CN103405423B - Chukrasone B在制备治疗肾癌药物中的应用 - Google Patents

Chukrasone B在制备治疗肾癌药物中的应用 Download PDF

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CN103405423B
CN103405423B CN201310386402.5A CN201310386402A CN103405423B CN 103405423 B CN103405423 B CN 103405423B CN 201310386402 A CN201310386402 A CN 201310386402A CN 103405423 B CN103405423 B CN 103405423B
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chukrasone
renal carcinoma
medicine
application
preparation treatment
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CN103405423A (zh
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吴俊华
姚林芳
江春平
王忠夏
黄蓉
张广
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Wang Yayan
Yang Jianbo
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Gu Xiangmao
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Abstract

本发明公开了Chukrasone？B在制备治疗肾癌药物中的应用，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，Chukrasone？B对人肾癌细胞株KC的生长也具有显著的抑制作用。因此，Chukrasone？B能用于制备抗肾癌药物，具有良好的开发应用前景。对于本发明涉及的Chukrasone？B在制备治疗肾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，而且其对于肾癌细胞的抑制活性强得意想不到。

Description

Chukrasone B在制备治疗肾癌药物中的应用
技术领域
本发明涉及化合物ChukrasoneB的新用途，尤其涉及ChukrasoneB在制备抗肾癌药物中的应用。
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ChukrasoneB是一个2012年发表(Liu,H.B.etal.,2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBlockerswithNewSkeletonsfromChukrasiatabularis.OrganicLetters14(17),4438–4441.)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钾离子通道抑制活性，对于本发明涉及的ChukrasoneB在制备治疗肾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，而且其对于肾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，同时用于肾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ChukrasoneB在制备抗肿瘤药物中的应用。
本发明采用如下技术方案：ChukrasoneB在制备抗肾癌药物中的应用，ChukrasoneB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，ChukrasoneB对人肾癌细胞株KC的生长也具有显著的抑制作用，抑制这1株细胞生长的IC50值分别为2.01±0.31μM。因此，ChukrasoneB能用于制备抗肾癌药物，具有良好的开发应用前景。
本发明涉及的ChukrasoneB在制备治疗肾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，而且其对于肾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，同时用于肾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ChukrasoneB的制备方法参见文献(Liu,H.B.etal.,2012.ChukrasonesAandB:PotentialKv1.2PotassiumChannelBlockerswithNewSkeletonsfromChukrasiatabularis.OrganicLetters14(17),4438–4441.)。
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ChukrasoneB片剂的制备：
取20克化合物ChukrasoneB，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ChukrasoneB胶囊剂的制备：
取20克化合物ChukrasoneB，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ChukrasoneB对人肾癌细胞株的生长抑制作用
1.方法：处于生长对数期的细胞：人肾癌细胞株KC(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，0.001μM，0.0001μM和0.00001μM的ChukrasoneB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100μLDMSO，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：ChukrasoneB对人肾癌细胞株KC的生长具有显著的抑制作用。该化合物抑制人肾癌细胞株KC生长的IC50值分别为：2.01±0.31μM。
由上述实施例表明，本发明的ChukrasoneB对人肾癌细胞株KC的生长具有很好的抑制作用。由此证明，本发明的ChukrasoneB具有抗肾癌活性，能用于制备抗肾癌药物。

Claims (1)

1.ChukrasoneB在制备治疗肾癌药物中的应用，所述化合物ChukrasoneB结构如式（Ⅰ）所示：
式（Ⅰ）。
CN201310386402.5A 2013-08-29 2013-08-29 Chukrasone B在制备治疗肾癌药物中的应用 Expired - Fee Related CN103405423B (zh)

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Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Chukrasone A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis;Liu,H.B.等;《Organic Letters》;20121231;第14卷(第17期);第4438–4441页 *
钾离子通道作为肿瘤治疗靶点的研究;王冬艳，等;《国外医学药学分册》;20060831;第33卷(第4期);第246-248，265页 *

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