CN103610678B - Trigolutesins A在治疗心肌缺血药物中的应用 - Google Patents

Trigolutesins A在治疗心肌缺血药物中的应用 Download PDF

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CN103610678B
CN103610678B CN201310613888.1A CN201310613888A CN103610678B CN 103610678 B CN103610678 B CN 103610678B CN 201310613888 A CN201310613888 A CN 201310613888A CN 103610678 B CN103610678 B CN 103610678B
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myocardial ischemia
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trigolutesins
trigolutesinsa
treatment myocardial
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CN103610678A (zh
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王贻英
仲云
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Dongtai Haibin Science And Technology Pioneer Park Management Co Ltd
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Abstract

本发明提供了Trigolutesins？A在制备治疗或者预防心肌缺血/再灌注药物中的应用，属于首次公开，由于骨架类型属于全新的骨架类型，而且其对于心肌缺血的抑制活性强，具备突出的实质性特点，同时用于抗心肌缺血显然具有显著的进步。

Description

Trigolutesins A在治疗心肌缺血药物中的应用
技术领域
本发明涉及化合物TrigolutesinsA的新用途，尤其涉及TrigolutesinsA在制备治疗心肌缺血药物中的应用。
背景技术
本发明人通过大量的实验发现，TrigolutesinsA有抗心肌缺血/再灌注损伤的药理作用，具有预防或者治疗心肌缺血疾病的医药用途。
本发明涉及的化合物TrigolutesinsA是一个2013年发表（Shan-ShanMa，etal.,TwoNewTypesofBisindoleAlkaloidfromTrigonostemonlutescens.OrganicLetters，2013，15（7）：1492–1495.）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抗乙酰胆碱酯酶（Shan-ShanMa，etal.,TwoNewTypesofBisindoleAlkaloidfromTrigonostemonlutescens.OrganicLetters，2013，15（7）：1492–1495.），本发明涉及的TrigolutesinsA在制备治疗心肌缺血药物中的用途属于首次公开。
发明内容
本发明提供了TrigolutesinsA制备治疗或预防心肌缺血/再灌注的药物中的应用。
本发明人通过具体实施方式中的实验证明了TrigolutesinsA具有治疗或预防心肌缺血药物疾病的作用。
所述化合物TrigolutesinsA结构如式（Ⅰ）所示：
式（Ⅰ）
本发明涉及的TrigolutesinsA在制备抗心肌缺血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，而且其对于心肌缺血的抑制活性强，具备突出的实质性特点，同时用于抗心肌缺血显然具有显著的进步。前3min舌下静脉注射普萘洛尔1.0mg/kg）。结扎30min后，剪断结扎线，复灌30min。快速取出心脏，用0.9%氯化钠冲洗干净。将心肌片放在1%的TTC溶液中，于37℃孵化5min。染色后立即用水冲洗去心肌片上多余的染料。剪去各心肌片被染色的非梗死区心肌，把未染色的梗死心肌和缺血心肌称重。
大鼠血流动力学实验：将大鼠随机分为5组：阳性对照组，阴性对照组，给药组3组，每组8只。给药组灌胃给药，两对照组每天给予同体积量的蒸馏水灌胃，各组连续灌胃5d。第6天腹腔注射乌拉坦10mg/kg麻醉。记录标准Ⅱ导联心电图。纵向切开右颈部皮肤，分离右颈总动脉，插入已充满肝素0.9%氯化钠的左室导管，将导管缓慢插入左心室腔。切开左下肢内侧皮肤，分离股动脉，插入动脉导管。接通压力换能器，把信号输至多媒体生物信号记录仪进行观察。平衡30min后，记录给药前各血流动力学指标。所有数据均以x±s表示，实验组和对照组数据分析用两样本均数的双侧t检验。
2）结果
缺血/再灌注损伤实验结果表明，给药组、阳性对照组、阴性对照组心肌梗死与结扎线下心肌重量百分比分别见表1。
表1TrigolutesinsA对心肌梗死与结扎线下心机重量比的影响
与阴性对照组比较，**p<0.01，*p<0.05
TrigolutesinsA对垂体后叶素引起的急性心肌缺血的影响见表2。
表2TrigolutesinsA对垂体后叶素引起的急性心肌缺血的影响
与阴性对照组比较，**p<0.01，*p<0.05
结论：TrigolutesinsA能够降低心肌梗死的发生，TrigolutesinsA可以明显改变心电度的变化，不改变心率。以上实验可以说明，TrigolutesinsA能够治疗心肌缺血/灌注。

Claims (1)

1.TrigolutesinsA在制备治疗心肌缺血药物中的应用，所述化合物TrigolutesinsA结构如式(Ⅰ)所示：
CN201310613888.1A 2013-11-26 2013-11-26 Trigolutesins A在治疗心肌缺血药物中的应用 Active CN103610678B (zh)

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Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
New Types of Bisindole Alkaloid from Trigonostemon lutescens;Shan-Shan Ma et al;《Organic Letters》;20130312;第15卷(第7期);第1492-1495页 *
Protective Effects of Melatonin Against Ischemia-Reperfusion Injury in the Isolated Rat Heart;Caroline Lagneux et al;《Life Sciences》;20001231;第66卷(第6期);第503-509页 *

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