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首页> 外文期刊>International immunopharmacology >Anti-inflammatory effects of vina-ginsenoside R2 and majonoside R2 isolated from Panax vietnamerzsis and their metabolites in lipopolysaccharide-stimulated macrophages
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Anti-inflammatory effects of vina-ginsenoside R2 and majonoside R2 isolated from Panax vietnamerzsis and their metabolites in lipopolysaccharide-stimulated macrophages

机译：vina-ginsenaine的抗炎作用与Panax vietnamerzsis中分离的vina-lietnoside r2和majonoside r2及其在脂多糖刺激巨噬细胞中的代谢物

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Panax vietnamensis Ha et Grushv., with its main constituents vina-ginsenoside R2 (VR2) and majonoside R2 (MR2), is used in traditional folk medicine in the hill tribes of Vietnam for anti-fatigue, anti-inflammatory, and life-saving purposes. In a preliminary study, VR2 and MR2 were shown to be metabolized to pseudoginsenoside RT4 (PRT4) and ocotillol by human gut microbiota. Therefore, we measured the anti-inflammatory effects of VR2, MR2, and their metabolites in lipopolysaccharide (LPS)-stimulated mouse peritoneal macrophages. Among these ginsenosides, only VR2 exhibited cytotoxicity against peritoneal macrophages. MR2, PRT4, and ocotillol inhibited LPS-stimulated transcription factor (NF)-kappa B activation, and expression of the proinflammatory cytokines tumor necrosis factor-alpha and interleukin (IL)-1. However, these ginsenosides did not inhibit peptidoglycan-induced NF-kappa B activation in the macrophages. These three ginsenosides also inhibited LPS-stimulated cyclooxygenase-2 and inducible NO synthase expression, and phosphorylation of NF-kappa B signal molecules IL-1 receptor-associated kinase 1 and tumor growth factor-beta-activated kinase 1 in peritoneal macrophages. Treatment with either PRT4 or ocotillol inhibited the Alexa Fluor 488-conjugated LPS-mediated shift of macrophages, as observed by flow cytometry. They also potently inhibited the binding of LPS to TLR4 on peritoneal macrophages, both with and without transfected MyD88 siRNA. Among the tested ginsenosides, ocotillol exhibited the strongest inhibitory effect on inflammation in LPS-stimulated macrophages via the NF-kappa B signaling pathway. Based on these findings, orally administered VR2 and MR2 of P. vietnamensis may be metabolized to ocotillol via PRT4, and the metabolites, particularly ocotillol, may inhibit inflammation by inhibiting the binding of LPS to TLR4 on macrophages. (C) 2015 Elsevier B.V. All rights reserved.
机译：Panax vietnamensis ha et grushv。，其主要成分vina-ginseniare r2（Vr2）和majonoside r2（mr2）用于越南山区的传统民间医学，用于抗疲劳，抗炎和救生目的。在初步研究中，VR2和MR2被证明由人体肠道微生物植物代谢至伪影甙RT4（PRT4）和塞甲醇。因此，我们测量了VR2，MR2及其代谢物在脂多糖（LPS）刺激的小鼠腹膜巨噬细胞中的抗炎作用。在这些人参皂苷中，仅VR2表现出对腹膜巨噬细胞的细胞毒性。 MR2，PRT4和塞特拿醇抑制LPS刺激的转录因子（NF）-Kappa B激活，以及促炎细胞因子肿瘤坏死因子-α和白细胞介素（IL）-1的表达。然而，这些人参皂甙在巨噬细胞中不抑制肽聚糖诱导的NF-κB活化。这三个人参皂苷还抑制了LPS刺激的环氧酶-2和诱导的NF-Kappa B信号分子IL-1受体相关激酶1和肿瘤生长因子 - β-活化激酶1的诱导型诱导的环氧氧酶的表达和诱导型巨噬细胞。如Prt4或ocotillol的处理抑制了通过流式细胞术的流式细胞术观察到的抗氧化物荧光488-缀合的LPS介导的血浆偏移。它们还突出地抑制LPS对TLR4对腹膜巨噬细胞的结合，无论是还原的myD88 siRNA。在测试的人参皂苷中，Ocotillol通过NF-Kappa B信号通路表现出对LPS刺激的巨噬细胞中炎症的最强的抑制作用。基于这些发现，口服给予的VR2和P.Vietnamensis的MR2可以通过PRT4代谢，并且代谢物，特别是塞耳醇，可以通过抑制LPS对巨噬细胞的TLR4结合来抑制炎症。 （c）2015 Elsevier B.v.保留所有权利。

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