CN102872029B - Gypensapogenin B在制备促进小肠蠕动药物中的应用 - Google Patents
Gypensapogenin B在制备促进小肠蠕动药物中的应用 Download PDFInfo
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- CN102872029B CN102872029B CN201210415417.5A CN201210415417A CN102872029B CN 102872029 B CN102872029 B CN 102872029B CN 201210415417 A CN201210415417 A CN 201210415417A CN 102872029 B CN102872029 B CN 102872029B
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- NNUMQZNZQGQGCN-AGHUFMIKSA-N gypensapogenin b Chemical compound O=C1C(=C(C)C)CC([C@@H]2[C@@H]3[C@@]([C@@]4(CCC5=C([C@H]6CC[C@H](O6)C5(C)C)[C@H]4CC3)C)(C)CC2)=C1 NNUMQZNZQGQGCN-AGHUFMIKSA-N 0.000 title claims abstract description 54
- 230000008855 peristalsis Effects 0.000 title claims abstract description 21
- 239000003814 drug Substances 0.000 title claims abstract description 15
- 230000001737 promoting effect Effects 0.000 title abstract description 8
- 210000000813 small intestine Anatomy 0.000 title abstract description 7
- 230000000968 intestinal effect Effects 0.000 claims description 16
- 238000002360 preparation method Methods 0.000 claims description 13
- 150000001875 compounds Chemical class 0.000 abstract description 11
- 230000000694 effects Effects 0.000 abstract description 4
- 238000002474 experimental method Methods 0.000 abstract description 4
- 239000003610 charcoal Substances 0.000 description 4
- 240000006509 Gynostemma pentaphyllum Species 0.000 description 3
- 235000002956 Gynostemma pentaphyllum Nutrition 0.000 description 3
- 235000010489 acacia gum Nutrition 0.000 description 3
- 239000001785 acacia senegal l. willd gum Substances 0.000 description 3
- 229930182490 saponin Natural products 0.000 description 3
- 150000007949 saponins Chemical class 0.000 description 3
- 235000017709 saponins Nutrition 0.000 description 3
- 150000003648 triterpenes Chemical class 0.000 description 3
- 238000012449 Kunming mouse Methods 0.000 description 2
- 241000699666 Mus <mouse, genus> Species 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 210000001187 pylorus Anatomy 0.000 description 2
- INLFWQCRAJUDCR-IQVMEADQSA-N (1R,2S,4S,5'S,6R,7S,8R,9S,12S,13S)-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icosane-6,2'-oxane] Chemical compound O([C@@H]1[C@@H]([C@]2(CC[C@@H]3[C@@]4(C)CCCCC4CC[C@H]3[C@@H]2C1)C)[C@@H]1C)[C@]11CC[C@H](C)CO1 INLFWQCRAJUDCR-IQVMEADQSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 235000003143 Panax notoginseng Nutrition 0.000 description 1
- 241000180649 Panax notoginseng Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 238000004140 cleaning Methods 0.000 description 1
- 230000001472 cytotoxic effect Effects 0.000 description 1
- OORMXZNMRWBSTK-UHFFFAOYSA-N dammaran Natural products C1CCC(C)(C)C2CCC3(C)C4(C)CCC(C(C)CCCC(C)C)C4CCC3C21C OORMXZNMRWBSTK-UHFFFAOYSA-N 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000001141 propulsive effect Effects 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
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- Medicines Containing Plant Substances (AREA)
- Steroid Compounds (AREA)
Abstract
本发明涉及GypensapogeninB在制备促进小肠蠕动药物中的应用。本发明提出GypensapogeninB在制备促进小肠蠕动药物中的应用。从药理实验看出，GypensapogeninB有较好的促进小肠蠕动的作用。本发明涉及的GypensapogeninB在制备促进小肠蠕动药物中的用途属于首次公开，由于骨架类型属于全新的骨架类型，而且其促进小肠蠕动活性强得意想不到，不存在由其他化合物给出任何启示的可能，具备突出的实质性特点，同时用于制备促进小肠蠕动药物显然具有显著的进步。
Description
技术领域
本发明涉及一种Gypensapogenin B的新药物用途。具体说就是在制备促进小肠蠕动药物中的应用，属于医药领域。
背景技术
本发明涉及的化合物Gypensapogenin B是一个2012年发表（Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173–178.）的新骨架化合物，该化合物拥有全新的骨架类型，目前的用途仅仅涉及人肿瘤细胞株的细胞毒活性（Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173–178.），对于本发明涉及的Gypensapogenin B在制备促进小肠蠕动药物中的用途属于首次公开，由于骨架类型属于全新的骨架类型，而且其促进小肠蠕动活性强得意想不到，不存在由其他化合物给出任何启示的可能，具备突出的实质性特点，同时用于制备促进小肠蠕动药物显然具有显著的进步。
发明内容
本发明提出Gypensapogenin B在制备促进小肠蠕动药物中的应用。从药理实验看出，Gypensapogenin B有较好的促进小肠蠕动的作用。可以用于多种小肠蠕动不良疾病的治疗。
由于本发明首次公开Gypensapogenin B在促进小肠蠕动方面的药用作用。
所述化合物Gypensapogenin B结构如式（Ⅰ）所示：
式（Ⅰ）
本发明涉及的Gypensapogenin B在制备促进小肠蠕动药物中的用途属于首次公开，由于骨架类型属于全新的骨架类型，而且其促进小肠蠕动活性强得意想不到，不存在由其他化合物给出任何启示的可能，具备突出的实质性特点，同时用于制备促进小肠蠕动药物显然具有显著的进步。
具体实施方式
本发明所涉及化合物Gypensapogenin B的制备方法参见文献（Li, N. et al., 2012. Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum. European Journal of Medicinal Chemistry 50, 173–178.和Wei, J.X. et al., 1982. Two new dammaran sapogenins from leaves of Panax notoginseng. Planta Medica, 45(3): 167-171.）。
以下通过实施例对本发明作进一步详细的说明，但本发明的保护范围不受具体实施例的任何限制，而是由权利要求加以限定。
实施例1：本发明所涉及化合物Gypensapogenin B片剂的制备：
取20克化合物Gypensapogenin B，加入制备片剂的常规辅料180克，混匀，常规压片机制成1000片。
实施例2：本发明所涉及化合物Gypensapogenin B胶囊剂的制备：
取20克化合物Gypensapogenin B，加入制备胶囊剂的常规辅料如淀粉180克，混匀，装胶囊制成1000片。
下面通过药效学实验来进一步说明其药物活性。
实验例：
1、实验动物：
昆明种小鼠，清洁级，体重20±2g，雌雄共用，
试剂及其他药品：
阿拉伯胶、炭末、生理盐水、Gypensapogenin B。
2、实验方法：
取昆明小鼠30只，20±5g，雌雄各半，按性别，体重随机分为3组，即空白组，Gypensapogenin B（0.06 mg/10g，0.24 mg/10g）两个剂量组。每组10只，Gypensapogenin B与5%炭末、10%阿拉伯胶制成混悬液，空白组不加药物直接给炭末、阿拉伯胶混悬，均用生理盐水配制。实验前小鼠禁食24小时。小鼠灌胃给药0.2 ml/10g，给药后30min处死。取幽门至回盲部消化管，不加牵引地平铺与薄板上，测全长及幽门至炭末前沿的距离，由此推算出推进百分率。
3、实验结果
统计结果表明Gypensapogenin B低剂量组小鼠的小肠推进性蠕动较空白组有所增加，差异有显著性意义（P<0.01）；Gypensapogenin B高剂量组较空白组，差异有显著性意义（P<0.001）结果如表1。
表1 Gypensapogenin B对小鼠小肠推进性蠕动的影响
与空白组比较，*p<0.01, **P<0.001
结论：Gypensapogenin B有较好的促进小肠蠕动的作用。可以用于多种小肠蠕动不良疾病的治疗。
Claims (1)
1.Gypensapogenin B在制备促进小肠蠕动药物中的应用，所述化合物Gypensapogenin B结构如式（Ⅰ）所示：
式（Ⅰ）。
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| CN201210415417.5A CN102872029B (zh) | 2012-10-26 | 2012-10-26 | Gypensapogenin B在制备促进小肠蠕动药物中的应用 |
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| CN201210415417.5A CN102872029B (zh) | 2012-10-26 | 2012-10-26 | Gypensapogenin B在制备促进小肠蠕动药物中的应用 |
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| CN102872029A CN102872029A (zh) | 2013-01-16 |
| CN102872029B true CN102872029B (zh) | 2013-10-23 |
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2012
- 2012-10-26 CN CN201210415417.5A patent/CN102872029B/zh active Active
Non-Patent Citations (2)
| Title |
|---|
| Ning Li 等.Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum.《European Journal of Medicinal Chemistry》.2012,第50卷173-178. |
| Triterpenes possessing an unprecedented skeleton isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum;Ning Li 等;《European Journal of Medicinal Chemistry》;20120203;第50卷;173-178 * |
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| CN102872029A (zh) | 2013-01-16 |
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