Ameliorating vascular endothelial injury for lipolysacharide-induced via mitochondrial targeting function of octaarginine-modified essential oil from Fructus Alpiniae zerumbet (EOFAZ) lipid microspheres

doi:https://doi.org/10.1016/j.chmed.2024.11.004

Archive > Volume 17 Issue 2 > 2025,17(2):340-351. DOI:https://doi.org/10.1016/j.chmed.2024.11.004 Prev Next

通过具有线粒体靶向作用的八聚精氨酸修饰的艳山姜挥发油脂微球缓解脂多糖诱导的血管内皮炎症损伤

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Ameliorating vascular endothelial injury for lipolysacharide-induced via mitochondrial targeting function of octaarginine-modified essential oil from Fructus Alpiniae zerumbet (EOFAZ) lipid microspheres

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摘要:

目的：探究经八聚精氨酸（R8）修饰后的艳山姜挥发油（EOFAZ）脂微球（LM）用于心血管疾病治疗的潜力。方法：通过将EOFAZ本身的挥发油特征与LM的油相结合，并利用LM具有的血管内皮损伤部位靶向优势，表面修饰细胞穿膜肽R8，制备了八聚精氨酸（Octaarginine , R8）修饰的艳山姜挥发油脂微球（EOFAZ@R8LM）。通过检测线粒体膜电位（MMP）、细胞内活性氧（ROS）水平和炎性因子白介素-6（IL-6）和白介素-1β（IL-1β）水平来评估该制剂缓解脂多糖（LPS）诱导的血管内皮炎症损伤能力。结果：EOFAZ@R8LM成功地将EOFAZ递送至血管炎症损伤部位并靶向血管内皮细胞中的线粒体，通过调节线粒体膜电位和降低细胞内ROS水平改善了线粒体功能障碍。此外，它还降低了炎症因子IL-6和IL-1β的表达水平，从而发挥血管内皮保护作用。结论：EOFAZ@R8LM在心血管治疗方面具有巨大潜力，本文为开发有效治疗心血管疾病的EOFAZ的临床应用新剂型提供了一种参考策略。

Abstract:

Objective: To investigate the therapeutic potential of octaarginine (R8)-modified essential oil from Fructus Alpiniae zerumbet (EOFAZ) lipid microspheres (EOFAZ@R8LM) for cardiovascular therapy. Methods: EOFAZ@R8LM was developed by leveraging the volatilization of EOFAZ and integrating it with the oil phase of LM, followed by surface modification with cell-penetrating peptide R8 to target the site of vascular endothelial injury. The therapeutic effects of this formulation in alleviating lipopolysaccharide-induced vascular endothelial inflammation were evaluated by assessing mitochondrial membrane potential (MMP), intracellular reactive oxygen species (ROS) levels, as well as inflammatory factors interleukin-6 (IL-6) and interleukin-1b (IL-1b) levels. Results: EOFAZ@R8LM effectively delivered EOFAZ to the site of injury and specifically targeted the mitochondria in vascular endothelial cells, thereby ameliorating mitochondrial dysfunction through regulation of MMP and reduction of intracellular ROS levels. Moreover, it attenuated the expression levels of IL-6 and IL-1b, exerting protective effects on the vascular endothelium. Conclusion: Our findings highlight the significant therapeutic potential of EOFAZ@R8LM in cardiovascular therapy, providing valuable insights for developing novel dosage forms utilizing EOFAZ for effective treatment against cardiovascular diseases.

关键词:

艳山姜挥发油;炎症;脂微球;线粒体功能障碍;八聚精氨酸;血管内皮损伤

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Project Supported:

This work was supported by the National Natural Science Foundation of China (Nos. 82260827 and U1812403-4-4), the Guizhou Provincial Science Technology Project (No. ZK [2022]380), the Guizhou Provincial Natural Science Foundation (Nos. [2020] 1Z069 and [2020]1Y210), the Guizhou Provincial Scientific and Technologic Innovation Base (No. [2023]003) and the Cultivation Project of National Natural Science Foundation of Guizhou Medical University (Nos. 21NSFCP47 and 20NSP053), the High level Innovation Talents (No. GCC[2023]048).

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通过具有线粒体靶向作用的八聚精氨酸修饰的艳山姜挥发油脂微球缓解脂多糖诱导的血管内皮炎症损伤

Original articles

Ameliorating vascular endothelial injury for lipolysacharide-induced via mitochondrial targeting function of octaarginine-modified essential oil from Fructus Alpiniae zerumbet (EOFAZ) lipid microspheres

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