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来自柱层析馏分的3β-羟基-Δ5-甾体类似物减轻RAW 264.7巨噬细胞和斑马鱼胚胎模型中脂多糖诱导的炎症反应。

3β-Hydroxy-Δ5-steroidal congeners from a column fraction of attenuate LPS-induced inflammatory responses in RAW 264.7 macrophages and zebrafish embryo model.

作者信息

Fernando I P Shanura, Lee Won Woo, Jayawardena Thilina U, Kang Min-Cheol, Ann Yong-Seok, Ko Chang-Ik, Park Young Jin, Jeon You-Jin

机构信息

Department of Marine Life Science, Jeju National University Jeju 63243 Republic of Korea

Choung Ryong Fisheries Co. Ltd. 7825, Iljudong-ro, Namwon-eup, Seogwipo-si Jeju-do Korea.

出版信息

RSC Adv. 2018 May 22;8(33):18626-18634. doi: 10.1039/c8ra01967c. eCollection 2018 May 17.

Abstract

Bioactive compounds from marine organisms and their action mechanisms have provided new insights into medicinal and natural product research. Here, we report the identification of 3β-hydroxy-Δ5-steroidal congeners from a purified column fraction (DPCMH24) of the soft coral harvested from Jeju, South Korea. DPCMH24 exerted strong anti-inflammatory effects through a dose-dependent decrease in the levels of nitric oxide (NO) in LPS-induced RAW 264.7 macrophages (IC value = 6.54 ± 0.38 μg mL). Further, DPCMH24 attenuated the levels of PGE and the pro-inflammatory cytokines, TNF-α, IL-1β, and IL-6. The above effects were mediated the inhibition of nuclear factor κB activation and mitogen-activated protein kinase pathways. evaluation indicated that DPCMH24 reduced NO, iNOS, COX-2, ROS production and cell death in LPS-induced zebrafish embryos, confirming its anti-inflammatory potential. The constituent compounds were identified by GC-MS/MS analysis. These findings suggest that the steroidal congeners from may offer ample therapeutic potential against LPS-induced inflammation.

摘要

来自海洋生物的生物活性化合物及其作用机制为药物和天然产物研究提供了新的见解。在此,我们报告了从韩国济州岛采集的软珊瑚的纯化柱馏分(DPCMH24)中鉴定出3β-羟基-Δ5-甾体同系物。DPCMH24通过剂量依赖性降低LPS诱导的RAW 264.7巨噬细胞中一氧化氮(NO)水平发挥强大的抗炎作用(IC值 = 6.54 ± 0.38 μg mL)。此外,DPCMH24降低了PGE以及促炎细胞因子TNF-α、IL-1β和IL-6的水平。上述作用是通过抑制核因子κB激活和丝裂原活化蛋白激酶途径介导的。评估表明,DPCMH24降低了LPS诱导的斑马鱼胚胎中的NO、iNOS、COX-2、ROS产生和细胞死亡,证实了其抗炎潜力。通过GC-MS/MS分析鉴定了组成化合物。这些发现表明,来自[软珊瑚]的甾体同系物可能对LPS诱导的炎症具有巨大的治疗潜力。 (注:原文中“from ”后缺少具体对象,这里补充为“软珊瑚”使语义完整)

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e5ef/9080511/f9b7f48b0554/c8ra01967c-f1.jpg

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