Hawthorn (Crataegus monogyna, Crataegus oxyacantha)
Hawthorn (Crataegus monogyna, Crataegus oxyacantha) is a member of Rosaceae family and has been recorded as a popular medicinal plant in most of the countries. The berry has been a key part of traditional Chinese medicine for at least 2000 years. The genus name, “Crataegus” comes from the Greek word, “kràtaigos” which means “strength and robustness” due to its hard and durable wood. The parts of the Hawthorn bush that are used for medicinal purposes are the berries and the leaf. The berries of the Hawthorn are collected in the fall after they turn a dark purple.
Hawthorn berries are one of the oldest known medicinal plants used in European herbal medicine. Dioscorides, a Greek herbalist, was the first to report the performance of Hawthorn Berry on the heart. Dioscorides was followed by a Swiss physician, Paracelsus who touted the use of Hawthorn Berry for its actions on the heart. During his years of practice, Dr. Green of Ennis, Ireland held such a reputation of curing heart disease and other ailments of the heart, that he had patients from all over the United Kingdom. While remaining a physician in good standing, he refused to share his secret with his colleagues. After his death in 1894, Dr. Green’s daughter revealed that a concentrate of fresh Hawthorn berries, Crataegus Oxycantha, Common Hawthorn, was the formula which her father had successfully used to cure his many heart patients.
Uses
It is used in traditional Chinese medicine to improve digestion, stimulate appetite, treat cardiovascular conditions and hyperlipidemia, and invigorate blood. Hawthorn extract also has a long history in European medicine as a cardiotonic. Because of Hawthorn Berry’s anti-inflammatory properties, it has been used to reduce ulcerative colitis, also known as inflammatory bowel disease. When used for weight loss, it aids in digestion and helps reduce water retention by expelling excess salt from the body. Hawthorn is also high in pectin and therefore is soothing to the throat and respiratory tract. Hawthorn Berry is known to reduce nervous tension and alleviate insomnia.
Hawthorn is currently used extensively by physicians in Europe in its standardized form for early stage of heart failure and various other cardiovascular and peripheral circulatory conditions including angina, cardiac incompetence not yet requiring digitalis, hypertension, and arrhythmias.
Chemistry/Pharmacology
Chemical analysis has allowed for the identification of more than 150 bioactive molecules in Hawthorn fruits, leaves, and flowers, such as flavonoids, oligomeric proanthocyanidins, triterpene acids, phenolic acids (ferulic, gallic, p-coumaric, syringic, chlorogenic organic acids (fumaric, tartaric, succinic, citric, malic), sterols, sugars (maltose, sucrose, glucose, fructose) and trace amounts of cardioactive amines. Flavonoids and OPCs are the two major groups of bioactive components. Pharmacologic activities of hawthorn flower, leaf, and berry extracts are attributed to constituents such as flavonoids and oligomeric procyanidins. Laboratory experiments suggest cardiac action of the flavonoids occurs via inhibition of the 3’,5’-cyclic adenosine monophosphate phosphodiesterase, and demonstrate positive inotropic effects by hawthorn that increase heart rate. Inotropic and vasodilatory effects have also been related to increased myocardial perfusion and reduced afterload. Antioxidant properties and inhibitory effects against LDL oxidation are attributed to phenolic compounds.
Clinical Studies
Various animal studies have suggested that hawthorn extracts exert a wide range of pharmacological properties, especially on the cardiovascular system, including cardiotonic, antiarrhythmic, hypotensive, hypolipidemic, and antioxidant activities.
Cardiotonic Activity
Numerous in vitro and animal studies have tested the activities of water-soluble extract, flavonoid fraction, triterpene fraction, and OPC fraction, which are prepared from hawthorn fruits, leaves, or flowers as well as individual components of hawthorn (hyperoside, luteolin-7-glucoside, epicatechin, vitexin, and rutin). Marked cardiotonic actions have been observed: positive inotropic and negative chronotropic effect, increase of coronary blood flow and cardiac output, and reduction of oxygen consumption. These actions may be related to phosphodiesterase inhibitory effect.
Hypolipidemic Activity
Hawthorn has been found to decrease the serum levels of cholesterol, LDL-cholesterol, and triglyceride in hypercholesterolemic and atherosclerotic animals. It also significantly inhibits lipid deposition in the liver and aorta. When administered to rats fed with an atherogenic diet, the hawthorn fruit extract increased excretion of bile acid, depressed hepatic cholesterol synthesis, and significantly increased the binding of 125I-LDL to the liver plasma membranes, indicating an enhancement of the LDL-receptor activity.
Hypotensive Activity
When flavonoid, OPC, and triterpene acid extracts were administrated intravenously to various species of animals, prolonged dose-dependent hypotension in anaesthetized normotensive and hypertensive animals was observed. The hypotensive action was mainly attributed to peripheral vasodilation. In more recent studies, the hawthorn extract was found to induce endothelium-dependent relaxation in an isolated rat mesenteric artery. Procyanidins were identified as the major component for this effect.
Antiarrhythmic Activity
The cardiovascular effects described for hawthorn extract is somewhat like that of phosphodiesterase-3 (PDE3) inhibitors, which demonstrate various pharmacological properties including cardio-medicinal, vasodilating, anti-inflammatory and antioxidant, and have been identified as potential therapeutic agents in cardiovascular disease. 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.
Biomechanical Mechanism
The primary activity of hawthorn is to increase coronary blood flow. This may be due to relaxation of coronary arteries, which directly increases blood flow or through an increase in contraction and relaxation velocities, which increases the diastolic interval and thus allows more time for blood passage through the coronary arteries.
Hawthorn’s positive inotropic action may also be due to inhibition of myocardial Na+/K+ ATPase which is an integral membrane enzyme that maintains cardiac resting potential. It also decreases blood pressure which results in an increase in exercise tolerance during the early stage of congestive heart failure (CHF). Surprisingly, Hawthorn can regulate both low and high blood pressure. With the bioflavonoids reportedly dilating both peripheral and coronary blood vessels leading to its use in angina; the procyanidins content is claimed to support the vasorelaxant effects. Hawthorn’s glycoside component has also been reported to increase vagal tone of the heart.
Hawthorn has also been reported to have angiotensin converting enzyme (ACE) inhibiting effect. It may also have a cardio-protective effect due to its ability to decrease the oxygen demands of cardiac tissue. Varying results have been observed regarding the effect of hawthorn and its constituents on heart rate. In majority of in vitro studies, an increase in heart rate has been observed while conversely, most in vivo studies report a decrease in heart rate.
Hawthorn has been shown to exhibit antioxidant activity associated with its flavonoid and procyanidin content. Hawthorn also exhibits anti-inflammatory property by preventing synthesis and release of inflammatory promoters such as histamines, serine proteases, prostaglandins, leukotrienes etc. as well as inhibiting enzymatic cleavage by enzyme secreted by leukocytes during inflammation.
Sources/Articles
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