Background: Perilla frutescens (L.) Britt., a classic medicinal plant, has been demonstrated to have anti-inflammatory and anti-allergic effects in asthma. Perilla leaves extract (PLE) exerted significant therapeutic effect against allergic asthma inflammation through Syk inhibition. But the active chemical ingredients from PLE are complex and unclear, it is difficult to fully elucidate its pharmacological mechanisms.
Methods: A method was established for rapid screening and characterization of active ingredients from PLE that targeted Syk, with which three potential active ingredients were identified. By using OVA-induced allergic asthma mouse model in vivo, OVA-induced human PBMCs inflammation model and DNP-IgE/BSA-induced RBL-2H3 cells model in vitro, the effects and mechanisms of PLE and its active components were evaluated.
Results: Using Syk-affinity screening method, roseoside (RosS), vicenin-2 (Vic-2) and rosmarinic acid (RosA) were identified from PLE. In vitro, PLE and its ingredients showed significant inhibitory activities against Syk, with their mixture (Mix, prepared by RosS, Vic-2 and RosA in accordance with their ratio in Syk-conjugated beads bound fraction) showing a stronger inhibitory activity. RosS, Vic-2 and RosA also showed significant effects on allergic asthma, and a synergistic effect of Mix was observed. Moreover, treatment with PLE, RosS, Vic-2, RosA, and Mix significantly inhibited the expression and phosphorylation of Syk, PKC, NF-κB p65, and cPLA₂ in allergic mice lung tissue and in RBL-2H3 cells.
Conclusion: PLE may alleviate allergic airway inflammation partly through the multiple components synergistic targeting on Syk and its downstream inflammatory pathway.



中文翻译：

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从紫苏叶中快速筛选出的多种成分通过协同靶向 Syk 减轻哮喘气道炎症

背景： 紫苏(L.) Britt. 是一种经典的药用植物，已被证明对哮喘具有抗炎和抗过敏作用。紫苏叶提取物 (PLE) 通过 Syk 抑制对过敏性哮喘炎症发挥显着的治疗作用。但PLE的活性化学成分复杂且不清楚，很难完全阐明其药理机制。
方法：建立了一种快速筛选和表征针对 Syk 的 PLE 活性成分的方法，并确定了三种潜在的活性成分。通过体内OVA诱导的过敏性哮喘小鼠模型、OVA诱导的人PBMCs炎症模型和体外DNP-IgE/BSA诱导的RBL-2H3细胞模型，评价了PLE及其活性成分的作用和机制。
结果：使用 Syk 亲和筛选方法，从 PLE 中鉴定出蔷薇苷 (RosS)、vicin-2 (Vic-2) 和迷迭香酸 (RosA)。在体外，PLE及其成分对Syk显示出显着的抑制活性，它们的混合物（由RosS、Vic-2和RosA根据它们在Syk缀合的珠结合部分中的比例制备的混合物）显示出更强的抑制活性。RosS、Vic-2 和 RosA 对过敏性哮喘也有显着影响，并观察到 ​​Mix 的协同作用。此外，PLE、RosS、Vic-2、RosA 和 Mix 处理显着抑制过敏小鼠肺组织和 RBL-2H3 细胞中 Syk、PKC、NF-κB p65 和 cPLA _{2的表达和磷酸化。}
结论：PLE可能通过多组分协同靶向Syk及其下游炎症通路，部分缓解过敏性气道炎症。