Rhoifolin (Flavone Glycoside · Cardioprotective · Lipid-modulating)

Compound	Rhoifolin (Apigenin-7-O-Neohesperidoside)
Chemical class	Polyphenol — Flavone O-Glycoside (apigenin + neohesperidose disaccharide)
CAS	17306-46-6
Primary source	Citrus aurantium (bitter orange), Citrus maxima (pomelo), Rhus cotinus
Key applications	Cardioprotective; lipid-modulating; anti-inflammatory; antioxidant
Claim strength	Moderate
Typical form	Grapefruit Extract Powder; Neohesperidin 98% (Bitter Orange); Citrus aurantium flavonoid extract
Buy from Herbuno	Grapefruit Extract Powder → Neohesperidin 98% Powder (Bitter Orange) | High-Purity Isolate | Citrus aurantium →

Name origin: Rhoifolin was first isolated from Rhus cotinus (the smoke tree, now Cotinus coggygria) — the genus name providing the compound name. It is apigenin's 7-O-neohesperidoside, meaning the sugar at C-7 of apigenin's A-ring is neohesperidose (rhamnose-α1→2-glucose) — the same bitter disaccharide found in neohesperidin and naringin. Traditional use: Citrus aurantium (bitter orange, Zhi Ke in TCM) is an important botanical with classical indications for qi stagnation, chest tightness, and abdominal distension. Rhoifolin is one of the characteristic flavone glycosides of bitter orange peel alongside neohesperidin, hesperidin, and sinensetin. Research trajectory: Rhoifolin's pharmacological profile is emerging, with activity identified in cardiovascular protection, lipid lowering, and anti-inflammatory models. It shares apigenin's GABAergic and anxiolytic background but requires differentiation from bitter orange's sympathomimetic protoalkaloid (synephrine) in commercial positioning. Commercial source: Rhoifolin is available from Herbuno via Grapefruit Extract Powder and Neohesperidin 98% Powder (Bitter Orange).

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Evidence for Rhoifolin Applications

Cardioprotective activity: Rhoifolin demonstrates myocardial protection in rat ischaemia-reperfusion models, reducing infarct size and attenuating troponin-I release via NF-κB inhibition and mitochondrial membrane potential stabilisation. The neohesperidoside sugar improves aqueous solubility versus apigenin aglycone, enhancing delivery to cardiac tissue. Claim strength: Emerging.

Lipid modulation: In hyperlipidaemic rodent models, rhoifolin supplementation reduces total cholesterol, LDL, and triglycerides while modestly elevating HDL. The mechanism appears to involve HMG-CoA reductase modulation and bile acid synthesis upregulation. Citrus flavonoids as a class have moderate lipid-modulating evidence; rhoifolin-specific clinical data are not yet available. Claim strength: Moderate (class); Emerging (isolated).

Anti-inflammatory: COX-2 inhibition and IL-6 suppression in macrophage models at 10–50 μM concentrations. Rhoifolin's apigenin backbone shares NF-κB and MAPK pathway inhibition, with the neohesperidose sugar adding moderate enhancement of aqueous bioavailability over pure apigenin. Claim strength: Moderate.

Antioxidant: DPPH and ABTS scavenging activity is moderate — consistent with a flavone bearing no catechol B-ring. In Citrus extract context, rhoifolin contributes to total antioxidant capacity alongside hesperidin, naringenin, and polymethoxylated flavones. Claim strength: Moderate.

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Dosage & Formulator Specification

No isolated rhoifolin clinical dosing data exist. Bitter orange extract preparations used for metabolic and cardiovascular endpoints use 500–1000 mg/day standardised extract. Rhoifolin is a minor constituent of the Citrus aurantium flavonoid complex; neohesperidin and hesperidin are present at 1–10% dry extract weight while rhoifolin typically appears at 0.1–0.5%.

Important formulation note: bitter orange extract also contains synephrine (a sympathomimetic protoalkaloid), subject to regulatory scrutiny in sports nutrition and banned substance frameworks. Formulators targeting rhoifolin's flavone benefits without synephrine should specify a synephrine-free, flavone-standardised Citrus aurantium extract, or use grapefruit-derived rhoifolin instead.

Citrus flavone glycosides are stable in solid dosage (capsule, tablet, sachet). Aqueous stability is moderate at pH 4–7. Standard GMP processing is sufficient for shelf-life.

Rhoifolin carries the neohesperidoside bitter taste shared with naringin and neohesperidin — relevant for uncoated tablet and liquid formulations targeting taste-neutral products.

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Frequently Asked Questions — Rhoifolin

What is the difference between rhoifolin and neohesperidin?
Both are Citrus aurantium O-glycosides carrying neohesperidose (rhamnose-α1→2-glucose). The difference is in the aglycone: rhoifolin's aglycone is apigenin; neohesperidin's is hesperetin (3′-methoxy, 4′-hydroxy). Both have the characteristic intense bitterness associated with the α-1→2 rhamnosyl linkage.

Does bitter orange extract always contain synephrine alongside rhoifolin?
Yes — Citrus aurantium extracts contain both protoalkaloids (synephrine, hordenine, octopamine) and flavonoids (neohesperidin, hesperidin, rhoifolin). For flavone-only applications, specify a flavonoid-standardised extract or use grapefruit-sourced rhoifolin.

Is rhoifolin bitter-tasting in formulations?
Rhoifolin carries the neohesperidoside sugar shared with naringin and neohesperidin, both intensely bitter. Bitterness masking or encapsulation should be considered for uncoated tablets and liquid formats.

What are the most relevant Herbuno products for rhoifolin-targeted formulations?
Grapefruit Extract Powder delivers rhoifolin alongside naringin and hesperidin. Neohesperidin 98% (Bitter Orange) is the highest-purity related flavonoid sharing rhoifolin's neohesperidoside chemistry. Both carry full CoA documentation.

Related compounds: Apigenin, Naringin, Neohesperidin, Chrysin

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Claim-strength scale – High = multiple human RCTs; Moderate = limited trials or strong preclinical convergence; Emerging = early-stage lab or animal data.

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