Hawthorn Berry (Crataegus) | Supplementopedia

Overview

Hawthorn (genus Crataegus) is a deciduous shrub whose berries, leaves, and flowers have been used for centuries in traditional medicine. Modern research focuses on the fruit (hawthorn berry) as a botanical supplement that primarily supports cardiovascular health by improving cardiac function and vascular tone.

Benefits

Cardiovascular support: Randomized trials show standardized hawthorn extracts improve left‑ventricular ejection fraction and reduce symptoms of chronic heart failure (NYHA class II–III) (e.g., 300 mg twice daily of a 2% flavonoid/18% pro‑cyanidin extract).
Blood‑pressure regulation: Acute studies report modest reductions in systolic/diastolic pressure (‑4 to ‑7 mm Hg) via endothelial nitric‑oxide (NO) enhancement.
Antioxidant activity: High‑flavonoid extracts scavenge reactive oxygen species, protecting endothelial cells from oxidative stress in vitro and in animal models.
Anti‑inflammatory: Flavonoid‑rich extracts reduce circulating C‑reactive protein (CRP) and TNF‑α in mild inflammatory conditions.
Metabolic support: Small trials suggest modest improvements in fasting glucose and lipid profiles (↑ HDL, ↓ LDL) when combined with diet.
Cognitive‑vascular link: By enhancing cerebral blood flow, hawthorn may modestly improve attention and memory in older adults, though data are limited.

How It Works

Antioxidant Effects: Hawthorn’s bioactivity derives largely from flavonoids (e.g., quercetin, vitexin, hyperoside) and oligomeric pro‑cyanidins. These compounds exert antioxidant effects by chelating metal ions and up-regulating Nrf2‑driven antioxidant enzymes (SOD, catalase).
NO-mediated Vasodilation: Flavonoids inhibit phosphodiesterase‑5, increasing cGMP, while pro‑cyanidins stimulate endothelial nitric‑oxide synthase (eNOS) phosphorylation via the PI3K/Akt pathway, enhancing NO‑mediated vasodilation.
Calcium Channel Blocking: Hawthorn flavonoids block L‑type calcium channels, reducing myocardial contractility and heart rate, akin to a mild calcium‑channel blocker.
Combined Effects: The combined NO‑enhancement and calcium‑blocking actions improve coronary blood flow and reduce after-load.
Anti-inflammatory Effects: Flavonoids modulate the NF‑κB pathway, dampening inflammatory cytokine production.
Mitochondrial Function: Flavonoids improve mitochondrial function, contributing to the observed cardioprotective and metabolic effects.

Dosage

Standardized extract (2 % flavonoids / 18 % oligomeric pro‑cyanidins): 250–500 mg taken 1–2 times daily (total 500–1000 mg) for chronic heart‑failure support.
Whole‑berry powder: 1–3 g daily, divided with meals, often used for general cardiovascular wellness.
Acute blood‑pressure studies: 500 mg of extract 30 min before a meal, once daily, for up to 4 weeks.
Special populations: Elderly or patients on cardiac medications may start at the low end (250 mg) and titrate upward under clinician supervision.
Timing: Most data support administration with food to improve absorption of flavonoids; avoid taking with high‑dose iron or calcium supplements that may reduce bioavailability.

Safety & Side Effects

Hawthorn is generally well‑tolerated.
Side Effects: Reported mild side effects include gastrointestinal discomfort (nausea, diarrhea) and occasional dizziness.
Contraindications:
- Patients on digoxin (may increase serum digoxin by 20–30 %)
- Those on beta‑blockers or calcium‑channel blockers (potential additive negative‑chronotropic effects).
Drug interactions: digoxin, anticoagulants (warfarin, DOACs), antihypertensives, and anti‑arrhythmics.
Pregnancy/lactation: Insufficient data; advisable to avoid.
Children: Use only under medical supervision; pediatric doses are not well-established.
Individuals with severe hypotension, advanced atrial fibrillation, or recent myocardial infarction should consult a healthcare provider before use.

Chemistry

Flavonoids: (quercetin‑3‑O‑glucoside, vitexin, hyperoside) – C₁₅H₁₀O₇ (quercetin) – molecular weight 302 g/mol; multiple hydroxyl groups confer high antioxidant capacity.
Pro‑cyanidins: (dimers B1–B8) – oligomeric flavan‑3‑ols with molecular formulas C₃₀H₂₆O₁₃ (B2) – 578 g/mol; contain catechin units linked via C4–C8 bonds.
Organic acids: (malic, citric, and hawthorn‑specific triterpenes—e.g., maslinic acid, C₃₀H₄₈O₃; MW 456 g/mol) contribute to anti‑inflammatory effects.
Molecular Properties: These molecules are poly‑hydroxylated, enabling strong free‑radical scavenging and interaction with protein kinases.
Standardization: The extract’s standardization is expressed as % flavonoids (by HPLC) and % pro‑cyanidins (by DMAC method).

Sources & Quality

Hawthorn berries are harvested primarily in Europe (Germany, Italy), North America (USA, Canada), and parts of China where C. monogyna and C. laevigata dominate.
Harvest: Harvest occurs in late summer/early autumn when flavonoid content peaks.
Extraction: Extraction typically uses 70 % ethanol or aqueous‑ethanol mixtures under controlled temperature (50–60 °C) to preserve flavonoids and pro‑cyanidins; subsequent spray‑drying yields a powdered extract.
Quality Control:
- HPLC quantification of quercetin‑derivatives (≥2 % total flavonoids)
- DMAC assay for oligomeric pro‑cyanidins (≥18 %).
Manufacturing Standards: Good Manufacturing Practice (GMP) facilities test for heavy metals, pesticides, and microbial load.
Preferred Sources: Standardized extracts from reputable botanical suppliers (e.g., European Pharmacopeia‑certified or USDA‑certified organic) are preferred for consistency and safety.