Saravanan S, Pandikumar P, Prakash Babu N, Hairul Islam V I, Thirugnanasambantham K, Gabriel Paulraj M, Balakrishna K, Ignacimuthu S
Division of Ethnopharmacology, Entomology Research Institute, Loyola College, Chennai, 600 034, Tamil Nadu, India.
Inflammation. 2014 Oct;37(5):1374-88. doi: 10.1007/s10753-014-9862-9.
Swertiamarin is a secoiridoid glycoside found in Enicostema axillare (Lam) A. Raynal, a medicinal plant used as a depurative in the Indian system of traditional medicine. The present study evaluated the immunomodulatory activity of isolated swertiamarin. In vivo immunomodulatory activity of swertiamarin (2, 5, and 10 mg/kg b.w.) was evaluated in a model of sheep red blood cells (SRBC) by assessing its effect on organ weight, hemagglutinating antibody titer (HA), plaque-forming cells (PFC), quantitative hemolysis of SRBC, and delayed type hypersensitivity (DTH). In vitro immunomodulatory potential was studied on isolated splenocytes, neutrophils, and peritoneal macrophages. In silico immunomodulatory effects were evaluated by docking of swertiamarin on proinflammatory cytokines to confirm its potential. In in vivo studies, the animals treated with swertiamarin showed a significant (P ≤ 0.05) increase in antibody titer, plaque-forming cells, and also in weight of the thymus and spleen. A decreased response to DTH reaction was recorded with the treatment of swertiamarin. In in vitro studies, treatment with swertiamarin modulated the messenger RNA (mRNA) and protein expression of IFN-γ, IL-10, and IL-4 significantly (P ≤ 0.05) and also favored Th2-mediated response on concanavalin A (Con A)-induced splenocytes. The compound inhibited the release of free radicals significantly (P ≤ 0.05) in phytohemagglutinin (PHA)-induced neutrophils and also ameliorated the mRNA and protein expression of proinflammatory cytokines (TNF-α, IL-1β, and IL-6) in lipopolysaccharide (LPS)-induced macrophages. In in silico, the best docked pose of swertiamarin with the target proteins (TNF-α, IL-1β, and IL-6) was confirmed that swertiamarin acted as an anti-inflammatory mediator.
獐牙菜苦苷是一种裂环烯醚萜苷，存在于腋花琴叶珊瑚苣苔（Enicostema axillare (Lam) A. Raynal）中，这是一种药用植物，在印度传统医学体系中用作净化剂。本研究评估了分离出的獐牙菜苦苷的免疫调节活性。通过评估獐牙菜苦苷（2、5和10毫克/千克体重）对器官重量、血凝抗体滴度（HA）、空斑形成细胞（PFC）、绵羊红细胞（SRBC）的定量溶血以及迟发型超敏反应（DTH）的影响，在绵羊红细胞模型中评估了其体内免疫调节活性。对分离出的脾细胞、中性粒细胞和腹腔巨噬细胞进行了体外免疫调节潜力研究。通过将獐牙菜苦苷与促炎细胞因子对接来评估其计算机模拟免疫调节作用，以确认其潜力。在体内研究中，用獐牙菜苦苷处理的动物抗体滴度、空斑形成细胞以及胸腺和脾脏重量均显著增加（P≤0.05）。用獐牙菜苦苷处理后，DTH反应的反应性降低。在体外研究中，用獐牙菜苦苷处理显著调节了干扰素-γ（IFN-γ）、白细胞介素-10（IL-10）和白细胞介素-4（IL-4）的信使核糖核酸（mRNA）和蛋白质表达（P≤0.05），并且还促进了刀豆蛋白A（Con A）诱导的脾细胞上Th2介导的反应。该化合物在植物血凝素（PHA）诱导的中性粒细胞中显著抑制自由基的释放（P≤0.05），并且还改善了脂多糖（LPS）诱导的巨噬细胞中促炎细胞因子（肿瘤坏死因子-α（TNF-α）、白细胞介素-1β（IL-1β）和白细胞介素-6（IL-6））的mRNA和蛋白质表达。在计算机模拟研究中，确认了獐牙菜苦苷与靶蛋白（TNF-α、IL-1β和IL-6）的最佳对接构象，表明獐牙菜苦苷可作为抗炎介质。
