CN102861070B - Houttuynoid E在治疗舌癌药物中的应用 - Google Patents
Houttuynoid E在治疗舌癌药物中的应用 Download PDFInfo
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- VCNWTZPWIVDHGN-SLBJRTIWSA-N 2-[4,5-dihydroxy-2-(2-oxoundecyl)phenyl]-5,7-dihydroxy-3-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-4-one Chemical compound CCCCCCCCCC(=O)CC1=CC(O)=C(O)C=C1C1=C(O[C@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O2)O)C(=O)C2=C(O)C=C(O)C=C2O1 VCNWTZPWIVDHGN-SLBJRTIWSA-N 0.000 title abstract description 39
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Abstract
本发明公开了Houttuynoid E在制备治疗舌癌药物中的应用，属于药物新用途技术领域。本发明通过体外MTT抗肿瘤活性评价发现，Houttuynoid E对人舌癌细胞株Tca8113和T6的生长也具有显著的抑制作用。因此，Houttuynoid E能用于制备抗舌癌药物，具有良好的开发应用前景。对于本发明涉及的Houttuynoid E在制备治疗舌癌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，而且其对于舌癌细胞的抑制活性强得意想不到。
Description
技术领域
本发明涉及化合物Houttuynoid E的新用途，尤其涉及HouttuynoidE在制备抗舌癌药物中的应用。
技术背景
癌症是对人类生命健康危害最大的疾病之一，每年都有大量的人死于癌症。抗癌药物的研发一直是药学研究的热点。抗肿瘤药物中有74%是天然产物或其衍生物，如紫杉醇及其衍生物就是目前临床上应用效果比较好的抗肿瘤药物。因此，从天然产物中寻找抗癌化合物或先导化合物具有重要的意义。
本发明涉及的化合物Houttuynoid E是一个2012年发表（Chen, S.D. et al., 2012. Houttuynoid E_E, Anti-Herpes SimplexVirus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772–1775.）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抗单纯疱疹病毒活性（Chen, S. D. et al., 2012. Houttuynoid E_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772–1775.），对于本发明涉及的Houttuynoid E在制备治疗舌癌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，而且其对于舌癌细胞的抑制活性强得意想不到，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，同时用于舌癌的防治显然具有显著的进步。
发明内容
本发明提供化合物Houttuynoid E在制备抗肿瘤药物中的应用。
本发明采用如下技术方案：Houttuynoid E在制备抗舌癌药物中的应用，Houttuynoid E的结构式如式（Ⅰ）所示：
本发明通过体外MTT抗肿瘤活性评价发现，Houttuynoid E对人舌癌细胞株Tca8113和T6的生长也具有显著的抑制作用，抑制这2株细胞生长的IC50值分别为0.23±0.04μM和1.49±0.14μM。因此，HouttuynoidE能用于制备抗舌癌药物，具有良好的开发应用前景。
本发明涉及的Houttuynoid E在制备治疗舌癌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，而且其对于舌癌细胞的抑制活性强得意想不到，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，同时用于舌癌的防治显然具有显著的进步。
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。
具体实施方式
本发明所涉及化合物Houttuynoid E的制备方法参见文献（Chen, S. D. et al., 2012. Houttuynoid E_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons fromHouttuynia cordata. Organic Letters 14 (7), 1772–1775.）。
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Houttuynoid E片剂的制备：
取20克化合物Houttuynoid E，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Houttuynoid E胶囊剂的制备：
取20克化合物Houttuynoid E，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：采用MTT法评价化合物Houttuynoid E对人舌癌细胞株的生长抑制作用
1．方法：处于生长对数期的细胞：人舌癌细胞株Tca8113和T6（购买自中国科学院细胞库）以1.5×104浓度种于96孔板中。细胞培养24h贴壁后吸去原来的培养基。试验分为空白对照组、药物处理组。空白组更换含10%胎牛血清的1640培养基；药物处理组更换含浓度为100μM，50 μM，10 μM，1 μM，0.1 μM，0.01 μM和0.001 μM的Houttuynoid E的培养基。培养48 h后，加入浓度5 mg/mL的MTT，继续放于CO2培养箱培养4 h，然后沿着培养液上部吸去100 μL上清，加入100 μL DMSO，暗处放置10 min，利用酶标仪（Sunrise公司产品）测定吸光值(波长570nm)，并根据吸光值计算细胞存活情况，每个处理设6个重复孔。细胞存活率(%)=ΔOD药物处理/ΔOD空白对照×100。
2. 结果：Houttuynoid E对人舌癌细胞株Tca8113和T6的生长具有显著的抑制作用。该化合物抑制人舌癌细胞株Tca8113和T6生长的IC50值分别为：0.23±0.04μM和1.49±0.14μM。
由上述实施例表明，本发明的Houttuynoid E对人舌癌细胞株Tca8113和T6的生长具有很好的抑制作用。由此证明，本发明的HouttuynoidE具有抗舌癌活性，能用于制备抗舌癌药物。
Claims (1)
1.Houttuynoid E在制备治疗舌癌药物中的应用，所述化合物Houttuynoid E结构如式（Ⅰ）所示：
式（Ⅰ）。
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