Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS) are challenging diseases with the high mortality in a clinical setting. Baicalin (BA) is the main effective constituent isolated from the Chinese medical herb Scutellaria baicalensis Georgi, and studies have proved that it has a protective effect on ALI induced by lipopolysaccharide (LPS) due to the anti-inflammatory efficacy. However, BA has low solubility which may limit its clinical application. Hence, we prepared a novel drug delivery system—Baicalin liposome (BA-LP) in previous research—which can improve some physical properties of BA. Therefore, we aimed to explore the effect of BA-LP on ALI mice induced by LPS. In pharmacokinetics study, the values of and AUC_0- in the BA-LP group were significantly higher than that of the BA group in normal mice, indicating that BA-LP could prolong the duration time in vivo of BA. The BA-LP group also showed a higher concentration in lung tissues than the BA group. Pharmacodynamics studies showed that BA-LP had a better effect than the BA group at the same dosage on reducing the W/D ratio, alleviating the lung injury score, and decreasing the proinflammatory factors (TNF-α, IL-1β) and total proteins in bronchoalveolar lavage fluids (BALF). In addition, the therapeutic effects of BA-LP showed a dose-dependent manner. Western blot analysis indicated that the anti-inflammatory action of BA could be attributed to the inhibition of the TLR4-NFκBp65 and JNK-ERK signaling pathways. These results suggest that BA-LP could be a valuable therapeutic candidate in the treatment of ALI.

中文翻译：

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黄芩苷脂质体通过抑制 TLR4/JNK/ERK/NF-κB 通路减轻脂多糖诱导的小鼠急性肺损伤

急性肺损伤 (ALI) 和急性呼吸窘迫综合征 (ARDS) 是临床环境中死亡率高的具有挑战性的疾病。黄芩苷（BA）是从中药黄芩中分离得到的主要有效成分，研究证明其具有抗炎作用，对脂多糖（LPS）诱导的ALI具有保护作用。然而，BA的溶解度低，这可能会限制其临床应用。因此，我们在之前的研究中制备了一种新的给药系统——黄芩苷脂质体（BA-LP）——它可以改善 BA 的一些物理性质。因此，我们旨在探索BA-LP对LPS诱导的ALI小鼠的影响。在药代动力学研究中，AUC _0-BA-LP 组在正常小鼠中显着高于 BA 组，表明 BA-LP 可以延长BA在体内的持续时间。BA-LP 组在肺组织中的浓度也高于 BA 组。药效学研究表明，BA-LP在降低W/D比、减轻肺损伤评分、降低促炎因子（TNF - α、IL- 1β）和总支气管肺泡灌洗液 (BALF) 中的蛋白质。此外，BA-LP 的治疗效果呈剂量依赖性。蛋白质印迹分析表明 BA 的抗炎作用可归因于抑制 TLR4-NF κBp65 和 JNK-ERK 信号通路。这些结果表明 BA-LP 可能是治疗 ALI 的有价值的候选药物。