CN105982946A - Preparation method and medicinal use of Pterocarpus santalinus antitumor extract and composition thereof - Google Patents
Preparation method and medicinal use of Pterocarpus santalinus antitumor extract and composition thereof Download PDFInfo
- Publication number
- CN105982946A CN105982946A CN201510081022.XA CN201510081022A CN105982946A CN 105982946 A CN105982946 A CN 105982946A CN 201510081022 A CN201510081022 A CN 201510081022A CN 105982946 A CN105982946 A CN 105982946A
- Authority
- CN
- China
- Prior art keywords
- methanol
- dichloromethane
- extract
- volume ratio
- mixed solvent
- 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.)
- Pending
Links
- 239000000284 extract Substances 0.000 title claims abstract description 91
- 230000000259 anti-tumor effect Effects 0.000 title claims abstract description 31
- 241000750718 Pterocarpus santalinus Species 0.000 title claims abstract description 16
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 239000000203 mixture Substances 0.000 title claims abstract description 12
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims abstract description 546
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims abstract description 459
- 239000012046 mixed solvent Substances 0.000 claims abstract description 78
- 239000000741 silica gel Substances 0.000 claims abstract description 57
- 229910002027 silica gel Inorganic materials 0.000 claims abstract description 57
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 52
- 238000001035 drying Methods 0.000 claims abstract description 42
- 239000003814 drug Substances 0.000 claims abstract description 39
- 239000003960 organic solvent Substances 0.000 claims abstract description 35
- 238000010828 elution Methods 0.000 claims abstract description 21
- 206010006187 Breast cancer Diseases 0.000 claims abstract description 6
- 208000026310 Breast neoplasm Diseases 0.000 claims abstract description 6
- 206010009944 Colon cancer Diseases 0.000 claims abstract description 6
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims abstract description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims abstract description 6
- 208000005718 Stomach Neoplasms Diseases 0.000 claims abstract description 6
- 201000007983 brain glioma Diseases 0.000 claims abstract description 6
- 206010017758 gastric cancer Diseases 0.000 claims abstract description 6
- 201000005202 lung cancer Diseases 0.000 claims abstract description 6
- 208000020816 lung neoplasm Diseases 0.000 claims abstract description 6
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims abstract description 6
- 208000008443 pancreatic carcinoma Diseases 0.000 claims abstract description 6
- 201000011549 stomach cancer Diseases 0.000 claims abstract description 6
- 201000007270 liver cancer Diseases 0.000 claims abstract description 5
- 208000014018 liver neoplasm Diseases 0.000 claims abstract description 5
- 238000002137 ultrasound extraction Methods 0.000 claims abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 54
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 45
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 33
- 238000000034 method Methods 0.000 claims description 28
- 239000003480 eluent Substances 0.000 claims description 27
- 235000008632 Santalum album Nutrition 0.000 claims description 23
- 238000011068 loading method Methods 0.000 claims description 23
- 240000000513 Santalum album Species 0.000 claims description 21
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 16
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 14
- 238000011161 development Methods 0.000 claims description 11
- IDGUHHHQCWSQLU-UHFFFAOYSA-N ethanol;hydrate Chemical compound O.CCO IDGUHHHQCWSQLU-UHFFFAOYSA-N 0.000 claims description 9
- 238000002156 mixing Methods 0.000 claims description 8
- 239000003208 petroleum Substances 0.000 claims description 8
- GBMDVOWEEQVZKZ-UHFFFAOYSA-N methanol;hydrate Chemical compound O.OC GBMDVOWEEQVZKZ-UHFFFAOYSA-N 0.000 claims description 7
- 238000000605 extraction Methods 0.000 claims description 6
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 5
- 229920000858 Cyclodextrin Polymers 0.000 claims description 5
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 5
- 201000010881 cervical cancer Diseases 0.000 claims description 5
- 208000029742 colonic neoplasm Diseases 0.000 claims description 5
- 201000002528 pancreatic cancer Diseases 0.000 claims description 5
- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid Substances OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 5
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 239000010302 Pterocarpus santalinus extract Substances 0.000 claims description 4
- 239000007919 dispersible tablet Substances 0.000 claims description 3
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 3
- 239000007962 solid dispersion Substances 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 238000004587 chromatography analysis Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 235000008216 herbs Nutrition 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 abstract description 6
- 201000011510 cancer Diseases 0.000 abstract description 4
- 230000002265 prevention Effects 0.000 abstract description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 abstract 1
- 208000019065 cervical carcinoma Diseases 0.000 abstract 1
- 201000010989 colorectal carcinoma Diseases 0.000 abstract 1
- 239000007788 liquid Substances 0.000 abstract 1
- 238000000926 separation method Methods 0.000 abstract 1
- 239000000243 solution Substances 0.000 description 25
- 235000019441 ethanol Nutrition 0.000 description 16
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 15
- 238000004108 freeze drying Methods 0.000 description 14
- 238000004809 thin layer chromatography Methods 0.000 description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 12
- 238000001291 vacuum drying Methods 0.000 description 10
- 210000004027 cell Anatomy 0.000 description 9
- 238000004458 analytical method Methods 0.000 description 8
- 150000001875 compounds Chemical class 0.000 description 8
- 239000002904 solvent Substances 0.000 description 7
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 6
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 6
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 6
- 238000011160 research Methods 0.000 description 6
- 238000002390 rotary evaporation Methods 0.000 description 6
- 238000005303 weighing Methods 0.000 description 6
- 244000086363 Pterocarpus indicus Species 0.000 description 5
- 235000009984 Pterocarpus indicus Nutrition 0.000 description 5
- 229920002472 Starch Polymers 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 238000007873 sieving Methods 0.000 description 5
- 235000019698 starch Nutrition 0.000 description 5
- 239000008107 starch Substances 0.000 description 5
- 238000003756 stirring Methods 0.000 description 5
- 230000000694 effects Effects 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 238000000227 grinding Methods 0.000 description 4
- 239000002609 medium Substances 0.000 description 4
- 238000012216 screening Methods 0.000 description 4
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 3
- 238000007605 air drying Methods 0.000 description 3
- WGLUMOCWFMKWIL-UHFFFAOYSA-N dichloromethane;methanol Chemical compound OC.ClCCl WGLUMOCWFMKWIL-UHFFFAOYSA-N 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- 238000010025 steaming Methods 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- 239000001116 FEMA 4028 Substances 0.000 description 2
- 208000032612 Glial tumor Diseases 0.000 description 2
- 206010018338 Glioma Diseases 0.000 description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 2
- 241000221035 Santalaceae Species 0.000 description 2
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 2
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 2
- 229960004853 betadex Drugs 0.000 description 2
- 230000000740 bleeding effect Effects 0.000 description 2
- 229960000913 crospovidone Drugs 0.000 description 2
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 2
- 239000012467 final product Substances 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 239000012535 impurity Substances 0.000 description 2
- 230000005918 in vitro anti-tumor Effects 0.000 description 2
- 239000010413 mother solution Substances 0.000 description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 230000008961 swelling Effects 0.000 description 2
- 210000004881 tumor cell Anatomy 0.000 description 2
- 239000000080 wetting agent Substances 0.000 description 2
- 239000002023 wood Substances 0.000 description 2
- AZKSAVLVSZKNRD-UHFFFAOYSA-M 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide Chemical compound [Br-].S1C(C)=C(C)N=C1[N+]1=NC(C=2C=CC=CC=2)=NN1C1=CC=CC=C1 AZKSAVLVSZKNRD-UHFFFAOYSA-M 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- XXBNRILXEBYOJY-UHFFFAOYSA-N CC1=CC=CC(C2(C3=CC=CC=C3)N=NN=N2)=C1C.Br Chemical compound CC1=CC=CC(C2(C3=CC=CC=C3)N=NN=N2)=C1C.Br XXBNRILXEBYOJY-UHFFFAOYSA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000220485 Fabaceae Species 0.000 description 1
- 244000071493 Iris tectorum Species 0.000 description 1
- 229920000881 Modified starch Polymers 0.000 description 1
- 239000012979 RPMI medium Substances 0.000 description 1
- 239000012980 RPMI-1640 medium Substances 0.000 description 1
- 101710151387 Serine protease 1 Proteins 0.000 description 1
- 102100032491 Serine protease 1 Human genes 0.000 description 1
- 101710119665 Trypsin-1 Proteins 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 229940041181 antineoplastic drug Drugs 0.000 description 1
- 238000007664 blowing Methods 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- GJYVZUKSNFSLCL-UHFFFAOYSA-N dichloromethanol Chemical compound OC(Cl)Cl GJYVZUKSNFSLCL-UHFFFAOYSA-N 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 239000012091 fetal bovine serum Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 229940127554 medical product Drugs 0.000 description 1
- 239000000401 methanolic extract Substances 0.000 description 1
- 238000007747 plating Methods 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention belongs to the technical field of medicines, and concretely relates to a preparation method of a Uygur medicine Pterocarpus santalinus antitumor extract and a composition thereof, and a use of the extract in prevention and treatment of brain glioma, breast cancer, lung cancer, stomach cancer, colorectal carcinoma, pancreas cancer, cervical carcinoma, liver cancer and other malignant tumors. The preparation method of the extract comprises the following steps: carrying out ultrasonic extraction on the Uygur medicine Pterocarpus santalinus with an organic solvent, concentrating the above obtained extract liquid, carrying out silica gel separation, eluting a sample introduced silica gel column with a dichloromethane and methanol mixed solvent with the volume ratio of dichloromethane to methanol of 100:4, continuously eluting the column with a dichloromethane and methanol mixed solvent with the volume ratio of dichloromethane to methanol of 100:14, and drying an eluate obtained through elution with the dichloromethane and methanol mixed solvent with the volume ratio of dichloromethane to methanol of 100:14 in order to obtain the extract; or eluting the column with a dichloromethane and methanol mixed solvent with the volume ratio of dichloromethane to methanol of 100:25, continuously eluting the column with a dichloromethane and methanol mixed solvent with the volume ratio of dichloromethane to methanol of 100:100, and drying an eluate obtained through elution with the dichloromethane and methanol mixed solvent with the volume ratio of dichloromethane to methanol of 100:100 in order to obtain the extract.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to a preparation method of an anti-tumor extract of Wiygur medicine santalum album and a composition thereof, and application of the anti-tumor extract in preparation of drugs for preventing and treating malignant tumors such as liver cancer, lung cancer, stomach cancer, colon cancer, pancreatic cancer, breast cancer, cervical cancer, brain glioma and the like.
Background
The product is Pterocarpus santalinus of Leguminosae. The rosewood is one of the most famous and precious wood in the world, is mainly produced in tropical areas of the Nanyang Islands, and is rare due to rare quantity and few people, so that the rosewood is valued by the people. According to the history, rosewood is produced mainly in tropical regions of the Nanyang Islands, and in the southeast Asia. Rosewood is also produced in Guangdong and Guangxi of China, but the quantity is small. Pterocarpus santalinus, also called as pterocarpus santalinus, is the most precious wood known at present and is the highest grade of the pterocarpus santalinus. Pterocarpus indicus has the main functions of relieving swelling, stopping bleeding and relieving pain. It is indicated for swelling and toxin, bleeding due to incised wound.
However, the effective components of the pterocarpus santalinus for resisting tumors are not clear, and the invention discovers that the pterocarpus santalinus also has good effects of preventing and treating malignant tumors such as breast cancer, cervical cancer, liver cancer, lung cancer, gastric cancer, colon cancer, pancreatic cancer, brain glioma and the like by systematically screening and researching the antitumor activity of the pterocarpus santalinus, and can be applied to the prevention and treatment of cancers.
Disclosure of Invention
The technical problem to be solved by the invention is to provide a santalum album extract.
The invention also provides a composition taking the pterocarpus santalinus extract as a main active ingredient.
The invention also provides preparation of the pterocarpus santalinus extract and the composition thereof and application of the pterocarpus santalinus extract and the composition thereof in preparing antitumor drugs.
The invention is realized by the following technical scheme:
ultrasonic extracting Uyghur medicine lignum Pterocarpi Indici with methanol, concentrating the extractive solution, separating with silica gel column, loading to silica gel column, extracting with dichloromethane: methanol-100: 0-0:100 mixed solvent gradient elution (dichloromethane: methanol, ratio see table 1), each dichloromethane: the methanol is mixed with solvent eluent in proportion, concentrated and dried, and then the antitumor activity of the eluent is tested by using an in vitro antitumor activity screening system, and the following unexpected findings are carried out by using dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:0-100:4, volume ratio) followed by elution with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:5-100:14, volume ratio) elution, dichloromethane: after the methanol eluent is dried at the ratio of 100:5-100:14, the antitumor activity is remarkable. Preferably, the reaction is first carried out with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) was eluted, followed by methanol: methanol mixed solutionAgent (dichloromethane: methanol, 100:14, volume ratio) elution, dichloromethane: drying the eluent with the ratio of 100:14 of methanol to obtain the product. The compound with antitumor activity can be enriched by the method, so that the compound is separated from other impurity components. The active extract is not reported in the literature, and the TLC analysis characterization of eluent of 100:5-100:14 is shown in figure 1, and the TLC analysis conditions are as follows: GF254Silica gel board, development system: petroleum ether: ethyl acetate: acetone (6:1:1), color development method: and (4) developing the color by vanillin-concentrated sulfuric acid.
Ultrasonic extracting Uyghur medicine lignum Pterocarpi Indici with methanol, concentrating the extractive solution, separating with silica gel column, loading to silica gel column, extracting with dichloromethane: methanol-100: 0-0:100 mixed solvent gradient elution (dichloromethane: methanol, ratio see table 1), each dichloromethane: the methanol is mixed with solvent eluent in proportion, concentrated and dried, and then the antitumor activity of the eluent is tested by using an in vitro antitumor activity screening system, and the following unexpected findings are carried out by using dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) was eluted, followed by methanol: methanol mixed solvent (dichloromethane: methanol, 100:30-100:100, volume ratio) elution, dichloromethane: after the methanol 100:100 eluent is dried, the antitumor activity is remarkable. Preferably, the reaction is first carried out with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) was eluted, followed by methanol: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) elution, dichloromethane: and (5) drying the eluent with the methanol ratio of 100:100 to obtain the product. The compound with antitumor activity can be enriched by the method, so that the compound is separated from other impurity components. The active extract has not been reported in the literature, and the TLC analysis of the active extract is characterized as shown in figure 2, and the TLC analysis conditions are as follows: GF254Silica gel board, development system: petroleum ether: ethyl acetate: acetone (1:1:1), color development method: and (4) developing the color by vanillin-concentrated sulfuric acid.
Specifically, the discovery process is as follows:
1. preparation of ultrasonic methanol extract of Wiygur medicinal lignum Pterocarpi Indici
Taking 20g of Uygur medicine sandalwood, ultrasonically extracting for 15min by 100ml of methanol, and concentrating an extracting solution to obtain an extract SN 0204A: 1.5691g, left sample: 0.0796g and 0.0752 g.
2. Dichloromethane-methanol mixed solvent gradient elution method and results
Taking 20g of Uygur medicine sandalwood, ultrasonically extracting for 15min by 100ml of methanol, and concentrating an extracting solution to obtain an extract SN 0204A: 1.5691g, left sample: 0.0796g and 0.0752 g. Column mounting: dissolving with methanol, mixing with silica gel 2g, mixing with blank silica gel 10g, eluting with a glass column with inner diameter of 2.0cm, and eluting with dichloro-methanol system with column volume of 25ml and gradient elution of 200 ml. Obtaining eluates of the eluates at different concentrations, and recovering solvent to obtain dichloromethane-methanol gradient elution extract, shown in Table 1, with TLC analysis results shown in FIG. 3 and FIG. 4, and TLC analysis conditions: GF254Silica gel board, development system: petroleum ether: ethyl acetate: acetone (6:1:1), petroleum ether: ethyl acetate: acetone (1:1:1), color development method: and (4) developing the color by vanillin-concentrated sulfuric acid.
TABLE 1
| Dichloromethane methanol | Volume (mL) | Numbering | Weight (mg) |
| 100:00 | 200 | SN0204A01 | 1.6 |
| 100:01 | 200 | SN0204A02 | 1.2 |
| 100:02 | 200 | SN0204A03 | 10.1 |
| 100:03 | 200 | SN0204A04 | 12.8 |
| 100:04 | 200 | SN0204A05 | 10.5 |
| 100:05 | 200 | SN0204A06 | 38 |
| 100:06 | 200 | SN0204A07 | 38.6 |
| 100:08 | 200 | SN0204A08 | 10.7 |
| 100:10 | 200 | SN0204A09 | 9.9 |
| 100:12 | 200 | SN0204A10 | 6.5 |
| 100:14 | 200 | SN0204A11 | 11 |
| 100:17 | 200 | SN0204A12 | 23.1 |
| 100:20 | 200 | SN0204A13 | 44.8 |
| 100:25 | 200 | SN0204A14 | 67.2 |
| 100:30 | 200 | SN0204A15 | 32.2 |
| 100:50 | 200 | SN0204A16 | 35.5 |
| 100:100 | 200 | SN0204A17 | 37 |
| 0:100 | 200 | SN0204A18 | 317.1 |
| Pure methanol | 200 | SN0204A19 | 297.6 |
3. Screening method and results for antitumor Activity
1) Conditions of the experiment
a) Information on cell lines
Rat glioma C6 was purchased from China center for type culture Collection cell Bank
b) Medicine and reagent
Under the aseptic condition of the sample, DMSO is dissolved to prepare a mother solution with the concentration of 100mg/mL, and when the sample is used, the mother solution is diluted to the required concentration (DMSO is less than or equal to 1 per thousand) by using an RPMI-1640 culture solution.
RPMI Medium 1640 Medium was purchased as dry powder from GIBCO, USA. Fetal bovine serum was purchased from the institute of biotechnology, yohima, beijing. Trypsin 1:250 and dimethyl diphenyl tetrazole bromide (MTT).
c) Instrument for measuring the position of a moving object
CO2Incubator (SANYO, Japan)
Vertical laminar flow clean bench (Shanghai clean and clean equipment Co., Ltd.)
Inverted biological microscope (Chongqing photoelectric instrument Co., Ltd.)
Low/high speed desk centrifuge (Shanghai' an pavilion scientific instrument factory)
Electronic balance (Aohaus instrument Co., Ltd.)
Enzyme mark instrument (Bole life medical products Co., Ltd.)
Vertical pressure steam sterilizer (Shanghai Shenan medical equipment factory)
Air-blast drying cabinet (Shanghai Yuejin medical equipment factory)
PH meter (SARTORIUS, Germany)
2) Experimental methods and procedures
Rat glioma C6 was plated at 4000/well density in 96-well plates, 100ul per well, and used 12h later. The components are dissolved in DMSO to be 100mg/mL stock solution and stored at-20 ℃ for later use. 12h after plating, the cell confluence rate was observed to be about 40%, and the drugs were added at concentrations of 100. mu.g/mL, 3 duplicate wells per fraction. Two control groups (medium + cells; medium + cells with 0.1% DMSO), 3 blank wells (medium only) were set up per plate of cells. After 24 hours of drug addition, 20. mu.l of tetramethylazozole salt chemically named 3- (4, 5-dimethylthiazole) -2, 5-diphenyltetrazolium bromide (3- (4, 5-dimethyl-2-thiazolyl) -2,5-diphenyl-tetrazolium bromide, MTT) was added and the culture was continued for 4 hours. The supernatant was completely discarded, 100. mu.l DMSO was added, and MTT was dissolved and bubbled. OD was measured at 490 nm.
3) Results of the experiment
TABLE 2
As a result, it was found that: the preferred technical scheme of the invention is as follows: ultrasonic extracting Uyghur medicine lignum pterocarpi indici with methanol, concentrating the extractive solution, separating with silica gel column, loading to silica gel column, extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) was eluted, followed by methanol: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) elution, dichloromethane: recovering organic solvent from the methanol 100:14 eluate, and drying to obtain high activity extract, i.e. the anti-tumor extract. The active extract has not been reported in the literature, and the TLC analysis of the active extract is characterized as shown in figure 1.
Ultrasonic extracting Uyghur medicine lignum pterocarpi indici with methanol, concentrating the extractive solution, separating with silica gel column, loading to silica gel column, extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) was eluted, followed by methanol: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) elution, dichloromethane: eluting with methanol 100:100, recovering organic solvent, and drying to obtain high activity extract, i.e. the anti-tumor extract. The active extract has not been reported in the literature, and the TLC analysis of the active extract is characterized as shown in figure 2.
4. Research on extraction method of anti-tumor extract
1) Species study of extraction solvent
Extracting with organic solvent such as methanol, ethanol, acetone, chloroform, ethyl acetate, methanol-water mixed solvent, and ethanol-water mixed solvent, respectively, and testing the extract for anti-tumor activity against C6 cells, the results are as follows:
TABLE 3
The research result shows that: the organic solvent for extraction may be methanol, ethanol, acetone, chloroform, ethyl acetate, methanol-water mixed solvent, or ethanol-water mixed solvent.
2) Research on the amount of extraction solvent
The extracts were extracted with 1, 2,5, 10, 20, 30, 40, 50-fold (weight/volume ratio) organic solvent, respectively, and tested for anti-tumor activity against C6 cells, and the results were as follows:
TABLE 4
The organic solvent for extracting the extract accounts for 2-50 times of the weight of the medicinal materials (weight/volume ratio).
3) Examination of drying method
The obtained antitumor active extract is dried by methods such as a vacuum drying method, a freeze drying method, an air-blast drying method, a centrifugal drying method, a rotary evaporation drying method and the like respectively, and the vacuum drying method, the freeze drying method, the air-blast drying method, the centrifugal drying method and the rotary evaporation drying method are found to be suitable for drying the antitumor active extract of the C6 cells by taking the water content, TLC and activity tests as indexes, wherein the vacuum drying method and the freeze drying method are most preferred.
TABLE 5
| Sample 20g | Vacuum drying method | Freeze drying method | Air-blast drying method | Centrifugal drying method | Rotary evaporation drying method |
| Water content (%) | 7.9 | 8.9 | 10.7 | 13.5 | 10.0 |
| Inhibition ratio (%) | 44.2 | 33.4 | 24.8 | 21.8 | 35.9 |
Preferably, the preparation method of the pterocarpus santalinus antitumor extract comprises the following steps:
ultrasonic extracting Uyghur medicine lignum pterocarpi indici with organic solvent, concentrating the extractive solution, separating with silica gel column, loading to silica gel column, extracting with dichloromethane: elution with a methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) was 2-50 column volumes, followed by elution with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) elutes 2-50 times column volume. Dichloromethane: methanol 100:100, recovering the organic solvent from the eluent, and drying to obtain the extract. The optimal method comprises the following steps of firstly using dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) was eluted 10 column volumes, followed by a column volume of dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) eluted 15 column volumes. Wherein,
1) the solvent for extracting extract can be methanol, ethanol, acetone, chloroform, ethyl acetate, methanol-water mixed solvent, or ethanol-water mixed solvent, preferably methanol and 95% ethanol. The organic solvent for extracting the extract accounts for 2-50 times of the weight of the medicinal materials (weight/volume ratio).
2) The extract drying method can be vacuum drying method, freeze drying method, forced air drying, centrifugal drying, rotary evaporation drying method, etc., preferably vacuum drying method and freeze drying method.
Ultrasonic extracting Uyghur medicine lignum Pterocarpi Indici with methanol, concentrating the extractive solution, separating with silica gel column, loading to silica gel column, extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) eluted 2-50 column volumes, followed by a column volume of dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) elution 2-50 times column volume. Dichloromethane: methanol 100:100, recovering the organic solvent from the eluent, and drying to obtain the extract. The above conditions are optimally determined by firstly using dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) was eluted 10 column volumes, followed by a column volume of dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) eluted 15 column volumes. Wherein,
1) the solvent for extracting extract can be methanol, ethanol, water, acetone, chloroform, ethyl acetate, methanol-water mixed solvent, or ethanol-water mixed solvent, preferably methanol and 95% ethanol. The organic solvent for extracting the extract accounts for 2-50 times of the weight of the medicinal materials (weight/volume ratio).
2) The extract drying method can be vacuum drying method, freeze drying method, forced air drying, centrifugal drying, rotary evaporation drying method, etc., preferably vacuum drying method and freeze drying method.
5. Research on antitumor activity of lignum pterocarpi indici antitumor extract (obtained by eluting with dichloromethane: methanol 100:25 and then with dichloromethane: methanol 100: 100) was performed
Respectively testing antitumor activity and IC of lignum Pterocarpi Indici antitumor extract with various tumor cells, such as brain glioma, breast cancer, lung cancer, gastric cancer, colon cancer, pancreatic cancer, cervical cancer, and hepatocarcinoma50The results are as follows:
TABLE 6
Therefore, we find that the lignum pterocarpi indici anti-tumor extract has anti-tumor activity and is expected to be used for preventing and treating various tumors such as breast cancer, lung cancer, gastric cancer, colon cancer, pancreatic cancer, cervical cancer, brain glioma, liver cancer and other malignant tumor cell strains.
6. Research on composition of anti-tumor extract of pterocarpus santalinus and preparation method thereof
1) Solid dispersion
Prescription
The preparation method comprises the following steps:
weighing the santalum album extract and a carrier polyvinylpyrrolidone (PVP) according to the mass ratio of 1:2, 1:4 and 1:6, respectively putting the materials into a beaker, adding absolute ethyl alcohol, stirring by a magnetic stirrer until the santalum album extract and the carrier are completely dissolved, transferring into a rotary steaming instrument to remove an organic solvent, drying, crushing, and sieving by a 80-mesh sieve to obtain the PVP inclusion compound of the santalum album extract.
2) Cyclodextrin inclusion compounds
Prescription:
the preparation method comprises the following steps:
grinding beta-cyclodextrin and 1-5 times of water uniformly, adding the santalum album extract (the water-insoluble one should be dissolved in a small amount of organic solvent at first) and fully grinding to paste, and drying at low temperature to obtain the final product.
3) The prescription of the dispersible tablet is as follows:
the preparation method comprises the following steps:
1. preparing a starch dispersion of the santalum album extract, precisely weighing the santalum album extract, adding a proper amount of sodium dodecyl sulfate, dissolving the sodium dodecyl sulfate in 70% ethanol, adding soluble starch in equal proportion, uniformly mixing, evaporating to dryness at the temperature of 70 ℃, crushing, and sieving by a 100-mesh sieve;
2. weighing the formula amount, namely the santalum album extract starch dispersoid, the crospovidone and the pregelatinized starch, using 70% ethanol as a wetting agent, adding while stirring, preparing wet granules, sieving with a 14-mesh sieve, standing at room temperature for 15min, drying in an oven at 60 ℃ for 45min, grading with a 16-mesh sieve, adding talcum powder and silica gel, mixing uniformly, and tabletting.
7. Research on detection method of anti-tumor extract of lignum pterocarpi indici
We found that the characteristics of the anti-tumor extract of santalum album can be well detected and labeled by thin layer chromatography, see fig. 1 and fig. 2.
The concrete conditions are as follows: GF254Silica gel board, development system: petroleum ether: ethyl acetate: acetone (6:1:1), petroleum ether: ethyl acetate: acetone (1:1:1), color development method: vanillin-concentrated sulfuric acid color development
Description of the drawings:
FIG. 1 TLC chromatogram of active extract of lignum Pterocarpi Indici;
FIG. 2 TLC chromatogram of active extract of lignum Pterocarpi Indici;
FIG. 3 TLC chromatogram of chemical components obtained from Pterocarpus santalinus;
FIG. 4 TLC chromatogram of the chemical components obtained from Pterocarpus santalinus.
Detailed Description
The following examples illustrate the utility of the invention, which is not limited thereby.
Example 1:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml methanol for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:14 recovering organic solvent from the eluent, and vacuum drying to obtain the extract. The yield thereof was found to be 0.57%.
Example 2:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml ethanol for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:14 recovering organic solvent from the eluate, and freeze drying to obtain the extract. The yield thereof was found to be 0.48%.
Example 3:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml acetone for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100: and (14) recovering the organic solvent from the eluent, and performing forced air drying to obtain the extract. The yield thereof was found to be 0.43%.
Example 4:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml of chloroform for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:14 recovering organic solvent from the eluent, and centrifugally drying to obtain the extract. The yield thereof was found to be 0.36%.
Example 5:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml ethyl acetate for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:14 recovering organic solvent from the eluent, and rotary steaming and drying to obtain the extract. The yield thereof was found to be 0.46%.
Example 6:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml methanol-water mixed solvent (methanol: water 1:1) for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:14 recovering organic solvent from the eluate, and freeze drying to obtain the extract. The yield thereof was found to be 0.51%.
Example 7:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml ethanol-water mixed solvent (ethanol: water 1:1) for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:14 recovering organic solvent from the eluent, and vacuum drying to obtain the extract. The yield thereof was found to be 0.47%.
Example 8:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml ethanol-water mixed solvent (ethanol: water: 90:10) for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:4, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:14, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:14 recovering organic solvent from the eluate, and freeze drying to obtain the extract. The yield thereof was found to be 0.53%.
Example 9:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml methanol for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:100, recovering the organic solvent from the eluent, and drying in vacuum to obtain the extract. The yield thereof was found to be 0.52%.
Example 10:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml ethanol for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100: recovering organic solvent from the eluent 100, and freeze-drying to obtain the extract. The yield thereof was found to be 0.47%.
Example 11:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml acetone for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:100, recovering the organic solvent from the eluent, and drying by blowing air to obtain the extract. The yield thereof was found to be 0.42%.
Example 12:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml of chloroform for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:100, recovering the organic solvent from the eluent, and centrifugally drying to obtain the extract. The yield thereof was found to be 0.41%.
Example 13:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml ethyl acetate for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:100, recovering the organic solvent from the eluent, and carrying out rotary evaporation and drying to obtain the extract. The yield thereof was found to be 0.44%.
Example 14:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml methanol-water mixed solvent (methanol: water 1:1) for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100: recovering organic solvent from the eluent 100, and freeze-drying to obtain the extract. The yield thereof was found to be 0.46%.
Example 15:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml ethanol-water mixed solvent (ethanol: water 1:1) for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100:100, recovering the organic solvent from the eluent, and drying in vacuum to obtain the extract. The yield thereof was found to be 0.47%.
Example 16:
ultrasonic extracting 20g of Uyghur medicine lignum Pterocarpi Indici with 100ml ethanol-water mixed solvent (ethanol: water: 90:10) for 15min, concentrating the extractive solution, separating with silica gel column, loading to silica gel column (2.0cm inner diameter column), extracting with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:25, volume ratio) eluted 15 column volumes, followed by a reaction with dichloromethane: methanol mixed solvent (dichloromethane: methanol, 100:100, volume ratio) eluted 20 column volumes. Dichloromethane: methanol 100: recovering organic solvent from the eluent 100, and freeze-drying to obtain the extract. The yield thereof was found to be 0.50%.
Example 17: solid dispersion
Weighing the santalum album extract and a carrier polyvinylpyrrolidone (PVP) according to the mass ratio of 1:2, 1:4 and 1:6, respectively putting the materials into a beaker, adding absolute ethyl alcohol, stirring by a magnetic stirrer until the santalum album extract and the carrier are completely dissolved, transferring into a rotary steaming instrument to remove an organic solvent, drying, crushing, and sieving by a 80-mesh sieve to obtain the PVP inclusion compound of the santalum album extract.
Example 18: cyclodextrin inclusion compounds
Grinding beta-cyclodextrin and 1-5 times of water uniformly, adding the santalum album extract (the water-insoluble one should be dissolved in a small amount of organic solvent at first) and fully grinding to paste, and drying at low temperature to obtain the final product.
Example 19: dispersible tablet
1. Weighing dried lignum Pterocarpi Indici extract, adding appropriate amount of sodium dodecyl sulfate, dissolving with 70% ethanol, adding water soluble starch and lignum Pterocarpi Indici extract (1: 1), stirring, mixing, drying at 70 deg.C, pulverizing, and sieving with 100 mesh sieve to obtain lignum Pterocarpi Indici extract dispersoid.
2. Precisely weighing the prescription amount, the santalum album extract dispersoid, the crospovidone and the compressible starch, using 70% ethanol as a wetting agent, stirring while adding, preparing wet granules by a 14-mesh sieve, standing for 15min at room temperature, drying for 45min in an oven at 70 ℃, granulating by a 16-mesh sieve, adding talcum powder and silica gel, mixing uniformly, and tabletting.
Claims (10)
1. An Uyghur medicine pterocarpus santalinus extract is characterized in that Uyghur medicine pterocarpus santalinus is subjected to ultrasonic extraction through an organic solvent, an extracting solution is concentrated and then is separated through a silica gel column, and a silica gel column after sample loading is firstly prepared by using dichloromethane with the volume ratio of 100:0-100: 4: eluting with a methanol mixed solvent, and then adding dichloromethane with the volume ratio of 100:5-100: 14: methanol mixed solvent elution, dichloromethane: methanol 100:5-100:14 drying the eluent to obtain the extract, or firstly adding dichloromethane with the volume ratio of 100: 25: eluting with a methanol mixed solvent, and then adding dichloromethane with the volume ratio of 100:30-100: methanol mixed solvent elution, dichloromethane: methanol 100:5-100:14 drying the eluent to obtain the extract.
2. The extract of santalum album of claim 1, wherein the organic solvent for extraction is methanol, ethanol, acetone, chloroform, ethyl acetate, methanol-water mixture or ethanol-water mixture, preferably methanol or 95% ethanol, and the amount of the organic solvent for extraction is 2-50 times (weight/volume ratio) the weight of the herbs.
3. The Uygur medicine lignum pterocarpi indici extract of claim 1, wherein the amount of the eluent is 2-50 column volumes.
4. The Uyghur medicine santalum album extract of claim 1, wherein the extract is prepared by first mixing dichloromethane in a volume ratio of 100: 4: methanol elution 10 column volumes followed by dichloromethane at a volume ratio of 100: 14: methanol eluted 15 column volumes.
5. The Uyghur medicine santalum album extract of claim 1, wherein the extract is prepared by first mixing dichloromethane in a volume ratio of 100: 25: methanol elution 10 column volumes followed by dichloromethane at a volume ratio of 100: methanol eluted 15 column volumes.
6. A pharmaceutical composition comprising the santalum album extract of any one of claims 1-5 and a pharmaceutically acceptable carrier.
7. A pharmaceutical preparation comprising the santalum album extract according to any one of claims 1-5 or the pharmaceutical composition according to claim 6.
8. The pharmaceutical formulation of claim 7, wherein the formulation is a solid dispersion, a cyclodextrin inclusion complex, a dispersible tablet.
9. Use of the extract of any one of claims 1 to 5, the composition of claim 6 or the pharmaceutical formulation of claim 7 for the preparation of an anti-tumor medicament, wherein the tumor is brain glioma, breast cancer, lung cancer, stomach cancer, colon cancer, pancreatic cancer, cervical cancer or liver cancer.
10. The extract of santalum album of any of claims 1-5, wherein the chromatography conditions, as determined by TLC, are: GF254Silica gel board, development system: petroleum ether: ethyl acetate: acetone (6:1:1), petroleum ether: ethyl acetate: acetone (1:1:1), color development method: and (4) developing the color by vanillin-concentrated sulfuric acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510081022.XA CN105982946A (en) | 2015-02-15 | 2015-02-15 | Preparation method and medicinal use of Pterocarpus santalinus antitumor extract and composition thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510081022.XA CN105982946A (en) | 2015-02-15 | 2015-02-15 | Preparation method and medicinal use of Pterocarpus santalinus antitumor extract and composition thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105982946A true CN105982946A (en) | 2016-10-05 |
Family
ID=57042249
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510081022.XA Pending CN105982946A (en) | 2015-02-15 | 2015-02-15 | Preparation method and medicinal use of Pterocarpus santalinus antitumor extract and composition thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105982946A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109060809A (en) * | 2018-08-28 | 2018-12-21 | 西藏民族大学 | A kind of Tibet red sandalwood quality standard and its detection method |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101637484A (en) * | 2009-09-08 | 2010-02-03 | 青海大学 | Active extract for sanwei sandalwood as well as extraction method and medical application thereof |
| CN102219782A (en) * | 2011-05-18 | 2011-10-19 | 华南农业大学 | Method for extracting and separating viterxin and isovitexin from natural product |
-
2015
- 2015-02-15 CN CN201510081022.XA patent/CN105982946A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101637484A (en) * | 2009-09-08 | 2010-02-03 | 青海大学 | Active extract for sanwei sandalwood as well as extraction method and medical application thereof |
| CN102219782A (en) * | 2011-05-18 | 2011-10-19 | 华南农业大学 | Method for extracting and separating viterxin and isovitexin from natural product |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109060809A (en) * | 2018-08-28 | 2018-12-21 | 西藏民族大学 | A kind of Tibet red sandalwood quality standard and its detection method |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN105983022A (en) | Preparation method and medicinal application of Viola tianschanica Maxim. antitumor extract and composition thereof | |
| CN105982945A (en) | Preparation method and medicinal application of euphorbium antitumor extract and composition thereof | |
| CN105982937A (en) | Preparation method and medicinal application of Atractylodes lancea antitumor extract and composition thereof | |
| CN105982946A (en) | Preparation method and medicinal use of Pterocarpus santalinus antitumor extract and composition thereof | |
| CN105982928A (en) | Medicinal use and preparation method and of seabuckthorn fruit antitumor extract and composition thereof | |
| CN105982927A (en) | Preparation method and medicinal use of Mesua ferrea L. antitumor extract and composition thereof | |
| CN104666595A (en) | Medical application of common physochlaina antitumor extract and composition thereof and preparation method | |
| CN114605422A (en) | A pair of enantiomer alkaloid dimer compounds, and preparation method and application thereof | |
| CN106031743A (en) | Medical uses and preparing method of mint anti-tumor extract product and composition of the extract product | |
| CN105982939A (en) | Preparation method and medicinal use of Brassica rapa L. antitumor extract and composition thereof | |
| CN105982955A (en) | Medicinal use and preparation method of Dracocephalum moldavica antitumor extract and composition thereof | |
| CN105982929A (en) | Preparation method and medicinal use of Fructus Terminaliae Billericae pulp antitumor extract and composition thereof | |
| CN105982917B (en) | The preparation method and medical usage of larva of a silkworm with batrytis antineoplastic extract and combinations thereof | |
| CN105982962A (en) | Medicinal use and preparation method of cinnamon leaf antitumor extract and composition thereof | |
| CN111454241A (en) | Biisopentenyl flavonoid compound and preparation method and application thereof | |
| CN105982934A (en) | Preparation method and medicinal use of Asarum europaeum L. antitumor extract and composition thereof | |
| CN105982932A (en) | Preparation method and medicinal application of Pimpinella anisum seed antitumor extract and composition thereof | |
| CN105982931A (en) | Medicinal use and preparation method of Axillary Choerospondias Fruit antitumor extract and composition thereof | |
| CN105982966A (en) | Medicinal use and preparation method of Syringa pinnatifolia Hemsl. root antitumor extract and composition thereof | |
| CN106031747A (en) | Application and preparation method of ramulus mori antitumor extract and composition thereof | |
| CN104873550A (en) | Medical application and preparation method Scabiosa anti-tumor extract and composition | |
| CN104688824A (en) | Fraxinus chinensis anti-tumor extractive as well as medical application and preparation method of composition thereof | |
| CN105982935A (en) | Preparation method and medicinal use of Acroptilon repens (L. ) DC dry fruit antitumor extract and composition thereof | |
| CN105982949A (en) | Preparation method and medicinal application of Astragalus saucocolla Dun gum antitumor extract and composition thereof | |
| CN105982942A (en) | Preparation method and medicinal application of Commiphora myrrha branch antitumor extract and composition thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20161005 |