Sulforaphane: benefits, dosage, contraindications

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Glucosinolates, present in all cruciferous vegetables, transform into isothiocyanates when they encounter a specific enzyme: myrosinase. This process, called hydrolysis, is triggered when the plant is processed: chewing, cutting, or digestion. Glucoraphanin is a glucosinolate precursor to sulforaphane, an active component directly in the body. Sulforaphane is thus a sulfur-containing isothiocyanate produced by the reaction of glucoraphanin with the enzyme myrosinase. Sulforaphane is present in particularly high quantities in broccoli sprouts, and other cruciferous vegetables like cabbage, cauliflower, kale, radish, as well as mustard, horseradish, arugula, and many others. However, cooking vegetables destroys the naturally occurring enzyme myrosinase, which can reduce the bioavailability of sulforaphane in these foods. Discovered in the 1990s, sulforaphane quickly attracted scientific interest for its numerous health-promoting properties. Studies have linked it to antioxidant, anti-inflammatory, and anticancer effects, as well as potential benefits in preventing cardiovascular, metabolic, and neurodegenerative diseases. Its mechanism of action is primarily based on the activation of the Nrf2 pathway, a key regulator of the body's antioxidant defenses. Through this pathway, sulforaphane increases the production of phase II detoxifying enzymes, which neutralize toxic substances and protect cells from oxidative and inflammatory damage. This mechanism makes it a promising candidate for preventing and treating various chronic pathologies. Studies have demonstrated that sulforaphane, through its action on the Nrf2 pathway, inhibits the proliferation of tumor cells. Clinically, it is valued for its role in cancer prevention, notably prostate cancer.

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Phytosubstances


Indications

Rating methodology

EFSA approval.

Several clinical trials (> 2) randomized controlled with double blind, including a significant number of patients (>100) with consistently positive outcomes for the indication.
Several clinical trials (> 2) randomized controlled with double blind, and including a significant number of patients (>100) with positive outcomes for the indication.
One or more randomized studies or multiple cohorts or epidemiological studies with positive outcomes for the indication.
Clinical studies exist but are uncontrolled, with conclusions that may be positive or contradictory.
Lack of clinical studies to date that can demonstrate the indication.


Prostate cancer
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PSA (Prostate-Specific Antigen) is a protein produced by prostate cells. Its measurement in blood is commonly used as a biological marker to assess prostate health. An abnormal elevation in PSA levels can indicate inflammation, benign enlargement, or, in some cases, prostate cancer. A study revealed that supplementation with 20 mg of sulforaphane (Prostaphane) three times a day for six months slows the increase in PSA levels, extending the PSA doubling time by 86% compared to placebo. Another research, using a sulforaphane-rich extract derived from broccoli sprouts (35.2 mg per day for 20 weeks), also increased this interval by 57% in patients with recurrent prostate cancer. A recent ESCAPE study showed that a weekly consumption of glucoraphanin-enriched soup (sulforaphane precursor) for 12 months in men under active surveillance significantly reduced changes in gene expression associated with oncogenic pathways, potentially decreasing cancer progression risk. These promising results suggest a beneficial role of sulforaphane in clinical management of prostate cancer.

Posologie

posologieOral administration

posologie35 - 60 mg

formulationstandardized extract


Synergies


Cognitive decline
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Clinical research has assessed the effect of sulforaphane on cognitive decline. A randomized study in older adults examined the impact of taking glucoraphanin, a precursor of sulforaphane, at a dosage of 30 mg per day for 12 weeks. The results showed modest improvements in working memory and processing speed compared to placebo. Another double-blind randomized study evaluated the impact of sulforaphane on cognitive decline in adults suffering from cognitive deficits linked to frontal brain injuries. The trial included 90 participants aged 18 to 65, divided into two groups, receiving either sulforaphane (Avmacol) or a placebo for 12 weeks, with dosage adjusted based on weight. Results showed that the sulforaphane-treated group exhibited modest but significant cognitive improvements, namely in working memory and processing speed, compared to the placebo group. These benefits were attributed to sulforaphane's action on brain protection mechanisms, such as reducing oxidative stress and inflammation. The study also explored brain and blood biomarkers, including glutathione (GSH), an essential antioxidant, and brain-derived neurotrophic factor (BDNF), crucial for synaptic plasticity. An increase in these markers was observed in the sulforaphane group, indicating potential cognitive function enhancements. Additional studies are needed to confirm these observations.

Posologie

posologieOral administration

posologie30 mg

formulationstandardized extract


Autism
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The effects of sulforaphane on autism are variable according to studies. In children aged 4 to 12 years, 10-20 mg of sulforaphane per day, combined with risperidone for 10 weeks, reduced irritability by 14% and hyperactivity by 12%, without impact on social interactions or communication. A study on young men (13-27 years) showed that weight-based treatment (8.8 to 26.6 mg per day) for 18 weeks improved behavioral scores by 33% and social scores by 17%, with these effects disappearing after discontinuation. A larger clinical trial conducted on 108 participants in China showed that a 12-week sulforaphane treatment allowed one-third of the participants to reduce their symptom scores by 30% or more, according to clinicians' assessments. The effects were more pronounced in children over 10 years, and sulforaphane was deemed safe and well-tolerated, including in younger participants.

Posologie

posologieOral administration

posologie8 - 30 mg

formulationstandardized extract


Properties


Anticancer

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Sulforaphane acts on several key mechanisms to slow tumor development. Firstly, sulforaphane stimulates phase II detoxification enzymes, such as glutathione-S-transferase, which neutralize carcinogens. In parallel, it inhibits phase I enzymes, like cytochrome P450, responsible for activating carcinogenic substances. These combined effects reduce the exposure of cells to carcinogens. Secondly, sulforaphane acts directly on tumor cells by blocking their growth cycle, inhibiting angiogenesis (the formation of new blood vessels feeding the tumor), and limiting metastasis. It also induces the death of cancer cells while sparing healthy cells. Finally, its antioxidant and anti-inflammatory action protects cells against oxidative damage and chronic inflammation, two processes involved in the initiation and progression of cancer. Research also shows that sulforaphane can enhance the efficacy of chemotherapy, such as cisplatin or doxorubicin, while reducing their side effects. These multiple actions make sulforaphane a promising ally in the prevention and complementary treatment of cancer.

Usages associés

Prostate cancer

Antioxidant

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Sulforaphane is recognized for its powerful antioxidant properties. It primarily acts by activating the Nrf2 pathway, a key factor in regulating cellular defenses against oxidative stress. Once activated, Nrf2 stimulates the production of protective enzymes such as heme oxygenase (HO-1), glutathione peroxidase (GPX), and quinone reductase (NQO1). These enzymes neutralize free radicals, reducing oxidative damage at the cellular level. This antioxidant action of sulforaphane is particularly beneficial in preventing conditions associated with oxidative stress, such as cardiovascular diseases, neurodegenerative disorders, and cancer. For instance, in animal models, sulforaphane has shown the ability to restore glutathione levels, a major antioxidant, and protect cells against oxidative damage caused by toxic or inflammatory agents. Furthermore, sulforaphane acts on mitochondrial metabolism, the primary sources of free radicals in cells. It protects mitochondria from lipid peroxidation and preserves their function, essential for cellular health.


Neurological

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Sulforaphane is promising in the prevention and treatment of neurodegenerative diseases due to its antioxidant and anti-inflammatory properties. By activating the Nrf2 pathway, it stimulates the production of protective enzymes that reduce the accumulation of toxic proteins linked to diseases like Alzheimer's and Parkinson's. In Alzheimer's disease, studies show that sulforaphane prevents the formation of amyloid plaques and phosphorylated tau, protects neurons, and improves cognition. Administered to affected mice, it restores antioxidant levels and reduces inflammation markers, with optimal effect if treatment starts early when degeneration is minimal. For Parkinson's disease, sulforaphane protects dopaminergic neurons by reducing oxidative stress and apoptosis, while improving motor functions and coordination. In multiple sclerosis, it reduces neuronal demyelination by decreasing pro-inflammatory cytokines and strengthening the blood-brain barrier. Additionally, preliminary research has explored its potential in the treatment of autism in children and young adults. The results indicate a modest improvement in social skills and behaviors, correlated with changes in urinary markers associated with oxidative stress, inflammation, and the metabolism of amino acids and the gut microbiome. Finally, sulforaphane is also studied for its potential impact on depression. It seems to modulate the hypothalamic-pituitary-adrenal (HPA) axis, a pathway involved in the stress response, while offering antioxidant and anti-inflammatory protection. These effects could improve depressive symptoms, especially in patients with oxidative stress or inflammatory imbalances. Thus, sulforaphane emerges as a promising candidate in managing neurological disorders, both for neurodevelopmental diseases and stress-related psychiatric disorders. Its neuroprotective potential could complement traditional treatments.

Usages associés

Cognitive decline, Autism

Cardiovascular

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Sulforaphane has shown protective effects on the cardiovascular system. By activating the Nrf2 signaling pathway, it stimulates the production of antioxidant enzymes that reduce oxidative stress and inflammation in cardiac and renal tissues. These actions could help reduce the risks of diseases such as hypertension and atherosclerosis. Additionally, studies on animal models suggest that sulforaphane improves cardiac function by modulating the expression of genes involved in the regulation of intracellular calcium, a key element in myocardial contraction and relaxation.


Safety dosage

Adult: 10 mg - 60 mg (standardized extract)

Mainly administered as broccoli sprout extracts containing glucoraphanin, a precursor of sulforaphane. - Prostaphane: 10-60 mg per day for 6 months. - BroccoMax: 180 mg of glucoraphanin per day for 8 weeks. - Aqueous extracts: Up to 35.2 mg of sulforaphane per day for 20 weeks.

Children: 8 mg - 26 mg

Sulforaphane administered as broccoli extracts containing glucoraphanin. Studied dosages: Vary according to weight: for example, 8.8 to 26.6 mg/day based on body mass in clinical studies.


Interactions

Médicaments

CYTOCHROME P450 1A2: moderate interaction

Sulforaphane may alter the levels and clinical effects of CYP1A2 substrates. It inhibits CYP1A2 enzyme activity according to in vitro studies, while its precursor, glucoraphanin, may boost the expression of this enzyme, influencing the metabolism of CYP1A2-dependent drugs. Examples: Caffeine, theophylline, clozapine, olanzapine.

Cytochrome P450 3A4: moderate interaction

Sulforaphane may increase the levels and effects of CYP3A4 substrates. Animal and in vitro studies suggest it inhibits CYP3A4 activity and reduces its expression, which could intensify the effect of drugs metabolized by this enzyme. Examples: Simvastatin, cyclosporine, midazolam, ethinylestradiol.


Precautions

Pregnant women: avoid

May be consumed in amounts present in food. No reliable data on medicinal doses.

Breastfeeding women: avoid

May be consumed in amounts present in food. No reliable data on medicinal doses.