CN107050015A - Ovum South America chrysanthemum element is used as the application prepared in anti-lung cancer, liver cancer and colon cancer drug - Google Patents
Ovum South America chrysanthemum element is used as the application prepared in anti-lung cancer, liver cancer and colon cancer drug Download PDFInfo
- Publication number
- CN107050015A CN107050015A CN201610921609.1A CN201610921609A CN107050015A CN 107050015 A CN107050015 A CN 107050015A CN 201610921609 A CN201610921609 A CN 201610921609A CN 107050015 A CN107050015 A CN 107050015A
- Authority
- CN
- China
- Prior art keywords
- ovum
- south america
- chrysanthemum
- chrysanthemum element
- cancer
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
Landscapes
- 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)
- Medicines Containing Plant Substances (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
It is that a kind of ovum South America chrysanthemum is plain as the application prepared in anti-lung cancer, liver cancer and colon cancer drug the present invention relates to pharmaceutical technology field；There is different degrees of inhibitory action to human lung carcinoma cell line A549, human hepatoma cell strain BEL 7402 and human colon cancer cell strain 29 3 kinds of cell lines of HT growth present invention firstly provides ovum South America chrysanthemum element；And ovum South America chrysanthemum element is substantially better than positive drug TPT to human hepatoma cell strain BEL 7402 and human colon cancer cell strain 29 two kinds of cell lines of HT growth in vitro inhibitory action（Topotecan hydrochloride）, to human lung carcinoma cell line A549 growth in vitro inhibitory action and positive drug TPT（Topotecan hydrochloride）Effect is more close；Illustrate that ovum South America chrysanthemum element has obvious antitumor action to external lung carcinoma cell, liver cancer cells and colon cancer cell, with preferable prospect in medicine.
Description
Technical field
It is that a kind of ovum South America chrysanthemum element is used as preparation anti-lung cancer, liver cancer and colon cancer medicine the present invention relates to pharmaceutical technology field
Application in thing.
Background technology
Cancer seriously threatens human health.The incidence of disease of cancer persistently rises in recent years, as being only second to cardiovascular and cerebrovascular disease
The second largest fatal disease of disease.With the progress of medical science, a large amount of antineoplastics are clinically emerged.But chemotherapeutics
Toxic side effect makes its clinical practice receive very big limitation, and excavate small, the cheap chemotherapeutics of toxic side effect turns into doctor
A medicine worker big problem urgently to be resolved hurrily.
Tumour is body under the effect of various carcinogenic factors, and some cell of local organization loses pair on gene level
Its normal regulation grown, causes abnormality formed by its clonal abnormality hyperplasia.The neoplastic disease number of cases of China is quite huge
Greatly, there is data to show and account for the 55% of whole world case load.
Husky Inula britannica chinensis (Inulasalsoloides (Turcz.) Ostenf.) is composite family Inula, and perennial herb is planted
Thing.It is mainly distributed on Xinjiang of China, Gansu, Shaanxi, the Inner Mongol, Hebei, North Qinghai and east, North of Shanxi and western Liaoning Province
Deng area.Also known as twist maggot climb (《Inner Mongol Chinese herbal medicine》), bald woman grass, yellow lama, artemisia annua, knotweed it is plain (《Soft science in China
Medicinal plant》), the Ursula (illiteracy name) of leaflet inular flower, E Lesen-I is smooth-all, sand ground Inula britannica chinensis, Huang Penghua, small Inula britannica chinensis,
Leopard cat eye.
The structure of natural products has novel and multifarious feature.The novel bioactive natural product of structure is guide's chemical combination
One of important sources of thing, it finds not only promote chemistry and the progress of study of pharmacy, it is also possible to cause medicine new target drone
It was found that.It is directly or indirectly from natural products, such as antineoplastic Japanese yew more than 60% in currently used antineoplastic
Alcohol and vinca alkaloids etc..The lead compound with antitumor activity, research are found from traditional Chinese medicine and medicinal plant
Its mechanism of action, so as to develop the focus that antineoplaston medicine is current research.
Husky Inula britannica chinensis main chemical compositions are compared with horn of plenty, and sesquiterpenoids is its characteristic constituents.In addition, the plant is also
Contain a small amount of triterpenes components.Sesquiterpenoids is the main active of husky Inula britannica chinensis, according to its carbon skeleton type Inula britannica chinensis
The sesquiterpenoids reported in platymiscium is broadly divided into acyclic sesquiterpene；Driffractive ring eucalyptus type；Olive alkane type；Germacrane and more wound
Wooden alkane type.In addition, Inulaplants also contain a small amount of diterpene-kind compound；Flavone compound and steroid compound.I
The husky Inula britannica chinensis of picking up from hotan area has been carried out by the chemical constitution study of system and has done anti tumor activity in vitro inspection
Survey, to the therefrom isolated compound with antitumor activity.
Ovum South America chrysanthemum element is the extract of husky Inula britannica chinensis, belongs to natural products, is germacrane sequiterpene.Ovum South America chrysanthemum
Element has significant supression to act on to human mouth epidermoid carcinoma cell KB and mouse lymphocyte leukaemia P-388, in
Document (Gopalakrishna E.M., Watson W.H..Ovatifolin, asesquiterpene lactone [J]
.J.Cryst.Mol.Struct..1977,7:49-57.) middle report.But, not yet have been reported that relevant ovum South America chrysanthemum element is right so far
Lung, liver, the supression effect of colon-cancer cell.With people going deep into its chemistry and biology research, its molecular mechanism of action
Will progressively clearly, this will further promote the modifying for chemical structure and structure activity study of such compound, and be favorably improved
The medical value of husky Inula britannica chinensis.
The content of the invention
The invention provides a kind of ovum South America chrysanthemum element as the application prepared in anti-lung cancer, liver cancer and colon cancer drug, gram
The deficiency of above-mentioned prior art is taken, it can effectively solve not yet to have been reported that relevant ovum South America chrysanthemum element is thin to lung, liver, intestinal cancer so far
The problem of supression of born of the same parents is acted on.
The technical scheme is that realized by following measures：A kind of ovum South America chrysanthemum element conduct preparation anti-lung cancer,
Application in liver cancer and colon cancer drug.
Here is the further optimization and/or improvements to foregoing invention technical scheme：
Above-mentioned ovum South America chrysanthemum element is to be extracted from husky Inula britannica chinensis or other Inulaplants, purified isolated；
Or, ovum South America chrysanthemum element obtains for chemical synthesis process.
The formulation of above-mentioned ovum South America chrysanthemum element is tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, ebonite
One kind in wafer, soft capsule, oral liquid, mouth containing agent, granule, electuary, pill, powder, parenteral solution, powder-injection.
The chemical structural formula of above-mentioned ovum South America chrysanthemum element is：
Present invention firstly provides ovum South America chrysanthemum element to human lung carcinoma cell line A549, Human Hepatic Carcinoma Cell Line BEL-7402 and people
The growth of tri- kinds of cell lines of colon cancer cell line HT-29 has different degrees of inhibitory action；And ovum South America chrysanthemum element is to human liver cancer
The growth in vitro inhibitory action of cell line BEL-7402 and human colon cancer cell strain two kinds of cell lines of HT-29 is substantially better than positive drug
TPT (topotecan hydrochloride), to human lung carcinoma cell line A549 growth in vitro inhibitory action and positive drug TPT, (hydrochloric acid topology is replaced
Health) act on more close；Illustrate that ovum South America chrysanthemum element has to external lung carcinoma cell, liver cancer cells and colon cancer cell obvious anti-
Function of tumor, with preferable prospect in medicine.
Brief description of the drawings
Accompanying drawing 1 is the plain structural formula of compound ovum South America chrysanthemum.
Accompanying drawing 2 is compound ovum South America chrysanthemum element1H-NMR。
Accompanying drawing 3 is compound ovum South America chrysanthemum element13C-NMR。
Accompanying drawing 4 is the one-dimensional NOE of compound ovum South America chrysanthemum element.
Accompanying drawing 5 is the plain two dimension HMBC spectrums of compound ovum South America chrysanthemum.
Accompanying drawing 6 is compound ovum South America chrysanthemum element two dimension1H-1HCOSY is composed.
Accompanying drawing 7 is the plain high resolution mass spectrum of compound ovum South America chrysanthemum.
Accompanying drawing 8 is the crucial COSY (thick line) and HMBC (arrow) signal graph of ovum South America chrysanthemum element.
Embodiment
The present invention is not limited by following embodiments, can technique according to the invention scheme and actual conditions it is specific to determine
Embodiment.
Embodiment 1, the ovum South America chrysanthemum element is used as the application prepared in anti-lung cancer, liver cancer and colon cancer drug.
Embodiment 2, as the optimization of above-described embodiment, ovum South America chrysanthemum element is to be planted from husky Inula britannica chinensis or other Inulas
Extracted in thing, it is purified isolated；Or, ovum South America chrysanthemum element obtains for chemical synthesis process.
Embodiment 3, as the optimization of above-described embodiment, the formulation of ovum South America chrysanthemum element is tablet, sugar coated tablet, Film coated tablets
Agent, enteric coated tablet, capsule, hard capsule, soft capsule, oral liquid, mouth containing agent, granule, electuary, pill, powder, note
The one kind penetrated in liquid, powder-injection.
Embodiment 4, as the optimization of above-described embodiment, the chemical structural formula of ovum South America chrysanthemum element is：
Application of the above-mentioned ovum South America chrysanthemum element in anti-lung cancer, liver cancer and colon cancer drug is prepared is as follows：
First, the preparation of ovum South America chrysanthemum element
Ovum South America chrysanthemum element can obtain for chemical synthesis process；Ovum South America chrysanthemum element or from husky Inula britannica chinensis or other are sheathed
Extract, can be extracted by existing method in flower plant, a) by husky Inula britannica chinensis (pick up from hotan regional, plant sample by
The medicine research department researcher Yang Wei person of outstanding talent's identification of nationality of Inst. of Pharmacology, Xinjiang Uygur Autonomous Regions, and keep sample in Xinjiang Uygur certainly
Food research sensing chamber of Zhi Qu institutes of materia medica, marked as S.X.F.0001) herb 80kg is 50% to 95% with volume fraction
Ethanol soak extraction, it is 5 times of husky Inula britannica chinensis quality of medicinal material to be extracted, common soak extraction that the ethanol volume used is soaked every time
3 times, every time 24 hours；Merge ethanol soaked extracting solution, be concentrated under reduced pressure into no ethanol flavor；Adopt and concentrate 3 is extracted with ethyl acetate
Secondary, each 24h, the acetic acid ethyl acetate extract that is concentrated under reduced pressure obtains medicinal extract；
B) 1 is pressed with petroleum ether and ethyl acetate:0~0:The mixed solution of 1 volume ratio formation carries out gradient elution, enters one
Step optimize in petroleum ether and ethyl acetate volume ratio be 7:3 eluent, is detected by thin-layer chromatography, collects petroleum ether and second
Under acetoacetic ester expansion system, Rf values about 0.6, sulfuric acid-ethanol shows the component of purple, after being concentrated under reduced pressure under the conditions of less than 60 DEG C
Mass crystallization is separated out, crystallization once obtains ovum South America chrysanthemum element through absolute ethyl alcohol recrystallization again.
Ovum South America chrysanthemum element is white powder crystallization, and ESI/MS provides quasi-molecule peak m/z329.1342 [M+Na]+,
345.1291[M+K]+, with reference to carbon spectrum, hydrogen spectrum, one-dimensional NOE, two dimension HMBC, two dimension1H-1HCOSY determines that molecular formula is C17H22O5。
The compound spectrum (Jeske F., Huneck S., Jakupovic J..Further sesquiterpene
lactones from Inulasalsoloides.Pergamon.1996.41(6):1539-
1542.) report is basically identical, therefore determines that it is ovatifolin, is named as ovum South America chrysanthemum element.
The Structural Identification data of ovum South America chrysanthemum element are as follows：
HRESI-MS:329.1342[M+Na]+,345.1291[M+K]+；
[α]20D (c=0.10, MeOH):- 61.0 ° (c=0.10, MeOH)；
UV(MeOH):λmax(logε):206(3.6)nm；
IRnmax:3452,1739,1730,1717,1662,1652,1653cm-1；
1H-NMR(400MHz in CDCl3)、13C-NMR100MHz in CDCl3) and HMBC spectral datas be shown in Table 1；
Fig. 1 is the plain structural formula of compound ovum South America chrysanthemum；Fig. 2 is compound ovum South America chrysanthemum element1H-NMR；Fig. 3 is compound ovum South America chrysanthemum
Element13C-NMR；Fig. 4 is the one-dimensional NOE of compound ovum South America chrysanthemum element；Fig. 5 is the plain two dimension HMBC spectrums of compound ovum South America chrysanthemum；Fig. 6 is change
Compound ovum South America chrysanthemum element two dimension1H-1HCOSY is composed；Fig. 7 is the plain high resolution mass spectrum of compound ovum South America chrysanthemum；Fig. 8 is ovum South America chrysanthemum element
Crucial COSY (thick line) and HMBC (arrow) signal graph.
The plain Structural Identification process of ovum South America chrysanthemum
Ovum South America chrysanthemum element is colourless crystallization, is soluble in chloroform.HR-ESI-MS provides its quasi-molecular ion peak [M+Na]+m/
z329.1342(calcd for C17H22O5Na, 329.1359), its molecular formula is released for C17H22O5, calculate its degree of unsaturation
For 7,1H H NMR spectroscopies (table 1, Fig. 2-3) show a methyl signals in δH1.64 (s, 15-CH3), an acetonyl signal
δH2.17 (s ,-CH3), 4 alkene hydrogen signals 6.37 (1H, d, J=4.0Hz, H-13a), 5.58 (1H, d, J=4.0Hz, H-
13b), 5.14 (1H, dd, J=12.0,4.4Hz, H-1), 4.86 (1H, t, J=18.4,9.6Hz, H-5).Carbon spectrum provides 17
Carbon signal, including three ethylene linkage carbon signal δC136.7 (C-1), 142.2 (C-4), 127.9 (C-5), 133.2 (C-10),
138.5 (C-11), 120.6 (C-13)；Two ester group carbon signal δC170.2 (C-12), 170.8 (- Ac) and three oxygen-containing carbon
Signal δC75.0 (C-6), 70.2 (C-8) and 63.2 (C-14).The nuclear magnetic data for analyzing the compound can be seen that except acetyl
Base, the compound parent nucleus has 15 carbon, deducts three double bonds, 5 degrees of unsaturation of two carbonyls, also 2 degrees of unsaturation, table
Bright SX-1 is dicyclic compound, with reference to its source of students, and the compound is probably bicyclic sesquiterpenoids.Comprehensive analysis two-dimensional nucleus
Magnetic data can release the planar structure (Fig. 1) of the compound.1H-1H COSY (Fig. 6) spectrums show two spin system (H-
1/H-2/H-3/, H-5/H-6/H-7/H-8/H-9), therefore the compound has two fragment (fragment I:C-1-C-2-C-3, fragment
II:C-5-C-6-C7-C-8-C-9 Fig. 8) is seen.In HMBC spectrums (Fig. 5), δH4.80ppm, 4.57ppm (H-14) and 136.7ppm
(C-1), 42.5ppm (C-9) and 170.8ppm (acetyl carbonyl) is related；Show that acetyl group is connected on 14 carbon, C-14 is connected on C-
On 10 olefinic carbons；δH1.64ppm (15-CH3) and 39.2ppm (C-3), 142.2ppm (C-4), 127.9ppm (C-5) are related, say
Bright 15-CH3 is connected on 4 olefinic carbons；δH2.44,2.39ppm (H-2), 2.40,2.18ppm (H-3), 4.86ppm (H-5),
5.24ppm (H-6) is related to 142.4ppm (C-4), δH2.40,2.18ppm (H-3), 5.24ppm (H-6), 2.76ppm (H-
7) it is related to 127.9ppm (C-5), show that the head of fragment I tail end and fragment II passes through4,5△ is connected；C-10 and δH
5.14ppm (H-1), 2.4ppm (H-2), 4.60ppm (H-8), 2.96,2.31ppm (H-9), point out fragment I head and fragment II
Afterbody pass through1,10△ is connected, i.e., the first of SX-1 ring is 10 yuan of rings containing two ethylene linkages.δH 5.24ppm(H-6)
With 138.5ppm (C-11), 170.2ppm (C-12) correlations, 2.76ppm (H-7) and 138.5ppm (C-11), 170.2ppm (C-
12), 120.6ppm (C-13) is related, points out 6,7 and is connected to a lactone ring five membered, because there is two alkene hydrogen letters on 120.6ppm carbon
Numbers 6.37,5.58ppm, so have an exocyclic double bond, and H-7 is related to 120.6ppm, so double bond exists11,13△；δH
5.24ppm (H-6), 2.76ppm (H-7) and 2.96,2.31ppm (H-9) are related to 71.4ppm, and hydroxyl should be connected on 8.So far,
Draw the planar structure (Fig. 1) of the compound.Literature survey finds that the compound is identical with the structure of document report.(Jeske,
F,Huneck S,Jakupovic J,et
al.Furthersesquiterpene lactones from
Inulasalsoloides.Phytochemistry.1996；41(6):1539-1542.)(GneccoS,Philip-
PoyserJ,SilvaM.Sesquiterpene lactones from
Podanthusovatifolius.Phytochemistry.1973；12(10):2469-2477.)(Gopalakrishna EM,
Watson WH.Ovatifolin,asesquiterpene lactone.JCrystMolStruct.1977；7:49-57.) should
Compound is defined as ovum South America chrysanthemum element.
2nd, antitumor activity is verified using MTS colorimetric methods
2nd, antitumor activity is verified using MTS colorimetric methods
Cell line processing
A549 human lung carcinoma cell lines, BEL-7402 human hepatoma cell strains, the strain of HT-29 human colon cancer cells, 37 DEG C, 5%
It is incubated under CO2 and saturated humidity environment containing 10% hyclone McCoy ' s5A culture mediums, RPMI1640 culture mediums, DMEM/F-
In 12 culture mediums, cell is passed on when increasing in logarithm, adjustment cell concentration to 1 × 104Individual/mL, is inoculated in the culture of 96 holes
Plate, 190 μ L are added per hole, are incubated 18h to 24h and are carried out subsequent experimental.
It is prepared by model
Tumor cell line is grouped at random：1. Normal group (control)：With the McCoy ' containing 10% hyclone
S5A culture mediums or 1640 culture mediums or DMEM/F-12 culture mediums continue to cultivate, and final volume is supplemented to 200 μ L (replenisher and samples
Solution is same)；2. screening sample group (sample)：The detection μ L of sample 10 are added per hole, final volume is up to 200 μ L, and compound is dense eventually
Spend for 5 μ g/mL, sample is incubated 72h with tumor cell line and carries out coherent detection jointly；3. positive drug group (positive)：Use
One line antineoplastic topotecan hydrochloride (TPT, MW of clinic：393.91) five concentration gradients are set, positive drug is added per hole
10 μ L, final volume is up to 200 μ L, and final concentration is followed successively by 5 μM, 1 μM, 0.2 μM, 0.04 μM, 0.008 μM, positive drug and tumour cell
The common 72h that is incubated of strain carries out coherent detection.
Activity determination
At the end of prepared by model, 100 μ L MTS mixed liquors are added per hole, continue to cultivate 4h colour developings, in ELIASA 490nm ripples
Strong point detects the absorbance value in each hole.
Select sample of the primary dcreening operation Tumor growth inhibition effect more than 50% to carry out secondary screening (activity is revalued), sample sieve and
The concentration gradient that cell is incubated jointly is set as the 1/10 to 1/3 of primary dcreening operation final concentration, sets 3 to 5 gradients, and other method is same
On, calculate IC after measurement light absorption value50。
Computational methods
Every group of cell detects light absorption value with MTS methods, and inhibiting rate of the sample to growth of tumour cell is calculated after measurement.With sample
The logarithm of product various dose is mapped to growth of tumour cell inhibiting rate, be can obtain dose-effect curve, is therefrom obtained the sample
50 3nhibitory dose IC50。
Sample inhibiting rate (%)=
[(ODcontrol-ODblank)-(ODsample-ODblank)]/(ODcontrol-ODblank) × 100%
ODsample：Sample treatment group light absorption value；ODcontrol：Normal group light absorption value；ODblank：Culture plate blank well
(acellular) light absorption value.
Experimental result
This experiment has carried out growth of tumour cell using the human tumor cells of in vitro culture as research object to ovum South America chrysanthemum element
Inhibitory activity is evaluated.
1st, to human lung carcinoma cell line A549 growth inhibition effect
Ovum South America chrysanthemum element can significantly inhibit human lung carcinoma cell line A549 growths in 5 μ g/mL of primary dcreening operation dosage, and inhibiting rate is
44.11%.Dose gradient is set to revalue in above-mentioned sample, growth of the ovum South America chrysanthemum element to human lung carcinoma cell line A549 presses down
Make of presentation dose dependent, IC50For 1.53 μ g/mL.Positive drug TPT (topotecan hydrochloride) IC50For 0.13 μ g/mL.
Ovum South America chrysanthemum element is suitable with positive drug TPT (topotecan hydrochloride) effect to human lung carcinoma cell line A549 growth inhibition effect.
2nd, to the growth inhibition effect of Human Hepatic Carcinoma Cell Line BEL-7402
5 μ g/mL ovum South America chrysanthemum elements can substantially suppress Human Hepatic Carcinoma Cell Line BEL-7402 growth, and inhibiting rate is 81.39%.It is right
Above-mentioned sample sets dose gradient to be revalued, growth inhibition effect of the ovum South America chrysanthemum element to Human Hepatic Carcinoma Cell Line BEL-7402
Dose dependent, IC is presented50For 3.10 μ g/mL.Positive drug TPT (topotecan hydrochloride) IC50For 30.82 μ g/mL.Ovum south
U.S. chrysanthemum element is all remarkably higher than positive drug TPT (topotecan hydrochloride) to the growth inhibition effect of Human Hepatic Carcinoma Cell Line BEL-7402.
3rd, to human colon cancer cell strain HT-29 growth inhibition effect
5 μ g/mL ovum South America chrysanthemum elements can substantially suppress human colon cancer cell strain HT-29 growths, and inhibiting rate is 82.69%.It is right
It sets dose gradient to be revalued, and ovum South America chrysanthemum element is presented to human colon cancer cell strain HT-29 growth inhibition effect
Dose dependent, IC50For 3.66 μ g/mL.Positive drug TPT (topotecan hydrochloride) IC50For 13.26 μ g/mL.Ovum South America chrysanthemum
Element is all remarkably higher than positive drug TPT (topotecan hydrochloride) to human colon cancer cell strain HT-29 growth inhibition effect.
Activity rating conclusion：Sample extracorporeal anti-tumor function evaluation is shown in Table 2, as can be seen from Table 2：
1st, ovum South America chrysanthemum element is to human lung carcinoma cell line A549, Human Hepatic Carcinoma Cell Line BEL-7402 and human colon cancer cell strain
The growth of tri- kinds of cell lines of HT-29 has different degrees of inhibitory action.Positive drug TPT is to A549, BEL-7402, HT-29 body
The IC that outgrowth suppresses50It is 0.13 μ g/mL, 30.82 μ g/mL, 13.26 μ g/mL.
2nd, ovum South America chrysanthemum element shows preferable extracorporeal anti-tumor function, and it is thin to human lung carcinoma cell line A549, human liver cancer
Born of the same parents strain BEL-7402 and human colon cancer cell strain tri- kinds of cell lines of HT-29 growth inhibition IC50It is 1.53 μ g/mL, 3.10 μ g/
mL、3.66μg/mL.And ovum South America chrysanthemum element is to Human Hepatic Carcinoma Cell Line BEL-7402 and human colon cancer cell strain two kinds of cells of HT-29
The growth in vitro inhibitory action of strain is substantially better than positive drug TPT (topotecan hydrochloride) (IC50For 30.82 μ g/mL and 13.26 μ g/
ML), the growth in vitro inhibitory action to human lung carcinoma cell line A549 is more close with positive drug TPT (topotecan hydrochloride) effects
(IC50：0.13μg/mL).Ovum South America chrysanthemum element has obvious antitumor action to tumor cell in vitro.
3rd, ovum South America chrysanthemum element has obvious antitumor action；It can be seen that：Ovum South America of the present invention chrysanthemum element is to external swollen
Oncocyte has significant antitumor activity, it is expected to be used to prepare anti-tumor medicinal preparation as active component, before medicinal
Scape.
In summary, present invention firstly provides ovum South America chrysanthemum element to human lung carcinoma cell line A549, human hepatoma cell strain
BEL-7402 and human colon cancer cell strain tri- kinds of cell lines of HT-29 growth have different degrees of inhibitory action；And ovum South America
Chrysanthemum element is bright to the growth in vitro inhibitory action of Human Hepatic Carcinoma Cell Line BEL-7402 and human colon cancer cell strain two kinds of cell lines of HT-29
It is aobvious to be better than positive drug TPT (topotecan hydrochloride), to human lung carcinoma cell line A549 growth in vitro inhibitory action and positive drug TPT
(topotecan hydrochloride) effect is more close；Illustrate ovum South America chrysanthemum element to external lung carcinoma cell, liver cancer cells and colon cancer cell
With obvious antitumor action, with preferable prospect in medicine.
Above technical characteristic constitutes embodiments of the invention, and it has stronger adaptability and implementation result, can basis
The non-essential technical characteristic of increase and decrease is actually needed, to meet the demand of different situations.
The ovum South America chrysanthemum element of table 11H-NMR、13C-NMR and HMBC spectral datas
The sample extracorporeal anti-tumor function of table 2 is evaluated
Claims (5)
1. a kind of ovum South America chrysanthemum element is used as the application prepared in anti-lung cancer, liver cancer and colon cancer drug.
2. the plain application as in preparation anti-lung cancer, liver cancer and colon cancer drug of ovum South America according to claim 1 chrysanthemum, its
It is characterised by that ovum South America chrysanthemum element is to be extracted from husky Inula britannica chinensis or other Inulaplants, it is purified isolated；Or, ovum
South America chrysanthemum element obtains for chemical synthesis process.
3. ovum South America according to claim 1 or 2 chrysanthemum element is used as answering in preparation anti-lung cancer, liver cancer and colon cancer drug
Formulation with, it is characterised in that ovum South America chrysanthemum element is tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, hard
One kind in capsule, soft capsule, oral liquid, mouth containing agent, granule, electuary, pill, powder, parenteral solution, powder-injection.
4. ovum South America according to claim 1 or 2 chrysanthemum element is used as answering in preparation anti-lung cancer, liver cancer and colon cancer drug
Chemical structural formula with, it is characterised in that ovum South America chrysanthemum element is：
5. the plain application as in preparation anti-lung cancer, liver cancer and colon cancer drug of ovum South America according to claim 3 chrysanthemum, its
It is characterised by that the plain chemical structural formula of ovum South America chrysanthemum is：
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610921609.1A CN107050015B (en) | 2016-10-21 | 2016-10-21 | Ovum South America chrysanthemum element is as the application in preparation anti-lung cancer, liver cancer and colon cancer drug |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610921609.1A CN107050015B (en) | 2016-10-21 | 2016-10-21 | Ovum South America chrysanthemum element is as the application in preparation anti-lung cancer, liver cancer and colon cancer drug |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107050015A true CN107050015A (en) | 2017-08-18 |
| CN107050015B CN107050015B (en) | 2019-08-27 |
Family
ID=59616950
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610921609.1A Active CN107050015B (en) | 2016-10-21 | 2016-10-21 | Ovum South America chrysanthemum element is as the application in preparation anti-lung cancer, liver cancer and colon cancer drug |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107050015B (en) |
-
2016
- 2016-10-21 CN CN201610921609.1A patent/CN107050015B/en active Active
Non-Patent Citations (2)
| Title |
|---|
| C. L. CESPEDES ET AL: "Comparative Study of Ovatifolin Antioxidant and Growth Inhibition Activities", 《J. AGRIC. FOOD CHEM.》 * |
| TIAGO B. OLIVEIRA ET AL: "Study of Chromatographic Retention of Natural Terpenoids by Chemoinformatic Tools", 《J. CHEM. INF. MODEL》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN107050015B (en) | 2019-08-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Shen et al. | Bioactive constituents of Clausena lansium and a method for discrimination of aldose enantiomers | |
| Li et al. | Lignans from the heartwood of Streblus asper and their inhibiting activities to hepatitis B virus | |
| CN101123880A (en) | Anti-tumor compounds with angeloyl groups | |
| CN101531644B (en) | New daphnane diterpene compounds in Daphne genkwa as well as preparation method and application of same | |
| CN108084060B (en) | Alkaloid oleraurea in purslane and extraction and separation method thereof | |
| CN111285767A (en) | Benzophenone compound and application thereof | |
| CN106008502A (en) | Alkaloid compounds with novel skeletons in purslane and extraction and separation method thereof | |
| Wei et al. | Antiproliferative piperidine alkaloids from giant taro (Alocasia macrorrhiza) | |
| CN108689851B (en) | Tiglic alkane type diterpene compound and preparation method and application thereof | |
| CN114105751A (en) | Terpenoid and preparation method and application thereof | |
| CN106279305A (en) | Amide alkaloid compound and extraction separation method thereof in Herba Portulacae | |
| KR100861320B1 (en) | A pharmaceutical composition containing daurinol for the prevention and treatment of cancers | |
| CN107501072B (en) | Compound colletotriconeA, preparation method thereof and application thereof in preparing antitumor drugs | |
| CN114213375B (en) | Sesquiterpene lactone compound and preparation method and application thereof | |
| CN113735918B (en) | Labdane diterpene glycoside compound and preparation method thereof | |
| CN107050015B (en) | Ovum South America chrysanthemum element is as the application in preparation anti-lung cancer, liver cancer and colon cancer drug | |
| CN113278026B (en) | Lignin compound with anti-tumor activity and preparation method and application thereof | |
| CN106619611B (en) | Application of eupatorium lactone in preparing medicine for resisting liver cancer and colon cancer | |
| CN114369022B (en) | Organic acid compound in purslane and extraction and separation method thereof | |
| Chen et al. | Cytotoxic picrotoxane-type sesquiterpenoid lactones from Dendrobium huoshanense | |
| CN110305094B (en) | Two flavonoid compounds in purslane and extraction and separation method and application thereof | |
| CN103191143A (en) | New application of cardiac glycoside compound | |
| CN109761977B (en) | Rhizoma polygonati alkaloid C and preparation method and application thereof | |
| KR20110087397A (en) | A composition comprising isodihydroauroglaucin as an active ingredient for treating and preventing cancer disease | |
| KR20110087395A (en) | A composition comprising pseurotin d as an active ingredient for treating and preventing cancer disease |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |