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首页> 外文期刊>The Journal of Antibiotics: An International Journal >3′-Demethyldihydromaldoxin and dihydromaldoxin, two anti-inflammtory diaryl ethers from a Steganospora species
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3′-Demethyldihydromaldoxin and dihydromaldoxin, two anti-inflammtory diaryl ethers from a Steganospora species

机译:3'-去甲基二氢麦芽毒素和二氢麦芽毒素,两种来自隐孢子虫的抗炎性二芳基醚

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摘要

CXCL10 (IP-10) is a highly inducible chemoattractant, which contributes to the recruitment of inflammatory cells such as macrophages and T-lymphocytes and thereby has important roles in chronic inflammatory conditions. In a search for new inhibitors of CXCL10 expression in MonoMac6 (MM6) cells, the new diaryl ether 3′-demethyldihydromaldoxin (1) along with the known compound dihydromaldoxin (2), were isolated from fermentations of a Steganospora species. The structures of the compounds were elucidated by a combination of one-and two-dimensional NMR spectroscopy and mass spectrometry. Compounds (1) and (2) inhibited lipopolysaccharide (LPS)/interferon-γ (IFN-γ)-induced CXCL10 promoter activity in transiently transfected MM6 cells in a dose-dependent manner with IC 50 values of 39-41 M and also reduced LPS/IFN-γ-induced CXCL10 protein synthesis and excretion.
机译:CXCL10(IP-10)是一种高度诱导性的化学引诱剂,可促进炎症细胞(如巨噬细胞和T淋巴细胞)的募集,因此在慢性炎症条件下具有重要作用。为了寻找在MonoMac6(MM6)细胞中表达CXCL10的新抑制剂,新的二芳基醚3'-去甲基二氢麦芽毒素(1)与已知的化合物二氢麦芽毒素(2)均已从隐孢子虫的发酵中分离出来。通过一维和二维NMR光谱法和质谱法的结合来阐明化合物的结构。化合物(1)和(2)以剂量依赖性方式抑制瞬时转染的MM6细胞中脂多糖(LPS)/干扰素-γ(IFN-γ)诱导的CXCL10启动子活性,IC 50值为39​​-41 M,并且也降低LPS /IFN-γ诱导的CXCL10蛋白合成和排泄。

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