Exploring Pharmacological Action of Crataegus Oxyacantha Mother Tincture

Dr Akash C Chudasama

The Frontier of Cardiovascular Diseases: Exploring Pharmacological Action of Homoeopathic remedy Crataegus Oxyacantha Mother Tincture.

Abstract:
Crataegus oxyacantha is one of the effective remedy for cardiovascular disease. This article provides pharmacological action of crataegus and how chemical composition of crataegus is act in human body. Crataegus mother tincture use in disease such as hypertension, valvular disease, arrythmias, atherosclerosis and cardiomyopathy. This article explores action of chemical composition in cardiovascular system.

Key words: Crataegus oxyacantha, hawthorn, flavonoids, hypertension, arrythmias, atherosclerosis, heart tonic.

Introduction:
Crataegus oxyacantha linn., commonly known as hawthorn, is one of the most widely used heart tonic. Hawthorn berries support the heart due to the high content of bioflavonoids. It increases the body’s ability to utilize oxygen, and the heart’s ability to utilise calcium. It dilates peripheral blood vessels, increases metabolism in the heart muscle, dilates coronary vessels and improves blood supply to the heart and thereby help in treating heart disease and mitigating symptoms in early stage of heart failure.

Accepted scientific plant name: crataegus laevigata ⁽¹⁾

Synonyms: crataegus oxyacantha ⁽¹⁾

Classification:

• Class: dicotyledons
• Order: rosales
• Family: rosaceae
• Genus: crataegus⁽¹⁾

Chemical composition:

1. vitamin c.
2. flavonoids: quercetin, hyperoside, rutin, flavonoglycosyls, vitexin-4′-rhamnoside.
3. oligomeric procyanidins (opc) – epicatechol.
4. anthocyanidins and proanthocyanidins (biflavans)
5. saponins and tannins.
6. cratetegin (most prevelant in flowers > leaves > berries).
7. other chemical constituents:

• Cardiotonic amines: phenylethylamine, tyramine, isobutylamine, omethoxy phenylethylamine
• Choline and acetylcholine
• Purine derivatives: adenosine, adenine, guanine, caffeic acid
• Amygdalin
• Pectin
• Triterpene acids: ursolic acid, oleonic acid, crategolic acid. From article⁽²⁾

Action of chemical composition of Crataegus oxyacantha on heart:

1. Quercitine – quercetin is one of the most common flavonoids. More and more studies have found that quercetin has great potential utilization value in cardiovascular diseases, such as antioxidant, antiplatelet aggregation, antibacterial, cholesterol lowering, endothelial cell protection⁽³⁾
2. Hyperoside – hyperoside is a flavonoid, showing significant anti-inflammatory effects. It is effective in sepsis associated dysfunction of heart.⁽⁴⁾
3. Rutine – rutine prevents cardiac hypertrophy by suppressing extracellular signal regulated kinase, Jun N – terminal kinase and mitogen activated protein kinase pathway. Rutin provides cardioprotective by activating silent mating type information regulation 2 homologue 1 (sirt1) /nuclear factor erythroid 2–related factor 2 (nrf2) pathway. Rutin attenuates cardiac fibrosis by decreasing growth factors and matrix matalloproteinases (mmp) expressions. Rutin reduces pathological cardiac remodeling.⁽⁵⁾
4. Flavonoids – flavonoid-rich flavonoids may reduce the risk of the hyper-activation of platelets, the progression of cardio vascular diseases, pain, and thrombosis. Flavonoids also reduce the risk of atherosclerosis and atherothrombotic diseases.⁽⁶⁾
5. Vitexin – vitexin exerts protective effects including anti-cancer, anti-oxidant, anti-inflammatory, anti-hypertensive and anti-hypoxia/ischemic.⁽⁷⁾
6. Glycosides – it works by inhibiting cell membrane from pumping sodium out. This increases the amount of sodium that stays in cells. This allows more calcium to build in the cells. This also slow down electrical signals in the atrioventricular node.⁽⁸⁾
7. Tannin – The tannins are reported to have a beneficial effect in certain diseases such as coronary artery disease, restrictive cardiomyopathy, dilated cardiomyopathy, endothelial dysfunction, and cardiac hypertrophy.⁽⁹⁾

Cardiovascular effects:
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. ⁽²⁾

Crataegus may improve coronary artery blood flow and the contractions of the heart muscle, hence used widely in cardiovascular disorders like arrhythmia, myocardial infarction, congestive heart failure. ⁽¹⁰⁾

Crataegus extracts also prevents elimination of plasma lipids such as total cholesterol, triglycerides and low density lipoprotein and very low density lipoprotein fractions. ⁽¹⁰⁾

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. Surprisingly, hawthorn has the ability to regulate both low and high blood pressure. With the bioflavanoids 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. ⁽²⁾

One mechanism, commonly proposed for its cardioactive effect is its ability to inhibit the enzyme phosphodiesterase which ultimately results in an increase in intracellular cyclic nucleotides and a subsequent positive inotropic effect. Interestingly, catechin, the flavonoid vitexin and flavonol kaempferol from hawthorn were observed to be structurally similar to papaverine and theophylline, the two chemical agents known to inhibit phosphodiesterase. Another constituent of hawthorn, ursolic acid has also been reported to interact with the digitaloid binding site for Na+ /k+ Atpase. ⁽²⁾

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. ⁽²⁾

Crataegus is used widely in cardiology. The standardised extract of fresh berries of crataegus oxyacantha have shown potent effect in patients with cardiac failure NYHA class ii. ⁽¹⁰⁾

Hawthorn has been shown to exhibit antioxidant activity associated with its flavanoid and procyanidin content. The most significant antioxidant activity was observed using an extract of fresh, young leaves followed by fresh floral buds and dried flowers. Hawthorn reportedly has the ability to increase intracellular vitamin c and has a protective effect on oxidative processes. The free radical scavenging activity contributes to hawthorn’s cardio-protective effect after ischemia and this property is primarily correlated with the oligomeric procyanidins. ⁽²⁾

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, not only this, crataegus also have significant collagen stabilising action by affecting collagen metabolism. It cross links collagen fibres to reinforce the collagen matrix of connective tissues. Mild to moderate sedative effect has been demonstrated in humans and animal studies with hawthorn constituents and opc’s are reported to be partially responsible for this effect. In a nut shell, hawthorn’s flavons, by inhibiting phosphodiesterase, have a positive effect on myocardium’s calcium metabolism resulting in an increase in contractile power (positive inotropic effect) and promoting normal rhythm. It does inhibit angiotensin converting enzyme (ACE). Its free radical scavenging capacity further protects myocardium particularly during ischemic situations. Hawthorn’s anti-inflammatory and collagen stabilizing properties are additional advantages of its therapeutic application. ⁽²⁾

A study had been done to check this activity experimentally which involves the use of a homeopathic crataegus preparation cralonin. In this study the efficacy of the homeopathic crataegus preparation for non-inferiority to standard treatment for mild cardiac insufficiency was compared. Multicentre non-randomised cohort study was conducted in patients aged 50-75 years in new york heart association class ii. Patients received cralonin (ns110) or ace inhibitor diuretics (ns102) for eight weeks. To adjust for confounding by baseline factors, populations were stratified according to propensity score. After adjusting, there were no statistically significant differences between treatment groups. The crataegus-based preparation cralonin is non-inferior to usual ace inhibitor diuretics treatment for mild cardiac insufficiency on all parameters except blood pressure reduction. ⁽¹⁰⁾

Currently, evidence is accumulating from various in vivo and in vitro studies that hawthorn extracts exert a wide range of cardiovascular pharmacological properties, including antioxidant activity, positive inotropic effect, anti-inflammatory effect, anticardiac remodeling effect, antiplatelet aggregation effect, vasodilating effect, endothelial protective effect, reduction of smooth muscle cell migration and proliferation, protective effect against ischemia/reperfusion injury, antiarrhythmic effect, lipid-lowering effect and decrease of arterial blood pressure effect. On the other hand, reviews of placebo-controlled trials have reported both subjective and objective improvement in patients with mild forms of heart failure (NYHA I–III), hypertension, and hyperlipidemia. ⁽¹¹⁾

Cratagaeous Oxyacantha from Boericke Materia Medica

• Produces giddiness, lowered pulse, and air hunger and reduction in blood-pressure.
• Acts on muscle of heart, and is a heart tonic.
• No influence on the endocardium.
• Failing compensation. Irregularity of heart.
• Insomnia of aortic sufferers; anaemia; oedema; cutaneous chilliness.
• High arterial tension. Is a sedative in cross, irritable patients with cardiac symptoms.
• Chronic heart disease, with extreme weakness. Very feeble and irregular
• Heart action. General anasarca.
• Very nervous, with pain in back of head and neck. Collapse of typhoid. Haemorrhage from bowels.
• Cold extremities, pallor; irregular pulse and breathing. Painful sensation of
• Pressure in left side of chest below the clavicle. Dyspepsia and nervous prostration, with heart failure. In the beginning of heart mischief after rheumatism.
• Said to have a solvent power upon crustaceous and calcareous deposits in arteries.
• Extreme dyspnoea on least exertion, without much increase of pulse.
• Heart dilated; first sound weak.
• Pulse accelerated, irregular, feeble, intermittent.
• Valvular murmurs, angina pectoris.
• Sustains heart in infectious diseases.⁽¹²⁾

Conclusion:
In conclusion we see that crataegus oxyacantha mother tincture is effective in cardiovascular disease. We can successfully treat cardiac disease from above pharmacological action of crataegus medicine. Pharmacological and chemical compound studies of this mother tincture are very effective to our homoeopathic fraternity.

References

1. United States Department of Agriculture’s GRIN (Germplasm Resources Information Network) database. botanic gardens conservation internationl. [Online]. [cited 1997 march. Available from: https://tools.bgci.org/plant_details.php?plantID=134799.
2. VERMA SK,JV,VDAKR. CRATAEGUS OXYACANTHA – A CARDIOPROTECTIVE HERB. Journal of Herbal Medicine and Toxicology. 2007 January; 1(0973 – 4643): 65 – 71.
3. Weiwei Zhang YZFYMD=YR. national library of medicine. [Online].; 2023 [cited 2024 may 30. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10694509/#:~:text=Quercetin%20is%20one%20of%20the,%2C%20endothelial%20cell%20protection%2C%20etc.
4. Jun Zhang YLLL. national library of medicine. [Online].; 2021 [cited 2024 may 30. Available from: https://pubmed.ncbi.nlm.nih.gov/34311527/.
5. hawa nordin siti jjayayk. sciencedirect.com. [Online].; 2020 [cited 2024 may 30. Available from: https://www.sciencedirect.com/science/article/pii/S1756464619305304#:~:text=Rutin%20prevents%20cardiac%20hypertrophy%20by,Rutin%20reduces%20pathological%20cardiac%20remodeling.
6. Zhao Chen1 SLZ. ANNALS OF PALLIATIVE MEDICONE. [Online].; 2021 [cited 2024 may 30. Available from: https://apm.amegroups.org/article/view/73669/html#:~:text=Flavonoid%2Drich%20flavonoids%20may%20reduce,and%20atherothrombotic%20diseases%20(74).
7. Juturu V. sciencedirect.com. [Online].; 2014 [cited 2024 may 30. Available from: https://www.sciencedirect.com/topics/neuroscience/vitexin#:~:text=Vitexin%20exerts%20protective%20effects%20including,IL%2D1%CE%B2%2Dtreated%20chondrocytes.
8. cleveland clinic. my.clevelandclinic.org. [Online].; 2022 [cited 2024 may 30. Available from: https://my.clevelandclinic.org/health/treatments/24512-cardiac-glycosides.
9. Gandhar Pradhan YAK. link.springer.com. [Online].; 2023 [cited 2024 may 30. Available from: https://link.springer.com/referenceworkentry/10.1007/978-3-031-30037-0_12-1#:~:text=A%20few%20of%20the%20tannins,endothelial%20dysfunction%2C%20and%20cardiac%20hypertrophy.
10. Dinesh Kumar VAZqABAKNP. The genus Crataegus: chemical and pharmacological perspectives. Brazilian Journal of Pharmacognosy. 2012 august; 22(0102 – 695X): 1187 – 1200.
11. Jie Wang XXBF. national library of medicine. [Online].; 2013 [cited 2024 may 30. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3891531/.
12. Boericke W. BOERICKE’S New Manual of Homoeopathic MATERIA MEDICA With REPERTORY. Third Revised & Augmented Edition Based on Ninth Edition ed. Noida: B. JAIN PUBLISHERS (P) LTD.; 2021.

Dr Akash C Chudasama
PG Scholar Part 1 (Practice of Medicine) C.D. Pachchigar College of Homoeopathic Medicine and Hospital, Surat, Gujarat.
Email : chudasamaakash65@gmail.com