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安痛定及其类似物对 RAW 264.7 巨噬细胞中脂多糖诱导的一氧化氮生成的抑制作用。

Inhibition of lipopolysaccharide-induced nitric oxide production by antofine and its analogues in RAW 264.7 macrophage cells.

机构信息

College of Pharmacy and Division of Life & Pharmaceutical Sciences, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-ku, Seoul 120-750, Korea.

出版信息

Chem Biodivers. 2010 Feb;7(2):409-14. doi: 10.1002/cbdv.200900040.

DOI:10.1002/cbdv.200900040
PMID:20151387
Abstract

Based on the anti-inflammatory activity of phenanthroindolizidine alkaloids, the inhibitory effect of antofine and its analogues on lipopolysaccharide (LPS)-induced nitric oxide (NO) production was examined, and structure-activity relationships are discussed. Antofine and several analogues suppressed NO production in LPS-stimulated RAW 264.7 cells. The MeO group at C(2), and the bulkiness of the substituents at C(3) and C(6) in the phenanthrene ring might be critical for this effect. Besides, regulation of iNOS expression might be involved in the inhibitory effect of antofine on LPS-induced NO production in macrophage cells.

摘要

基于菲并吲哚里西啶生物碱的抗炎活性，研究了 antofine 及其类似物对脂多糖 (LPS) 诱导的一氧化氮 (NO) 产生的抑制作用，并讨论了构效关系。Antofine 和几种类似物抑制了 LPS 刺激的 RAW 264.7 细胞中的 NO 产生。在菲并吲哚里西啶环中 C(2)上的 MeO 基团，以及 C(3)和 C(6)上取代基的体积可能对此作用至关重要。此外，iNOS 表达的调节可能参与了 antofine 对巨噬细胞中 LPS 诱导的 NO 产生的抑制作用。

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