CN102885807B - Aphanamixoid A在制备促进小肠蠕动药物中的应用 - Google Patents
Aphanamixoid A在制备促进小肠蠕动药物中的应用 Download PDFInfo
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- CN102885807B CN102885807B CN201210412955.9A CN201210412955A CN102885807B CN 102885807 B CN102885807 B CN 102885807B CN 201210412955 A CN201210412955 A CN 201210412955A CN 102885807 B CN102885807 B CN 102885807B
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- 229930193702 aphanamixoid Natural products 0.000 title claims abstract description 24
- 230000000968 intestinal effect Effects 0.000 title claims abstract description 22
- 230000008855 peristalsis Effects 0.000 title claims abstract description 21
- 239000003814 drug Substances 0.000 title claims abstract description 15
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 230000001737 promoting effect Effects 0.000 title abstract description 6
- 229940079593 drug Drugs 0.000 title abstract description 5
- 150000001875 compounds Chemical class 0.000 abstract description 7
- 230000000694 effects Effects 0.000 abstract description 4
- 238000002474 experimental method Methods 0.000 abstract description 4
- 230000000144 pharmacologic effect Effects 0.000 abstract description 3
- 239000003610 charcoal Substances 0.000 description 4
- 240000003906 Aphanamixis grandifolia Species 0.000 description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 3
- 235000010489 acacia gum Nutrition 0.000 description 3
- 239000001785 acacia senegal l. willd gum Substances 0.000 description 3
- 150000002630 limonoids Chemical class 0.000 description 3
- 230000003389 potentiating effect Effects 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
- 239000000203 mixture Substances 0.000 description 2
- 210000001187 pylorus Anatomy 0.000 description 2
- 241000238631 Hexapoda Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 230000001887 anti-feedant effect Effects 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000001141 propulsive effect Effects 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
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Abstract
本发明涉及Aphanamixoid A在制备促进小肠蠕动药物中的应用。本发明提出Aphanamixoid A在制备促进小肠蠕动药物中的应用。从药理实验看出，AphanamixoidA有较好的促进小肠蠕动的作用。本发明涉及的Aphanamixoid A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Aphanamixoid A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Aphanamixoid A是一个2012年发表（Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524–2527.）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昆虫拒食活性（Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524–2527.），对于本发明涉及的Aphanamixoid A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Aphanamixoid A在制备促进小肠蠕动药物中的应用。从药理实验看出，Aphanamixoid A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，且无毒副作用。
由于本发明首次公开Aphanamixoid A在促进小肠蠕动方面的药用作用。
所述化合物Aphanamixoid A结构如式（Ⅰ）所示：
式（Ⅰ）
本发明涉及的Aphanamixoid A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Aphanamixoid A的制备方法参见文献（Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524–2527.）。
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Aphanamixoid A片剂的制备：
取20克化合物Aphanamixoid A，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Aphanamixoid A胶囊剂的制备：
取20克化合物Aphanamixoid A，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、Aphanamixoid A。
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，Aphanamixoid A（0.06 mg/10g，0.24 mg/10g）两个剂量组。每组10只，Aphanamixoid A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Aphanamixoid A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）；Aphanamixoid A高剂量组较空白组，差异有显著性意义（P<0.01）结果如表1。
表1 Aphanamixoid A对小鼠小肠推进性蠕动的影响（
）
与空白组比较，*p<0.01
结论：Aphanamixoid A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.Aphanamixoid A在制备促进小肠蠕动药物中的应用，所述化合物Aphanamixoid A结构如式（Ⅰ）所示：
式（Ⅰ）。
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| CN102885807B true CN102885807B (zh) | 2014-04-16 |
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- 2012-10-25 CN CN201210412955.9A patent/CN102885807B/zh active Active
Non-Patent Citations (2)
| Title |
|---|
| Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya;Jie-Yun Cai etal;《ORGANIC LETTERS》;20120427;第14卷(第10期);第2524-2527页 * |
| Jie-Yun Cai etal.Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya.《ORGANIC LETTERS》.2012,第14卷(第10期),第2524-2527页. |
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