Barsby R W, Salan U, Knight D W, Hoult J R
Pharmacology Group, King's College London, U.K.
Planta Med. 1993 Feb;59(1):20-5. doi: 10.1055/s-2006-959596.
Preparations of fresh or dried feverfew (Chrysanthemum parthenium) are widely consumed in the U.K. as a remedy for arthritis and migraine, but the pharmacological basis for this has not been established. We have, therefore, compared the properties of extracts of fresh plants with those of dried powdered leaves available commercially from health food shops. The two extracts differed radically in their content of alpha-methylbutyrolactones and in their pharmacological profile when tested in vitro on the rabbit aortic ring and rat anococcygeus preparations. Extracts of fresh leaves caused does- and time-dependent inhibition of the contractile responses of aortic rings to all receptor-acting agonists so far tested; the effects were irreversible and may represent a toxic modification of post-receptor contractile function in the smooth muscle. The presence of potentially -SH reactive parthenolide and other sesquiterpene alphamethylenebutyrolactones in these extracts, and the close parallelism of the actions of pure parthenolide, suggest that the inhibitory effects are due to these compounds. In contrast , chloroform extracts of dried powdered leaves were not inhibitory but themselves elicited potent and sustained contractions of aortic smooth muscle that were not antagonised by ketanserin (5-HT2 receptor antagonist). These extracts did not contain parthenolide or butyrolactones according to a chemical-HPLC assay, We conclude that there are marked differences in the pharmacological potency and profiles between preparations from fresh and dried feverfew and that this may relate to their lactone content. As the effects of the lactones are potentially toxic, it will be necessary to compare the clinical profiles and side effects of preparations obtained from the two sources.
新鲜或干燥的小白菊(Chrysanthemum parthenium)制剂在英国被广泛用作治疗关节炎和偏头痛的药物,但尚未确定其药理学依据。因此,我们比较了新鲜植物提取物与从健康食品店购买的干燥粉末状叶子提取物的特性。当在兔主动脉环和大鼠肛门尾骨肌制剂上进行体外测试时,这两种提取物在α-甲基丁内酯含量和药理学特征上有很大差异。新鲜叶子提取物对主动脉环对所有迄今测试的受体激动剂的收缩反应产生剂量和时间依赖性抑制;这些作用是不可逆的,可能代表平滑肌中受体后收缩功能的毒性改变。这些提取物中存在潜在的-SH反应性小白菊内酯和其他倍半萜α-亚甲基丁内酯,以及纯小白菊内酯作用的密切平行性,表明抑制作用是由于这些化合物。相比之下,干燥粉末状叶子的氯仿提取物没有抑制作用,但本身会引起主动脉平滑肌的强烈和持续收缩,而酮色林(5-HT2受体拮抗剂)不能拮抗这种收缩。根据化学-HPLC分析,这些提取物不含小白菊内酯或丁内酯。我们得出结论,新鲜和干燥小白菊制剂在药理效力和特征上存在显著差异,这可能与其内酯含量有关。由于内酯的作用可能有毒,有必要比较从这两种来源获得的制剂的临床特征和副作用。