Woelkart K, Marth E, Suter A, Schoop R, Raggam R B, Koidl C, Kleinhappl B, Bauer R
Institute of Pharmaceutical Sciences, Department of Pharmacognosy, Karl Franzens University, Graz, Austria.
Int J Clin Pharmacol Ther. 2006 Sep;44(9):401-8. doi: 10.5414/cpp44401.
Echinacea is a widely used herbal remedy for the prevention and treatment of the common cold. Recently, many new insights concerning the molecular mode of action of the main lipophilic constituents, the alkamides, have renewed interest in this plant. In order to compare the bioavailability of alkamides from liquid and tablet preparations of E. purpurea (Echinaforce) in humans and to study the effects on ex vivo stimulated blood cells, a randomized, single-dose, crossover study with 10 (8 test, 2 placebo) volunteers has been performed. They received either 4 ml of the standardized E. purpurea (Echinaforce) tincture or 12 E. purpurea (Echinaforce) tablets or placebo. Both doses contained the same amount (0.07 mg) of the major alkamides, dodeca-2E,4E,8Z, 10E/Z-tetraenoic acid isobutylamides. Liquid chromatography electrospray ionization ion-trap mass spectrometry was used to determine the content of alkamides in serum. It was found that the arithmetic mean C(max) of dodeca-2E,4E, 8Z,10E/Z-tetraenoic acid isobutylamides absorbed after oral application of the Echinaforce tincture appeared after 30 min (0.40 ng/ml serum). In comparison, the t(max) of tablets was 45 min with a C(max) of 0.12 ng/ml. An ex vivo stimulation of blood by LPS was carried out to measure the influence of E. purpurea on the innate and adaptive immune system. Both E. purpurea preparations led to the same effects on the immune system according to the concentration of pro-inflammatory cytokines TNF-alpha and IL-8. 23 hours after oral application a significant down-regulation of TNF-alpha and IL-8 in LPS pre-stimulated whole blood was found. However, no significant changes in the concentration of IL-6 were observed. Although a quarter of the dodeca-2E,4E,8Z, 10E/Z-tetraenoic acid isobutylamides was absorbed from the tablets, the study shows that the formulations trigger the same effects on the measured immune parameters.
紫锥菊是一种广泛用于预防和治疗普通感冒的草药。最近，关于主要亲脂性成分烷酰胺的分子作用模式的许多新见解重新引发了人们对这种植物的兴趣。为了比较紫锥菊（紫锥菊力量）液体和片剂制剂中烷酰胺在人体中的生物利用度，并研究其对体外刺激血细胞的影响，对10名（8名试验者，2名安慰剂组）志愿者进行了一项随机、单剂量、交叉研究。他们分别接受4毫升标准化紫锥菊（紫锥菊力量）酊剂、12片紫锥菊（紫锥菊力量）片剂或安慰剂。两种剂量都含有相同量（0.07毫克）的主要烷酰胺，十二碳-2E,4E,8Z,10E/Z-四烯酸异丁酰胺。采用液相色谱电喷雾电离离子阱质谱法测定血清中烷酰胺的含量。结果发现，口服紫锥菊力量酊剂后吸收的十二碳-2E,4E,8Z,10E/Z-四烯酸异丁酰胺的算术平均C(max)在30分钟后出现（血清中为0.40纳克/毫升）。相比之下，片剂的t(max)为45分钟，C(max)为0.12纳克/毫升。通过脂多糖对血液进行体外刺激，以测量紫锥菊对先天和适应性免疫系统的影响。根据促炎细胞因子TNF-α和IL-8的浓度，两种紫锥菊制剂对免疫系统产生相同的影响。口服23小时后，发现脂多糖预刺激的全血中TNF-α和IL-8有显著下调。然而，未观察到IL-6浓度有显著变化。尽管从片剂中吸收了四分之一的十二碳-2E,4E,8Z,10E/Z-四烯酸异丁酰胺，但该研究表明，这些制剂对所测量的免疫参数产生相同的影响。
