CN103446133A - Lycojaponicumin B在治疗舌癌药物中的应用 - Google Patents
Lycojaponicumin B在治疗舌癌药物中的应用 Download PDFInfo
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- CN103446133A CN103446133A CN2013104383380A CN201310438338A CN103446133A CN 103446133 A CN103446133 A CN 103446133A CN 2013104383380 A CN2013104383380 A CN 2013104383380A CN 201310438338 A CN201310438338 A CN 201310438338A CN 103446133 A CN103446133 A CN 103446133A
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Abstract
本发明公开了Lycojaponicumin B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，Lycojaponicumin B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，Lycojaponicumin B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Lycojaponicumin B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Lycojaponicumin B的新用途，尤其涉及Lycojaponicumin B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Lycojaponicumin B是一个2012年发表（Wang,X.J.et al.,2012.Lycojaponicumins A-C,Three Alkaloids with an Unprecedented Skeleton fromLycopodium japonicum.Organic Letters14(10),2614-2617.）的新骨架化合物，该化合物拥有全新的骨架类型，对于本发明涉及的Lycojaponicumin B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Lycojaponicumin B在制备抗肿瘤药物中的应用。
本发明采用如下技术方案：Lycojaponicumin B在制备抗舌癌药物中的应用，Lycojaponicumin B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，Lycojaponicumin B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2.69±0.18μM和1.33±0.18μM。因此，Lycojaponicumin B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Lycojaponicumin B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Lycojaponicumin B的制备方法参见文献（Wang,X.J.et al.,2012.Lycojaponicumins A-C,Three Alkaloids with an Unprecedented Skeleton from Lycopodium japonicum.Organic Letters14(10),2614-2617.）。
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Lycojaponicumin B片剂的制备：
取20克化合物Lycojaponicumin B，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Lycojaponicumin B胶囊剂的制备：
取20克化合物Lycojaponicumin B，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Lycojaponicumin B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，50μM，10μM，1μM，0.1μM，0.01μM和0.001μM的Lycojaponicumin B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：Lycojaponicumin B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：2.69±0.18μM和1.33±0.18μM。
由上述实施例表明，本发明的Lycojaponicumin B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Lycojaponicumin B具有抗舌癌活性，能用于制备抗舌癌药物。
Claims (1)
1.Lycojaponicumin B在治疗舌癌药物中的应用，所述化合物Lycojaponicumin B结构如式（Ⅰ）所示：
式（Ⅰ）。
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103059043A (zh) * | 2011-10-24 | 2013-04-24 | 中国医学科学院药物研究所 | 伸筋草碱a-c、其制法和其药物组合物与用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103059043A (zh) * | 2011-10-24 | 2013-04-24 | 中国医学科学院药物研究所 | 伸筋草碱a-c、其制法和其药物组合物与用途 |
Non-Patent Citations (1)
| Title |
|---|
| XIAO-JING WANG, ET AL: "Lycojaponicumins A-C,Three Alkaloids with an Unprecedented Skeleton from Lycopodium japonicum", 《ORGANIC LETTERS》, vol. 14, no. 10, 8 May 2012 (2012-05-08), pages 2614 - 2617, XP055066237, DOI: 10.1021/ol3009478 * |
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