Synthesis and Biological Evaluation of Hyperforin Analogues. Part I. Modificatio

Over the past few years, clinical evidence for the antidepressant activity of St. John's wort (Hypericum perforatum L., Hypericaceae) extracts has sparked great interest in the chemistry and biochemistry of this plant, generating also coverage in the mainstream press. Despite the lack of a clear correlation between the chemical composition of St. John's wort extracts and in vivo activity which would explain the clinical benefits of the plant, Hypericum preparations are licensed in Continental Europe for the treatment of depression and anxiety. They have been suggested for the first-line treatment of mild to severe depression, especially in the primary care setting, and are also available over-the-counter or as food supplements in Great Britain and the United States. St. John's wort extracts have per se an excellent record of safety and side effects, but induction of a broad range of drug-metabolizing enzymes and the transport protein P-glycoprotein has been reported, with severe interactions with many important drugs.

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