CN103638005B - Hippolachnin A在治疗或预防口腔溃疡药物中的应用 - Google Patents
Hippolachnin A在治疗或预防口腔溃疡药物中的应用 Download PDFInfo
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Abstract
本发明涉及Hippolachnin？A在制备治疗或预防口腔溃疡药物中的应用，属于首次公开，由于骨架类型属于全新的骨架类型，而且其治疗口腔溃疡活性强，具备突出的实质性特点，同时用于治疗口腔溃疡显然具有显著的进步。
Description
技术领域
本发明涉及化合物HippolachninA的新用途，尤其涉及HippolachninA在制备治疗或预防口腔溃疡药物中的应用。
背景技术
复发性口腔溃疡是口腔粘膜病中最常见的疾病。患病率居口腔粘膜病的首位。Sircus(1975)调查1587人，患病率为20％。由此可见，口腔溃疡患者是一个十分庞大的群体。复发性口腔溃疡的病因复杂，至今仍不明确，可能与病毒感染、细菌感染以及机体的内分泌紊乱、免疫功能失调等因素有关。近年来出现的局部使用的口腔含片虽然携带、使用方便，口感及依从性较好，如溶菌酶含片、西瓜霜含片、华素片等，但这些药物在杀菌、抗炎、止痛等方面各有侧重。
本发明涉及的化合物HippolachninA是一个2013年发表(Shu-JuanPiao，etal.,HippolachninA,aNewAntifungalPolyketidefromtheSouthChinaSeaSpongeHippospongialachne.OrganicLetters，2013,15(14):3526–3529.)的新化合物，该化合物拥有全新的骨架类型，目前的用途发现其能抗菌(Shu-JuanPiao，etal.,HippolachninA,aNewAntifungalPolyketidefromtheSouthChinaSeaSpongeHippospongialachne.OrganicLetters，2013,15(14):3526–3529.)，本发明涉及的HippolachninA在制备治疗或预防口腔溃疡药物中的用途属于首次公开。
发明内容
本发明的目的在于根据现有HippolachninA研究中未发现其具有治疗或预防口腔溃疡的报道的现状，提供了HippolachninA在制备治疗或预防口腔溃疡药物中的应用。
所述化合物HippolachninA结构如式(Ⅰ)所示：
本发明涉及的HippolachninA在制备治疗或预防口腔溃疡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，而且其治疗或预防口腔溃疡活性强，具备突出的实质性特点，同时用于治疗或预防口腔溃疡显然具有显著的进步。
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HippolachninA的制备方法参见文献(Shu-JuanPiao，etal.,HippolachninA,aNewAntifungalPolyketidefromtheSouthChinaSeaSpongeHippospongialachne.OrganicLetters，2013,15(14):3526–3529.)，按照上述方法制备化合物HippolachninA。
实施例1：本发明所涉及化合物HippolachninA片剂的制备：
取5克化合物HippolachninA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HippolachninA胶囊剂的制备：
取5克化合物HippolachninA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。
试验例1：HippolachninA抗口腔溃疡试验研究
1、试验目的：用苯酚制造口腔溃疡模型，每天给予口腔溃疡模型大鼠一定次数的HippolachninA，观察HippolachninA是否有减少溃疡的作用。
2、受试药物及试剂
华素片(北京四环医药科技股份有限公司)；苯酚
动物：Wistar大鼠，雄性，体重240～280g，南京医科大学实验动物中心。
3、试验方法
取大鼠50只，雄性，体重240～280g，10％水合氯醛麻醉，剂量：0.35ml/100g，麻醉后将90％苯酚棉球的塑料滴管(内径：3mm)下端平置于大鼠左侧口角约1mm处的颊膜上，灼烧30min，即见该处约3mm的白色损害。24小时后随即分组，每组10只，分5组，即模型组(辅料4次/日，不含药物)；HippolachninA高剂量组(4次/日，0.5mg/次)；HippolachninA中剂量(4次/日，0.1mg/次)；HippolachninA低剂量组(4次/日，0.02mg/次)；阳性对照组：华素片组(4次/日，0.5mg/次)。HippolachninA与华素片含片在使用前研成粉末，给药以覆盖创面为度。连续给药5天，给药前及每次给药后次日观察溃疡面积大小(以溃疡的直径计)及溃疡愈合情况(无肉眼可见的溃疡视为愈合)，首次给药至末次给药分别记录为1、2、3、4、5、6天。溃疡面积大小用t检验，溃疡愈合率用X2检验。
4、试验结果
溃疡面积比较(表1)：HippolachninA高剂量组与模型组比较，从给药第3天起到试验结束，对应每天比较有显著性差异；华素片组与模型组比较，从给药第3天起到试验结束，对应每天比较有显著性差异；HippolachninA中剂量组与模型组比较，从给药第3天起到试验结束，对应每天比较有显著性差异；HippolachninA低剂量组与模型组比较，从给药第5天起到试验结束，对应每天比较有显著性差异；HippolachninA中剂量组与华素片组比较，从给药第1天起到试验结束，对应每天比较有显著性差异。
表1对大鼠溃疡面积的影响
注：与模型组比较，*p<0.05，*p<0.01。
愈合率(表2)：模型组及HippolachninA低剂量组从给药第1天起到试验结束，溃疡没有愈合；而HippolachninA高剂量组从给药第4天起，就有溃疡愈合，到试验结束，达90％；华素片组从给药第4天起，有溃疡愈合，到试验结束，达60％；HippolachninA中剂量组从给药第5天起，有溃疡愈合，到试验结束，达40％。
表2对大鼠溃疡愈合时间的影响
注：与模型组比较，*p<0.05，*p<0.01。
5、结论
HippolachninA具有明显促进口腔溃疡愈合的作用。
Claims (1)
1.HippolachninA在制备治疗或预防口腔溃疡药物中的应用，所述化合物HippolachninA结构如式(Ⅰ)所示：
式(Ⅰ)。
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| CN201310646845.3A CN103638005B (zh) | 2013-12-04 | 2013-12-04 | Hippolachnin A在治疗或预防口腔溃疡药物中的应用 |
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| CN201310646845.3A CN103638005B (zh) | 2013-12-04 | 2013-12-04 | Hippolachnin A在治疗或预防口腔溃疡药物中的应用 |
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| Publication Number | Publication Date |
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| CN103638005A CN103638005A (zh) | 2014-03-19 |
| CN103638005B true CN103638005B (zh) | 2015-12-30 |
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Non-Patent Citations (2)
| Title |
|---|
| Hippolachnin A, a New Antifungal Polyketide from the South China Sea Sponge Hippospongia lachne;Shu-Juan Piao,et al.;《Organic Letters》;20130705;第15卷(第14期);第3526-3529页 * |
| 氟康唑粉剂局部喷洒治疗真菌性口腔溃疡;赵君等;《中国民间疗法》;20110430;第19卷(第4期);第22页 * |
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