Department of Life and Nanopharmaceutical Sciences and Department of Pharmacy, Kyung Hee University, 1, Hoegi, Dongdaemun-Ku, Seoul, 130-701, Republic of Korea.
Inflammation. 2011 Oct;34(5):344-51. doi: 10.1007/s10753-010-9240-1.
The anti-inflammatory activities of kakkalide, a major constituent of the flower of Pueraria thunbergiana, and irisolidone, a metabolite of kakkalide produced by intestinal microflora, against carrageenan-induced inflammation in air pouches on the backs of mice and in lipopolysaccharide (LPS)-stimulated peritoneal macrophages were investigated. Kakkalide and irisolidone down-regulated the gene expression of cytokines [tumor necrosis factor alpha (TNF-α) and interleukin-1 beta (IL-1β)] and cyclooxygenase-2 (COX-2) and the production of pro-inflammatory cytokines, TNF-α and IL-1β, and inflammatory mediators, NO and prostaglandin E(2) (PGE(2)), in LPS-stimulated peritoneal macrophages. These agents also inhibited the phosphorylation of IκB-α and the nuclear translocation of nuclear factor-kappa B (NF-κB). Orally administered kakkalide and irisolidone significantly reduced carrageenan-induced inflammatory markers, leukocyte number, and protein amount in the exudates of the air pouch. These constituents also inhibited PGE(2) production and COX-2 inducible nitric oxide synthase, IL-1β, and TNF-α expression. These agents also inhibited NF-κB activation. The anti-inflammatory effects of irisolidone were more potent than those of kakkalide. Based on these findings, kakkalide and irisolidone may inhibit inflammatory reactions via NF-κB pathway, and irisolidone, a metabolite of kakkalide, may more potently inhibit these inflammatory reactions.
研究了葛根花的主要成分甲羟异黄酮和肠道微生物产生的甲羟异黄酮代谢产物鸢尾苷元对卡拉胶诱导的小鼠气囊炎症和脂多糖（LPS）刺激的腹腔巨噬细胞炎症的抗炎活性。甲羟异黄酮和鸢尾苷元下调细胞因子[肿瘤坏死因子-α（TNF-α）和白细胞介素-1β（IL-1β）]和环氧化酶-2（COX-2）的基因表达以及促炎细胞因子 TNF-α和 IL-1β的产生，以及炎症介质一氧化氮（NO）和前列腺素 E2（PGE2）在 LPS 刺激的腹腔巨噬细胞中。这些药物还抑制了 IκB-α 的磷酸化和核因子-κB（NF-κB）的核转位。口服给予甲羟异黄酮和鸢尾苷元可显著减少卡拉胶诱导的气囊渗出物中的炎症标志物、白细胞数量和蛋白含量。这些成分还抑制了 PGE2 的产生和 COX-2 诱导的一氧化氮合酶、IL-1β 和 TNF-α 的表达。这些药物还抑制了 NF-κB 的激活。鸢尾苷元的抗炎作用强于甲羟异黄酮。基于这些发现，甲羟异黄酮和鸢尾苷元可能通过 NF-κB 途径抑制炎症反应，而甲羟异黄酮的代谢产物鸢尾苷元可能更有效地抑制这些炎症反应。
