Sosa Silvio, Pace Roberto, Bornancin Anna, Morazzoni Paolo, Riva Antonella, Tubaro Aurelia, Della Loggia Roberto
Dipartimento dei Materiali e delle Risorse Naturali, Università di Trieste, Trieste, Italy.
J Pharm Pharmacol. 2007 May;59(5):703-9. doi: 10.1211/jpp.59.5.0011.
Three preparations of Hypericum perforatum L. (a hydroalcoholic extract, a lipophilic extract and an ethylacetic fraction) and the pure compounds hypericin, adhyperforin, amentoflavone, hyperoside, isoquercitrin, hyperforin dicyclohexylammonium (DHCA) salt and dicyclohexylamine were evaluated for their topical anti-inflammatory activity. H. perforatum preparations provoked a dose-dependent reduction of Croton-oil-induced ear oedema in mice, showing the following rank order of activity: lipophilic extract > ethylacetic fraction > hydroalcoholic extract (ID50 (dose that inhibited oedema by 50%) 220, 267 and >1000 microg cm(-2), respectively). Amentoflavone (ID50 0.16 micromol cm(-2)), hypericin (ID50 0.25 micromol cm(-2)), hyperforin DHCA salt (ID50 0.25 micromol cm(-2)) and adhyperofrin (ID50 0.30 micromol cm(-2)) had anti-inflammatory activity that was more potent or comparable to that of indometacin (ID50 0.26 micromol cm(-2)), whereas isoquercitrin and hyperoside were less active (ID50 about 1 micromol cm(-2)). As dicyclohexylamine alone was inactive, the effect of hyperforin DHCA salt can be attributed completely to the phloroglucinol moiety. The pharmacological activity and phytochemical profile of the tested extracts and fraction suggest that different constituents are involved in the topical antiphlogistic property of H. perforatum in-vivo.
对贯叶连翘的三种制剂（一种水醇提取物、一种亲脂性提取物和一个乙酸乙酯级分）以及纯化合物金丝桃素、去甲伪金丝桃素、穗花杉双黄酮、金丝桃苷、异槲皮苷、金丝桃素二环己铵（DHCA）盐和二环己胺进行了局部抗炎活性评估。贯叶连翘制剂可使巴豆油诱导的小鼠耳部水肿呈剂量依赖性减轻，其活性顺序如下：亲脂性提取物＞乙酸乙酯级分＞水醇提取物（ID50（使水肿抑制50%的剂量）分别为220、267和＞1000μg cm⁻²）。穗花杉双黄酮（ID50 0.16μmol cm⁻²）、金丝桃素（ID50 0.25μmol cm⁻²）、金丝桃素DHCA盐（ID50 0.25μmol cm⁻²）和去甲伪金丝桃素（ID50 0.30μmol cm⁻²）的抗炎活性比吲哚美辛（ID50 0.26μmol cm⁻²）更强或相当，而异槲皮苷和金丝桃苷的活性较弱（ID50约为1μmol cm⁻²）。由于单独的二环己胺无活性，金丝桃素DHCA盐的作用可完全归因于间苯三酚部分。受试提取物和级分的药理活性和植物化学特征表明，不同成分参与了贯叶连翘在体内的局部抗炎特性。
