Issue: 67 Page: 32
Study on Valerian/Hops Combination Sheds Light on Mechanism of Action in Promoting Sleep
by Heather S. Oliff, PhD
HerbalGram. 2005; 67:32 American Botanical Council
Study on Valerian/Hops Combination Sheds Light on Mechanism of Action in Promoting Sleep
Reviewed: Schellenberg R, Sauer S, Abourashed EA, Koetter U, Brattström
A. The fixed combination of valerian and hops (Ze91019) acts via a central adenosine
mechanism. Planta Med. July 2004;70(7):594-597.
Sleep cycles go through a sleep-wake
rhythm during the entire night. The rhythm is related to changes in adenosine
concentration within the central nervous system (CNS). Studies have shown that
CNS administration of adenosine induces sleep. Valerian (Valeriana
officinalisL., Valerianaceae) and hops (Humulus lupulus L., Cannabaceae) are used as sleep
aids. Valerian contains constituents that can bind to the adenosine receptor.
This enables some of these valerian compounds, and/or their metabolites, to act
like adenosine in the brain. Their action resembles that of a “partial
agonist” in that they do not stimulate the receptor
as fully as adenosine itself. Caffeine also acts on the adenosine receptors.
It works as an antagonist—inhibiting adenosine from binding to the receptor
and inducing sleep. As a result, caffeine causes CNS arousal. The excitation
produced by caffeine is most pronounced 1-3 hours after consumption. A study
conducted in 1929 suggests that the caffeine excitation might be blocked by simultaneous
administration of valerian. Modern technology enables this early finding to be
evaluated and validated. The present study evaluated the competition between
the compounds in a valerian/hops extract and caffeine for CNS adenosine binding
sites. The goal was to better understand the mechanism of action of valerian/hops
extract.
Healthy men (N = 48) participated in this randomized, placebo-controlled,
blinded study approved by the Hessen Medical Association (Germany). The subjects
did not use coffee, nicotine, or CNS drugs; they had no history of psychiatric
and/or neurological diseases, and no drug, alcohol, or caffeine abuse. Subjects
received either 6 tablets of placebo, 6 tablets of valerian/hops extract (Ze
91019 by Max Zeller AG, Romanshorn, Switzerland; imported and marketed as Alluna® Sleep
in the U.S. by Enzymatic Therapy, Green Bay, WI), or 2 tablets of valerian/hops
extract and 4 tablets of placebo. Each active tablet contained 250 mg valerian
extract and 60 mg hops extract, both standardized by a defined manufacturing
procedure. Simultaneously, the subjects received 200 mg caffeine (Coffeinum® N
0.2, Merck, Germany). An electroencephalogram (EEG), which is placed on the head,
was used to record CNS activation.
The caffeine arousal effect was dose-dependently
neutralized by oral administration of the valerian/hops extract. The full dose
of valerian/hops (6 tablets) inhibited, rather than reduced (2 tablets), the
caffeine-induced arousal. Valerian had an early action—within one hour
the full dose had neutralized the caffeine. This suggests that valerian might
induce sleep by activating adenosine receptors.
The authors conclude that valerian/hops
extract acts as a sleep aid by suppressing arousal via a central adenosine-mediated
mechanism. Also, the onset of action is relatively fast. Since only men and non-coffee
drinkers were studied, the onset of action and efficacy may be different in women
and in habitual coffee or tea drinkers.
—Heather S. Oliff, PhD
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