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.

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