CN103372004B - Chukrasone B在制备抗人体真菌药物中的应用 - Google Patents
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Abstract
本发明涉及Chukrasone B在制备抗人体真菌药物中的应用，属于医药领域。Chukrasone B具有很强的抑制红色毛癣菌、羊毛状小孢子菌或断发癣菌的作用，因此Chukrasone B可作为具有抗人体真菌的化合物，并有望在制备相关药物中得到应用。本发明涉及的Chukrasone B在制备治疗抗人体真菌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，而且其对于人体真菌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，同时用于人体真菌感染的防治显然具有显著的进步。
Description
技术领域
本发明涉及Chukrasone B的用途，尤其涉及Chukrasone B在制备抗人体真菌药物中的应用。
背景技术
致病菌的扩散及其耐药性的增强严重威胁着人类的健康和生命，抗菌药物已作为常规用药广泛用于艾滋病、器官移植以及慢性消耗性疾病（如癌症、糖尿病、尿毒症等）的治疗，虽然目前临床上使用的抗菌药剂（如酮康唑、阿米卡星、庆大霉素、活力康唑、伊曲康唑、特比萘芬、二性霉素、氟康唑等）对皮肤及浅表部位感染的疗效较好，但这些抗菌药物的蓄积毒性较强，常常引起肝肾损伤、消化道刺激、头晕、过敏等，所以寻找作用机理独特的新型抗菌药物成为当今药物研发的热点之一。
本发明涉及的化合物Chukrasone B是一个2012年发表（Liu, H. B. et al., 2012. Chukrasones A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons fromChukrasia tabularis. Organic Letters 14 (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活性钾离子通道抑制活性（Liu, H. B. et al., 2012.Chukrasones A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis. Organic Letters 14 (17), 4438–4441.），对于本发明涉及的Chukrasone B在制备治疗抗人体真菌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，而且其对于人体真菌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，同时用于人体真菌感染的防治显然具有显著的进步。
发明内容
本发明的目的在于：
提供一种本发明的Chukrasone B在制备抗人体真菌药物中的应用。
所述化合物Chukrasone B结构如式（Ⅰ）所示：
式（Ⅰ）
Chukrasone B具有很强的抑制红色毛癣菌、羊毛状小孢子菌或断发癣菌的作用，所以Chukrasone B可作为具有抗人体真菌作用的化合物，并有望在制备抗人体真菌药物中得到应用。
本发明涉及的Chukrasone B在制备治疗抗人体真菌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，而且其对于人体真菌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，同时用于人体真菌感染的防治显然具有显著的进步。
具体实施方式
本发明所涉及化合物Chukrasone B的制备方法参见文献（Liu, H.B. et al., 2012. Chukrasones A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons fromChukrasia tabularis. Organic Letters 14 (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Chukrasone B片剂的制备：
取20克化合物Chukrasone 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Chukrasone B胶囊剂的制备：
取20克化合物Chukrasone 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：Chukrasone B抗人体真菌活性
抗人体真菌活性实验是采用浓度稀释的方法，每次测定重复三次，测试病原菌有红色毛癣菌、羊毛状小孢子菌和断发癣菌，菌液浓度为105个/mL。Chukrasone B起始浓度为50.0 μg/mL（5％二甲基亚砜DMSO），梯度稀释至0.098 μg/mL，等量体积的菌液和测试样品混合培养在96孔板中，人体真菌培养温度分别为28 ℃，培养时间24h后观察，若发现没有菌落形成时为样品最低抗人体真菌浓度，即MIC值。该实验阳性对照为酮康唑，Chukrasone B抗人体真菌结果见表1。
表1 Chukrasone B抗人体真菌MIC值（μg/mL）
结论：Chukrasone B具有很强的抗人体真菌活性，因此本发明的Chukrasone B有望被用于制备新型抗人体真菌药物。
Claims (1)
1.Chukrasone B在制备抗人体真菌药物中的应用，所述化合物Chukrasone B结构如式（Ⅰ）所示：
式（Ⅰ）。
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310280815.5A CN103372004B (zh) | 2013-07-04 | 2013-07-04 | Chukrasone B在制备抗人体真菌药物中的应用 |
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| CN201310280815.5A CN103372004B (zh) | 2013-07-04 | 2013-07-04 | Chukrasone B在制备抗人体真菌药物中的应用 |
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| Publication Number | Publication Date |
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| CN103372004A CN103372004A (zh) | 2013-10-30 |
| CN103372004B true CN103372004B (zh) | 2015-05-13 |
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2013
- 2013-07-04 CN CN201310280815.5A patent/CN103372004B/zh active Active
Non-Patent Citations (1)
| Title |
|---|
| "Chukrasone A and B:Potential Kvl.2Potassium Channel Blockers with New Skeletons from Chukrasia tabularis";hongbing liu etc.;《organic letters》;20121008;第14卷(第17期);4438-4441 * |
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