College of Pharmacy & Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Republic of Korea.
Int Immunopharmacol. 2010 May;10(5):556-61. doi: 10.1016/j.intimp.2010.02.002. Epub 2010 Feb 6.
Xanthohumol (XN) and its related compounds were evaluated for their effects on modulating the production of interleukin (IL)-12, the most important factor driving T helper 1 immune responses. XN showed the strongest inhibitory effect on IL-12 production in macrophages stimulated by lipopolysaccharide (LPS) or LPS/interferon-gamma. Xanthohumol 4'-O-beta-D-glucopyranoside (XNG) inhibited IL-12 production less effectively than XN. Isoxanthohumol and 8-prenylnaringenin showed comparatively lower inhibitory effects on IL-12 production than XNG. (2S)-5-methoxy-8-prenylnaringenin 7-O-beta-D-glucopyranoside did not exert any effect on IL-12 production. We then tested how these compounds affected NF-kappaB binding activity to the kappaB site in the nucleus. The compounds inhibited kappaB binding in macrophages with the same potency order as IL-12 inhibition. Furthermore, we investigated whether XN, which showed the most effective reduction of IL-12 production, attenuated skin inflammation. Chronic allergic contact dermatitis, an experimental model for psoriasis, was used to determine the anti-inflammatory effects of XN in vivo. XN treatment reduced the degree of ear thickening induced by oxazolone. Taken together, XN might be effective as an anti-inflammatory agent to reduce skin inflammation by inhibiting IL-12 production.
黄腐酚（XN）及其相关化合物的作用在于调节白细胞介素（IL）-12 的产生，而后者是驱动 T 辅助 1 免疫反应的最重要因素。在脂多糖（LPS）或 LPS/干扰素-γ刺激的巨噬细胞中，XN 对 IL-12 产生的抑制作用最强。黄腐酚 4′-O-β-D-吡喃葡萄糖苷（XNG）的抑制作用不如 XN 强。异黄腐酚和 8-异戊烯基柚皮素对 IL-12 的抑制作用低于 XNG。（2S）-5-甲氧基-8-异戊烯基柚皮素 7-O-β-D-吡喃葡萄糖苷对 IL-12 的产生没有影响。然后，我们测试了这些化合物如何影响 NF-κB 与核中κB 位点的结合活性。这些化合物在巨噬细胞中抑制 κB 结合的活性与抑制 IL-12 的活性相同。此外，我们研究了在体内显示出最有效的 IL-12 产生抑制作用的 XN 是否可以减轻皮肤炎症。慢性变应性接触性皮炎是银屑病的实验模型，我们用它来确定 XN 的抗炎作用。XN 治疗可减轻 2,4-二氧代-1,3-环己二酮诱导的耳部增厚。总之，XN 可能通过抑制 IL-12 的产生而成为一种有效的抗炎药物，以减轻皮肤炎症。
