The methanolic extract of the leaves of artichoke (Cynara scolymus L.) was found to inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Among the constituents of the extract, six sesquiterpene lactones (cynaropicrin, grosheimin, 11β,13-dihydrocynaropicrin, 3β-hydroxy-8α-[(S)-3-hydroxy-2-methylpropionyloxy]guaia-4(15),10(14),11(13)-trien-1α,5α,6βH-12,6-olide, 3β-hydroxy-8α-[2-methoxymethyl-2-propenoyloxy]guaia-4(15),10(14),11(13)-trien-1α,5α,6βH-12,6-olide, and deacylcynaropicrin) inhibited NO production and/or inducible nitric oxide synthase (iNOS) induction. The acyl group having an α,β-unsaturated carbonyl group at the 8-position and the α-methylene-γ-butyrolactone moiety were important for the strong inhibitory activity. Our results suggested that these sesquiterpene lactones inhibited the LPS-induced iNOS expression via the suppression of the JAK-STAT signaling pathway in addition to the κNF-κB signaling pathway. With regard to the target molecules of the sesquiterpene lactones, high-affinity proteins of cynaropicrin were purified from the cell extract. ATP/ADP translocase 2 and tubulin were identified and suggested to be involved in the cytotoxic effects of cynaropicrin, although the target molecules for the inhibition of iNOS expression were not clarified.

已发现朝鲜蓟（Cynara scolymus L.）叶片的甲醇提取物可抑制脂多糖（LPS）刺激的RAW264.7细胞中一氧化氮（NO）的产生。在提取物的成分中，有六个倍半萜烯内酯（氰菊酯，罗汉宁，11β，13-二氢氰菊酯，3β-羟基-8α-[[ S）-3-羟基-2-甲基丙酰氧基] guaia-4（15），10（14），11（13）-trien-1α，5α，6βH-12,6-olide，3β-hydroxy-8α-[2-甲氧基甲基-2-丙烯酰基氧基] guaia-4（15），10（14），11（13）-三烯-1α，5α，6βH-12,6-内酰胺和去酰基炔诺哌啶）抑制NO生成和/或诱导型一氧化氮合酶（iNOS）归纳。在8位具有α，β-不饱和羰基的酰基和α-亚甲基-γ-丁内酯部分对于强抑制活性是重要的。我们的结果表明，这些倍半萜内酯除κNF-κB信号传导途径外，还通过抑制JAK-STAT信号传导途径抑制LPS诱导的iNOS表达。关于倍半萜内酯的靶分子，从细胞提取物中纯化了西诺卡比林的高亲和力蛋白。