CN103405407A - 一种化合物在制备治疗胰腺癌药物中的应用 - Google Patents
一种化合物在制备治疗胰腺癌药物中的应用 Download PDFInfo
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Abstract
本发明公开了Nardoaristolones A在制备治疗胰腺癌药物中的应用，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，Nardoaristolones A对人胰腺癌细胞株PANC-1和BXPC-3的生长也具有显著的抑制作用。因此，Nardoaristolones A能用于制备抗胰腺癌药物，具有良好的开发应用前景。对于本发明涉及的Nardoaristolones A在制备治疗胰腺癌药物中的用途属于首次公开。
Description
技术领域
本发明涉及化合物Nardoaristolones A的新用途，尤其涉及Nardoaristolones A在制备治疗胰腺癌药物中的应用。
背景技术
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Nardoaristolones A是一个2013年发表（Ming-Li Liu,Ying-Hui Duan,Yun-Long Hou,et al.Nardoaristolones A and B,Two Terpenoids with Unusual Skeletons from Nardostachys chinensis Batal.Organic Letters，2013，15（5）：1000–1003.）的新化合物，该化合物拥有全新的骨架类型，目前的用途仅仅对双氧水诱导的心肌损伤有保护作用（Ming-Li Liu,Ying-Hui Duan,Yun-Long Hou,et al.Nardoaristolones A and B,Two Terpenoids with Unusual Skeletons from Nardostachys chinensis Batal.Organic Letters，2013，15（5）：1000–1003.），本发明涉及的Nardoaristolones A在制备治疗胰腺癌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Nardoaristolones A研究中未发现其具有抗胰腺癌活性的报道的现状，提供了Nardoaristolones A在制备抗胰腺癌药物中的应用。
所述化合物Nardoaristolones A结构如式（Ⅰ）所示：
本发明通过体外MTT抗肿瘤活性评价发现，Nardoaristolones A对人胰腺癌细胞株PANC-1和BXPC-3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1.75±0.25μM和1.61±0.73μM。因此，Nardoaristolones A能用于制备抗胰腺癌药物，具有良好的开发应用前景。
对于本发明涉及的Nardoaristolones A在制备治疗胰腺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，而且其对于胰腺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，同时用于胰腺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Nardoaristolones A的制备方法参见文献（Ming-Li Liu,Ying-Hui Duan,Yun-Long Hou,et al.Nardoaristolones A and B,Two Terpenoids with Unusual Skeletons from Nardostachys chinensis Batal.Organic Letters，2013，15（5）：1000–1003.）
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Nardoaristolones A片剂的制备：
取5克化合物Nardoaristolones A，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Nardoaristolones A胶囊剂的制备：
取5克化合物Nardoaristolones A，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：采用MTT法评价化合物Nardoaristolones A对人胰腺癌细胞株的生长抑制作用
1.方法：处于生长对数期的细胞：人胰腺癌细胞株PANC-1和BXPC-3（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，50μM，10μM，1μM，0.1μM，0.01μM和0.001μM的Nardoaristolones A的培养基。培养48h后，加入浓度5mg/mL的MTT，继续放于CO2培 养箱培养4h，然后沿着培养液上部吸去100μL上清，加入100μL DMSO，暗处放置10min，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：Nardoaristolones A对人胰腺癌细胞株PANC-1和BXPC-3的生长具有显著的抑制作用。该化合物抑制人胰腺癌细胞株PANC-1和BXPC-3生长的IC50值分别为1.75±0.25μM和1.61±0.73μM。
由上述实施例表明，本发明的Nardoaristolones A对人胰腺癌细胞株PANC-1和BXPC-3的生长具有很好的抑制作用。由此证明，本发明的Nardoaristolones A具有抗胰腺癌活性，能用于制备抗胰腺癌药物。
Claims (1)
1.Nardoaristolones A在制备治疗胰腺癌药物中的应用，所述化合物Nardoaristolones A结构如式（Ⅰ）所示：
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105250249A (zh) * | 2015-11-07 | 2016-01-20 | 淄博齐鼎立专利信息咨询有限公司 | Nardoaristolone B在制备治疗肺癌药物中的应用 |
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Non-Patent Citations (3)
| Title |
|---|
| MING-LI LIU, ET AL: "Nardoaristolones A and B, Two Terpenoids with Unusual Skeletons from Nardostachys chinensis Batal", 《ORGANIC LETTERS》 * |
| 万新等: "甘松属植物化学成分与药理作用", 《国外医药•植物药分册》 * |
| 万新等: "甘松属植物化学成分与药理作用", 《国外医药•植物药分册》, vol. 22, no. 1, 31 December 2007 (2007-12-31), pages 1 - 6 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105250249A (zh) * | 2015-11-07 | 2016-01-20 | 淄博齐鼎立专利信息咨询有限公司 | Nardoaristolone B在制备治疗肺癌药物中的应用 |
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