CN103462993B - Aphanamgrandiol A在制备抗人体真菌药物中的应用 - Google Patents
Aphanamgrandiol A在制备抗人体真菌药物中的应用 Download PDFInfo
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Abstract
本发明涉及Aphanamgrandiol A在制备抗人体真菌药物中的应用，属于医药领域。Aphanamgrandiol A具有很强的抑制红色毛藓菌、羊毛状小孢子菌或断发藓菌的作用，因此Aphanamgrandiol A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Aphanamgrandiol A在制备治疗抗人体真菌药物中的用途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
本发明涉及化合物Aphanamgrandiol A的新用途，尤其涉及Aphanamgrandiol A在制备抗人体真菌药物中的应用。
背景技术
真菌（Fungus）是一种真核生物。最常见的真菌是各类蕈类，另外真菌也包括霉菌和酵母。现在已经发现了七万多种真菌，估计只是所有存在的一小半。大多真菌原先被分为动物或植物。目前，真菌在分类学上已独立为界，与动物界、植物界、原核生物界和原生生物界平行。真菌具有坚固的细胞壁和真正的细胞核，不含叶绿素，是异养性的，以寄生或腐生方式生存，典型者兼有有性生殖和无性生殖，产生各种形态的孢子。根据生长特性与形态差异，可将真菌简单分为酵母、真菌和蕈(蘑菇)。其中对人类有致病性的真菌约有300多个种类。除新型隐球菌和蕈外，医学上有意义的致病性真菌几乎都是霉菌。根据侵犯人体部位的不同，临床上将致病真菌分为浅部真菌和深部真菌。真菌性肠炎即属于深部真菌病。浅部真菌(癣菌)仅侵犯皮肤、毛发和指(趾)甲，而深部真菌能侵犯人体皮肤、黏膜、深部组织和内脏，甚至引起全身播散性感染。深部真菌感染肠道即表现为真菌性肠炎，可独立存在如婴儿念珠菌肠炎，或为全身性真菌感染的表现之一，如艾滋病并发播散性组织胞浆菌病，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Aphanamgrandiol A是一个2013年发表（Qi Zeng,Bin Guan,Jie Ren,et al.Aphanamgrandiol A,a new triterpenoid with a unique carbon skeleton from Aphanamixis grandifolia.Fitoterapia,86(2013)217–221.）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胃癌、卵巢癌、结肠癌、肝上皮癌细胞的增值（Qi Zeng,Bin Guan,Jie Ren,et al.Aphanamgrandiol A,a new triterpenoid with a unique carbon skeleton from Aphanamixis grandifolia.Fitoterapia,86(2013)217–221.），对于本发明涉及的Aphanamgrandiol A在制备抗人体真菌药物中的用途属于首次公开，由于属于全新的结构类型。
发明内容
本发明的目的在于根据现有Aphanamgrandiol A研究中未发现其具有抗人体真菌活性的报道的现状，提供了Aphanamgrandiol A在制备抗人体真菌药物中的应用。
所述化合物Aphanamgrandiol A,结构如式（Ⅰ）所示：
Aphanamgrandiol A具有很强的抑制红色毛藓菌、羊毛状小孢子菌或断发藓菌的作用，所以Aphanamgrandiol A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Aphanamgrandiol A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，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Aphanamgrandiol A的制备方法参见文献（Qi Zeng,Bin Guan,Jie Ren,et al.Aphanamgrandiol A,a new triterpenoid with a unique carbon skeleton from Aphanamixis grandifolia.Fitoterapia,86(2013)217–221.）
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Aphanamgrandiol A片剂的制备：
取5克化合物Aphanamgrandiol A,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Aphanamgrandiol A胶囊剂的制备：
取5克化合物Aphanamgrandiol A，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1：Aphanamgrandiol A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 藓菌、羊毛状小孢子菌和断发藓菌，菌液浓度为105个/mL。Aphanamgrandiol A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，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，Aphanamgrandiol A抗人体真菌结果见表1。
表1Aphanamgrandiol A抗人体真菌MIC值（μg/mL）
结论：Aphanamgrandiol A具有很强的抗人体真菌活性，因此本发明的Aphanamgrandiol A有望被用于制备新型抗人体真菌药物。
Claims (1)
1.Aphanamgrandiol A在制备抗人体真菌药物中的应用，所述化合物Aphanamgrandiol A结构如式（Ⅰ）所示：
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