Scientific name: Crataegus
RosalesFamily = RosaceaeGenus = CrataegusSpecies = C. oxyacantha
Binomial name = Crataegus Oxyacantha
Chemical composition:1 Vitamin C.2 Flavonoids : Quercetin, Hyperoside, Rutin, Flavonoglycosyls,Vitexin-4′-rhamnoside. 3 Glycosides. 4 Oligomeric procyanidins (OPC) – epicatechol. Anthocyanidins and Proanthocyanidins (biflavans). 6 Saponins and Tannins.
7 Cratetegin (most prevalent in flowers > leaves >berries) 8 Other chemical constituents: a) Cardiotonic amines : Phenylethylamine, Tyramine, Isobutylamine, Omethoxy phenylethylamine; b) Choline and acetylcholine; c) Purine derivatives : Adenosine, Adenine, Guanine, Caffeic acid; d) Amygdalin; e) Pectins; f) Triterpene acids : Ursolic acid, Oleonic acid, Crategolic acid.
Saponins, glycosides, ascorbic acid, tannin; Oligomeric procyanidins including procyanidin B2, epicatechin and catechin; flavonoids including quercetin glycosides (hyperoside, rutin) and particularly flavone-C-glycosides; amines, catechols, carboxylic acid and triterpene acids
Procyanidin B2 was the principal procyanidin in all plant tissues. The procyanidins B4, B5 and Cl could also be detected in all samples as well as (-)-epicatechin.
Total phenolics, proanthocyanidins, catechins, flavonoids, and phenolic acids. The best correlations were established with total phenols while activities in leaves seem to be influenced by flavonoids and in flowers and fruits by proanthocyanidins and catechins.
Polyphenols (e.g., epicatechin, procyanidin B2, procyanidin B5, procyanidin C1, hyperoside, isoquercitrin and chlorogenic acid).
The results of spectrophotometric investigations indicate that the content of total phenol compounds in the investigated extracts varied from 2.12 to 30.63 mg GAE g-1 of fresh hawthorn sample. The content of anthocyanins ranged from 0.3207 to 3.168 mg of cyanidin-3-O-glucoside g-1 of fresh hawthorn fruit. The fruit extracts showed high antioxidant activity with DPPH radical transformation value as high as 89.9 % in the methanol-water (50/50, v/v%)) extract. The ethanol extract exhibited antimicrobial activity against all test microorganisms except two, Bacillus subtilis and Staphylococcus aureus, and one species of fungi, Aspergillus niger. Flavonoid structure influenced the extract’s selectivity towards Gram-positive and Gram negative bacteria.
Also, phenolic acids were identified by RP-HPLC and chlorogenic acid was the predominant phenolics in the samples.
The proanthocyanidin and flavonoid constituents of hawthorn appear to be responsible for beneficial physiological effects on cardiovascular system. Hawthorn also seems to have antioxidant activity (Liu et al., 2010). The main constituents of hawthorn are flavonoids, phenolic acids, proanthocyanidins (especially B-type procyanidins), organic acids and some amines (Urbonaviciute et al., 2006; Arslan et al., 2010). The leaf, flower, and fruit constituents responsible for free radical scavenging activity are especially epicatechin, hyperoside, and chlorogenic acid. They are also among the best antilipoperoxidants (Kwok et al., 2010; Jurikova et al., 2012). Among the fruits belonging to the Rosaceae, Hawthorn fruit (C. pinnatifida Bge.) show the highest rate of neuro-protective phenols (gallic acid, 4- aminobenzoic acid, rutin and quercitrin). To date, more than 50 flavonoids have been isolated from genus
Flowers revealed the highest tocopherols and ascorbic acid contents, as also the best n‐6/n‐3 fatty acids ratio. Over ripened fruits showed the highest levels of carbohydrates, sugars and SFA. Unripe fruits presented the highest PUFA contents with the best PUFA/SFA ratio, as also the highest levels of phenolics and the most promising antioxidant properties
To date, more than 50 flavonoids have been isolated from genus Crateagus spp. [8,29,30]. Determination of total flavonoids aglycone content gave 0.18%. The percentage of hyperoside, as the main flavonol component, was 0.14% . Aside from hyperoside , the presence of O-glycosides like luteolin-7-glycoside, rutin, and the C-glycosides vitexin, vitexin rhamnoside and monoacetylvitexin rhamnoside in Crateagus sp. fruits was also confirmed. Regarding the total contents of flavonol glycosides, the fruits of C. pinnatifida var. major contained less flavonol glycosides (0.4 mg/G DM as average content of 10 cultivars in the species) than those of other species. On the other hand, the fruit of C. pinnatifida var. major contained the highest level (1.1 mg/g DM) among all the tested hawthorn species .
Kaempferol is the dominant flavonol in Chinese hawthorn fruit , however, the presence of rutin in some cultivars of C. pinnatifida var. major was confirmed [7,25]. Compounds of the same molecular weight were found in fruits of C. pinnatifida var. major and were identified as quercetin rhamnosyl hexoside and quercetin (dirhamnosyl hexoside) and isoquercetin  (Figure 2). Most C-glycosyl flavones in hawthorn berries are derivatives of apigein and luteolin . Cui et al.  determined the polyphenol profile of four types of Chinese hawthorn fruit extract by high performance liquid chromatography with UV detection (HPLC-UV) profile and found vitexin-2”-O-rhamnoside—one of the typical components of Chinese hawthorn leaves.https://www.mdpi.com/1420-3049/17/12/14490/htm
Chlorogenic acid (A, Figure 1) has been found in fruits and leaves of all hawthorn species investigated . The presence of this compound in fruit of Chinese hawthorn was confirmed by several studies [7,14,17,25]. However, its isomer 5-O-caffeoylquinic acid (neochlorogenic acid) was reported only in fruits of C. grayana [8,25]. In addition to the dominant phenolic acid in Chinese hawthorn fruit, 4-hydroxybenzoic acid , 4-aminohydroxybenzoic acid along with gallic acid [14,27] were also present. The presence of protocatechuic acid (B, Figure 1) in fruit of C. pinnatifida. Bge. caffeic acid was only seen in fruit of European hawthorn (Procyanidins as the Main Component of Chinese Hawthorn Fruit Procyanidins, as the second most abundant group of natural phenolics after lignins, are widespread throughout the plant kingdom where they display multiple biochemical properties, mainly involving interactions with proteins, the chelation of metals and antioxidant activity, which are the basis of their various protective functions for plants [32,33,34].
Procyanidins are a class of proanthocyanidins consisting primarily of epicatechin as the flavan-3-ol units or catechin. Epicatechin (A, Figure 3) predominates in fruits of Chinese hawthorn. The content of epicatechin in the fruits analysed varied from 0.9–11.7 mg/g DM. Most samples contained between 2 and 6 mg/g DM of epicatechin, but several samples had extremely high levels of the compound, especially “Shandongdajinxing” of C. pinnatifidavar. major (11.7 mg/g DM) [7,25]. Svedstrom et al. also identified catechin in fruits of Crataegus spp. in monomer form and as a constituent unit of oligomeric and polymeric procyanidins . On the other hand, catechin has not been identified in Chinese hawthorn fruits [10,25]. For procyanidins of each degree of polymerization, several isomers may exist. In Chinese hawthorn fruits, the yields of procyanidins monomer, dimer, trimer, tetramer and pentamer were 50.5%, 30.3%, 23%, 14.6% and 12.5%, respectively
The antioxidant and anti-inflammatory bioassay-guided fractionation of the extract of hawthorn seeds has led to the isolation of eight new lignans, hawthornnins A–H (1–8), and seven known analogues (9–15). Their structures were elucidated by spectroscopic techniques, including 1D and 2D NMR and CD spectra. The radical-scavenging effects of all isolated compounds were investigated. 1–6 and 8 showed moderate activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH), whereas 1–6 and 14 displayed good 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radical-scavenging activities that were even more potent than that of trolox. In addition, all isolates were evaluated for their anti-inflammatory activities by detecting the nitric oxide (NO) and tumor necrosis factor α (TNF-α) production by the LPS-induced murine macrophage cell line RAW264.7, and compounds 1–7, 13, and 14 exhibited potent inhibition of NO and TNF-α production https://pubs.acs.org/doi/abs/10.1021/acs.jafc.5b02835 – reword
Constituents Explained: Mostly Hawthorne most active constituents are cholines, chlorogenic acids, caffeinic acids, and ascorbic acids
This is a thorny shrub, or small tree.
It is a spiny shrub growing in its native state in an area of northern Europe, stretching from Northern Italy to Southern France, and from England east to Latvia. It grows in wooded temperate climate areas (Leung and Foster, 1996). Budavari (1996) mentions that it is now naturalized for garden use in part of North America. Plants for use in Phytomedicine come from both European (Bulgaria, Romania, Albania, Poland) (Wichtl and Bisset, 1994) and former Yugoslavia. and United Kingdom countries (BHP, 1996).
There is a long history of safe use, especially with evidence of benefits to the heart and cardiovascular system, with its edible berries (fruits) dating back to Dioscorides, the first century Greek herbalist, supported by Paracelsus (1493-1541), the Swiss physician (Weihmayr and Ernst, 1996). As such, it becomes one of the oldest known plants to be included in medicine in Europe, although Anschutz (1900); Hobbs and Foster, (1990) are of the opinion that it was not used for cardiovascular diseases, including heart issues before the nineteenth century.
It has sometimes been called the emblem of hope. The stem is hard wood. The gray coloured bark is smooth. As the tree gets older it develops vertical ridges. The branches are thorny. The thorns which grow from the branch or the trunk are usually 1-3cm long.
The leaf, which grows in a spiral pattern is normally wider than it is long. The leaf is small, shiny with toothed leaves that are dark green on top and bluish-green underneath. The flowers are white and grow in groups. The flowers grow in terminal corymbs.
The berry-like fruit, which is structurally a pome, is sometimes called a “haw” and has 2-3 seeds. It is a scarlet red colour on the outside, and has a yellowish pulp on the inside. It contains 1-5 pyrenes, which are similar to the “stones” of plums and peaches etc., which are in the same subfamily.
Birds commonly feed on the fruit and distribute the seeds in their dropping.
Many hybrids have been cultivated for use as an ornamental shrub. Commonly it is used as a hedge plant.
The sturdiness of the wood has seen it being used for tools and fences.
The leaves are often used in salads.
A cardiovascular herb which has been traditionally considered by herbalists to the king of herbs for the heart.
A fantastic heart food and cardiac tonic. coronary circulation, coronary complications and weak heart, heart and circulatory disturbances, hypotension, and arteriosclerosis
It may help slow the heart rate, improve oxygen uptake, and increase the pumping efficiency. It seems to stimulate or slow the heart depending on what is needed. Commonly used in cases of palpitations. It has been used for heart weakness and angina pectoris.
At one time the berries were the plant part primarily used, now more people are appreciating the medicinal use of the leaves and flowers.
It seems to be used in cases of both high and low blood pressure, arteriosclerosis and angina. Its also been used for nerves and an ability to relax to get to sleep.1
The main student of the father of American Herbalist Dr Richard Schulze claims he fixes his inherited heart deformity with this herb, in conjunction with lifestyle change.
An irish Dr Green, is known to have used it secretly, for many patients with heart ailments, until his death in 1894, after which it was found that his remedy was a preperation of hawthorn berries.
Generally most herbal practitioners feel that Hawthorn can act in a synergistic manner with digitalis glycosides and beta-blockers.
Crataegus laevigata is a medicinal plant most commonly used for the treatment of heart failure and psychosomatic disorders. Based on previous experimental findings, this double-blind placebo-controlled study was aimed at finding beneficial effects of C. laevigata on biomarkers of coronary heart disease (CHD).
The study included 49 diabetic subjects with chronic CHD who were randomly assigned to the treatment for 6 months with either a micronized flower and leaf preparation of C. laevigata (400 mg three times a day) or a matching placebo.
Blood cell count, lipid profile, C-reactive protein, neutrophil elastase (NE) and malondialdehyde were analyzed in plasma at baseline, at one month and six months. The main results were that NE decreased in the C. laevigata group compared to the placebo group.
In the C. laevigata group, baseline figures (median and interquartile range) were 35.8 (4.5) and in the placebo group 31 (5.9).
At the end of the study, values were 33.2 (4.7) ng/ml and 36.7 (2.2) ng/ml, respectively. C. laevigata, added to statins, decreased LDL cholesterol (LDL-C) (mean±SD) from 105±28.5 mg/dl at baseline to 92.7±25.1 mg/dl at 6 months and non-HDL cholesterol from 131±37.5 mg/dl to 119.6±33 mg/dl.
Differences between the groups did not reach statistical significance at 6 months. No significant changes were observed in the rest of parameters. In conclusion, C. laevigata decreased NE and showed a trend to lower LDL-C compared to placebo as add-on-treatment for diabetic subjects with chronic CHD.
Hawthorn (Crataegus laevigata) leaves, flowers and berries are used by herbal practitioners in the UK to treat hypertension in conjunction with prescribed drugs. A randomised controlled trial investigated the effects of hawthorn for hypertension in patients with type 2 diabetes taking prescribed drugs.
Patients with type 2 diabetes were randomised to daily 1200 mg hawthorn extract or placebo for 16 weeks. At baseline and outcome a wellbeing questionnaire was completed and blood pressure and fasting blood samples taken. A food frequency questionnaire estimated nutrient intake.
Hypotensive drugs were used by 71% of the study population with a mean intake of 4.4 hypoglycaemic and/or hypotensive drugs. Fat intake was lower and sugar intake higher than recommendations, and low micronutrient intake was prevalent.
There was a significant group difference in mean diastolic blood pressure reductions: the hawthorn group showed greater reductions than the placebo group. There was no group difference in systolic blood pressure reduction from baseline.
Although mean fat intake met current recommendations, mean sugar intake was higher and there were indications of potential multiple micronutrient deficiencies. No herb-drug interaction was found and minor health complaints were reduced from baseline in both groups.
This is the first randomised controlled trial to demonstrate a hypotensive effect of hawthorn in patients with diabetes taking medication.https://www.liebertpub.com/doi/abs/10.1089/jmf.2012.2672
Protection from myocardial damage
The attenuation of the LDH release by crataegus pretreatment suggests a preservation of the cell membrane and a protection from myocardial damage.https://europepmc.org/abstract/med/8821513
Hawthorn contains a valuable component of (-)-epicatechin and related proanthocyanidins. These are cardio protective as they have great free radical scavenging properties.https://www.thieme-connect.com/products/ejournals/html/10.1055/s-2002-32547
When exposed to drought and stress from cold, Crataegus increases its levels of (−)-epicatechin and hyperoside in both species. This also results in an increase of antioxidants and secondary metabolites in the leaves.
Enhanced myocardial contractibility (Ammon and Kau11994b) associated with mechanisms including inhibition of c-AMP and c-GMP phosphodiesterases (Weihmayr and Ernst 1996) was demonstrated on water or alcoholic extract heart preparations. Out of flavonoid-rich fractions, and isolated flavonoids such as vitexin-2′ -O-rhamnoside, luteolin-7 -O-glucoside, rutin, quercetin (Ammon and Kaul 1994b; Schussler et al. 1995) flavanolic fractions, such as total, polymeric and more particularly oligomeric proanthocyanidins were found to exert an important influence. Loew (1997), showed a neutral or moderately positive increase in heart rate (Blesken, 1992) with atrio-ventricular conductibility enhanced (Weihmayr and Ernst 1996). https://link.springer.com/chapter/10.1007/978-3-662-08616-2_3
Hawthorn & hair loss
The C. pinnatifida extract promoted hair growth by inducing anagen phase in mice in telogen, reflected by color of skin, thickness of hair shaft, and density of hair. The ratio of anagento telogen was determined by shape of hair follicles in vertically sectioned slide and increased by oral administration of C. pinnatifida extract. The number and the size of hair follicles were also enlarged, indicating anagen phase induction. The proliferation of human dermal papilla cells (hDPC) was accelerated by addition of C. pinnatifida extract, which activated the signaling of mitogen‐activated protein kinases (Erk, p‐38, and JNK) and Akt. Moreover, the ratio of Bcl‐2/Bax as the determinant of cell fate was also raised in skin. These results suggest that the C. pinnatifida extract promotes hair growth by inducing anagen phase, which might be mediated by the activation of cellular signalings that enhance the survival of cultured hDPC and the increase of the ratio of Bcl‐2 to Bax that protects cells against cell death.
Hair growth with increased density, in mice,has been promoted with the C. pinnatifida extract, by inducement of the anagen phase, possibly associated with the cellular signalings being activated, that increase the ratio of Bcl‐2 to Bax that protects cells against cell death.and to aid survival of cultured hDPC.
Hawthorn & weight loss
Lowered lipid levels, with combined Hawthorn and simvastatin use were shown in
hyperlipidemic albino rats.
Hawthorn & arrthymia
Wistar rats that had arrhythmia induced by digoxin, benefited from Crataegus oxyacantha alcoholic extract, which may have similar effect in humans, although the potential hypotensive effect would need to be taken into consideration.
Crataegus extract is suggest to have certain antiarrhythmic properties.
Hawthorn, anti inflammatory & anti oxidant
Hawthorn is thought to drive blood to the liver avoiding necrosis (cell death).
Hawthorn & lowering cholesterol
Studies showing a reduction in blood cholesterol, induced by Chinese hawthorn fruit, added to the already known benefits from anti-oxidant, anti-tumour and anti-inflammatory actions.
Hawthorn & low toxicity
C. pinnatifida has been found to have favourable therapeutic effects on the digestive, cardiovascular, and endocrine systems, as well as pathogenic microorganisms, and is widely used as pharmacological therapy due to its low toxicity levels..
Hawthorn & oligomeric procyandins
In an ischemia-reperfusion model in rats, oligomeric procyandins [OPC]: 18.75%) were demonstrated.
Hawthorn, hypertension & cardiovascular system
There was a prevention of L‐NAME‐induced hypertension in rats with cardiovascular benefits associated with the hyperoside fraction of C. tanacetifolia.
Polyphenols & anti bacterial properties
There were strong antioxidant and antibacterial activities due to high levels of polyphenols in C. elbursensis pulp and seed extract
Pulp and seed extract of C. elbursensis fruit, showed high bacteriostatic and bactericidal activity against four food borne and food spoilage bacteria.
Cardio protection on blood deprived heart
There is a cardioprotective effect, induced by Crataegus extract (0.05%), on the ischemic-reperfused heart.
6 uses of hawthorn
Hawthorn is valuable to support treatment of Hypertension, Angina, Arrhythmias, Congestive Heart Failure (NYHA class I & II) and Peripheral vascular disorders along with being an Antioxidant and lipid regulating agent.
Dalli E, Colomer E, Tormos MC, Cosin-Sales J, Milara J, Esteban E, Saez G. “Crataegus Laevigata Decreases Neutrophil Elastase And Has Hypolipidemic Effect: A Randomized, Double-Blind, Placebo-Controlled Trial.” 2011 June http://www.ncbi.nlm.nih.gov/pubmed/21242072
Walker AF, Marakis G, Simpson E, Hope JL, Robinson PA, Hassanein M, Simpson HC. “Hypotensive Effects Of Hawthorn For Patients With Diabetes Taking Prescription Drugs: A Randomised, Controlled Trial.” 2006 June http://www.ncbi.nlm.nih.gov/pubmed/16762125