<br>BP-1-102 对 STAT3 的药理抑制通过调节炎症反应抑制小鼠颅内动脉瘤形成和破裂,Pharmacology Research & Perspectives

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BP-1-102 对 STAT3 的药理抑制通过调节炎症反应抑制小鼠颅内动脉瘤形成和破裂
Pharmacology Research & Perspectives ( IF 2.9 ) Pub Date : 2021-01-20 , DOI: 10.1002/prp2.704
Zhixian Jiang ₁ , Jiaxin Huang ₁ , Lingtong You ₁ , Jinning Zhang ₁ , Bingyu Li ₂

Affiliation

作为STAT3的抑制剂，BP-1-102可以通过抑制JAK/STAT3/NF-κB通路来调节血管平滑肌细胞（VSMC）引起的炎症反应，从而减轻颅内动脉瘤（IA）的症状。通过立体定向注射弹性蛋白酶建立IA小鼠模型来评价BP-1-102的效果。采用qRT-PCR检测平滑肌标志物和基质金属蛋白酶（MMP）的表达水平，采用ELISA和qRT-PCR检测炎症因子的水平。通过Western blot检测NF-κB信号通路因子的蛋白水平。 BP-1-102 降低动脉瘤小鼠的血压，上调平滑肌细胞标志物 MHC、SMA 和 SM22，并下调血管组织中 MMP2 和 MMP9 的表达。同时，BP-1-102还下调炎症反应因子和NF-κB通路蛋白的表达水平。在IA模型中，BP-1-102可以通过抑制JAK/STAT3/NF-κB通路蛋白的激活，减少与NF-κB结合的炎症因子和MMP的表达，进而恢复血管壁弹性蛋白，从而减少血液压力，从而治疗动脉瘤。

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Pharmacological inhibition of STAT3 by BP‐1‐102 inhibits intracranial aneurysm formation and rupture in mice through modulating inflammatory response

As an inhibitor of STAT3, BP‐1‐102 can regulate the inflammation response caused by vascular smooth muscle cells (VSMCs) by inhibiting the JAK/STAT3/NF‐κB pathway, thereby attenuating the symptoms of intracranial aneurysm (IA). IA mouse model was established by stereotactic injection of elastase to evaluate the effect of BP‐1‐102. The expression levels of smooth muscle markers and matrix metalloproteinases (MMPs) were detected by qRT‐PCR, and the levels of inflammatory factors were detected by ELISA and qRT‐PCR. The protein levels of the NF‐κB signaling pathway factors were examined by Western blot. BP‐1‐102 reduced blood pressure in aneurysm mice, up‐regulated smooth muscle cell markers MHC, SMA, and SM22, and down‐regulated the expression of MMP2 and MMP9 in vascular tissues. At the same time, BP‐1‐102 also down‐regulated the expression levels of inflammatory response factors and the NF‐κB pathway proteins. In the IA model, BP‐1‐102 can reduce the expression of inflammatory factors and MMPs bound to NF‐κB by inhibiting the activation of the JAK/STAT3/NF‐κB pathway proteins, and then restore the vascular wall elastin to reduce blood pressure, thereby treating aneurysm.

更新日期：2021-01-21

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