Novel isonahocol E3 exhibits anti-inflammatory and anti-angiogenic effects in endothelin-1-stimulated human keratinocytes.

Novel isonahocol E3 exhibits anti-inflammatory and anti-angiogenic effects in endothelin-1-stimulated human keratinocytes.
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新型 isonahocol E3 在内皮素 1 刺激的人角质形成细胞中表现出抗炎和抗血管生成作用。

DOI:
10.1016/j.ejphar.2013.09.077
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发表时间:
2013
影响因子:
5
通讯作者:
Tae
Tae
中科院分区:
医学2区
文献类型:
--
作者:
S. Sah;Byung;G. Park;Sunghwan Kim;Kyoung Hwa Jang;Ju Eun Jeon;Jongheon Shin;Tae

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内皮素-1 (ET-1)是一种有效的促有丝分裂和促血管生成因子,在生理和病理过程中都起着至关重要的作用。ET-1参与真皮细胞增殖和皮肤疾病,如牛皮癣和特应性皮炎。ET-1、内皮素eta受体和内皮素eta受体可能是开发特异性治疗此类疾病的潜在靶点。在这里,我们首次报道了褐藻esarg假设siliquastruma中的异纳hocol[2,-5-二羟基-3-(13-羟基-3,-7,-11,-15-四甲基-12-氧-十六-2,-6,-14-三烯基)-苯基]-乙酸甲酯(异纳hocol E3)对ET-1诱导的炎症和促血管生成作用具有功能性拮抗活性。异萘酚e3显著抑制et -1诱导的细胞增殖,以及永生化人角质形成细胞中白细胞介素-6 (IL-6)、白细胞介素-8 (IL-8)、肿瘤坏死因子-α (TNF-α)等炎症介质和金属蛋白酶等促血管生成因子。我们还发现异烟碱醇e3降低了内皮素eta受体和内皮素etb受体的表达水平,并抑制了et -1诱导的细胞外信号调节激酶(ERK)磷酸化。综上所述,我们的研究结果表明异烟碱醇e3至少通过调节ET-1受体的表达和ERK信号通路发挥抗炎和抗血管生成活性。
Endothelin-1 (ET-1) is reported to be a potent mitogenic and pro-angiogenic factor that plays a vital role in both physiological and pathological processes. ET-1 is implicated in dermal cell proliferation and skin disorders, such as psoriasis and atopic dermatitis. ET-1, endothelin ETAreceptor, and endothelin ETBreceptor could be potential targets for developing specific therapeutics to treat such disorders. Here, we provide the first report that an isonahocol [2,-5-dihydroxy-3-(13-hydroxy-3,-7,-11,-15-tetramethyl-12-oxo-hexadeca-2,-6,-14-trienyl)-phenyl]-acetic acid methyl ester (isonahocol E3) from the brown algaeSargassumsiliquastrumhas functional antagonistic activities against ET-1 induced inflammatory and pro-angiogenic effects. Isonahocol E3significantly inhibited ET-1-induced cell proliferation, as well as inflammatory mediators, such as interleukin-6 (IL-6) and interleukin-8 (IL-8) and tumor necrosis factor-α (TNF-α), and pro-angiogenic factors including metalloproteinases in immortalized human keratinocytes. We also found that isonahocol E3reduced expression level of endothelin ETAreceptor, and endothelin ETBreceptor as well as suppressed ET-1-induced extracellular signal-regulated kinase (ERK) phosphorylation. Taken together, our results suggest that isonahocol E3can exert anti-inflammatory and anti-angiogenic activities at least by regulating the expression of ET-1 receptors and ERK signaling pathway.
DOI: 10.1165/ajrcmb.16.5.9160841
发表时间: 1997-05-01
影响因子: 6.4
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Endothelin-1 是一种旁分泌生长因子,可调节人类黑素细胞的黑素生成并参与其对紫外线辐射的反应。
DOI: --
发表时间: 1998
期刊: Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research.
影响因子: --
作者:
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DOI: 10.1165/ajrcmb.10.3.7509612
发表时间: 1994
影响因子: 6.4
作者:
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通讯作者: Puett,D