Grapefruit Bioflavonoids
Also known as: Citrus bioflavonoids, Citrus flavonoids, Grapefruit flavonoids, Hesperidin, Naringin, Polymethoxylated flavones, Grapefruit Bioflavonoids
Overview
Grapefruit bioflavonoids are a class of polyphenolic compounds found in citrus fruits like grapefruits, oranges, and lemons. These compounds, including hesperidin, naringin, and polymethoxylated flavones, are known for their antioxidant, anti-inflammatory, and vasodilatory properties. As supplements, they are used for their potential health benefits, such as improving endothelial function, reducing cardiovascular risk, and managing blood sugar levels. Research on grapefruit bioflavonoids is moderately mature, with several systematic reviews and meta-analyses available, indicating a good level of evidence supporting their effects. They are available in various forms, including tablets, capsules, and extracts, often standardized by rutin equivalence.
Benefits
Grapefruit bioflavonoids offer several evidence-based benefits. A systematic review and meta-analysis showed that citrus flavonoid supplementation significantly improved flow-mediated vasodilation (FMD) by 2.75%, indicating enhanced endothelial function. Citrus fruit intake, rich in bioflavonoids, is associated with reduced risks of cardiovascular diseases, coronary heart disease, and stroke. Some studies suggest potential benefits for glycemic control through DPP-4 inhibition, although more clinical trial data is needed. Additionally, citrus fruit intake has been linked to reduced risks of certain cancers. These benefits are particularly relevant for adults at risk of cardiovascular diseases. Improvements in endothelial function can be observed within weeks to months of supplementation.
How it works
Grapefruit bioflavonoids act through multiple mechanisms. They exhibit antioxidant activity, reducing oxidative stress and inflammation. They can inhibit dipeptidyl peptidase-4 (DPP-4), influencing glucose metabolism. These compounds also enhance nitric oxide production, leading to vasodilation and improved endothelial function. By interacting with the cardiovascular system, they improve vascular function and reduce blood pressure. They also influence glucose regulation within the metabolic system. Molecular targets include DPP-4, endothelial nitric oxide synthase (eNOS), and various inflammatory pathways. The bioavailability of these bioflavonoids varies, but they are generally absorbed and metabolized into active forms.
Side effects
Grapefruit bioflavonoids are generally considered safe when consumed in recommended doses. Common side effects are rare, but some individuals may experience gastrointestinal discomfort. Uncommon side effects include allergic reactions. Rare side effects may include severe allergic reactions and interactions with certain medications. Grapefruit bioflavonoids can interact with medications like statins and blood thinners due to their effect on cytochrome P450 enzymes. Individuals with known allergies to citrus fruits or those taking interacting medications should avoid these supplements. Pregnant or breastfeeding women should consult healthcare providers before use due to limited safety data in these populations.
Dosage
The minimum effective dose for improving endothelial function is around 200 mg/day of citrus flavonoids. Optimal dosages range from 200 mg to 500 mg per day, depending on the specific bioflavonoid and desired health outcome. There is no established maximum safe dose, but doses above 1000 mg/day are not typically studied. Consistent daily intake is recommended for sustained benefits. Supplements are available in tablets, capsules, or extracts. Bioavailability can be enhanced with the presence of vitamin C, which is often included in citrus bioflavonoid supplements. Vitamin C may act as a cofactor to enhance absorption and efficacy.
FAQs
Are grapefruit bioflavonoids safe?
Grapefruit bioflavonoids are generally safe, but interactions with medications and allergic reactions need to be considered. Consult a healthcare provider if you have concerns.
When should I take grapefruit bioflavonoids?
Consistent daily intake is recommended, and the timing can be flexible but should be consistent. Choose a time that fits your routine for best adherence.
How long before I see results?
Improvements in endothelial function and cardiovascular health can be expected within several weeks to months of consistent supplementation.
Can I replace my medication with this supplement?
While grapefruit bioflavonoids have health benefits, they should not be used as a replacement for medical treatment without consulting a healthcare provider.
Research Sources
- https://pubmed.ncbi.nlm.nih.gov/38561995/ – This systematic review and dose-response meta-analysis of 8 RCTs (596 participants) found that citrus flavonoids supplementation significantly improved flow-mediated vasodilation (FMD) by 2.75%. The study also revealed a linear dose-response relationship, with each 200 mg/d increase in CFS leading to a 1.09% increase in FMD, suggesting a beneficial impact on endothelial function.
- https://www.mdpi.com/1420-3049/27/15/4741 – This analytical study assessed the citrus bioflavonoid content and DPP-4 inhibition potential of various supplements. The study found wide variability in rutin equivalence among supplements, with CBF-7 showing the highest potential for beneficial effects in glycemic regulation due to its high rutin content, highlighting the importance of supplement standardization.
- https://journals.plos.org/plosone/article/file?id=10.1371%2Fjournal.pone.0286143&type=printable – This umbrella review of meta-analyses and systematic reviews examined the impact of citrus fruit and hesperidin intake on multiple health outcomes. The review found that citrus fruit intake was associated with reduced risks of all-cause mortality, cardiovascular diseases, coronary heart disease, stroke, type 2 diabetes mellitus, and several cancers, indicating broad health benefits.
- https://journals.lww.com/jno/fulltext/2023/03000/impact_of_citrus_fruit_and_hesperidin_intake_on.3.aspx – This umbrella review analyzed the impact of citrus fruit and hesperidin intake on various health outcomes. The study revealed associations between citrus fruit consumption and reduced risks of cardiovascular diseases, stroke, and certain cancers, underscoring the potential of citrus bioflavonoids in promoting overall health.
- https://www.researchgate.net/publication/8047915_Hesperidn_a_citrus_bioflavonoid_decreases_the_oxidative_stress_produced_by_carbon_tetrachloride_in_rat_liver_and_kidney – This study investigated the effects of hesperidin, a citrus bioflavonoid, on oxidative stress in rat liver and kidney induced by carbon tetrachloride. The findings indicated that hesperidin decreased oxidative stress, suggesting its potential protective role against oxidative damage in these organs.
Supplements Containing Grapefruit Bioflavonoids

N.O.-Xplode Fruit Punch
BSN

N.O.-Xplode Fruit Punch
BSN

Superior Vitamin C 1000 mg
Country Life
Citrus Bioflavonoids 500 mg
Country Life

Citrus Bioflavonoids And Rutin 1000 mg
Country Life

Bio-Rutin Complex 500 mg / 500 mg
Country Life

Liquid Multivitamin Formula Fruit Punch Flavor
Garden of Life Vitamin Code

Liquid Multivitamin Formula Fruit Punch
Garden of Life Vitamin Code