CN103638010B - Artoxanthochromane在制备抗细菌药物中的应用 - Google Patents
Artoxanthochromane在制备抗细菌药物中的应用 Download PDFInfo
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- VHDAXQOBUDDCHU-VXKWHMMOSA-N artoxanthochromane Natural products CC1(C)[C@H]([C@@H](Oc2cc(O)ccc12)c3ccc(O)cc3O)c4cc(O)cc(O)c4 VHDAXQOBUDDCHU-VXKWHMMOSA-N 0.000 title claims abstract description 21
- 229940124350 antibacterial drug Drugs 0.000 title claims abstract description 7
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- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 5
- 241001302000 Illicium oligandrum Species 0.000 description 3
- 230000000840 anti-viral effect Effects 0.000 description 3
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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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
本发明涉及Artoxanthochromane在制备抗细菌药物中的应用，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，可作为具有抗细菌的化合物，属于首次公开，而且其对于细菌抑制活性强，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
技术领域
本发明涉及化合物Artoxanthochromane的新用途，尤其涉及Artoxanthochromane在制备抗细菌药物中的应用。
背景技术
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Artoxanthochromane是一个2013年发表（Shuang-Gang Ma，et al.,Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters，2013，15（17）：4450–4453.）的新化合物，该化合物拥有全新的骨架类型，目前的用途发现其能清除氧自由基（Shuang-Gang Ma，et al.,Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters，2013，15（17）：4450–4453.），本发明涉及的Artoxanthochromane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Artoxanthochromane研究中未发现其具有抗细菌活性的报道的现状，提供了Artoxanthochromane在制备抗细菌药物中的应用。
所述化合物Artoxanthochromane结构如式（Ⅰ）所示：
实验研究表明Artoxanthochromane具有抑制大肠杆菌、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Artoxanthochromane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，属于首次公开，而且其对于细菌抑制活性强，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
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。
本发明所涉及化合物Artoxanthochromane的制备方法参见文献（Shuang-Gang Ma，et al.,Antiviral Spirooliganones A and B with Unprecedented Skeletons from the Roots of Illicium oligandrum Organic Letters，2013，15（17）：4450–4453.），按照上述方法制备化合物Artoxanthochromane。
实施例1：本发明所涉及化合物Artoxanthochromane片剂的制备：
取5克化合物Artoxanthochromane，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Artoxanthochromane胶囊剂的制备：
取5克化合物Artoxanthochromane，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：Artoxanthochromane抗菌活性的实验研究
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。Artoxanthochromane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，Artoxanthochromane抗菌结果见表1。
表1Artoxanthochromane抗菌MIC值（μg/mL）
结论：Artoxanthochromane具有很强的抗细菌活性，因此本发明的Artoxanthochromane有望被用于制备新型抗菌药物。
Claims (1)
1.Artoxanthochromane在制备抗细菌药物中的应用，所述化合物Artoxanthochromane结构如式(Ⅰ)所示：
式(Ⅰ)。
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| CN201310638305.0A CN103638010B (zh) | 2013-12-02 | 2013-12-02 | Artoxanthochromane在制备抗细菌药物中的应用 |
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| CN103638010A CN103638010A (zh) | 2014-03-19 |
| CN103638010B true CN103638010B (zh) | 2015-04-15 |
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- 2013-12-02 CN CN201310638305.0A patent/CN103638010B/zh not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| A Novel Monoterpene-Stilbene Adduct with a 4,4-Dimethyl-2,3-diphenylchromane Skeleton from Artocarpus xanthocarpus;Horng-Huery Ko et al;《CHEMISTRY BIODIVERSITY》;20130731;第10卷(第7期);1269-1275 * |
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