Kim Ji Young, Kim Dong Hee, Jeong Hye Gwang
Department of Pharmacy, College of Pharmacy, Research Center for Proteineous Materials, Chosun University, Kwangju, South Korea.
Biofactors. 2006;26(1):17-28. doi: 10.1002/biof.5520260103.
Previous studies reported that kahweol, a coffee-specific diterpene, inhibits cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression in cultured lipopolysaccharide-activated macrophages. The aim of this study was to confirm the anti-inflammatory effects of kahweol by examining its effect on the inflammatory response induced by carrageenan in a rat using an acute air pouch inflammation model. Kahweol significantly reduced the levels of the inflammatory process markers in the air pouch, such as the volume of exudates, the amount of protein and the number of leukocytes and neutrophils. The levels of nitrite, TNF-alpha and prostaglandin E2 (PGE2) were also markedly lower in the air pouch of the kahweol-treated animals than in the controls. Immunoblot analysis showed that kahweol reduced the COX-2 and iNOS expression level in the exudate cells. The histological examination showed that there was a lower inflammatory response in the pouch tissues from the kahweol-treated animals. In addition, kahweol significantly reduced the paw edema induced by carrageenan and also markedly reduced the level of PGE2 production in the inflamed paw. These results suggest that kahweol has significant anti-inflammatory effects in vivo, which might be due to the inhibition of iNOS and COX-2 expression in the inflammatory sites.
先前的研究报道，咖啡特有的二萜类化合物咖啡豆醇可抑制培养的脂多糖激活巨噬细胞中环氧合酶-2（COX-2）和诱导型一氧化氮合酶（iNOS）的表达。本研究的目的是通过使用急性气袋炎症模型检测咖啡豆醇对角叉菜胶诱导的大鼠炎症反应的影响，以证实其抗炎作用。咖啡豆醇显著降低了气袋中炎症过程标志物的水平，如渗出液体积、蛋白量以及白细胞和中性粒细胞数量。在经咖啡豆醇处理的动物气袋中，亚硝酸盐、肿瘤坏死因子-α（TNF-α）和前列腺素E2（PGE2）的水平也明显低于对照组。免疫印迹分析表明，咖啡豆醇降低了渗出细胞中COX-2和iNOS的表达水平。组织学检查显示，经咖啡豆醇处理的动物气袋组织中的炎症反应较低。此外，咖啡豆醇显著减轻了角叉菜胶诱导的爪水肿，也显著降低了炎症爪中PGE2的产生水平。这些结果表明，咖啡豆醇在体内具有显著的抗炎作用，这可能是由于其抑制了炎症部位iNOS和COX-2的表达。
