PDF (Download) |
- Hops (Humulus lupulus)
- Pharmacological Profile
- Sedative Activity
| Date: 08-31-2008 | HC# 040382-359 |
Re: Pharmacological Profile of Hops
Zanoli P, Zavatti M. Pharmacognostic and pharmacological profile of Humulus lupulus L. J Ethnopharmacol. 2008;116: 383-396.
Hops (Humulus lupulus) has been used traditionally for medicinal
purposes, particularly for the treatment of sleep disorders, as a mild
sedative, and as a bitter for the activation of gastric function. In addition,
hops was used internally and topically to relieve muscle spasms and nerve pain.
Another long-time use of the plant has been in the brewing industry. Its female
inflorescences (hop cones) are used to preserve beer and give it a
characteristic aroma and flavor. These authors describe the morphological,
phytochemical, and ethnopharmacological aspects of the plant and summarize
their most interesting findings obtained in preclinical and clinical research.
According to the authors,
only a few findings of H. lupulus
exist in Europe from prehistoric periods.
There are more findings from the early Middle Ages because of its increased use
in the brewing process. The cultivation of hops started from the middle of the
ninth century in Germany,
where it extended from north to south during the early and high Medieval
period, as well as to other regions of central Europe.
Currently, the brewing industry accounts for 98% of the world use of hops.
Native American tribes used
hops as a sedative, antirheumatic, analgesic, and as a urinary aid for
"gravel" and inflammation. In India, the Ayurvedic Pharmacopoeia
recommends hops to treat restlessness associated with nervous tension,
headache, and indigestion. In traditional Chinese medicine, hops is used to
treat insomnia, restlessness, dyspepsia, and lack of appetite.
The German Commission E and
European Scientific Cooperative on Phytotherapy approved hops as a treatment
for excitability, mood disturbances (restlessness, anxiety), and sleep
disturbances.
The main structural classes
of chemical compounds identified from mature hop cones include terpenes
(0.3-1.0% dry wt.), bitter acids (5-20% dry wt.), and chalcones. They are also
rich in flavonol glycosides and catechins. The bitter acids are phloroglucinol
derivatives usually classified as α-acids (humulones) and β-acids (lupulones)
and are present in hops as a complex mixture of variable composition and
concentrations. Several prenylflavonoids have been identified from hop cones.
According to the authors, the most important compound is the chalcone
xanthohumol (up to 1% dry wt.), which can be converted to the prenylflavonone
isoxanthohumol (IX) with thermal treatment and increased pH value. IX can be
converted by the intestinal flora and/or liver cytochrome P450 to
8-prenylnaringenin (8-PN), a potent phytoestrogen.
The authors cite a number of
studies of mice and rats (including their own studies) investigating the use of
different extracts of hops as a mild sedative. A CO2 extract
administered orally enhanced pentobarbital-sleep and reduced behavioral despair
test immobility time, suggestive of antidepressant activity, at a 10 mg/kg dose
in rats. The CO2 extract fraction containing a-acids elicited the same effects, while the b-acid fraction appeared to provide contributory activities. "In
spite of these recent studies, the identity of the active sedative principle/s
of hops as well as the mechanism/s of action is still questionable," they
say. No randomized, double-blind, placebo-controlled clinical trials using hops
extract alone have been conducted.
Combinations of hops and
valerian have shown promising results as useful and safe alternatives to the
classic sedative drugs. However, say the authors, "no meaningful
information regarding the potential clinical efficacy of hops can be
extrapolated by using clinical formulations containing hops in combination with
other medical plants. Therefore the real efficacy of hops in sleep disturbances
remains to be ascertained."
The authors cite several in
vivo investigations performed to study the estrogenic properties of the hop
cone extracts and 8-PN. In addition, they cite a randomized, double-blind,
placebo-controlled study on the use of a standardized hops extract in
menopausal women, in which a decrease in hot flashes and other discomforts
associated with estrogen deficiency were reported. Other studies support the
plant's efficacy in relieving menopausal symptoms. "Although further
clinical studies are needed, hop-derived prenylated flavonoids could provide an
attractive alternative treatment for the relief of menopausal symptoms,"
say the authors.
During the past 10 years,
several in vitro studies have been performed to evaluate the potential activity
of hops components including the bitter acids as chemopreventive agents. Among
the components, "xanthohumol (XH) has received the major attention because
it seems to inhibit in vitro initiation, promotion, and progression stages of
carcinogenesis."
The authors cite several
studies reporting antibacterial and antifungal activities of certain hops
constituents.
Regarding its effect on the
stomach, the authors cite a study of an aqueous preparation of H. lupulus in patients affected by
chronic hyposecretory gastritis. The study reported that the treatment
stimulated gastric secretion.
Among the reported side
effects of hops are bronchial irritation, dry cough, and dyspnea in
hop-processing workers, as well as occupational dermatitis associated with
fresh and dried hops. However, the authors note that "no clinical case of
allergy or anaphylaxis resulting from the therapeutic use of hops has been
published."
The authors conclude that the
"use of chemically characterized hop extracts for biological assays and
for clinical trials is the right approach to study their pharmacokinetic and
pharmacological profile and to perform comparative studies, with the aim to
validate the mentioned properties of hops." Much work is needed "to
achieve a reliable standardized product and to link it to a specific biological
activity and to specific therapeutic applications."
—Shari Henson
|