO are tested.Detected by CCK-8 method, discovery PD can effectively inhibit human lung cancer,
Breast cancer, the growing multiplication of ovarian cancer cell are active (table 1).In action time section (for 24 hours), PD can inhibit in concentration dependent
Human lung cancer, breast cancer, the activity of ovarian cancer cell line.
PD handles human lung cancer cell line LTEP-A-2 with GLC-82 in corresponding IC for 24 hours50Be respectively as follows: 395.23 μ g/mL and
303.54μg/mL；
PD handles human breast cancer cell line MDA-MB-231 with MDA-MB-453 in corresponding IC for 24 hours50It is respectively as follows:
395.57 μ g/mL and 305.87 μ g/mL；
PD handles abortion syndrome SKOV-3 with 3AO in corresponding IC for 24 hours50Be respectively as follows: 316.55 μ g/mL and
392.72μg/mL。
Embodiment 6
Taxol inhibits a variety of human lung cancers, breast cancer, the activity of Ovarian Cancer tumour cell.
We select human lung cancer cell line LTEP-A-2 and GLC-82, human breast cancer cell line MDA-MB-231 and MDA-
MB-453, abortion syndrome SKOV-3 and 3AO are tested.It is detected by CCK-8 method, discovery Taxol can effectively inhibit
Human lung cancer, breast cancer, the growing multiplication of ovarian cancer cell are active (table 1).In action time section (for 24 hours), Taxol can be in dense
It spends dependence and inhibits human lung cancer, breast cancer, the activity of ovarian cancer cell.
Taxol handles human lung cancer cell line LTEP-A-2 with GLC-82 in corresponding IC for 24 hours50Be respectively as follows: 5.71 μ g/mL and
7.35μg/mL；
Taxol handles human breast cancer cell line MDA-MB-231 with MDA-MB-453 in corresponding IC for 24 hours50It is respectively as follows:
0.89 μ g/mL and 1.51 μ g/mL；
Taxol handles abortion syndrome SKOV-3 with 3AO in corresponding IC for 24 hours50Be respectively as follows: 4.23 μ g/mL and
2.90μg/mL。
1 polygonin of table acts on each cell corresponding IC50 value for 24 hours with taxol.
Embodiment 7
Composition collaboration of the invention inhibits human lung cancer, breast cancer, the activity of Ovarian Cancer tumour cell.
We select human lung cancer cell line LTEP-A-2 and GLC-82, human breast cancer cell line MDA-MB-231 with
MDA-MB-453, abortion syndrome SKOV-3 and 3AO are tested, and are detected by CCK-8 method, are found this hair
Bright composition is compared with respective single medicine effect, to human lung cancer, breast cancer, the growing multiplication activity suppression effect of ovarian cancer cell
Significantly (Fig. 1, Fig. 2, Fig. 5, Fig. 6, Fig. 9, Figure 10).In action time section (for 24 hours), PD and Taxol composition can significantly inhibit
Human lung cancer, breast cancer, ovarian cancer cell growth activity.
In Fig. 1, the quality proportioning of the two composition is respectively as follows: (I) mPD:mTaxol=71.82:1；(II)mPD:mTaxol=
131.67: 1；(III)mPD:mTaxol=263.33:1；(IV)mPD:mTaxol=790.00:1.
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (71.82-790.00): when 1, with respective single medicine
It compares, there is significant inhibiting effect to human lung cancer cell line LTEP-A-2.
In Fig. 2, the quality proportioning of the two composition is respectively as follows: (I) mPD:mTaxol=40.47:1；(II)mPD:mTaxol=
86.71: 1；(III)mPD:mTaxol=151.75:1；(IV)mPD:mTaxol=607.00:1.
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (40.47-607.00): when 1, with respective single medicine
It compares, there is significant inhibiting effect to human lung cancer cell line GLC-82.
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (71.82-607.00): thin to human lung cancer when 1
Born of the same parents system LTEP-A-2 and GLC-82 has significant inhibiting effect.
In Fig. 5, the quality proportioning of the two composition is respectively as follows: (I) mPD:mTaxol=395.50:1；(II)mPD:mTaxol=
791.00: 1。
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (395.50-791.00): when 1, with respective single medicine
It compares, there is significant inhibiting effect to human breast cancer cell line MDA-MB-231.
In Fig. 6, the quality proportioning of the two composition is respectively as follows: (I) mPD:mTaxol=255.00:1；(II)mPD:mTaxol=
(510.00:1 embodiment 4).
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (255.00-510.00): when 1, with respective single medicine
It compares, there is significant inhibiting effect to human breast cancer cell line MDA-MB-453.
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (395.50-510.00): when 1, to human breast carcinoma
Cell line MDA-MB-231 and MDA-MB-453 have significant inhibiting effect.
In Fig. 9, the quality proportioning of the two composition is respectively as follows: (I) mPD:mTaxol=79.13:1；(II)mPD:mTaxol=
158.25: 1；(III)mPD:mTaxol=316.50:1；(IV)mPD:mTaxol=633.00:1.
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (79.13-633.00): when 1, with respective single medicine
It compares, there is significant inhibiting effect to abortion syndrome SKOV-3.
In Figure 10, the quality proportioning of the two composition is respectively as follows: (I) mPD:mTaxol=440.17:1 (embodiment 2)；(II)
mPD: mTaxol=880.34:1.
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (440.17-880.34): when 1, with respective single medicine
It compares, there is significant inhibiting effect to abortion syndrome 3AO.
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (440.17-633.00): when 1, to human ovarian cancer
Cell line SKOV-3 and 3AO have significant inhibiting effect.
Experiments have shown that: the m of polygonin paclitaxel compositionPD:mTaxolFor (440.17-510.00): when 1, to above-mentioned people's lung
Cancerous cell line LTEP-A-2 and GLC-82, human breast cancer cell line MDA-MB-231 and MDA-MB-453, abortion syndrome
SKOV-3 and 3AO has significant inhibiting effect.
Embodiment 8
Composition of the invention plays the therapeutic effect of attenuation synergistic.
We select human lung cancer cell line LTEP-A-2 and GLC-82, human breast cancer cell line MDA-MB-231 and MDA-
MB-453, abortion syndrome SKOV-3 and 3AO are tested, and are detected by CCK-8 method, discovery PD and Taxol composition
Compared with Taxol mono- medicine effect, to human lung cancer, breast cancer, the growing multiplication activity suppression significant effect of ovarian cancer cell (Fig. 3,
Fig. 4, Fig. 7, Fig. 8, Figure 11, Figure 12).In action time section (for 24 hours), PD and Taxol composition can significantly inhibit human lung cancer,
The growth activity of breast cancer, ovarian cancer cell, and effect and respective TaxolIC50Group is compared to preferable.In Fig. 3, the two composition
Quality proportioning be respectively as follows: (I) mPD:mTaxol=131.67:1；(II)mPD: mTaxol=263.33:1；(III)mPD:mTaxol=
790.00:1.In Fig. 4, the quality proportioning of the two composition is respectively as follows: (I) mPD:mTaxol=86.71:1；(II)mPD:mTaxol=
151.75:1；(III)mPD:mTaxol=607.00:1.In Fig. 7, the quality proportioning of the two composition is respectively as follows: mPD:mTaxol=
791.00:1.In Fig. 8, the quality proportioning of the two composition is respectively as follows: mPD:mTaxol=510.00:1.In Figure 11, the two combination
The quality proportioning of object is respectively as follows: (I) mPD:mTaxol=158.25:1；(II) mPD:mTaxol=316.50:1；(III)mPD:mTaxol
=633.00:1.In Figure 12, the quality proportioning of the two composition is respectively as follows: mPD:mTaxol=880.34:1.
It is above-mentioned the experimental results showed that, by polygonin and paclitaxel composition within the scope of mass ratio 440.17-510.00:1
Joint compatibility with can preferably cooperate with inhibit human lung cancer, breast cancer, ovarian cancer cell growth activity；It at the same time can also be compared with
The therapeutic effect of attenuation synergistic is played well.Because PD and Taxol composition have the function of this, therefore it can be used as effective component preparation tool
Have inhibit human lung cancer, breast cancer, Ovarian Cancer growth of tumour cell drug.
Leading reference:
1.Jemal A,Bray F,Center MM,et al.Global cancer statistics.CA Cancer J
Clin.2011；61(2):69-90.
2.Parkin DM,Bray F,Ferlay J,et al.Global cancer statistics,2002[J].CA
Cancer J Clin,2005,55(2):74-108.
3.Jemal A,Bray F,Center MM,et al.Global cancer statistics[J].CA
Cancer J Clin,2011,61(2):69-90.
4. Zhong Wei is blue, Lu Meiyu, spring maple is taken charge of, breast cancer targeted Therapy [J] modern times medical oncology is waited,
2018,26(4):622-626.
5.Ramalingam P.Morphologic,Immunophenotypic,and Molecular Features of
Epithelial Ovarian Cancer[J].Oncology(Williston Park),2016,30(2):166-76.
6.Newman DJ,Cragg GM.Natural products as sources of new drugsover the
last 25years.Nat Prod.2007；70(3):461–477.
7.Wani MC,Taylor HL,Wall M E,et al.Plant antitumor agents.VI.The
isolation and structure of taxol,a novel antileukemic and antitumor agent
from Taxus brevifolia.J Am Chem Soc,1971,93(9):2325.
8.Gao JP,Chen CX,Gu WL,et al.Effects of polydatin on attenuating
ventricular remodeling in isoproterenol-induced mouse and pressure-overload
rat models.Fitoterapia.2010；81(7):953-960.
9.Zhang LP,Ma HJ,Bu HM,et al.Polydatin attenuates ischemia/
reperfusion-induced apoptosis in myocardium of the rat.Sheng Li Xue Bao.2009；
61:367-72.
10.Zhang PW,Yu CL,Wang YZ,et al.Influence of 3,4,5-trihydroxystibene-
3-beta-mono-D- glucoside on vascular endothelial epoprostenol and platelet
aggregation.Acta Pharmacologica Sinica.1995；16:265–268.
11.Wang X,Song R,Chen Y et al.Polydatin-a new mitochondria protector
for acute severe hemorrhagic shock treatment.Expert Opin Investig Drugs.2013；
22(2):169-179.
12.Wang X,Song R,Bian HN,et al.Polydatin,a natural polyphenol,
protects arterial smooth muscle cells against mitochondrial dysfunction and
lysosomal destabilization following hemorrhagic shock.Am J Physiol Regul
Integr Comp Physiol.2012；302(7):R805-814.
13.Cheng Y,Zhang HT,Sun L,et al.Involvement of cell adhesion
molecules in polydatin protection of brain tissues from ischemia-reperfusion
injury.Brain Res.2006；1110(1):193-200.
14.Miao Q,Wang S,Miao S,et al.Cardioprotective effect of polydatin
against ischemia/reperfusion injury:roles of protein kinase C and mito K(ATP)
activation.Phytomedicine.2011；19(1):8-12.
15.Indraccolo U,Barbieri F.Effect of palmitoylethanolamide-polydatin
combination on chronic pelvic pain associated with endometriosis:preliminary
observations.Eur J Obstet Gynecol Reprod Biol.2010；150(1):76-79.
16.Yao J,Wang JY,Liu L,et al.Polydatin ameliorates DSS-induced
colitis in mice through inhibition of nuclear factor-kappa B
activation.Planta Med.2011；77(5):421-427.
17.Liu PL,Tsai JR,Charles AL,et al.Resveratrol inhibits human lung
adenocarcinoma cell metastasis by suppressing heme oxygenase 1-mediated
nuclear factor-kappaB pathway and subsequently downregulating expression of
matrix metalloproteinases.Mol Nutr Food Res.2010；54(suppl 2):S196–S204.
18.Zhou HB,Chen JJ,Wang WX,et al.Anticancer activity of resveratrol
on implanted human primary gastric carcinoma cells in nude mice.World J
Gastroenterol.2005；11(2):280–284.
19.Busquets S,Ametller E,Fuster G,et al.Resveratrol,a natural
diphenol,reduces metastatic growth in an experimental cancer model.Cancer
Lett.2007；245(1-2):144–148.
20.Kim KH,Back JH,Zhu Y,et al.Resveratrol targets transforming growth
factor-β2 signaling to block UV-induced tumor progression.J Invest
Dermatol.2011；131(1):195-202 .
Claims (4)
1. polygonin paclitaxel composition, it is characterized in that the polygonin and taxol group that are 440.17-510.00:1 by mass ratio
At.
2. composition according to claim 1, it is characterized in that the molecular formula of the polygonin is C20H22O8；Structural formula formula
(I) shown in:
3. composition according to claim 1, it is characterized in that the molecular formula of the taxol is C47H51NO14；Structural formula is used
Shown in formula (II):
4. the polygonin paclitaxel composition of one of claim 1-3 is in preparation prevention and treatment human lung cancer drug, prevention and treatment human breast carcinoma medicine
Object or the purposes for preventing and treating human ovarian cancer drug.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019165987A1 (en) * | 2018-03-02 | 2019-09-06 | 天津市肿瘤医院 | Polydatin paclitaxel composition, and application in preparing medicament for preventing and treating gastric malignant tumor |
| CN110974840A (en) * | 2019-12-27 | 2020-04-10 | 天津市肿瘤医院 | Steroid sulfatase inhibitor and pharmaceutical application thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102058609A (en) * | 2010-12-30 | 2011-05-18 | 苏州大学 | Application of polydatin to preparing antineoplastic drug |
-
2018
- 2018-09-10 CN CN201811049845.4A patent/CN109045050A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102058609A (en) * | 2010-12-30 | 2011-05-18 | 苏州大学 | Application of polydatin to preparing antineoplastic drug |
Non-Patent Citations (6)
| Title |
|---|
| HU, MENGYIN 等: "Polymer micelle-based combination therapy of paclitaxel and resveratrol with enhanced and selective antitumor activity.", 《RSC ADVANCES》 * |
| KUBOTA T 等: "Combined effects of resveratrol and paclitaxel on lung cancer cells.", 《 ANTICANCER RES.》 * |
| ZHAO, WEIGUO 等: "Resveratrol down-regulates survivin and induces apoptosis in human multidrug-resistant SPC-A-1/CDDP cells.", 《ONCOLOGY REPORTS》 * |
| 吴异兰等: "白藜芦醇对肺癌紫杉醇耐药细胞的增殖抑制作用及其机制.", 《CARCINOGENESIS, TERTOGENESIS & MUTAGENSIS》 * |
| 崔秀娟: "白藜芦醇与紫杉醇联合应用对肺癌细胞PC9的杀伤效应.", 《蚌埠医学院学报》 * |
| 张玉松.: "虎杖苷抗肿瘤作用及机制研究.", 《苏州大学博士学位论文》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019165987A1 (en) * | 2018-03-02 | 2019-09-06 | 天津市肿瘤医院 | Polydatin paclitaxel composition, and application in preparing medicament for preventing and treating gastric malignant tumor |
| CN110974840A (en) * | 2019-12-27 | 2020-04-10 | 天津市肿瘤医院 | Steroid sulfatase inhibitor and pharmaceutical application thereof |
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