CN103462966A - Incarviatone A在治疗结直肠癌药物中的应用 - Google Patents

Incarviatone A在治疗结直肠癌药物中的应用 Download PDF

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CN103462966A
CN103462966A CN2013104325309A CN201310432530A CN103462966A CN 103462966 A CN103462966 A CN 103462966A CN 2013104325309 A CN2013104325309 A CN 2013104325309A CN 201310432530 A CN201310432530 A CN 201310432530A CN 103462966 A CN103462966 A CN 103462966A
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colorectal cancer
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CN103462966B (zh
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江春平
黄蓉
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Fengyang County Economic Development Investment Co ltd
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Nanjing Guangkangxie Biomedical Technology Co Ltd
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Abstract

本发明公开了Incarviatone A在制备治疗人结直肠癌药物中的应用，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，Incarviatone A对人结直肠癌细胞株LOVE1、LoVo、SW620和SW480的生长也具有显著的抑制作用。因此，Incarviatone A能用于制备抗结直肠癌药物，具有良好的开发应用前景。对于本发明涉及的Incarviatone A在制备治疗人结直肠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，而且其对于人结直肠癌细胞的抑制活性强得意想不到。

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Incarviatone A在治疗结直肠癌药物中的应用
技术领域
本发明涉及化合物Incarviatone A的新用途，尤其涉及Incarviatone A在制备抗结直肠癌药物中的应用。
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Incarviatone A是一个2012年发表（Shen, Y.H. et al., 2012. Incarviatone A, a structurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi, and its absolute configuration via calculated electronic circular dichroic spectra. RSC Advances 2, 4175–4180.）的新骨架化合物，该化合物拥有全新的骨架类型，目前没有关于该化合物活性方面的报道，对于本发明涉及的Incarviatone A在制备治疗结直肠癌药物中的用途属于首次公开，而且由于骨架类型属于全新的骨架类型，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，同时用于结直肠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Incarviatone A在制备抗肿瘤药物中的应用。
本发明采用如下技术方案：Incarviatone A在制备抗结直肠癌药物中的应用，Incarviatone A的结构式如式（Ⅰ）所示：
Figure BDA0000385182471
本发明通过体外MTT抗肿瘤活性评价发现，Incarviatone A对人结直肠癌细胞株LOVE1、LoVo、SW620和SW480的生长也具有显著的抑制作用，抑制这4株细胞生长的IC50值分别为1.25±0.19μM、1.07±0.11μM、1.33±0.22μM和2.41±0.41μM。因此，Incarviatone A能用于制备抗结直肠癌药物，具有良好的开发应用前景。
本发明涉及的Incarviatone A在制备治疗结直肠癌药物中的用途属于首次公开，而且由于骨架类型属于全新的骨架类型，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，同时用于结直肠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Incarviatone A的制备方法参见文献（Shen,Y. H. et al., 2012. Incarviatone A, a structurallyunique natural product hybrid with a new carbon skeleton from Incarvillea delavayi, and its absolute configuration via calculated electronic circular dichroicspectra. RSC Advances 2, 4175–4180.）。
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Incarviatone A片剂的制备：
取20克化合物Incarviatone A，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Incarviatone A胶囊剂的制备：
取20克化合物Incarviatone A，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Incarviatone A对人结直肠癌细胞株的生长抑制作用
1．方法：处于生长对数期的细胞：人结直肠癌细胞株LOVE1、LoVo、SW620和SW480（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24 h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100 μM，50 μM，10 μM，1 μM，0.1 μM，0.01 μM和0.001 μM的Incarviatone A的培养基。培养48 h后，加入浓度5mg/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：Incarviatone A对人结直肠癌细胞株LOVE1、LoVo、SW620和SW480的生长具有显著的抑制作用。该化合物抑制人结直肠癌细胞株LOVE1、LoVo、SW620和SW480生长的IC50值分别为：1.25±0.19μM、1.07±0.11μM、1.33±0.22μM和2.41±0.41μM。
由上述实施例表明，本发明的Incarviatone A对人结直肠癌细胞株LOVE1、LoVo、SW620和SW480的生长具有很好的抑制作用。由此证明，本发明的Incarviatone A具有抗结直肠癌活性，能用于制备抗结直肠癌药物。

Claims (1)

1.Incarviatone A在治疗结直肠癌药物中的应用，所述化合物Incarviatone A结构如式（Ⅰ）所示：
Figure 2013104325309100001DEST_PATH_IMAGE001
式（Ⅰ）。
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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005021496A2 (en) * 2003-08-27 2005-03-10 The Trustees Of Columbia University In The City Of New York Synthesis of derivatives of ginkgolide c
EP1939166A1 (en) * 2006-12-19 2008-07-02 InterMed Discovery GmbH Plants extracts for use in brain modulation

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005021496A2 (en) * 2003-08-27 2005-03-10 The Trustees Of Columbia University In The City Of New York Synthesis of derivatives of ginkgolide c
EP1939166A1 (en) * 2006-12-19 2008-07-02 InterMed Discovery GmbH Plants extracts for use in brain modulation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SHEN,Y.H.ET AL.,: "ncarviatone A,a structurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi,and its absolute configuration via calculated electronic circular dichroic spectra", 《RSC ADVANCES2》, 31 December 2012 (2012-12-31), pages 4175 - 4180 *

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