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Clincal Studies
References
Hawthorn is a cardiac tonic, used for cardiovascular conditions such as congestive heart failure (CHF), coronary circulation problems and arrhythmias. It is also used to increase cardiac output reduced by hypertension or pulmonary disease, to treat both hypotension (low pressure) and hypertension (high blood pressure), atherosclerosis, hyperlipidemia and Buerger's disease. Hawthorn is also used as an antispasmodic, astringent and diuretic.
The constituents responsible for the pharmacological effects of hawthorn preparations include flavonoids and procyanidins. Other active compounds are vitexin, rutin and hyperoside. Hawthorn preparations act on the heart muscle by increasing force of contraction, reducing peripheral vascular resistance associated with hypertension (high blood pressure), reducing oxygen consumption and increasing nerve conductivity. Flavonoids and oligomeric procyanidins (OPCs) increase blood flow in the coronary arteries due to vasodilation.
Hawthorn has also been reported to reduce lipid levels. It also has antibacterial, spasmolytic and pain relieving effects.
Published Clinical Studiesclin
1
Phenolic constituents and antioxidant capacities of Crataegus monogyna (Hawthorn) callus extracts.
Bahorun T, Aumjaud E, Ramphul H, Rycha M, Luximon-Ramma A, Trotin F, Aruoma OI.
Department of Biological Sciences, Faculty of Science, University of Mauritius, Reduit. tbahorun@uom.ac.mu
Crataegus (Hawthorn) has long been used as a folk medicine and is widely utilized in pharmaceutical preparations mainly because of its neuro- and cardiosedative actions and its low toxicity. The pharmacological effects of Crataegus have mainly been attributed to the polyphenolic contents. In this study, the production of polyphenols by ten-year-old Crataegus monogyna calli was studied in relation to growth variation and antioxidant capacity within a subculture period. Assays based on the Trolox equivalent antioxidant capacity (TEAC), ferric reducing antioxidant power (FRAP) and stability in oil-in-water emulsion were used to characterize the antioxidant actions of the callus cultures. High TEAC (3.66 micromol/g dry weight) and FRAP (208.19 micromol Fe2+/g dry weight) values were observed when maximal growth was reached(days 30-35), and this seemed to be influenced by optimum total phenol (47.40 mg/g dry weight), proanthocyanidin (20.81 mg/g dry weight), flavonoid (7.01 mg/g dry weight), anthocyanin (6.18 mg/g dry weight), (-)-epicatechin (1.77 mgl/g dry weight), procyanidin B2 (3.97 mg/g dry weight), and chlorogenic acid (1.11 mg/g dry weight) production during that period. The TEAC values were strongly associated with total flavonoids and to a lesser extent with total phenols, anthocyanins and total proanthocyanidins. The FRAP antioxidant values correlated to total phenols, proanthocyanidins and flavonoids, respectively. The polyphenolic rich calli were as effective as butylated hydroxytoluene (BHT) in preventing hydroperoxide and conjugated diene formation in a 30% oil-in-water emulsion prepared with stripped sunflower oil, during 7days storage at 30 degrees C. Crataegus monogyna cell culture represents an important alternative source for natural antioxidants.
PMID: 12866623 [PubMed - indexed for MEDLINE]
2
A randomised double blind placebo controlled clinical trial of a standardised extract of fresh Crataegus berries (Crataegisan) in the treatment of patients with congestive heart failure NYHA II.
Degenring FH, Suter A, Weber M, Saller R.
Bioforce AG, Roggwil, Switzerland.
A placebo controlled, randomised, parallel group, multicentre trial conducted in accordance with the guidelines of Good Clinical Practice (GCP) shows the efficacy and safety of a standardised extract of fresh berries of Crataegus oxyacantha L. and monogyna Jacq. (Crataegisan) in patients with cardiac failure NYHA class II. A total of 143 patients (72 men, 71 women, mean age of 64.8 (8.0 years) were recruited and treated with 3 times 30 drops of the extract (n = 69) or placebo (n = 74) for 8 weeks. The primary variable for the evaluation of efficacy was the change in exercise tolerance determined with bicycle exercise testing, secondary variables included the blood pressure-heart rate product (BHP). Subjective cardiac symptoms at rest and at higher levels of exertion were assessed by the patient on a categorical rating scale. An overall assessment of efficacy at the final visit was provided by the patient and the investigator. In the ITT population there was a significant increase in exercise tolerance in both groups between visit 1 and visit 3. The difference between the treatment groups was 8.3 watts in favour of the standardised extract of fresh Crataegus berries (p = 0.045). The result is confirmed in the PP population (p = 0.047). Changes in BHP at 50 watts and at comparable maximum load were in favour of Crataegus extract but the results are not statistically significant. The subjective assessment of cardiac symptoms at rest and at higher levels of exertion did not change significantly and the patient and investigator overall assessment of efficacy were similar for the two groups. The medication was well tolerated and had a high level of patient acceptability. The significant improvement, due to the fact that dyspnoea and fatigue do not occur until a significantly higher wattage has been reached in the bicycle exercise testing allows the conclusion that the recruited NYHA II patients may expect an improvement in their heart failure condition under long term therapy with the standardised extract of fresh Crataegus berries.
Publication Types:
PMID: 12833999 [PubMed - indexed for MEDLINE]
Hawthorn.3
Fong HH, Bauman JL.
Program for Collaborative Research in the Pharmaceutical Sciences, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, USA.
Crataegus monogyna Jacq (Lindm), C. laevigata (Poir) DC, or related Crataegus species, collectively known as hawthorn, have been used in the treatment of cardiovascular diseases. Clinical studies have found that standardized extracts show promise as adjunctive agents for the treatment of left ventricular dysfunction. Other trials consistently demonstrate its ability to improve exercise tolerance and symptoms of mild to moderate heart failure. Preliminary evidence indicates that it improves left ventricular performance, as measured by ejection fraction. In order to properly use hawthorn in the treatment of heart failure, a large, controlled, multicenter trial in which mortality serves as the primary endpoint is needed.
Publication Types:
PMID: 12597258 [PubMed - indexed for MEDLINE]
Search for potential angiotensin converting enzyme (ACE)-inhibitors from plants.4
Lacaille-Dubois, Franck U, Wagner H.
Laboratoire de Pharmacognosie, Unite de Molecules d'Interet Biologique, Faculte de Pharmacie, Universite de Bourgogne, Dijon, France. malacd@u-bourgogne.fr
MeOH extracts, fractions and pure substances from Musanga cecropioides, Cecropia species and Crataegus oxyacantha /C. monogyna were screened by using an in vitro bio-assay based on the inhibition of Angiotensin Converting Enzyme (ACE), as measured from the enzymatic cleavage of the chromophore-fluorophore-labelled substrate dansyltriglycine into dansylglycine and diglycine. Phenolic acids showed no significant ACE-inhibition whereas flavonoids and proanthocyanidins demonstrated inhibitory activity at 0.33 mg/ml using this test system.
PMID: 11292239 [PubMed - indexed for MEDLINE]
Procyanidins in crataegus extract evoke endothelium-dependent vasorelaxation in rat aorta.5
Kim SH, Kang KW, Kim KW, Kim ND.
College of Pharmacy, Seoul National University, Korea.
The extract of Crataegus, a mixture of flavonoids and procyanidins extracted from hawthorn, Crataegus oxyacantha, L. and C. monogyna Jacq., relaxed vascular tone or increased production of cyclic GMP in the rat aorta, but flavonoid components of Crataegus extract, hyperoside, rutin and vitexin, did not affect the vascular tone. The aim of the present study was to characterize the endothelium-dependent relaxation elicited by procyanidins fractionated from Crataegus extract in isolated rat aorta. Procyanidins caused endothelium-dependent relaxation which was associated with the production of cyclic GMP. Both responses to these procyanidins were inhibited by methylene blue or N(G)-nitro-L-arginine, but not by indomethacin. Relaxation in response to procyanidins was not affected by atropine, diphenhydramine, [D-Pro2,D-Trp7,9]substance P, propranolol, nifedipine, verapamil and glibenclamide, but were markedly reduced by tetraethylammonium. These findings showed that procyanidins in Crataegus extract may be responsible for the endothelium-dependent nitric oxide-mediated relaxation in isolated rat aorta, possibly via activation of tetraethylammonium-sensitive K+ channels.
PMID: 10901280 [PubMed - indexed for MEDLINE]
6
Inhibition of platelet aggregation and 5-HT release by extracts of Australian plants used traditionally as headache treatments.
Rogers KL, Grice ID, Griffiths LR.
Genomics Research Centre and School of Health Science, Griffith University, PMB 50, GCMC, Gold Coast, Australia.
To identify potential migraine therapeutics, extracts of eighteen plants were screened to detect plant constituents affecting ADP induced platelet aggregation and [14C]5-hydroxytryptamine (5-HT) release. Extracts of the seven plants exhibiting significant inhibition of platelet function were reanalysed in the presence of polyvinyl pyrrolidone (PVP) to remove polyphenolic tannins that precipitate proteins. Two of these extracts no longer exhibited inhibition of platelet activity after removal of tannins. However, extracts of Crataegus monogyna, Ipomoea pes-caprae, Eremophila freelingii, Eremophila longifolia, and Asteromyrtus symphyocarpa still potently inhibited ADP induced human platelet [14C]5-HT release in vitro, with levels ranging from 62 to 95% inhibition. I. pes-caprae, and C. monogyna also caused significant inhibition of ADP induced platelet aggregation. All of these plants have been previously used as traditional headache treatments, except for C. monogyna which is used primarily for protective effects on the cardiovascular system. Further studies elucidating the compounds that are responsible for these anti-platelet effects are needed to determine their exact mechanism of action.
PMID: 10664475 [PubMed - indexed for MEDLINE]
Extracts from Viscum and Crataegus are cytotoxic against larynx cancer cells.7
Departamento Farmacia y Tecnologia Farmaceutica, Facultad de Farmacia, Sevilla, Spain.
The effects of hexanoic extracts of Viscum cruciatum Sieber parasitic on Crataegus monogyna Jacq. (I), Crataegus monogyna Jacq. parasitized with Viscum cruciatum Sieber (II), and Crataegus monogyna Jacq. non-parasitized (III), and of a triterpenes enriched fractions isolated from I, II and III (CFI, CFII, CFIII respectively), on the growth of HEp-2 cells have been evaluated. All the samples demonstrated significant cytotoxic activity against cultured HEp-2 cells, and all of them showed a stronger in vitro activity than 6-mercaptopurine solution used as a positive control. With the hexanoic extracts I, II and III almost similar activity was obtained, but the hexanoic extract I showed comparably better results. Almost complete inhibition was observed with triterpenes-enriched fractions CFI, CFII and CFIII, at the dose 6 micrograms/ml, after 72 h of treatment. The most intense response was obtained with the triterpenes-enriched fraction CFIII (from Crataegus monogyna non-parasitized), where the inhibition was 93%, but the fraction CFI and CFII showed similar inhibition (92% and 83%).
PMID: 9090065 [PubMed - indexed for MEDLINE]
8
The effects of a triterpene fraction isolated from Crataegus monogyna Jacq. on different acute inflammation models in rats and mice. Leucocyte migration and phospholipase A2 inhibition.
Ahumada C, Saenz T, Garcia D, De La Puerta R, Fernandez A, Martinez E.
Departamento de Farmacia, Tecnologia Farmaceutica y Farmacologia, Facultad de Farmacia, Sevilla, Spain.
The plant Crataegus monogyna has action against cardiac insufficiency, angina and arrhythmia. The anti-inflammatory properties of the cycloartenol fraction from this plant have been investigated. Chromatographic fractionation of the hexane extract of Crataegus monogyna Jacq. (Rosaceae) furnished a triterpene fraction containing cycloartenol as the main component (80.87%). The anti-inflammatory activity of the fraction was tested against hind-paw oedema induced by carrageenan in rats. At the highest oral dose (40 mg kg-1) inhibition was 61.5 and 52.5% at 3 and 5 h respectively. In the mouse carrageenan peritonitis test, the triterpene fraction given orally inhibited peritoneal leucocyte infiltration (41.9, 64.7 and 89.4% at 10, 20 and 40 mg kg-1, respectively). The fraction also showed weak inhibition of phospholipase A2 (PLA2) in-vitro. These results suggest that the fraction containing cycloartenol as the main component exerts an important anti-inflammatory action in-vivo by reducing the oedema.
PMID: 9231356 [PubMed - indexed for MEDLINE]
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