Wurglics Mario, Schubert-Zsilavecz Manfred
Institute of Pharmaceutical Chemistry, ZAFES, J.W. Goethe University, Frankfurt am Main, Germany.
Clin Pharmacokinet. 2006;45(5):449-68. doi: 10.2165/00003088-200645050-00002.
Hypericum perforatum (St John's Wort [SJW]) counts among the most favourite herbal drugs, and is the only herbal alternative to classic synthetic antidepressants in the therapy of mild to moderate depression. Several clinical studies have been conducted to verify the effectiveness of ethanolic or methanolic extracts of SJW. Alcoholic SJW extracts are a mixture of substances with widely varying physical and chemical properties and activities. Hyperforin, a phloroglucinol derivative, is the main source of pharmacological effects caused by the consumption of alcoholic extracts of SJW in the therapy of depression. However, several studies indicate that flavone derivatives, e.g. rutin, and also the naphthodianthrones hypericin and pseudohypericin, take part in the antidepressant efficacy. In contrast to the amount of documentation concerning clinical efficacy, oral bioavailability and pharmacokinetic data about the active components are rather scarce. The hyperforin plasma concentration in humans was investigated in a small number of studies. The results of these studies indicate a relevant plasma concentration, comparable with that used in in vitro tests. Furthermore, hyperforin is the only ingredient of H. perforatum that could be determined in the brain of rodents after oral administration of alcoholic extracts. The plasma concentrations of the hypericins were, compared with hyperforin, only one-tenth and, until now, the hypericins could not be found in the brain after oral administration of alcoholic H. perforatum extracts or pure hypericin. Until now, the pharmacokinetic profile of the flavonoids in humans after oral administration of an alcoholic H. perforatum extract has been investigated in only one study. More data are available for rutin and the aglycone quercetin after administration of pure substances or other flavonoid sources.
贯叶连翘（圣约翰草 [SJW]）是最受欢迎的草药之一，也是治疗轻至中度抑郁症时经典合成抗抑郁药唯一的草药替代品。已经进行了多项临床研究来验证贯叶连翘乙醇提取物或甲醇提取物的有效性。贯叶连翘的酒精提取物是具有广泛不同物理、化学性质和活性的物质的混合物。金丝桃素，一种间苯三酚衍生物，是贯叶连翘酒精提取物在抑郁症治疗中产生药理作用的主要来源。然而，多项研究表明黄酮衍生物，如芦丁，以及萘骈二蒽酮金丝桃素和假金丝桃素也参与了抗抑郁功效。与关于临床疗效的文献数量相比，有关活性成分的口服生物利用度和药代动力学数据相当稀少。少数研究对人体中的金丝桃素血浆浓度进行了调查。这些研究结果表明其血浆浓度与体外试验中使用的浓度相当。此外，金丝桃素是贯叶连翘中唯一在口服酒精提取物后能在啮齿动物脑中检测到的成分。与金丝桃素相比，金丝桃素类的血浆浓度仅为其十分之一，而且到目前为止，口服贯叶连翘酒精提取物或纯金丝桃素后在脑中未发现金丝桃素类。到目前为止，仅在一项研究中调查了口服贯叶连翘酒精提取物后人体中黄酮类化合物的药代动力学概况。在给予纯物质或其他黄酮类来源后，有更多关于芦丁和苷元槲皮素的数据。
