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Hawthorn—A Health Food
HAN Junyan
1,a
, TAN Dehong
2,b
, LIU Guangchun
1,c
1.
College of Biological and Environmental Engineering, Shenyang University, Shenyang,
China.110044
2.
College of Food, Shenyang Agricultural University, Shenyang, China.110866
a
Hanjunyan@yahoo.cn,
b
tandehongsy@126.com,
c
liugc@yahoo.cn (corresponding author)
Key words: crataegus; hawthorn; flavonoid; Shanzha; caridiac
Abstract: The genus of Crataegus (hawthorn) is cultivated in many parts of the world. and regarded
as medicinal plant in many countries. Hawthorn fruit is commonly used to cure scurvy, constipation
and digestive disorders, Hawthorn flowers and leaves are often used against mild cardiac disorders.
Modern studies found extracts of Hawthorn fruits, flowers and leaves possess a wide range of
pharmacological properties, the pharmacological properties of Hawthorn are mostly related to the
involved phenolic compounds including flavonoids. In this article, the active chemical properties
and medicinal value of Hawthorn are reviewed.
Introduction
The genus of Crataegus (hawthorn) belongs to the rosaceae family, comprising approximately 280
species, is cultivated in many parts of the world. Hawthorn is regarded as medicinal plant in many
countries[1]. Modern studies found extracts of Hawthorn fruits, flowers and leaves possess a wide
range of pharmacological properties, the pharmacological properties of Hawthorn are mostly related
to the involved phenolic compounds including flavonoids[2].
In this article, the active chemical properties, medicinal value and safety issue of Hawthorn are
reviewed.
Chemical properties
General chemical properties and composition of Hawthorn fruit Özcan et al.[3]
established chemical properties and minerals content of hawthorn fruits (Crataegus spp.). The
energy, protein, cellulose, oil, ash, acidity and water-soluble extract values of hawthorn fruits are
34.02 kcal/g, 2.48%, 4.67%, 0.87%, 2.28%, 1.98% and 32.31%, respectively. The minerals of Ca, K,
Mg, Na and P, are 3046.37 ppm, 13,531.96 ppm, 1502.55 ppm, 312.18 ppm and 1477.88 ppm,
respectively.
Functional compounds of hawthorn The dominant functional components in hawthorn
fruits, leaves and flowers are phenolics, including flavonoids (e.g. hyperoside, isoquercitrin,
quercitin), proanthocyanins (e.g. epicatechin) and phenolic acid (e.g. chlorogenic acid) [4].
Medicinal value of Hawthorn
Antioxidant effects The antioxidant effects and the active constituents of hawthorn have
been widely studied, which are closely related with other pharmacological properties of Hawthorn.
[5]. Polyphenols scavenge free radicals collaborating with other antioxidants and metals [6], which
possess the ideal chemical structure for scavenging free radicals. The highest radical scavenging
activity is exhibited by compounds that have an ortho 30, 40 - dihydroxy structure at ring B (e.g.
catechin, quercetin) or hydroxyl groups in position meta, e.g. 5, 7 - dihydroxy at ring A (e.g.
kaempferol, apigenin), as well as those that have a double bond between the C2 and C3 and the C3 -
hydroxyl group at ring C. The activity is also influenced by the flavonoid particle glycosylation [7].
Applied Mechanics and Materials Vol. 140 (2012) pp 350-354
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Medicinal effects on cardiovascular system Hawthorn was first documented as a treatment
for various cardiovascular disorders in Europe in the late 1800s [8], now, hawthorn products have
become popular herbal supplements for cardiomedicinal purpose, including cardiovascular
protection, endothelium-dependent vasorelaxation, improvement of coronary circulation, and
hypolipidemic effects, etc, are used for improving cardiac function, arrhythmia cholesterolemia and
hypertension [9].
Improving cardiac function
Preclinical studies A number of experimental studies performed on whole animals, show
extracts of hawthorn can increase cardiac contractility, increase cardiac blood flow and decrease
blood pressure[10]. Studies conducted on isolated cardiac muscle or vascular tissue demonstrate
positive inotropic effects, mild chronotropic effects, increased cardiac flux from improved ejection
volume, and vasorelaxation[11].
The mechanism of action was assumed previously to include an increase in force of contraction of
the heart and a vasorelaxant effect, particularly on coronary vessels [12]. The later studies showed
the strengthening of the heart contraction in isolated perfused hearts was only evident to a relatively
small extent, while the increase in coronary flow was more noticeable. Hawthorn extracts also
possessed a relatively strong relaxant effect on the vascular smooth muscle (aorta), implying
Hawthorn can decrease the preload for the heart [13].
Clinical studies Hawthorn leave and flower extracts were shown to reduce the incidence of
sudden cardiac death in certain patients [14] and be effective in treating chronic heart failure [15].
Several double-blind clinical studies of patients diagnosed with Chronic Heart Failure (CHF) have
shown beneficial effects of hawthorn. Clinical trials with New York Heart Association (NYHA)
stage-II or -III CHF demonstrated that Hawthorn extracts (WS 1442 and Crataegutt novo 450)
effectively improved cardiac performance, including decreased ankle edema, improved ejection
fraction, mildly reduce blood pressure[16]. In a study, hawthorn was found to be as effective as
captopril in improving exercise tolerance. Based on ergometric performance parameters, the
minimum effective daily dose of hawthorn extract is 300 mg. In most trials, the maximum benefit
was seen after 6 to 8 weeks of therapy[17].
Compared to digitalis, hawthorn has a wider therapeutic range, lower risk in case of toxicity, has
less of an arrhythmogenic potential, is safer to use in renal impairment, and can be safely used with
diuretics and laxatives[18].
Antiarrhythmic effect
The cardiovascular effects described for hawthorn extract is some what like that of
phosphodiesterase-3 (PDE3) inhibitors, which demonstrate various pharmacological properties
including cardiomedicinal, vasodilating, anti-inflammatory and antioxidant, and have been
identified as potential therapeutic agents in cardiovascular disease[19]. However, Hawthorn extracts
show unique chronotropic effects that it appears to be antiarrhythmic but capable of inducing
rhythmicity in quiescent cardiomyocytes, suggesting Hawthorn extracts may contain unique PDE3
inhibitors without arrhythmogenic potential [20].
Hypocholesterolemic and atheroscleroprotective effect
Hawthorn possesses the benefits of hypocholesterolemic and atheroscleroprotective activity.
Consumption of hawthorn can alter cholesterol metabolism of the liver, increases hepatic LDL
receptor activity [21], and reduce blood lipid and cholesterol levels [22]. In addition, the abundant
amount of antioxidants contained in hawthorn can protect LDL from oxidation, slow down the
development of atherosclerosis [23].
Hawthorn improves serum lipid metabolism with increased LDL and decreased HDL. Kwok et
al.[24] investigated the hypocholesterolemic and atheroscleroprotective potentials of dietary
consumption of hawthorn in high-cholesterol diet (HCD) rats, the results showed an increased
plasma total cholesterol and LDL-cholesterol with a decreased HDL-cholesterol in HCD-fed rats for
4 weeks. Hawthorn markedly suppressed the elevated total cholesterol and LDL-lipoprotein levels
plus an increased HDL cholesterol level. Hawthorn also prevented the development of fatty liver,
and elevated oxidative stress (estimated by the decreased levels of anti-oxidant enzymes) associated
Applied Mechanics and Materials Vol. 140 351
with HCD. In additionally, Hawthorn improved the blunted relaxation of isolated aortas induced by
acetylcholine of HCD-fed rats. The results indicate benefits of Hawthorn on lipid metabolism and
blood vessels.
Hypotensive effect
Hawthorn leaves, flowers and fruits are used to treat mild hypertension alone or in conjunction with
prescribed drugs. In a pilot study of mild hypertension, there were promising hypotensive responses
to 500 mg of hawthorn extract per day after 10 weeks. Walker et al. [25] investigated the effects of
hawthorn for hypertension in patients with type II diabetes. Results showed there was a significant
group difference in mean diastolic blood pressure reductions (P = 0.035): the hawthorn group
showed greater reductions (baseline: 85.6 mmHg, 95% confidence interval [CI] = 83.3 to 87.8;
outcome: 83.0 mmHg, 95% CI = 80.5 to 85.7) than the placebo group (baseline: 84.5 mmHg, 95%
CI = 82 to 87; outcome: 85.0 mmHg, 95% CI = 82.2 to 87.8). There was no group difference in
systolic blood pressure reduction from baseline (3.6 and 0.8 mmHg for hawthorn and placebo
groups, respectively; P = 0.329). In a double-blind, placebo-controlled clinical trial to determine the
effects of the C. curvisepala leaves and flowers extract for mild hypertension, results showed a
significant decrease in both systolic and diastolic blood pressure after 3 months (p < 0.05), and a
time-dependent antihypertensive effect [26].
The mechanism for hypotension of Hawthorn is regard to be related to the inhibition of Angiotensin
I - Converting Enzyme (ACE), which is considered to be a useful therapeutic approach in the
treatment of high blood pressure. Within the enzyme cascade of the renin-angiotensin system, ACE
removes histidyl-leucine from angiotensin I to form the octapeptide angiotensin II, which is one of
the most potent vasoconstrictors. Angiotensin II also stimulates the synthesis and release of
aldosterone which promotes sodium and water retention, resulting in increasing of blood
pressure[27]. Using an in vitro ACE-inhibition assay, Inokuchi et al. [28] found ACE-inhibitory
fractions in Hawthorn fruits. Lacaille-Dubois et al.[29] found flavonoids and proanthocyanidins
from the flowers and leaves of C. oxyacantha/ monogyna demonstrated inhibitory activity at 0.33
mg/ml, while phenolic acids showed no significant ACE-inhibition.
Conclusion
Based on the present review, we learn that hawthorn possesses medical value especially in
cardiovascular field. For further developing hawthorn to commercial products, more works still
need to be done, e.g. purifying the active constituents, clarifying the molecular mechanisms for its
medical action, etc. which may lead to a new era for utilization of hawthorn.
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