De Souza K C B, Bassani V L, Schapoval E E S
Programa de Pós-graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Phytomedicine. 2007 Feb;14(2-3):102-8. doi: 10.1016/j.phymed.2005.10.007. Epub 2005 Nov 15.
The flavonoids quercetin, 3-O-methylquercetin and luteolin play an important role in the anti-inflammatory activity of Achyrocline satureioides ethanol extracts when administered intraperitoneally. The present work describes the oral anti-inflammatory effect of quercetin and A. satureioides extracts and the role played by the solvent concentration, adjuvant and drying processes of freeze-drying (FD) or spray-drying (SD) on the effect. The best anti-edema effect was observed with 250 mg/kg body wt of the freeze-dried powder (FDP), prepared with 40% (v/v) ethanol (FDP40). In contrast, 250 mg/kg body wt of FDP80, prepared with ethanol 80% (ES80), did not significantly inhibit the carrageenan-induced rat paw edema. However, when ES80 was freeze-dried in the presence of polysorbate 80 (FDP80-P80) or spray-dried in the presence of colloidal silicon dioxide (CSD) and P80 (SDP80), both dried extracts became more active. Quercetin suspension in saline did not inhibit paw edema, but the mixture of quercetin with polysorbate 80 was effective in edema inhibition by the oral route. Aqueous extract (ESAQ), freeze-dried (FDPAQ, FDPAQ-P80) or spray-dried (SDPAQ) did not exhibit the edema-inhibition effect. Taken together, the results point to the following order of efficacy (at 4 h, for example): FDP40 > indomethacin > SDP40 > SDP80 = FDP80-80 > Quercetin-P80. Additionally, the FDP40, SDP40 (prepared from 40% v/v ethanol added of CSD) and SDP80 reduced the total leukocyte and polymorphonuclear cell migration in the pleural cavity.
黄酮类化合物槲皮素、3 - O - 甲基槲皮素和木犀草素在腹腔注射时，对牛膝菊乙醇提取物的抗炎活性起重要作用。本研究描述了槲皮素和牛膝菊提取物的口服抗炎作用，以及溶剂浓度、佐剂和冷冻干燥（FD）或喷雾干燥（SD）干燥过程对该作用的影响。用40%（v/v）乙醇制备的250 mg/kg体重冻干粉末（FDP）显示出最佳的抗水肿效果（FDP40）。相比之下，用80%乙醇（ES80）制备的250 mg/kg体重FDP80对角叉菜胶诱导的大鼠足爪水肿没有显著抑制作用。然而，当ES80在聚山梨酯80存在下冷冻干燥（FDP80 - P80）或在胶体二氧化硅（CSD）和P80存在下喷雾干燥（SDP80）时，两种干燥提取物的活性均增强。槲皮素生理盐水混悬液不抑制足爪水肿，但槲皮素与聚山梨酯80的混合物经口服途径可有效抑制水肿。水提取物（ESAQ），无论是冷冻干燥（FDPAQ，FDPAQ - P80）还是喷雾干燥（SDPAQ），均未表现出水肿抑制作用。综上所述，结果表明以下疗效顺序（例如在4小时时）：FDP40＞吲哚美辛＞SDP40＞SDP80 = FDP80 - 80＞Quercetin - P80。此外，FDP40、SDP40（由添加CSD的40% v/v乙醇制备）和SDP80减少了胸腔中白细胞和多形核细胞的总数。
