CN101829173A - Preparation of calotropis gigantea leaf extract and application of antineoplastic medicament - Google Patents
Preparation of calotropis gigantea leaf extract and application of antineoplastic medicament Download PDFInfo
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- CN101829173A CN101829173A CN 201010190506 CN201010190506A CN101829173A CN 101829173 A CN101829173 A CN 101829173A CN 201010190506 CN201010190506 CN 201010190506 CN 201010190506 A CN201010190506 A CN 201010190506A CN 101829173 A CN101829173 A CN 101829173A
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Abstract
The invention discloses preparation of a calotropis gigantea leaf extract and application of an antineoplastic medicament. The preparation of the calotropis gigantea leaf extract is characterized by comprising the following steps of: using calotropis gigantea leaves as a raw material; extracting and concentrating the raw material to obtain the calotropis gigantea leaf extract comprising cardiac glycoside active constituents; and according to the conventional preparation process, preparing the extract into tablets, capsules, granules, dripping pills, oral liquid or injections applied in the antineoplastic medicament. Compared with the prior art, the preparation has the advantages of convenient extraction of an antineoplastic active substance, simple operation, low cost and significant antineoplastic curative effect, and provides a new medicament for treating tumors.
Description
Technical field
The present invention relates to the Chinese medicine technical field, the especially a kind of preparation of calotropis gigantea leaf extract and the application of antitumor drug.
Background technology
Calotropis gigantea leaf is asclepiadaceae (Asclepiadaceae), belongs to the leaf of (Calotropis) plant Radix Calotropis giganteae (Calotropis gigantea L.).Calotropis has 6 kinds approximately, is distributed widely in the tropical and subtropical zone area in Asia and Africa.China abounds with wherein two kinds, and a kind of is Radix Calotropis giganteae (Calotropis giganteaI.), is distributed in Hainan, Guangdong, Sichuan and Yunnan, and is another kind of for spending Radix Calotropis giganteae (CalotropisproceraL.) in vain, in Guangdong, there is fragmentary distribution in Guangxi, Yunnan.
The Calotropis plant, has a medical value widely among the people, the white juice at its root, stem, leaf, fruit and each position is all pharmaceutically acceptable, has antibiotic, antiinflammatory, anthelmintic, reduces phlegm, effect such as detoxifcation, is used for treatment of diseases such as asthma, cough, leprosy, ulcer, hemorrhoid, tumor.The foreign scholar has carried out going deep into systematic research to the chemical constituent of Radix Calotropis giganteae, in acting in accordance with YIN YANG changes in four seasons and the leaf isolation identification more than 10 kind of cardiac glycoside, cardiac glycoside shows powerful antitumor activity (" Chemical Pharmaceutical Bulletin ", 1998.46B:528 mostly; " Journal of Natural Products ", 2006,69 (18): 1249).Domestic, only China tropic Agriculture Academy Sciences tropic Biotechnology Research Institute has reported from Radix Calotropis giganteae and to have separated 3 cardiac glycosidees and anti tumor activity in vitro (" Modern Pharmaceutical Research ", 2008,1 (2): 49.) that obtain.Chinese patent publication number: CN1414010A discloses " a kind of cardiac glycoside compounds for the treatment of cancer and preparation method thereof " and has related to cardiac glycoside compounds extraction process etc. in the Radix Calotropis giganteae root; Patent " the new application in the preparation antitumor drug of Radix Calotropis giganteae and extract thereof " relates to the anticancer usage of Radix Calotropis giganteae root ethanol extraction through the cardiac glycoside extract of purification by macroporous resin; Patent " antineoplastic new usage of the cardiac glycoside chemical compound in the Radix Calotropis giganteae " relates to the anticancer usage of the cardiac glycoside chemical compound that separation obtains in the Radix Calotropis giganteae root.These patents are object of study with the Radix Calotropis giganteae root all, and do not relate to research and application to calotropis gigantea leaf, and bibliographical information and patent disclosure are not seen in the application of the extract of relevant calotropis gigantea leaf in the preparation antitumor drug so far.
Summary of the invention
The preparation of a kind of calotropis gigantea leaf extract of providing at the deficiencies in the prior art and the application of antitumor drug are provided, it adopts low polar organic solvent reflux, extract, from calotropis gigantea leaf to have the antineoplastic active substance, it is remarkable to be applied to the antineoplastic therapeutical effect, for oncotherapy provides a kind of new medicine.
The object of the present invention is achieved like this: a kind of preparation of calotropis gigantea leaf extract, be characterized in the calotropis gigantea leaf being raw material, and through extracting, concentrate to such an extent that have the calotropis gigantea leaf extract of cardiac glycoside active component, concrete preparation comprises the steps:
A, once extraction
With methanol or low polar organic solvent serves as that extraction solvent, exsiccant calotropis gigantea leaf are raw material, place extraction pot after crushed, extract 2～3 times with extracting solvent refluxing, extracting solution is behind decompression and solvent recovery, extract is dispersed in becomes suspension in the water, extract through low polar organic solvent then, the calotropis gigantea leaf extract A that remaining water liquid must have the cardiac glycoside active component after concentrated, extracting solvent and raw material is 8～10: 1 by weight, and reflux extracting time is 2 hours/time;
B, second extraction
With the medicinal residues after the said extracted, use methanol extraction 2～3 times, extracting solution must have the calotropis gigantea leaf extract B of cardiac glycoside active component behind reclaim under reduced pressure methanol, and methanol and medicinal residues are 8～10: 1 by weight, and extraction time is 2 hours/time.
Described low polar organic solvent is dichloromethane, chloroform or normal hexane.
A kind of calotropis gigantea leaf extract prepares the application of antitumor drug, be characterized in that the calotropis gigantea leaf extract preparation process routinely that will have the cardiac glycoside active component adds proper quantity of medicinal auxiliary material and is applied in the antitumor drug, make tablet, capsule, granule, drop pill, oral liquid or injection tumor is had certain inhibition.
The present invention compared with prior art has the antineoplastic active substance and extracts conveniently, and simple to operate, cost is low, and is remarkable for the antineoplastic therapeutical effect, for oncotherapy provides a kind of new medicine.
Description of drawings
Fig. 1 is that extract A is to K562 and 293 cell growth effect curve charts
Fig. 2 is that extract A is to K562 and 293 cell growth effect curve charts
Fig. 3 is that extract B is to K562 and 293 cell growth effect curve charts
Fig. 4 is that extract B is to KB and PC-3 cell growth effect curve chart
The specific embodiment
The present invention is described in further detail with the embodiment of concrete preparation and application below.
Embodiment 1
A, once extraction
Getting calotropis gigantea leaf dry product 5.0Kg is raw material, 40.0Kg normal hexane for extracting solvent, calotropis gigantea leaf places extraction pot after crushed, extract 3 times with extracting solvent refluxing, 2 hours/time, extracting solution was dispersed in extract and becomes suspension in the water behind the reclaim under reduced pressure normal hexane, then through the dichloromethane organic solvent extraction, remaining water liquid must have the cardiac glycoside active component after concentrating calotropis gigantea leaf extract A.
B, second extraction
With the medicinal residues after the said extracted, the methanol extraction of usefulness 30.0Kg 2 times, 2 hours/time, extracting solution must have the calotropis gigantea leaf extract B of cardiac glycoside active component behind reclaim under reduced pressure methanol.
C, preparation
Above-mentioned calotropis gigantea leaf extract A or B with cardiac glycoside active component added appropriate amount of starch and microcrystalline Cellulose mixing, make 1000 after drying then and get final product.
Embodiment 2
A, once extraction
Getting calotropis gigantea leaf dry product 2.5Kg is raw material, 20.0Kg methanol for extracting solvent, calotropis gigantea leaf places extraction pot after crushed, extract 2 times with extracting solvent refluxing, 2 hours/time, extracting solution was dispersed in extract and becomes suspension in the water behind reclaim under reduced pressure methanol, then through n-hexane extraction, remaining water liquid must have the cardiac glycoside active component after concentrating calotropis gigantea leaf extract A.
B, preparation
Above-mentioned calotropis gigantea leaf extract A with cardiac glycoside active component is added an amount of lactose and carboxymethyl starch sodium mixing, make 1000, incapsulate behind dry, the granulate and get final product with 30 POVIDONE K 30 BP/USP 30.
Adopt mtt assay to test the external antitumor activity screening test that calotropis gigantea leaf extract A of the present invention and extract B are carried out chronic myeloid leukemia cells K562, human mouth epidermal carcinoma cell KB, prostate gland cancer cell PC-3 and people's renal epithelial cell cancer 293 cell strains, activity test method is as follows:
(1) calotropis gigantea leaf extract A 95mg is dissolved among the 0.2ml DMSO (475mg/ml), calotropis gigantea leaf extract B144mg is dissolved among the 0.2ml DMSO (720mg/ml), be made into the concentration of 85 times of dilutions successively, for writing conveniently, maximum concentration is decided to be 1, and other 7 degree of depth are decided to be 2,3,4,5,6,7,8 successively according to the attenuating of concentration.
(2) the PC-3 cell need add the 10%FBS cultivation with F12DMEM, each cell dyes the method counting with trypan blue row, cell density with 5000/ hole or 10000/ hole is inoculated in 96 orifice plates, every hole adds cell suspension 99ul, be inoculated in B2-B11, C2-C11, D2-D11, E2-E11, F2-F11, the G2-G11 of 96 orifice plates, A2-A11 only adds culture fluid and does not add cell, as the zeroing hole; All the other holes add equal-volume PBS, increase to avoid the culture medium evaporation to cause resultant error.
(3) cell culture dosing after 24 hours, every hole adds the 1ul medicinal liquid, 6 multiple holes of each concentration.
(4) cell is at 37 ℃, 100% relative humidity, 5%CO
2Incubator in continuous culture 24 hours, every then hole adds 10ul MTT (PBS preparation), continues cultivation 4 hours.
(5) centrifugal, inhale and remove supernatant.Every hole adds 150ul DMSO, and light shaking was surveyed the OD value at 570nm wavelength place after 15 minutes, calculated growth inhibition ratio by following formula:
Growth inhibition ratio (%)=(the average OD value of the average OD value/negative control group of medication group) * %
(6) being abscissa with the sample concentration, is vertical coordinate with the suppression ratio, and the concentration IC that suppression ratio is 50% o'clock sample is obtained in mapping
50, sample is active result promptly represent with half-inhibition concentration (IC50).
Calotropis gigantea leaf extract A and extract B see the following form 1 to the toxic action of K562, KB, PC-3,293 tumor cell lines,
Table 1:
| Cell line | The source | ??IC50(ug/ml)??A????B |
| ??KB | People's epithelium oral cancer | ??3.330.401 |
| ??293 | People's renal epithelial cell system | ??0.3153.45 |
| ??PC-3 | Human Prostate Cancer Cells | ??2.047.28 |
| ??K-562 | Human leukemia | ??0.0880.044 |
With IC50＜20ug/ml serves as effective
Consult accompanying drawing 1～accompanying drawing 4, calotropis gigantea leaf extract A and the influence of extract B to different growth of tumour cell curves, extract A of the present invention and extract B are screened through anti tumor activity in vitro, and the statistical disposition result shows to have better antitumor activity.
More than just the present invention is further illustrated, is not in order to the restriction this patent, all for the present invention's equivalence enforcement, all should be contained within the claim scope of this patent.
Claims (3)
1. the preparation of a calotropis gigantea leaf extract is characterized in that with the calotropis gigantea leaf being raw material, and through extracting, concentrate to such an extent that have the calotropis gigantea leaf extract of cardiac glycoside active component, concrete preparation comprises the steps:
A, once extraction
With methanol or low polar organic solvent serves as that extraction solvent, exsiccant calotropis gigantea leaf are raw material, place extraction pot after crushed, extract 2～3 times with extracting solvent refluxing, extracting solution is behind decompression and solvent recovery, extract is dispersed in becomes suspension in the water, extract through low polar organic solvent then, the calotropis gigantea leaf extract A that remaining water liquid must have the cardiac glycoside active component after concentrated, extracting solvent and raw material is 8～10: 1 by weight, and reflux extracting time is 2 hours/time;
B, second extraction
With the medicinal residues after the said extracted, use methanol extraction 2～3 times, extracting solution must have the calotropis gigantea leaf extract B of cardiac glycoside active component behind reclaim under reduced pressure methanol, and methanol and medicinal residues are 8～10: 1 by weight, and extraction time is 2 hours/time.
2. according to the preparation of the described calotropis gigantea leaf extract of claim 1, it is characterized in that described low polar organic solvent is dichloromethane, chloroform or normal hexane.
3. application that calotropis gigantea leaf extract prepares antitumor drug, it is characterized in that the calotropis gigantea leaf extract preparation process routinely that will have the cardiac glycoside active component adds proper quantity of medicinal auxiliary material and is applied in the antitumor drug, make tablet, capsule, granule, drop pill, oral liquid or injection tumor is had certain inhibition.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104324043A (en) * | 2013-04-11 | 2015-02-04 | 中国热带农业科学院热带作物品种资源研究所 | Use of cardiac glycoside compound |
| CN107158058A (en) * | 2017-04-27 | 2017-09-15 | 黄惠民 | The extracting method of cardiac glycoside general glycoside |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101352468A (en) * | 2008-07-02 | 2009-01-28 | 中国热带农业科学院热带生物技术研究所 | Novel uses of Calotropis gigantea and extract thereof in preparing anti-tumor medicament |
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2010
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101352468A (en) * | 2008-07-02 | 2009-01-28 | 中国热带农业科学院热带生物技术研究所 | Novel uses of Calotropis gigantea and extract thereof in preparing anti-tumor medicament |
Non-Patent Citations (1)
| Title |
|---|
| 《河南大学学报(医学版)》 20090228 戴好富 牛角瓜属植物化学成分与药理活性研究进展 1-7 第28卷, 第1期 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104324043A (en) * | 2013-04-11 | 2015-02-04 | 中国热带农业科学院热带作物品种资源研究所 | Use of cardiac glycoside compound |
| CN104324043B (en) * | 2013-04-11 | 2017-06-23 | 中国热带农业科学院热带作物品种资源研究所 | A kind of purposes of cardiac glycoside compound |
| CN107158058A (en) * | 2017-04-27 | 2017-09-15 | 黄惠民 | The extracting method of cardiac glycoside general glycoside |
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Application publication date: 20100915 |