Rossi A, Ligresti A, Longo R, Russo A, Borrelli F, Sautebin L
Department of Experimental Pharmacology, University of Naples, Federico II, Italy.
Phytomedicine. 2002 Sep;9(6):530-5. doi: 10.1078/09447110260573164.
The effect of an ethanolic extract of propolis, with and without CAPE, and some of its components on cyclooxygenase (COX-1 and COX-2) activity in J774 macrophages has been investigated. COX-1 and COX-2 activity, measaured as prostaglandin E2 (PGE2) production, were concentration-dependently inhibited by propolis (3 x 10(-3) - 3 x 10(2) microgml(-1)) with an IC50 of 2.7 microgml(-1) and 4.8 x 10(-2) microgml(-1), respectively. Among the compounds tested pinocembrin and caffeic, ferulic, cinnamic and chlorogenic acids did not affect the activity of COX isoforms. Conversely, CAPE (2.8 x 10(-4) - 28 microgml(-1); 10(-9) - 10(-4) M) and galangin (2.7 x 10(-4) - 27 microgml(-1); 10(-9) - 10(-4) M) were effective, the last being about ten-twenty times less potent. In fact the IC50 of CAPE for COX-1 and COX-2 were 4.4 x 10(-1) microgml(-1) (1.5 x 10(-6) M) and 2 x 10(-3) microgml(-1) (6.3 x 10(-9) M), respectively. The IC50 of galangin were 3.7 microgml(-1) (15 x 10(-6) M) and 3 x 10(-2) microgml(-1) (120 x 10(-9) M), for COX-1 and COX-2 respectively. To better investigate the role of CAPE, we tested the action of the ethanolic extract of propolis deprived of CAPE, which resulted about ten times less potent than the extract with CAPE in the inhibition of both COX-1 and COX-2, with an IC50 of 30 microgml(-1) and 5.3 x 10(-1) microgml(-1), respectively. Moreover the comparison of the inhibition curves showed a significant difference (p < 0.001). These results suggest that both CAPE and galangin contribute to the overall activity of propolis, CAPE being more effective.
研究了含有和不含咖啡酸苯乙酯（CAPE）的蜂胶乙醇提取物及其某些成分对J774巨噬细胞中环氧化酶（COX - 1和COX - 2）活性的影响。以前列腺素E2（PGE2）生成量衡量的COX - 1和COX - 2活性，受到蜂胶（3×10⁻³ - 3×10²μg/ml⁻¹）浓度依赖性抑制，COX - 1和COX - 2的半数抑制浓度（IC50）分别为2.7μg/ml⁻¹和4.8×10⁻²μg/ml⁻¹。在所测试的化合物中，松属素以及咖啡酸、阿魏酸、肉桂酸和绿原酸均不影响COX同工酶的活性。相反，咖啡酸苯乙酯（2.8×10⁻⁴ - 28μg/ml⁻¹；10⁻⁹ - 10⁻⁴M）和高良姜素（2.7×10⁻⁴ - 27μg/ml⁻¹；10⁻⁹ - 10⁻⁴M）有效，高良姜素的效力约低10至20倍。实际上，咖啡酸苯乙酯对COX - 1和COX - 2的IC50分别为4.4×10⁻¹μg/ml⁻¹（1.5×10⁻⁶M）和2×10⁻³μg/ml⁻¹（6.3×10⁻⁹M）。高良姜素对COX - 1和COX - 2的IC50分别为3.7μg/ml⁻¹（15×10⁻⁶M）和3×10⁻²μg/ml⁻¹（120×10⁻⁹M）。为了更好地研究咖啡酸苯乙酯的作用，我们测试了不含咖啡酸苯乙酯的蜂胶乙醇提取物的作用，结果发现其在抑制COX - 1和COX - 2方面的效力比含咖啡酸苯乙酯的提取物低约10倍，IC50分别为30μg/ml⁻¹和5.3×10⁻¹μg/ml⁻¹。此外，抑制曲线的比较显示出显著差异（p < 0.001）。这些结果表明，咖啡酸苯乙酯和高良姜素均对蜂胶的整体活性有贡献，其中咖啡酸苯乙酯更有效。
