Hyperforin, Hypericin And Kampferol In Hypericum Extract And Their Effect On Serotonin And Depression
St johns wort or Hypericum extract had significant antidepressant effect that is comparable to drugs so several clinical studies were done to find out how hypericum extract or its active principle could affect the body.
Hypericum extract was improved cognitive functions and it had relaxant properties when it was compared to Maprotiline.
Radioactive serotonin was used in this study to find the effect of hypericum extract on serotonin uptake at post synaptic receptors. Serotonin uptake was inhibited by Hypericum extract.
Full hypericum extract was found to have significant antidepressant activity in comparison to hypericin and kampferol. Hypericum extract reduced the uptake of serotonin and norepinephrine.
Some studies about Hyperforin are discussed here. They are about its antibacterial activity. Some studies are about its claim and later withdrawal from being the chief chemical in hypericum extract with antidepressant activity.
Comparison Of Hypericum With Maprotiline (1994):
Maprotiline and hypericum are compared in a randomized double blind study with 24 healthy persons. Hypericum improved cognitive functions and also had relaxant properties.
AU: Johnson-D, Ksciuk-H, Woelk-H, Sauerwein-Giese-E, Frauendorf-A
J Geriatrric Psychiatry Neur 1994; 7 (Suppl 1). S44-S46
Hypericum Extract Having Effect On Serotonin Uptake By Post Synaptic Receptors (1995):
The brain of adult rats were dissected and processed in a special way resulting in separation of post-synaptic membranes and enrichment of post-synaptic receptors. The synaptosomes were then incubated with different concentrations of hypericum extract.
Uptake of Serotonin was initiated by adding radioactive Serotonin and then measure later on by Spectrometry.
Results demonstrated that Serotonin uptake was inhibited by hypericum extract. And this reuptake inhibition shows a dose dependent relationship.
It was also suggested that further studies should be done to measure this effect on human brain. There is possibility of achieving faster effect of st. john’s wort by administering it in high initial dose.
The slow accumulation of hypericin in brain is responsible for slower onset of antidepressant action and slow elimination might be responsible for longer effects. The benign side effects are also related to this pharmacokinetic behavior.
AU: Perovic-S and Mueller-W-E-G
SO: Arzneimittel-Forschung/Drug Research 45 (II), 11, 1145-1148(1995)
St. John’s Wort – Hypericin, Kampferol in Hypericum Extract With Anti-depressant Action (1996):
Based on the above study, the reuptake of norepinephrine and Serotonin in rat brains are measured. The effect of Serotonin and norepinephrine on Imipramine receptors is also studied.
Hypericum extract was found to reduce the uptake of serotonin and norepinephrine. Pure hypericin and kampferol were poor inhibitor in comparison to full hypericum extract. However researchers didn’t assume that this could be the mechanism of action of hypericum for antidepressant action.
Au: Müller W.E. and Schäfer C.S
Deutsche Apotheker Zeitung vol 136 Nr 13 1996 page 1015-1022
Hyperforin Related Studies:
Hyperforin With Antibacterial Role:
Hyperforin was found to have antibacterial effect against methicillin resistant Staphylococcus aureus (MRSA).
Is Hyperforin As The Phytochemical With Antidepressant Activity?
Some researchers attributed hyperforin to be the chief phytochemical with antidepressant activity in hypericum as it has been shown to inhibit the uptake of 5HT, GABA, dopamine, noradrenaline and glutamate.
Chatterjee SS, Bhattacharya SK, Wonnemann M, Singer A, Muller WE (1998a). Hyperforin as a possible antidepressant component of hypericum extracts. Life Sci 63 (6), 499-510.
Later dose dependent relationships indicated that there might be other ingredients responsible for antidepressant effect.
Chatterjee SS, Noldner M, Koch E, Erdelmeier C (1998b). Antidepressant activity of hypericum perforatum and hyperforin: the neglected possibility. Pharmacopsychiatry 31 (Suppl 1), 7-15.
Still other studies have confirmed that there are other active ingredients beside hyperforin that are responsible for antidepressant activity of hypericum. So whole herb hypericum extract is considered as the active principle of st. john’s wort.
Schrader E, et al (2000). Equivalence of St John’s wort extract (Ze 117) and fluoxetine: a randomized, controlled study in mild-moderate depression. Int Clin Psychopharmacology 15, 61-68.