David L. Hoffmann BSc Hons MNIMHCrataegus oxyacantha & C. monogyna
Part used
Whilst the berries are the most often used part of this shrub, the
flowers and leaves may also have a role to play.
Constituents
Its constituents highlight the importance of flavones and flavonoids in
many remedies that have a healing impact upon the cardio-vascular system. There are two main groups:
- flavonoids – flavonoglycosyls, hyperoside, rutin
- oligomeric procyanadins, 1-epicatechol.
This invaluable heart remedies does not contain cardiac glycosides.
Acantolic-Acid
Acetyl-Choline
Acetyl-Vitexin-4′-Rhamnoside
Adenine
Adenosine
Aesculin
Aluminum
Aminopurine
Amygdalin
Ascorbic-Acid
Caffeic-Acid
Calcium
Carbohydrates
Beta-Carotene
Catechin
Catechin-Tannins
Chlorogenic-Acid
Choline
Chromium
Citric-Acid
Cobalt
Crataegolic-Acid
Trans-Crataegolic-Acid
Dimethylamine
Epicatechin
L-Epicatechol
Ethanolamine
Ethylamine
Fat
Fiber
Glucose
Guanine
2, , 3, 3′, 4, 4′, 5, 7-Hepta-Hydroxyavanbioside
Hyperoside
Iron
Isoamylamine
Isobutylamine
Lauric-Acid
Leucoanthocyanidin
Linoleic-Acid
Linolenic-Acid
Lipase
Magnesium
Manganese
O-Methoxy-Beta-Phenethylamine
Neoategolic-Acid
Niacin
Nonacosan-10-Ol
Octacosane
Oxalic-Acid
Palmitic-Acid
Pectin
Beta-Phenethylamine
Phlobaphene
Phosphorus
Potassium
Procyanidin
Protein
Quercetin-3-Rhamnogalactoside
Quercitrin
Rhamnose
Riboavin
Rutin
Selenium
Silicon
Beta-Sitosterol
Beta-Sitosterol
Sodium
Sorbitol
Starch
Sugar
Tartaric-Acid
Thiamin
Tin
Trimethylamine
Tyramine
Uric-Acid
Ursolic-Acid
Vitexin
Vitexin-4′-Rhamnoside
Vitexin-4′, L-Rhamno-D-Glucoside
Vitexin-4′, 7-Di-D-Glucoside
Zinc
Aesculin ;Esculin; Aesculin; Crataegin;
This 6-glucoside of esculetin is widely occurring; e.g., in the bark of
Aesculus hippocastanum , in the bark of Crataegus oxyacantha, in
the bark of Fraxinus spp. and in the leaves of Bursaria
spinosa.
Inhibits chemically induced carcinogenic action. It is a growth inhibitor of
Bacillus subtilis.
Caffeic acid;; 3, 4-Dihydroxycinnamic acid
Widespread occurrence: e.g., in green and roasted coffee beans (Coffea
arabica) and in the root bark of Cinchona cuprea, in Conium
maculatum , and in the resin of various conifers. Also, it occurs in
herbaceous plants such as Digitalis purpurea , the leaves and flowers of
Papaver somniferum, the roots of Taraxacum officinale, and the
flowers of Anthemis nobilis and Achillea millefolium . It often
occurs in bound form as chlorogenic acid .
Antibacterial, antifungal, antiviral and antioxidant activities. It is an
analgesic and an anti-inflammatory agent, with antihepatotoxic, antiulcerogenic
and clastogenic activities also. It inhibits platelet aggregation in vitro and
gonadotropin release, and affects both DNA binding and prostaglandin
induction.
(+)-Catechin; Catechinic acid; Catechol; Catechuic acid; (+)-Cyanidanol;
(+)-Cyanidan-3-ol
Widespread occurrence in nature, especially in woody plants, e.g., in willow
catkin, Salix caprea.
Biologically highly active. It is used as a haemostatic drug, and in the
treatment of various liver diseases, especially acute hepatitis. It shows
strong liver protective and potent antiperoxidative activities, so that it may
act as a “radical scavenger” by neutralizing free radicals produced by
hepatotoxic substances. However, prolonged treatment with (+) catechin can
induce several adverse reactions, most of them immunomediated, such as
haemolysis, acute renal failure and skin rashes.
Kaempferol; 3, 5, 7, 4′-Tetrahydroxyflavone
Very widespread occurrence, both free and bound as glycosides. The
3-arabinofuranoside, juglanin, and 3-rhamnofuranoside occur in the leaves and
flowers of Aesculus hippocastanum. The 3-rhamnopyranoside, afzelin,
occurs in the heartwood of Afzelia spp. , and the 3-galactoside
trifolin, occurs in the leaves of Trifolium pratense .
Radical scavenger. It shows anti-inflammatory, antibacterial and mutagenic
activities. It inhibits the proliteration of rat Iymphocytes at a concentration
of 10 J M. Also, it inhibits iodothyronine deiodinase, :5-lipoxygenase, and
ionophore-induced arachidonlc acid release and metabolism.
Luteolin; 5, 7, 3′, 4′-Tetrahydroxyflavone
Very widespread occurrence, especially as the 7-glucoside and 7-glucuronide,
e.g., in the petals of Antirrhinum majus . The 7-galactoside and
7-rutinoside occur in Capsella bursa-pastoris, the 3′-glucoside in
Dracocephalum thymiflorum , and the 4′-glucoside in the flowers of
Spartium junceum . The aglycone is also very common, especially in leaf
exudates.
Anti-inflammatory and antibacterial activities. It inhibits iodothyronine
deiodinase, protein kinase C, NADH-oxidase, succinoxidase, lens aldose
reductase, etc. It acts as a nodulation signal to the bacterium Rhizobium
leguminosarum in pea roots and the bacterium R. meliloti in
lucerne.
Procyanidin; Proanthocyanidin A2; Epicatechin
Occurs in the nuts of Cola acuminata, the berries of Vaccinium
vitis-idaea, and the fruits of the horse-chestnut, Aesculus
hippocastanum and Persea gratissima.
Quercetin;; 3, 5, 7, 3′, 4′-Pentahydroxyflavone
The commonest flavonoid in higher plants, usually present in glycosidic form,
but also isolated free from the families Compositae, Passiflorae, Rhamnaceae
and Solanaceae.
Inhibits many enzymes, e.g., protein kinase C, lipogenases, lens aldose
reductase, 3′, 5′-cyclic adenosine monophosphate phosphodiesterases. It is a
radical scavenger. Quercetin also inhibits smooth muscle contraction, and
proliferation of rat Iymphocytes. It is antigonadotropic, anti inflammatory,
antibacterial, antiviral and antihepatotoxic, and shows some mutagenic activity
and allergenic properties.
Rhamnetin; Quercetin 7-methyl ether
Many glycosides are known: e.g., the 3-glucoside in Thalictrum foetidum
, the 3-rhamnoside (xanthorhamnin) in the fruit of Rhamnus
cathartica and the 3′-glucuronide in Tamarix aphylla. The aglycone
has been found in the aerial parts of many Compositae and Labiatae, and in the
leaf resin of Cistus spp. .
Rhamnetin and its 3-glucoside show antibacterial activity against
Pseudomonas maltophilia and Enterobacter cloacae. It also shows a
moderate contact sensitizing (allergenic) capacity.
Rutin; Quercetin 3-rutinoside; Rutoside
Very widespread occurrence in higher plants, e.g., in Polygonum spp. .
First isolated from rue, Ruta graveolens.
Radical scavenger. Medicinally, it is used against capillary fragility and
varicosis. A more soluble derivative, hydroxyethylrutoside, is also used
clinically. It shows antiviral and antibacterial activities, and it inhibits
lens aldose reductase and _5-lipoxygenase. It is a feeding attractant to the
beetle Gastrophysa atrocynea, which feeds on Polygonum, but a
feeding deterrent to larvae of Heliothis zea. Also, it is a contact
oviposition stimulant to the butterfly Papilio xuthus for laying eggs on
citrus leaves .
Actions: Cardio-tonic, diuretic, astringent, hypotensive.
Hawthorn is the best known of the cardiac tonics, and possibly the most
valuable tonic remedy for the cardiovascular system found in the plant kingdom.
The American Herbalist, Ellingwood said of Hawthorn that “… it is superior to
any of the well known and tried remedies at present in use for the treatment of
heart disease, because it seems to cure while other remedies are only
palliative at best.”
It can be considered in most cardio-vascular disease. However, the
therapeutic benefts are only gained when a whole plant preparation is used.
When the isolated constituents were tested seperately in the laboratory, their
individual effects were insignificant, whilst the whole plant has unique and
valuable properties. Herbal synergy!
Following a four year study commissioned by the German Federal Ministry of
Health, Hawthorn has gained full recognition as a heart remedy. The monograph
concludes that the , it gently increases the strength and normalizes the rhythm
of the heart beat, as well as increasing coronary and myocardial circulation,
through a dilation of the coronary arteries.
Its main clinical applications are in the long-term treatment of ‘loss of
cardiac function’, any situation where there is a subjective feelings of
congestion and ‘oppression’ in the heart region, mild arrythmia’s and
especially for conditions of the ageing heart that do not warrant the use of
Foxglove.
Cardio-vascular degenerative disease, angina pectoris, coronary artery disease
and associated conditions.
For essential hypertension, used in conjunction with other hypotensives,
Hawthorn will maintain the heart in a healthy condition, preventing the
development of coronary disease. No toxicity, accumulation or habituation
accurs, thus it may be used long term, achieving result entirely safely,
especially in the elderly. Most significantly is the finding that no
contra-indications or side effects were noted at all.
Dosage and preparations
As one of the more aesthetic herbal remedies, a very pleasant tea can
be made from 1-2 teaspoonfuls of the dried berries infused in hot water and
drunk regularly. 1ml of the tincture are taken 3 times daily, then morning
& evening as a maintenance dose. This may be taken over long periods of
time as their is no fear of toxicity problems. Up to 5ml three times daily can
taken quite safely.
Citations from the Medline database for the genus Crataegus:
Hawthorn
Ammon HP Handel M
[Crataegus, toxicology and pharmacology. Part III: Pharmacodynamics and
pharmacokinetics]
Planta Med (1981 Dec) 43(4):313-22 Published in German
Ammon HP Handel M
[Crataegus, toxicology and pharmacology. Part II: Pharmacodynamics (author’s
transl)]
Planta Med (1981 Nov) 43(3):209-39 Published in German
Ammon HP Handel M
[Crataegus, toxicology and pharmacology, Part I: Toxicity (author’s
transl)]
Planta Med (1981 Oct) 43(2):105-20 Published in German
Beier A Konigstein RP Samec V
[Clinical experiences with a crataegus pentaerythrityl-tetranitrate
combination drug in heart diseases due to coronary sclerosis in old age]
Wien Med Wochenschr (1974 Jun 15) 124(24):378-81 Published in German
Blesken R
[Crataegus in cardiology]
Fortschr Med (1992 May 30) 110(15):290-2 Published in German
The fact that the effectiveness of numerous phyto-preparations, so- called,
has been demonstrated to the satisfaction of traditional medicine has led to
increasing interest in phytotherapy. This also applies to Crataegus
(whitethorn), the effects of which have been demonstrated in numerous
pharmacological studies. These effects, produced mainly by the flavonoids,
indicate a simultaneous cardiotropic and vasodilatory action, as confirmed
clinically in controlled double-blind studies. This means that Crataegus can be
employed for cardiological indications for which digitalis is not (yet)
indicated. Prior to use, however, a Crataegus preparation must meet certain
preconditions with respect to dosage, pharmaceutical quality of the
preparation, and an accurate definition of the later.
Ciplea AG Richter KD
The protective effect of Allium sativum and crataegus on isoprenaline-
induced tissue necroses in rats.
Arzneimittelforschung (1988 Nov) 38(11):1583-92
Di Renzi L Cassone R Lucisano V Leggio F Gambelli G
[On the use of injectable crataegus extracts in therapy of disorders of
peripheral arterial circulation in subjects with obliterating arteriopathy of
the lower extremities]
Boll Soc Ital Cardiol (1969) 14(4):577-85 Published in Italian
Fehri B Aiache JM Boukef K Memmi A Hizaoui B
Valeriana officinalis & C. oxyacantha: toxicity from repeated
administration
J Pharm Belg (1991 May-Jun) 46(3):165-76 Published in French
Hammerl H Kranzl C Pichler O Studlar M
[Clinico-experimental metabolic studies using a Crataegus extract]
Arztl Forsch (1967 Jul 10) 21(7):261-4 Published in German
Kharchenko NS
[Medicinal value of Crataegus ucrainica]
Vrach Delo (1965 Jan) 1:116-7 Published in Russian
Massoni G
Hawthorn extract (Crataegus) in the treatment of certain ischemic myocardial
diseases in old age
G Gerontol (1968 Sep) 16(9):979-84 Published in Italian
Mavers WH Hensel H
Changes in myocardial blood circulation following administration of
Crataegus extract in non-narcotized dogs
Arzneimittelforschung (1974 May) 24(5):783-5 Published in German
Muth HW
[Indications for treatment with crataegus]
Ther Ggw (1976 Feb) 115(2):242-55 Published in German
Nasa-Y; Hashizume-H; Ehsanul-Hoque-A-N; Abiko-Y
Protective effect of Crataegus extract on the cardiac mechanical dysfunction
in isolated perfused working rat heart.
Arzneimittel-Forschung (1993) 43(9): 945-949
The effect of the water-soluble fraction of Crataegus (Crataegus extract) on
the cardiac mechanical and metabolic function was studied in the isolated,
perfused working rat heart during ischemia and reperfusion. Ischemia (15 min)
was produced by removing afterload pressure, and reperfusion (20 min) was
produced by returning it to the original pressure. In the control (no drug)
heart, ischemia decreased mechanical function to the lowest level, which did
not recover even after the end of reperfusion. Crataegus extract (0.01 or
0.05%) was applied to the heart from 5 min before ischemia through the first 10
min after reperfusion. With the high concentration of Crataegus extract (0.05%)
the mechanical function recovered during reperfusion incompletely without
increasing coronary flow, but the low concentration of Crataegus extract
(0.01%) did not. In the heart treated with the high concentration of Crataegus
extract, the reperfusion-induced recovery of the energy metabolism was
accelerated, and the level of lactate during ischemia was lower than that in
the control heart, although the myocardial levels of free fatty acids during
ischemia and reperfusion were not greatly affected. These results demonstrate
that Crataegus extract (0.05%) has a cardioprotective effect on the
ischemic-reperfused heart, and that the cardioprotective effect is not
accompanied by an increase in coronary flow.
O’Conolly M Jansen W Bernhoft G Bartsch G
Treatment of decreasing cardiac performance. Therapy using standardized
crataegus extract in advanced age
Fortschr Med (1986 Nov 13) 104(42):805-8 Published in German
Rewerski W Lewak S
[Some pharmacological properties of flavan polymers isolated from hawthorn
(Crataegus oxyacantha)]
Arzneimittelforschung (1967 Apr) 17(4):490-1 Published in German
Rewerski W Piechocki T Rylski M Lewak S
[Pharmacological properties of oligomeric procyanidine isolated from
hawthorn (Crataegus oxyacantha)]
Arzneimittelforschung (1971 Jun) 21(6):886-8 Published in German
Schmidt U., Kuhn U., Ploch M., Hubner
Efficacy of the Hawthorn (Crataegus) Preparation Ll 132 in 78 patients with
chronic congestive heart failure defined as NYHA functional class ll.
Phytomedicine Vol. 1/1994, pp. 17-24
Seventy-eight male and female patients between the ages of 45 and 73, who
were affected by chronic heart failure defined as NYHA functional class 11,
were treated either with Crataegus ex tract or with a placebo preparation. The
extract Ll 132 was administcred to the patients hl the form of 3 dragees a day
(verum preparation) corresponding to a daily dose of 600 mg. Treatment was
continued over a period of 8 weeks, with a wash-out phase of one week. The
confirmatory parameter used to asses the efficacy of the preparation was the
patients’ working capacity which was measured using an ergometer bicycle.
Before the start of the study, an increase in the patients’ working capacity of
at least half an exercise step on the ergometer bicycle (12.5 watt) was
determined to be clinically relevant. Apart from the compatibility of the
preparation, a score system was used to assess the severity Ievel of the
typical symptoms. From day 0 to day 56 of thc trial, the median values obtained
for the working capacity of the patients treated with the verum preparation
were found to have increased by 28 watt, while the increasc in thc working
capacity of the placebo patients was as little as 5 watt. Thc diffcrcnce was
statistically siL:nificallt (p < O.OOl ). Apart from that, a significant reduction of thc systolic blood prcssure, of the heart ratc and of the prcssure/rate product was observed for thc patiellts treated with thc verum prepara tion, compared to the patients treated with the placcbo preparation. Also, the clinical symptoms were found to havc improved significant!y. There were no severe side effects observed.
Thompson EB Aynilian GH Gora P Farnworth NR
Preliminary study of potential antiarrhythmic effects of Crataegus
monogyna.
J Pharm Sci (1974 Dec) 63(12):1936-7
Wagner H Grevel J
[Cardioactive drugs IV. Cardiotonic amines from Crataegus oxyacantha
(author’s transl)]
Planta Med (1982 Jun) 45(2):98-101 Published in German
Wang SL Li YD Zhao Q
[Effects of Crataegus pinnatifidae, Astragalus memoranaceus and Acanthopanax
senticosus on cholesterol metabolism in the guinea pig]
Chung Hsi I Chieh Ho Tsa Chih (1987 Aug) 7(8):483-4, 454 (Published in
Chinese)
Wolkerstorfer H [Treatment of heart disease with a digoxin-crataegus
combination]
Munch Med Wochenschr (1966 Feb 25) 108(8):438-41 Published in German
Hyla Cass MD
Tom Ferguson MD