Hyperforin Mechanism of Action
Hyperforin is a naturally occurring compound from St. John's Wort — not a synthesized drug — and it is now recognized as the key ingredient behind the plant's antidepressant effects.
What it does
Hyperforin blocks the reuptake of three important brain chemicals — norepinephrine, serotonin and dopamine — which act as messengers that regulate mood. When these are out of balance, the result can be depression, anxiety or fatigue; increasing their availability helps restore emotional balance. Hyperforin also slows the reuptake of GABA, which promotes relaxation and eases anxiety. In effect it treats many of the same conditions as SSRIs like Prozac and Paxil.
An unusual mechanism
Where most SSRIs bind directly to neurotransmitter transporters, hyperforin works as a non-competitive reuptake inhibitor, acting through sodium channels rather than binding the transporters themselves. This different route may help explain why it tends to cause fewer side effects than prescription SSRIs.
References
- Di Carlo, G., Borrelli, F., Izzo, A. A. & Ernst, E. (2001). St. John's wort: "Prozac from the plant kingdom." Trends in Pharmacological Sciences, 22(11):557–9.
- Laakmann, G., Jahn, G. & Schüle, C. (2002). Hypericum perforatum extract in the treatment of mild to moderate depression. Der Nervenarzt, 73(7):600–12.
- Teufel-Mayer, R. & Gleitz, J. (1997). Effects of long-term administration of hypericum extracts on the affinity and density of central serotonergic 5-HT1A and 5-HT2A receptors. Pharmacopsychiatry, 30 Suppl 2:113–6.
- Calapai, G., Crupi, A., Firenzuoli, F., et al. (1999). Effects of Hypericum perforatum on levels of 5-hydroxytryptamine, noradrenaline and dopamine in the rat. Journal of Pharmacy and Pharmacology, 51(6):723–8.