The invention discloses a cantharidin derivative used as an MMP_9 inhibitor and an application for preparing brain protective drugs. Studies have shown that MMP_9 plays an important role in blood-brain barrier injury. Inhibition of MMP_9 contributes to maintaining the integrity of blood-brain barrier and reducing the effect of adverse stimuli on brain injury (MMP_2, MMP_9 in blood-brain barrier injury), Volume 5, Phase 5, 2008, Chinese Medical Equipment; Research on the relationship between VEGF and MMP_and ischemic stroke Progress in Chinese clinical pharmacology and therapeutics, Vol. twentieth, volume third, 2015. Inhibitors of MMP 9 can be used to prepare brain protective drugs. The cantharidin derivatives provided by the present invention can maintain the integrity of the blood-brain barrier by inhibiting the expression of MMP_9, and thus have the prospect of making brain protective drugs; the existing technology has not reported that the cantharidin derivatives mentioned above have this effect, and there is no technical enlightenment, so it is not obvious to those skilled in the field. Having the creativity stipulated in the patent law.
【技术实现步骤摘要】
一种斑蝥素衍生物用作MMP-9抑制剂和用于制备脑保护药物的应用
本专利技术属于医药领域,具体涉及一种斑蝥素衍生物用作MMP-9抑制剂和用于制备脑保护药物的应用。
技术介绍
MMP-9为血清基质金属蛋白酶-9,又名明胶酶B。基质金属蛋白酶(MMPs)是一种内源性钙锌依赖性内切酶家族,因其辅助因子为钙离子、锌离子而得名。目前已发现其家族有28个成员,分离鉴别编号为MMP-1~MMP-28,根据功能不同将其分为5大类:胶原酶、明胶酶、基质水解酶、膜型MMPs及其他MMPs。其中MMP-9能够特异地水解细胞外基质(ECM)和基底膜(BM)的化学成分Ⅳ型胶原、Ⅴ型胶原、黏连蛋白等,其结构域从羧基端至氨基端依次为类血红素结合蛋白酶区、富含脯氨酸铰链区、催化活性区、前肽区和信号肽区等。研究表明,MMP-9在血脑屏障损伤中发挥了重要作用,抑制MMP-9有助于维持血脑屏障完整性,减少不利刺激对脑部损伤(参考文献:MMP-2、MMP-9在血脑屏障损伤中的作用,中国医学装备2008年第5卷第5期;VEGF和MMP-9与缺血性脑卒中关系的研究进展,中国临床药理学与治疗学2015年第20卷 ...
【技术保护点】
1.如下斑蝥素衍生物用作MMP‑9抑制剂的医药用途,化学结构式如下:
【技术特征摘要】
1.如下斑蝥素衍生物用作MMP-9抑制剂的医药用途,化学结构式如下:2.权利要求1所述的斑蝥素衍生物用于制备保护血脑屏障的药物的医药用途。3.权利要求1所述的斑蝥素衍生物用于制备脑保护的药物的医药用...
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