CN115414352A - 异土木香内酯在制备治疗急性肝损伤药物中的应用 - Google Patents
异土木香内酯在制备治疗急性肝损伤药物中的应用 Download PDFInfo
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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Abstract
本发明提供了异土木香内酯在制备治疗急性肝损伤药物中的应用，通过异土木香内酯对小鼠急性肝损伤实验，证明异土木香内酯对对乙酰氨基酚引起的小鼠急性肝损伤有较好的治疗作用。本发明使用异土木香内酯保护对乙酰氨基酚引起的小鼠急性肝损伤，试验中未见显著的毒性作用，且具有较高的治愈率。因此白术挥发油可以用于新药开发，并对药物靶标确认有着重要意义。
Description
技术领域
本发明涉及异土木香内酯在制备治疗急性肝损伤药物中的应用，属于医药领域。
背景技术
异土木香内酯是从菊科植物土木香根中提取得到，具有驱虫、抗原虫作用，对须癣毛菌、大小孢菌有明显的抑制作用。具有很强的抗结核杆菌和其他微生物的作用。目前未见到异土木香内酯具有抗炎作用。
肝脏是脊柱动物重要的代谢器官，随着社会快速发展，临床药物更新速度越来越快，更多的利用多种药物组合应用，药物性肝损伤(DILI)已经成为诱发急性肝损伤最常见的因素。急性肝损伤极易引发肝衰竭，位置危及到生命。据回顾性研究报告统计，我国在308个医疗中心共有25927名患有药物诱发的肝损伤的患者接受治疗。
发明内容
本发明发现了异土木香内酯保护由急性肝损伤造成的肝脏损伤。
本发明发现了异土木香内酯对由对乙酰氨基酚引起的小鼠急性肝损伤具有较好的治疗作用。
本发明技术方案优选异土木香内酯在制备治疗急性肝损伤药物中的应用。
附图说明
图1为肝脏制作病理切片，观察药物对急性肝损伤的保护作用；
图control为空白对照组，图APAP为模型组，图APAP+Iso为药物治疗组Y为药物对照组，Iso为药物治疗组(100mg/kg)；
图2为谷丙转氨酶实验图；
图3为谷草转氨酶实验图；
图4为丙二醛含量测定图。
具体实施方式
通过以下实施例进一步举例描述本发明，并不以任何方式限制本发明，在不背离本发明的技术解决方案的前提下，对本发明所作的本领域普通技术人员容易实现的任何改动或改变都将落入本发明的权利要求范围之内。
小鼠急性肝损伤的实验治疗学研究
1.小鼠急性肝损伤模型的建立
体重在18-20g的雄性C57BL/6小鼠，经腹腔注射200μL(500mg/kg)对乙酰氨基酚溶液，建立小鼠急性肝损伤模型。
2.病理学实验
将体况相同的C57BL/6小鼠随机分组。在注射对乙酰氨基酚前一小时对药物组腹腔注射给予浓度为200μL异土木香内酯挥发油(100mg/kg)；模型组在相同的时间点经腹腔注射给予200μL的生理盐水溶剂；药物对照组同样在相同的时间点经腹腔注射给予200μL异土木香内酯(100mg/kg)。按给药方案给药后，5小时后取肝脏制作病理切片，观察药物对急性肝损伤的保护作用。结果见附图1。
3.谷草转氨酶与谷丙转氨酶实验
将体况相同的C57BL/6小鼠随机分组。在注射对乙酰氨基酚前一小时对药物组腹腔注射给予浓度为200μL异土木香内酯挥发油(100mg/kg)；模型组在相同的时间点经腹腔注射给予200μL的生理盐水溶剂；药物对照组同样在相同的时间点经腹腔注射给予200μL异土木香内酯(100mg/kg)。按给药方案给药后，5小时后取肝脏制作病理切片，测定其中谷草转氨酶与谷丙转氨酶水平。在使用药物后，血液中AST和ALT的水平与模型组相比明显降低。结果见附图2、3。
4.丙二醛含量测定
将体况相同的C57BL/6小鼠随机分组。在注射对乙酰氨基酚前一小时对药物组腹腔注射给予浓度为200μL异土木香内酯挥发油(100mg/kg)；模型组在相同的时间点经腹腔注射给予200μL的生理盐水溶剂；药物对照组同样在相同的时间点经腹腔注射给予200μL异土木香内酯(100mg/kg)。按给药方案给药后，6小时后取血液，测定其中丙二醛含量水平。在使用药物后，血液中MDA的水平与模型组相比明显降低。结果见附图4。
4.保护率试验
将体况相同的C57BL/6小鼠随机分组。在注射对乙酰氨基酚(900mg/kg)前一小时对药物组经腹腔注射给予200μL异土木香内酯(100mg/kg)；模型组在相同的时间点腹腔注射给予200μL的生理盐水溶剂。药物对照组相同的时间点经腹腔注射给予200μL异土木香内酯(100mg/kg)异土木香内酯。按给药方案给药后，分别记录6，12，24小时内小鼠的死亡率。药物对照组与模型对照组24小时内无死亡小鼠，表中记录了模型组及药物治疗组。
表3.异土木香内酯降低对乙酰氨基酚引起的小鼠急性肝损伤的死亡率
Claims (2)
1.异土木香内酯在制备保护由急性肝损伤造成的肝脏损伤药物应用。
2.如权利要求1所述的应用，其特征在于所述的急性肝损伤是指由对乙酰氨基酚引起的急性肝损伤，其中肝损伤是指对乙酰氨基酚引起的急性肝损伤。
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107157983A (zh) * | 2017-05-19 | 2017-09-15 | 苏州大学附属第医院 | 土木香内酯在制备防治肝脏损伤药物中的应用 |
| CN107468683A (zh) * | 2017-09-30 | 2017-12-15 | 东北师范大学 | 土木香内酯及其衍生物在预防和治疗脂肪肝损伤中的用途 |
| CN111012815A (zh) * | 2020-01-03 | 2020-04-17 | 吉林大学 | 白术挥发油在制备治疗急性肝损伤药物中的应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN107157983A (zh) * | 2017-05-19 | 2017-09-15 | 苏州大学附属第医院 | 土木香内酯在制备防治肝脏损伤药物中的应用 |
| CN107468683A (zh) * | 2017-09-30 | 2017-12-15 | 东北师范大学 | 土木香内酯及其衍生物在预防和治疗脂肪肝损伤中的用途 |
| CN111012815A (zh) * | 2020-01-03 | 2020-04-17 | 吉林大学 | 白术挥发油在制备治疗急性肝损伤药物中的应用 |
Non-Patent Citations (2)
| Title |
|---|
| 田其健 等: "藏木香化学成分及药理作用研究进展", 中国民族医药杂, vol. 27, no. 7, 31 July 2021 (2021-07-31), pages 45 - 49 * |
| 魏伟: "药理研究方法学", vol. 1, 31 May 2021, 中国医药科学技术出版社, pages: 356 - 359 * |
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