CN103655537B - Oleaceran在治疗促进小肠蠕动药物中的应用 - Google Patents
Oleaceran在治疗促进小肠蠕动药物中的应用 Download PDFInfo
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- CN103655537B CN103655537B CN201310643744.0A CN201310643744A CN103655537B CN 103655537 B CN103655537 B CN 103655537B CN 201310643744 A CN201310643744 A CN 201310643744A CN 103655537 B CN103655537 B CN 103655537B
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- XEOIJMSRWFEZRQ-HXUWFJFHSA-N oleaceran Natural products COc1cccc2c1CO[C@@]23Oc4cc(C)cc5ccc(O)c3c45 XEOIJMSRWFEZRQ-HXUWFJFHSA-N 0.000 title claims abstract description 35
- 230000000968 intestinal effect Effects 0.000 title claims abstract description 21
- 230000008855 peristalsis Effects 0.000 title claims abstract description 17
- 239000003814 drug Substances 0.000 title claims abstract description 12
- 238000002360 preparation method Methods 0.000 claims abstract description 11
- 150000001875 compounds Chemical class 0.000 claims description 13
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- 238000011156 evaluation Methods 0.000 abstract description 3
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 6
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- 239000003610 charcoal Substances 0.000 description 3
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
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- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
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Abstract
本发明涉及Oleaceran在制备促进小肠蠕动药物中的应用，从药理实验看出，Oleaceran有较好的促进小肠蠕动的作用，本发明涉及的Oleaceran在制备促进小肠蠕动药物中的用途属于首次公开，属于全新的骨架类型，而且其促进小肠蠕动活性强，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
本发明涉及化合物Oleaceran的新用途，尤其涉及Oleaceran在制备治疗促进小肠蠕动药物中的应用。
背景技术
本发明涉及的化合物Oleaceran是一个2013年发表（RiteshRaju，etal.,Oleaceran:ANovelSpiro[isobenzofuran-1,20–naptho[1,8-bc]furan]IsolatedfromaTerrestrialStreptomycessp.OrganicLetters，2013,15(14):3487–3489.）的新化合物，该化合物拥有全新的骨架类型，目前的用途仅仅发现其能抗真菌和结肠癌（RiteshRaju，etal.,Oleaceran:ANovelSpiro[isobenzofuran-1,20–naptho[1,8-bc]furan]IsolatedfromaTerrestrialStreptomycessp.OrganicLetters，2013,15(14):3487–3489.），本发明涉及的Oleaceran在制备治疗促进小肠蠕动药物中的用途属于首次公开。
发明内容
本发明提出Oleaceran在制备促进小肠蠕动药物中的应用。从药理实验看出，Oleaceran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Oleaceran在促进小肠蠕动方面的药理作用。
所述化合物Oleaceran结构如式（Ⅰ）所示：
本发明通过对小鼠的药理对比试验发现，Oleaceran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）；Oleaceran高剂量组较空白组，差异有显著性意义。因此，Oleaceran用于制备多种小肠蠕动不良疾病的药物，具有良好的开发应用前景。
具体实施方式
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。
本发明所涉及化合物Oleaceran的制备方法参见文献（RiteshRaju，etal.,Oleaceran:ANovelSpiro[isobenzofuran-1,20–naptho[1,8-bc]furan]IsolatedfromaTerrestrialStreptomycessp.OrganicLetters，2013,15(14):3487–3489.），按照上述方法制备化合物Oleaceran。
实施例1：本发明所涉及化合物Oleaceran片剂的制备：
取5克化合物Oleaceran，加入糊精195克，混匀，常规压片制成1000片。
实施例2：本发明所涉及化合物Oleaceran胶囊剂的制备：
取5克化合物Oleaceran，加入淀粉195克，混匀，装胶囊制成1000粒。
下面通过药效学实验来进一步说明其药物活性。
实验例1：采用药理实验法评价化合物Oleaceran对小肠推动性蠕动的影响
1、方法：取昆明小鼠30只，20±5g，南京中医药大学实验动物中心，雌雄各半，按性别，体重随机分为3组，即空白组，Oleaceran（0.06mg/10g，0.24mg/10g）两个剂量组。每组10只，Oleaceran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0.2ml/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。
2.结果：统计结果表明Oleaceran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）；Oleaceran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1Oleaceran对小鼠小肠推进性蠕动的影响（x+s）
与空白组比较，**P<0.001*P<0.01
由上述实验例表明，本发明的Oleaceran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）；Oleaceran高剂量组较空白组，差异有显著性意义。由此证明，本发明的Oleaceran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.Oleaceran在制备用于促进小肠蠕动药物中的应用，所述化合物Oleaceran结构如式(Ⅰ)所示：
式(Ⅰ)。
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310643744.0A CN103655537B (zh) | 2013-12-04 | 2013-12-04 | Oleaceran在治疗促进小肠蠕动药物中的应用 |
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| CN201310643744.0A CN103655537B (zh) | 2013-12-04 | 2013-12-04 | Oleaceran在治疗促进小肠蠕动药物中的应用 |
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| Publication Number | Publication Date |
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| CN103655537A CN103655537A (zh) | 2014-03-26 |
| CN103655537B true CN103655537B (zh) | 2015-11-25 |
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| CN201310643744.0A Expired - Fee Related CN103655537B (zh) | 2013-12-04 | 2013-12-04 | Oleaceran在治疗促进小肠蠕动药物中的应用 |
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Non-Patent Citations (1)
| Title |
|---|
| Oleaceran: a novel spiro[isobenzofuran-1,2"-naptho[1,8-bc]furan]isolated from a terrestrial streptomyces sp.;Ritesh Raju等;《organic letters》;20130626;第15卷(第14期);3487-3489 * |
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