CN1108308C - 一种匙羹藤提取物及其制备方法和用途 - Google Patents
一种匙羹藤提取物及其制备方法和用途 Download PDFInfo
- Publication number
- CN1108308C CN1108308C CN99103588A CN99103588A CN1108308C CN 1108308 C CN1108308 C CN 1108308C CN 99103588 A CN99103588 A CN 99103588A CN 99103588 A CN99103588 A CN 99103588A CN 1108308 C CN1108308 C CN 1108308C
- Authority
- CN
- China
- Prior art keywords
- extract
- gymnema sylvestre
- time
- extraction
- triterpenoid saponin
- 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.)
- Expired - Fee Related
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 10
- 239000000284 extract Substances 0.000 title claims description 62
- 241000208253 Gymnema sylvestre Species 0.000 title claims description 43
- 238000000605 extraction Methods 0.000 claims abstract description 28
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims abstract description 9
- 150000008130 triterpenoid saponins Chemical class 0.000 claims abstract description 9
- 239000003814 drug Substances 0.000 claims abstract description 4
- 229930182486 flavonoid glycoside Natural products 0.000 claims abstract description 3
- 150000007955 flavonoid glycosides Chemical class 0.000 claims abstract description 3
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 22
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 13
- 238000000034 method Methods 0.000 claims description 9
- 239000007788 liquid Substances 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- -1 triterpenoid saponin compounds Chemical class 0.000 claims description 8
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims description 7
- 239000002775 capsule Substances 0.000 claims description 6
- 239000000469 ethanolic extract Substances 0.000 claims description 6
- 230000002218 hypoglycaemic effect Effects 0.000 claims description 6
- 239000000796 flavoring agent Substances 0.000 claims description 5
- 235000019634 flavors Nutrition 0.000 claims description 5
- 235000012054 meals Nutrition 0.000 claims description 5
- 238000010992 reflux Methods 0.000 claims description 5
- 241000240378 Gymnema latifolium Species 0.000 claims description 4
- 230000000702 anti-platelet effect Effects 0.000 claims description 4
- 239000003146 anticoagulant agent Substances 0.000 claims description 4
- VEVZSMAEJFVWIL-UHFFFAOYSA-O cyanidin cation Chemical compound [O+]=1C2=CC(O)=CC(O)=C2C=C(O)C=1C1=CC=C(O)C(O)=C1 VEVZSMAEJFVWIL-UHFFFAOYSA-O 0.000 claims description 4
- 239000002904 solvent Substances 0.000 claims description 4
- 235000007336 cyanidin Nutrition 0.000 claims description 2
- 150000004676 glycans Chemical class 0.000 claims description 2
- 229920001282 polysaccharide Polymers 0.000 claims description 2
- 239000005017 polysaccharide Substances 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 abstract description 11
- 239000008280 blood Substances 0.000 abstract description 11
- 150000002632 lipids Chemical class 0.000 abstract description 6
- 239000000203 mixture Substances 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 4
- 206010012601 diabetes mellitus Diseases 0.000 abstract description 2
- XBZYWSMVVKYHQN-MYPRUECHSA-N (4as,6as,6br,8ar,9r,10s,12ar,12br,14bs)-10-hydroxy-2,2,6a,6b,9,12a-hexamethyl-9-[(sulfooxy)methyl]-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-icosahydropicene-4a-carboxylic acid Chemical compound C1C[C@H](O)[C@@](C)(COS(O)(=O)=O)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CCC(C)(C)C[C@H]5C4=CC[C@@H]3[C@]21C XBZYWSMVVKYHQN-MYPRUECHSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 14
- 241000700159 Rattus Species 0.000 description 13
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 239000000243 solution Substances 0.000 description 8
- 210000002966 serum Anatomy 0.000 description 6
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 5
- 239000000741 silica gel Substances 0.000 description 5
- 229910002027 silica gel Inorganic materials 0.000 description 5
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 4
- 241000283973 Oryctolagus cuniculus Species 0.000 description 4
- 229930006000 Sucrose Natural products 0.000 description 4
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 4
- KNHUKKLJHYUCFP-UHFFFAOYSA-N clofibrate Chemical compound CCOC(=O)C(C)(C)OC1=CC=C(Cl)C=C1 KNHUKKLJHYUCFP-UHFFFAOYSA-N 0.000 description 4
- 229960001214 clofibrate Drugs 0.000 description 4
- 239000008103 glucose Substances 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 239000005720 sucrose Substances 0.000 description 4
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 3
- 208000031226 Hyperlipidaemia Diseases 0.000 description 3
- 235000013305 food Nutrition 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 235000021590 normal diet Nutrition 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- ICFJFFQQTFMIBG-UHFFFAOYSA-N phenformin Chemical compound NC(=N)NC(=N)NCCC1=CC=CC=C1 ICFJFFQQTFMIBG-UHFFFAOYSA-N 0.000 description 3
- 229960003243 phenformin Drugs 0.000 description 3
- 239000013641 positive control Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 238000005303 weighing Methods 0.000 description 3
- 241000037488 Coccoloba pubescens Species 0.000 description 2
- 241000208251 Gymnema Species 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 235000012000 cholesterol Nutrition 0.000 description 2
- 239000012153 distilled water Substances 0.000 description 2
- 229930183009 gymnemic acid Natural products 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 239000002504 physiological saline solution Substances 0.000 description 2
- 210000004623 platelet-rich plasma Anatomy 0.000 description 2
- 239000000080 wetting agent Substances 0.000 description 2
- BHQCQFFYRZLCQQ-UHFFFAOYSA-N (3alpha,5alpha,7alpha,12alpha)-3,7,12-trihydroxy-cholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 BHQCQFFYRZLCQQ-UHFFFAOYSA-N 0.000 description 1
- 241000208327 Apocynaceae Species 0.000 description 1
- 239000004380 Cholic acid Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 101001046633 Homo sapiens Junctional adhesion molecule A Proteins 0.000 description 1
- 102100022304 Junctional adhesion molecule A Human genes 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 208000004880 Polyuria Diseases 0.000 description 1
- 208000004078 Snake Bites Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 238000010241 blood sampling Methods 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 235000019416 cholic acid Nutrition 0.000 description 1
- BHQCQFFYRZLCQQ-OELDTZBJSA-N cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 description 1
- 229960002471 cholic acid Drugs 0.000 description 1
- KXGVEGMKQFWNSR-UHFFFAOYSA-N deoxycholic acid Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 KXGVEGMKQFWNSR-UHFFFAOYSA-N 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 230000035619 diuresis Effects 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000007710 freezing Methods 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 201000004792 malaria Diseases 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- PMRYVIKBURPHAH-UHFFFAOYSA-N methimazole Chemical compound CN1C=CNC1=S PMRYVIKBURPHAH-UHFFFAOYSA-N 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 210000004279 orbit Anatomy 0.000 description 1
- 239000006201 parenteral dosage form Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 238000005453 pelletization Methods 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 210000002381 plasma Anatomy 0.000 description 1
- 239000001508 potassium citrate Substances 0.000 description 1
- 229960002635 potassium citrate Drugs 0.000 description 1
- QEEAPRPFLLJWCF-UHFFFAOYSA-K potassium citrate (anhydrous) Chemical compound [K+].[K+].[K+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O QEEAPRPFLLJWCF-UHFFFAOYSA-K 0.000 description 1
- 235000011082 potassium citrates Nutrition 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229960002178 thiamazole Drugs 0.000 description 1
- 229940098465 tincture Drugs 0.000 description 1
- KWEUUBDPVVHQAL-MSQVLRTGSA-K trisodium;[[(2r,3s,4r,5r)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] phosphate Chemical compound [Na+].[Na+].[Na+].C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP([O-])(=O)OP([O-])([O-])=O)[C@@H](O)[C@H]1O KWEUUBDPVVHQAL-MSQVLRTGSA-K 0.000 description 1
Classifications
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
本发明涉及一种匙羹藤提取物，该提取物主要由总三萜皂甙、黄酮甙、花色素、多糖等成分组成，其中总三萜皂甙的含量为50-99%，在该总三萜皂甙中有25-40%的六种新三萜皂甙化合物。该提取物具有降糖、降脂和抗血小板凝聚的活性作用，本发明还涉及该提取物的制备方法和它的用途，尤其是它在制备治疗糖尿病药物方面的用途。此外本发明还涉及含有该提取物的药物组合物。
Description
本发明涉及一种匙羹藤提取物，该提取物具有降糖、降脂和抗血小板凝聚的活性作用，本发明还涉及该提取物的制备方法和它的用途，尤其是它在制备治疗糖尿病药物方面的用途。此外，本发明又涉及了含有该提取物作活性成分的药物组合物。
匙羹藤为萝摩科植物Gymnema sylvestre R.Br.，由于它在印度民间用于抗肿毒、蛇伤、解疟、利尿和降血糖等，所以人们对它所含的成分进行了许多研究和报导，发现其中所含的匙羹藤酸具有降糖活性。发明人经过大量的试验研究，进一步发现匙羹藤提取物的功效优于单一的匙羹藤酸，因为在匙羹藤提取物中含有特定含量的六种新三萜皂甙化合物，到目前为止，尚没有发现含有这六种新三萜皂甙的匙羹藤提取物的文献报导。
本发明的目的是提供一种匙羹藤提取物。
本发明的另一目的是提供该提取物的制备方法。
本发明的又一目的是提供含有该提取物作活性成分的药物组合物。
本发明涉及的匙羹藤提取物是这样得到的：将匙羹藤叶粗粉用60-95％的乙醇回流提取1-4次，每次提取溶剂用量为6ml/g，提取时间1-3小时，合并乙醇提取液，加压回收至无醇味，用环己烷萃取所得到的浓缩液1-3次，每次使用溶剂量为500ml，然后再用500ml的正丁醇萃取1-3次，合并正丁醇萃取液，减压回收，得到干浸膏状物，即为本发明匙羹藤提取物。其中乙醇的优选浓度为75％。优选提取次数为3次，优选提取时间为2小时。环己烷的优选萃取次数为3次，正丁醇的优选萃取次数为3次。
发明人经过深入研究，发现本发明涉及的匙羹藤提取物主要由总三萜皂甙、黄酮甙、花色素、多糖等成分组成，其中总三萜皂甙的含量为50-99％。在该总三萜皂甙中含有25-40％的六种新三萜皂甙化合物，本说明书中用GA-1到GA-6来表示，它们分别具有式I或式II的结构：当R1＝H时，为GA-1；当R1＝
时，为GA-2；当R1＝H并且R2＝
时，为GA-3；当R1＝
并且R2＝H时，为GA-4；当R1＝
并且R2＝
时，为GA-5；当R1＝H并且R2＝
为GA-6。
这六种新三萜皂甙化合物在本发明提取物中的含量分别为1.25-2.10％的GA-1、0.89-1.50％的GA-2、2.40-3.80％的GA-3、2.10-3.40％的GA-4、2.74-4.60％的GA-5、3.24-5.40％的GA-6。优选含量分别为1.60％的GA-1、1.20％的GA-2、3.10％的GA-3、2.70％的GA-4、3.60％的GA-5和4.30％的GA-6。当本发明提取物中含有上述优选含量的六种新三萜皂甙化合物时，本发明提取物的疗效最佳。
本发明匙羹藤提取物具有降糖、降脂和抗血小板凝聚的活性作用。胃肠给药时，该提取物的LD50为4880mg/kg，胃肠外给药时，该提取物的LD50为107.0mg/kg。因此可用它作活性成分制备具有降糖、降脂和抗血小板凝聚作用的药物组合物。
本发明匙羹藤提取物可以作为活性成分与药学上可接受的赋型剂一起用于制备药物组合物，该药物组合物可以采用本领域的常规方法制备成各种剂型，如胶囊、丸剂、片剂、口服液、颗粒剂、酊剂等肠道给药的剂型和注射液等胃肠外给药剂型。根据剂型的不同，该药物组合物使用的赋型剂也不同，常用赋型剂包括稀释剂、湿润剂、润滑剂、填充剂、防腐剂等。其中稀释剂为乳糖、淀粉、糊精、微晶纤维素、微粉硅胶等，湿润剂为水和50-85％不同浓度的乙醇。含有本发明匙羹藤提取物的药物组合物的优选剂型是口服制剂，最好为胶囊。给药剂量为100-400mg/人/次，每天3次。
以下通过实施例和试验例来详细地说明本发明。
实施例1
称取匙羹藤干叶粗粉1000g，用600ml的60％的乙醇回流提取3次，每次2小时，合并提取液，减压回收至无醇味，得到浓缩液，把所得到的浓缩液用500ml的环己烷萃取3次，然后再用500ml的正丁醇萃取3次，合并3次正丁醇萃取液，减压回收得到64.0g干浸膏，即本发明匙羹藤提取物。
实施例2
称取匙羹藤叶粗粉1000g，用6.0L 75％的乙醇回流提取3次，每次2小时，合并乙醇提取液，把该乙醇提取液减压回收至无醇味，把浓缩液用500ml的环己烷萃取，再用500ml的正丁醇萃取3次，合并正丁醇萃取液，减压回收，得到干浸膏状物72.0g。
实施例3
称取匙羹藤叶粗粉1000g，用6L 95％的乙醇回流提取3次，每次2小时，合并乙醇提取液，把该乙醇提取液减压回收至无醇味，把浓缩液用500ml的环己烷萃取，再用500ml的正丁醇萃取3次，合并正丁醇萃取液，减压回收，得到干浸膏状物61.0g。
实施例4
把本发明匙羹藤提取物100mg和微粉硅胶200mg充分混合均匀，过筛，加入适量的硬脂酸镁，混匀，用干法造粒机制粒，过筛，筛取40-80目之间的颗粒，装入胶囊，每粒装0.3g。
实施例5
按照实施例4所述方法制备胶囊，不同的是使用200mg的本发明匙羹藤提取物、100mg微粉硅胶和适量的硬脂酸镁。实施例6
按照实施例4所述方法制备胶囊，不同的是使用250mg的本发明匙羹藤提取物、50mg微粉硅胶和适量硬脂酸镁。
实施例7
按照实施例4所述方法制备胶囊，不同的是使用450mg的本发明匙羹藤提取物、50mg微粉硅胶和适量硬脂酸镁。
试验例1：本发明匙羹藤提取物对蔗糖致大鼠血糖升高的影响
雌性SD大鼠，禁食24h后，随机分为实验组，一次口服给予本发明匙羹藤提取物50，100，200mg/kg，阳性对照组分别给予降糖灵100mg/kg，正常组及对照组及空白对照组口服给予等容量蒸馏水，给药体积为10ml/kg，30min后，除正常组外，各组口服给予蔗糖溶液1g/kg(5ml/kg)，并分别于其后30，60，120min，由大鼠眼眶采血100μl，测定血清葡糖含量。
结果，大鼠口服蔗糖后30，60min内，血糖值明显上升，本发明匙羹藤提取物100mg/kg在30min，本发明匙羹藤提取物200mg/kg和降糖灵100mg/kg在30，60min均使大鼠升高的血糖值显著下降，且两者作用强度相近，见表1。表1：本发明匙羹藤提取物对蔗糖致大鼠血糖升高的影响(X±SD，n＝10)
| 组别 | 剂量(mg/kg) | 血糖值(mmol/L) | ||
| 30min | 60min | 120min | ||
| 正常组 | 3.56±0.64 | 4.12±0.72 | 3.76±0.69 | |
| 对照组 | 6.58±0.87ΔΔ | 5.93±1.27ΔΔ | 4.54±1.37 | |
| 本发明匙羹藤提取物 | 50 | 6.03±0.86 | 6.42±0.78 | 4.26±1.03 |
| 100 | 5.12±1.29* | 5.77±1.09 | 4.53±0.94 | |
| 200 | 4.43±0.72** | 4.73±0.83* | 4.07±0.70 | |
| 降糖灵 | 100 | 4.24±0.87** | 4.74±0.90* | 4.79±1.03 |
ΔΔp＜0.01，与正常组比较；*p＜0.05，**p＜0.01，与对照组比较。试验例2：本发明匙羹藤提取物对高脂血症大鼠血清甘油三酯、胆固醇含量的影响
雄性SD大鼠，体重130-170g，正常组给予普通饲料，其它各组给予高脂饲料(1％胆固醇、10％猪油、0.3％胆酸、0.2％甲硫基咪唑和88.5％普通饲料，自制成块状饲料)。连续14天，大鼠禁食12h后，按试剂盒法测定大鼠血清甘油三酯及胆固醇含量，然后，按血脂值进行随机分组。实验组口服给予50、100、200mg/kg，阳性对照组分别口服安妥明100mg/kg，对照组给予蒸馏水，给药体积为10ml/kg，连续10天，各组在给药前5天仍饲以高脂饲料，后5天饲以普通饲料，末次给药前禁食11h，给药后1h采血测血清中甘油三酯及胆固醇含量。
结果，大鼠给予高脂饲料10天后，血清甘油三酯及胆固醇含量明显升高，本发明匙羹藤提取物50、100、200mg/kg及安妥明100mg/kg均使高脂血症大鼠血清甘油三酯及胆固醇水平明显下降，本发明匙羹藤提取物200mg/kg的降血脂作用与安妥明100mg/kg相近，见表2。表2：本发明匙羹藤提取物对高脂血症大鼠血脂含量的影响(X±SD，n＝9-10)
| 组别 | 剂量(mg/kg) | 甘油三酯(mmol/L) | 总胆固醇(mmol/L) | ||
| 给药前 | 给药后 | 给药前 | 给药后 | ||
| 正常组 | 1.02±0.22 | 1.04±0.15 | 2.43±0.41 | 1.99±0.47 | |
| 对照组 | 2.64±0.82 | 3.04±0.93 | 4.10±0.51ΔΔ | 4.77±0.63ΔΔ | |
| 本发明匙羹藤提取物 | 50 | 2.72±0.61 | 2.41±0.44 | 4.29±0.60 | 3.92±0.58** |
| 100 | 2.54±0.90 | 1.75±0.53** | 4.02±0.59 | 2.94±0.66** | |
| 200 | 2.72±0.76 | 1.37±0.40** | 4.18±0.61 | 2.31±0.74** | |
| 安妥明 | 100 | 2.51±0.77 | 2.72±0.74 | 4.33±0.51 | 2.15±0.76** |
ΔΔp＜0.01，与正常组比较；**P＜0.01，与对照组比较试验例3：本发明匙羹藤提取物对体外家兔血小板聚集的影响
家兔心脏穿刺取血，3.8％枸橼酸钾抗凝(1：9)，1000rpm离心5min，取上层作为富血小板血浆(PRP)，再以4000rpm离心10min，上清液为贫血小板血浆(PPP)。将PPP 200μl移入比浊管，再加入不同浓度的本发明匙羹藤提取物生理盐水溶液10μl，终浓度分别为250，500，1000μg/ml，阳性对照管加入阿斯匹林生理盐水10μl，终浓度为250μg/ml，空白对照管加入生理盐水10μl，37℃温育2min后，放入测定孔，搅拌加入ADP钠盐生理盐水溶液10μl，终浓度为1.0×10-5M，在PAM-1血小板聚集仪上观察3min内的最大聚集率。
结果，本发明匙羹藤提取物500，1000μg/ml，阿斯匹林250μg/ml显著抑制家兔血小板聚集。见表3。表3：本发明匙羹藤提取物对体外家兔血小板聚集的影响(X±SD，n＝8)
| 组别 | 终浓度(ug/ml) | 最大聚集率(％) | 抑制率(％) |
| 对照组 | 47.9±5.2 | ||
| 本发明匙羹藤提取物 | 250 | 43.6±7.0 | 9.0 |
| 500 | 35.9±4.5** | 25.1 | |
| 1000 | 27.8±4.8** | 42.0 | |
| 阿斯匹林 | 250 | 23.7±6.0** | 50.3 |
**p＜0.01，与对照组比较。
Claims (11)
1.一种匙羹藤提取物的制备方法，它包括下列步骤：将匙羹藤叶粗粉用60-95％的乙醇回流提取1-4次，每次提取溶剂用量为6ml/g，提取时间1-3小时，合并乙醇提取液，加压回收至无醇味，用环己烷萃取所得到的浓缩液1-3次，每次使用溶剂量为500ml，然后再用500ml的正丁醇萃取1-3次，合并正丁醇萃取液，减压回收，得到干浸膏状物即得。
2.根据权利要求1所述的方法，其特征为使用75％的乙醇。
3.根据权利要求1或2所述的方法，其特征为提取次数为3次，提取时间为2小时。
4.根据权利要求1-3中任何一个所述的方法，其特征为环己烷萃取次数为3次，正丁醇的萃取次数为3次。
5.权利要求1-4中任一方法制备的匙羹藤提取物，其特征为它主要由总三萜皂甙、黄酮甙、花色素、多糖等成分组成，其中总三萜皂甙的含量为50-99％。
6.根据权利要求5所述的匙羹藤提取物，其特征为所述的总三萜皂甙中含有25-40％的六种新三萜皂甙化合物，其中用GA-1到GA-6表示的六种新三萜皂甙化合物分别具有式I或式II的结构：
当R1＝H时，为GA-1；当R1＝
时，为GA-2；当R1＝H并且R2＝
时，为GA-3；当R1＝
并且R2＝H时，为GA-4；当R1＝
并且R2＝
时，为GA-5；当R1＝H并且R2＝
时，为GA-6。
7.根据权利要求6所述的匙羹藤提取物，其特征为这六种新三萜皂甙化合物在提取物中的含量分别为1.25-2.10％的GA-1、0.89-1.50％的GA-2、2.40-3.80％的GA-3、2.10-3.40％的GA-4、2.74-4.60％的GA-5、3.24-5.40％的GA-6。
8.根据权利要求7所述的匙羹藤提取物，其中六种新三萜皂甙化合物在提取物中的含量分别为1.60％的GA-1、1.20％的GA-2、3.10％的GA-3、2.70％的GA-4、3.60％的GA-5和4.30％的GA-6。
9.权利要求5-8中任一所述的匙羹藤提取物在制备降糖、降脂和抗血小板凝聚的药物方面的用途。
10.一种含有权利要求5-8中任一所述的匙羹藤提取物作活性成分的药物组合物。
11.一种含有权利要求5-8中任一所述的匙羹藤提取物作活性成分的胶囊。
Priority Applications (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN99103588A CN1108308C (zh) | 1999-04-05 | 1999-04-05 | 一种匙羹藤提取物及其制备方法和用途 |
| US09/913,322 US6833443B1 (en) | 1999-02-11 | 2000-01-21 | Gymnemic acid derivatives, process for the preparation thereof and use thereof as medicine |
| DE60004353T DE60004353T2 (de) | 1999-02-11 | 2000-01-21 | Derivate der gymnemischen säure, verfahren zu ihrer herstellung und ihre verwendung als medikamente |
| CA2362864A CA2362864C (en) | 1999-02-11 | 2000-01-21 | New gymnemic acid derivatives, their preparation, pharmaceutical composition containing them and their medical use |
| PCT/CN2000/000010 WO2000047594A1 (fr) | 1999-02-11 | 2000-01-21 | Nouveau derives d'acide gymnemique, leur procede de preparation et leur application comme medicaments |
| KR1020017010217A KR100625222B1 (ko) | 1999-02-11 | 2000-01-21 | 신규 짐넴산 유도체, 그 제조 방법, 및 그의 약학적 용도 |
| AU20909/00A AU2090900A (en) | 1999-02-11 | 2000-01-21 | Novel gymnemic acid derivatives, process for the preparation thereof and use thereof as medicine |
| JP2000598513A JP4903309B2 (ja) | 1999-02-11 | 2000-01-21 | 新規ギムネマ酸誘導体、その製造、それらを含む医薬組成物、およびそれらの医薬的使用 |
| EP00901035A EP1176149B1 (en) | 1999-02-11 | 2000-01-21 | Novel gymnemic acid derivatives, process for the preparation thereof and use thereof as medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN99103588A CN1108308C (zh) | 1999-04-05 | 1999-04-05 | 一种匙羹藤提取物及其制备方法和用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1268515A CN1268515A (zh) | 2000-10-04 |
| CN1108308C true CN1108308C (zh) | 2003-05-14 |
Family
ID=5271355
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN99103588A Expired - Fee Related CN1108308C (zh) | 1999-02-11 | 1999-04-05 | 一种匙羹藤提取物及其制备方法和用途 |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1108308C (zh) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100335073C (zh) * | 2005-08-19 | 2007-09-05 | 浙江大学 | 木鳖子含三萜皂甙成分提取物的制备方法 |
| CN100424092C (zh) * | 2005-11-18 | 2008-10-08 | 华南理工大学 | 三萜烯糖苷天然甜味抑制剂的提取方法 |
| CN100455298C (zh) * | 2006-09-15 | 2009-01-28 | 江苏大学 | 一种匙羹藤总皂甙包合物及其制备方法 |
| CN106306817A (zh) * | 2015-07-08 | 2017-01-11 | 李凤军 | 一种防治糖尿病的保健食品组合物 |
| CN106474281A (zh) * | 2015-10-16 | 2017-03-08 | 赫博美国际有限公司 | 一种治疗ⅱ型糖尿病及其并发症的中药组合物及其制剂和制法 |
| CN106518950B (zh) * | 2016-10-21 | 2018-10-30 | 广西中医药大学 | 香树脂醇桂皮酸酯提取物及其制备方法 |
| CN108095054B (zh) * | 2017-12-19 | 2021-06-15 | 哈尔滨仑傲科技有限公司 | 一种减少膳食中糖分消化和吸收的植物性胶囊及其制备方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5843909A (en) * | 1997-06-13 | 1998-12-01 | Kowa Chemical Industries Co., Ltd. | (3-β), 4-α, 16-β)-16, -23, 28-trihdroxyolean-12-ene-3-yl-β-D-glucopyranuronic acid derivatives, as glucose absorption inhibiting agents |
-
1999
- 1999-04-05 CN CN99103588A patent/CN1108308C/zh not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5843909A (en) * | 1997-06-13 | 1998-12-01 | Kowa Chemical Industries Co., Ltd. | (3-β), 4-α, 16-β)-16, -23, 28-trihdroxyolean-12-ene-3-yl-β-D-glucopyranuronic acid derivatives, as glucose absorption inhibiting agents |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1268515A (zh) | 2000-10-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US4555504A (en) | Inclusion complex of β-cyclodextrin and digoxin | |
| CN101787061B (zh) | 曲札茋苷在制备防治心脑缺血疾病制剂中的应用及其制备方法 | |
| CN101537187B (zh) | 花色苷磷脂复合物及其制备方法 | |
| CN100594898C (zh) | 水飞蓟宾的药用组合物及其制备方法 | |
| CN101229316B (zh) | 一种知母提取物 | |
| US4515785A (en) | Neem bark extracts | |
| CN1108308C (zh) | 一种匙羹藤提取物及其制备方法和用途 | |
| EP1013278B1 (en) | The extract of pine needle and the use thereof | |
| CN101244190A (zh) | 一种薤白总甾体皂苷提取物的制备方法及其用途 | |
| EP1559703A1 (en) | A natural compound useful for treating diabetes, its preparation and use | |
| CN102827001A (zh) | 一种苦丁茶冬青提取物 | |
| US20170087201A1 (en) | Use of overground part of hedychium coronarium koenig in reducing blood glucose; extracts and compositions of overground part of hedychium coronarium koenig and their uses | |
| EP3750923A1 (en) | Separated saposhnikovia divaricata polysaccharide and use thereof | |
| CN101040917A (zh) | 具有降血糖活性的中药组合物 | |
| EP0014471B1 (en) | Acylated derivatives of a water extract of anemarrhenae rhizoma and hypoglycemic agents containing said derivatives | |
| US6833443B1 (en) | Gymnemic acid derivatives, process for the preparation thereof and use thereof as medicine | |
| US6475520B1 (en) | Pharmaceutical composition with low toxicity for anti-inflammation and anti-exudation | |
| CN1068790C (zh) | 含有西洋参茎叶总皂甙的药物组合物 | |
| JPS6183130A (ja) | 多糖類，その単離法および用途 | |
| KR20060114600A (ko) | 차가버섯 자실체로부터 추출한 신규의 항당뇨 활성 추출물및 이를 유효성분으로 함유한 항당뇨 활성 조성물 | |
| CN1108307C (zh) | 一种新皂甙化合物及其制备方法和用途 | |
| KR20040079285A (ko) | 인진호 추출물과 그 추출물을 함유한 당뇨병 관련 질환치료제 | |
| CN1095669C (zh) | 含原人参二醇组分皂甙的药物组合物,其制备方法及应用 | |
| CN1108306C (zh) | 一种新皂甙化合物及其制备方法和用途 | |
| KR0173814B1 (ko) | 해당화 근부 추출물을 포함하는 건강보조식품 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| ASS | Succession or assignment of patent right |
Owner name: GUILIN JIQI PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: SHANDONG GREEN LEAF PHARMACEUTICAL CO., LTD. Effective date: 20010928 |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20010928 Address after: 541004 No. 55 Yucai Road, Qixing District, Guilin, Guangxi Applicant after: Guilin Jiqi Pharmaceutical Industry Co., Ltd. Address before: 264003, No. 9, Po Yuen Road, Laishan District, Shandong, Yantai Applicant before: Luye Pharmaceutical Co., Ltd., Shandong |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| ASS | Succession or assignment of patent right |
Owner name: GUILIN JIQI PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: GUILIN JIQI PHARMACEUTICAL INDUSTRY CO., LTD. Effective date: 20110907 |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20110907 Address after: Huan Cheng Nan Qixing District, Guilin city 541004 the Guangxi Zhuang Autonomous Region Road No. 36 Building 2 water treatment plant Patentee after: Guilin Ji Qi Pharmaceutical Co., Ltd. Address before: 541004 No. 55 Yucai Road, Qixing District, Guilin, Guangxi Patentee before: Guilin Jiqi Pharmaceutical Industry Co., Ltd. |
|
| DD01 | Delivery of document by public notice |
Addressee: Feng Wenxin Document name: Notification of Passing Examination on Formalities |
|
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20030514 Termination date: 20160405 |