CN103356517B - Scopariusins在制备抗细菌药物中的应用 - Google Patents

Scopariusins在制备抗细菌药物中的应用 Download PDF

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CN103356517B
CN103356517B CN201310337806.5A CN201310337806A CN103356517B CN 103356517 B CN103356517 B CN 103356517B CN 201310337806 A CN201310337806 A CN 201310337806A CN 103356517 B CN103356517 B CN 103356517B
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scopariusins
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medicines
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antibacterial
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CN103356517A (zh
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徐立明
邹文杰
吕永亮
高忠青
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Wang Yayan
Yang Jianbo
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Zibo Qidingli Patent Information Consulting Co Ltd
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    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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Abstract

本发明涉及Scopariusins在制备抗细菌药物中的应用，属于医药领域。Scopariusins具有很强的抑制大肠杆菌、荧光假单孢菌、金黄色葡萄球、变形杆菌、新生隐球菌的作用，因此Scopariusins可作为具有抗细菌的化合物，并有望在制备相关药物中得到应用。本发明涉及的Scopariusins在制备抗细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，同时用于细菌感染的防治显然具有显著的进步。

Description

Scopariusins在制备抗细菌药物中的应用
技术领域
本发明涉及化合物Scopariusins的新用途，尤其涉及Scopariusins在制备抗细菌药物中的应用。
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、活力康唑、伊曲康唑、特比萘芬、二性霉素等）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Scopariusins是一个2013年发表（Min Zhou，et al.,Scopariusins,A New Class of ent-Halimane Diterpenoids Isolated from Isodonscoparius,and Biomimetic Synthesis of Scopariusin A and Isoscoparin N.OrganicLetters，2013，15（2）：314–317.）的新化合物，该化合物拥有全新的骨架类型，目前的用途仅仅涉及抑制丙型肝炎病毒（Min Zhou，et al.,Scopariusins,A New Class ofent-Halimane Diterpenoids Isolated from Isodon scoparius,and Biomimetic Synthesisof Scopariusin A and Isoscoparin N.Organic Letters，2013，15（2）：314–317.），本发明涉及的Scopariusins在制备抗细菌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Scopariusins研究中未发现其具有抗细菌活性的报道的现状，提供了Scopariusins在制备抗细菌药物中的应用。
所述化合物Scopariusins结构如式（Ⅰ）所示：
Scopariusins具有很强的抑制大肠杆菌、荧光假单孢菌、金黄色葡萄球、变形杆菌、新生隐球菌的作用，所以Scopariusins可作为具有抗菌作用的化合物，并有望在制备抗菌药物中得到应用。
Scopariusins在制备抗细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，而且其对于细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，同时用于细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Scopariusins的制备方法参见文献（Min Zhou，et al.,Scopariusins,A New Class of ent-Halimane Diterpenoids Isolated from Isodonscoparius,and Biomimetic Synthesis of Scopariusin A and Isoscoparin N.OrganicLetters，2013，15（2）：314–317.）
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Scopariusins片剂的制备：
取5克化合物Scopariusins，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Scopariusins胶囊剂的制备：
取5克化合物Scopariusins，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：Scopariusins抗菌活性
抗菌活性实验是采用浓度稀释的方法，每次测定重复三次，测试病原菌有大肠杆菌、荧光假单孢菌、金黄色葡萄球、变形杆菌、新生隐球菌，菌液浓度为105个/mL。Scopariusins起始浓度为50.0μg/mL（5％二甲基亚砜DMSO），梯度稀释至0.098μg/mL，等量体积的菌液和测试样品混合培养在96孔板中，细菌培养温度分别为37℃，培养时间24h后观察，若发现没有菌落形成时为样品最低抗菌浓度，即MIC值。该实验阳性对照为硫酸阿米卡星，Scopariusins抗菌结果见表1。
表1Scopariusins抗菌MIC值（μg/mL）
结论：Scopariusins具有很强的抗细菌活性，因此本发明的Scopariusins有望被用于制备新型抗菌药物。

Claims (1)

1.Scopariusins在制备抗细菌药物中的应用，所述化合物Scopariusins结构如式(Ⅰ)所示：
CN201310337806.5A 2013-08-05 2013-08-05 Scopariusins在制备抗细菌药物中的应用 Expired - Fee Related CN103356517B (zh)

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