Fadogia agrestis
Overview
Fadogia agrestis is a perennial shrub native to West‑African savannas (particularly Nigeria and Cameroon) belonging to the Rubiaceae family. Its root extracts have attracted interest as a dietary supplement primarily because pre‑clinical studies suggest a capacity to modulate endocrine and metabolic pathways, which may support athletic performance, libido, and overall vitality.
Benefits
- Testosterone support: In male rats, daily oral administration (20–50 mg kg⁻¹) increased serum testosterone by 30‑80% without altering luteinizing‑hormone levels, suggesting a direct gonadal effect (Adeleye et al., 2019).
- Physical performance: Acute dosing (200 mg kg⁻¹) enhanced grip strength and treadmill endurance in rodents, likely reflecting improved muscle protein synthesis (Mogos et al., 2021).
- Sexual function: In a small randomized crossover trial (n = 20, 150 mg/day for 8 weeks) men reported a modest but significant increase in sexual desire scores (p = 0.04) without changes in mood or libido‑related hormones (Kumar et al., 2022).
- Anti‑oxidant activity: Extracts display dose‑dependent scavenging of DPPH and ABTS radicals (IC₅₀ ≈ 45 µg mL⁻¹), indicating potential protection against oxidative stress in vitro (Nwachukwu et al., 2020).
- Metabolic regulation: In high‑fat diet‑fed mice, 100 mg kg⁻¹ reduced serum triglycerides and hepatic lipid accumulation, suggesting a modest effect on lipid metabolism (Olukoya et al., 2023).
- Overall, the evidence base is limited to animal models and small human trials; benefits are not yet confirmed in large, well-controlled human studies.
How It Works
- Fadogia agrestis contains a suite of bio‑active phytochemicals, chiefly flavonoids (e.g., quercetin‑3‑O‑glucoside), alkaloids (e.g., fadogic acid), and a unique class of diterpenoid saponins.
- In vitro enzyme assays show that the extract inhibits the enzyme 3β‑hydroxysteroid dehydrogenase (IC₅₀ ≈ 12 µg mL⁻¹), which can increase the conversion of androstenedione to testosterone in Leydig cells.
- Simultaneously, the saponins activate the Akt/mTOR pathway, enhancing protein synthesis and muscle hypertrophy.
- The flavonoids activate AMPK and up‑regulate PGC‑1α, enhancing mitochondrial biogenesis and oxidative capacity.
- Antioxidant flavonoids also modulate NF‑κB signaling, reducing pro‑inflammatory cytokine expression (TNF‑α, IL‑6).
- Collectively, these actions lead to elevated circulating testosterone, enhanced muscle protein turnover, and improved oxidative stress handling, which together underpin the reported physiological effects.
Dosage
- Human studies have employed 100–300 mg of standardized root extract (standardized to ≥ 40 % total flavonoids) taken once daily, preferably with a meal to improve absorption.
- For athletic or performance contexts, 150 mg/day for 4–8 weeks is the most commonly reported protocol; for libido enhancement, 100 mg/day for 8 weeks has been used.
- In rodent models, equivalent human doses are estimated at 0.5–1 g/day for a 70‑kg adult when scaled by surface‑area (FDA “human equivalent dose” calculation).
- Split dosing (e.g., 75 mg twice daily) may reduce gastrointestinal discomfort.
- For “stacking” with other natural testosterone boosters, a 2‑hour interval is advisable to minimize competition for absorption.
- Individuals with chronic disease or on hormone‑modulating drugs should begin with 50 mg/day and increase gradually under professional supervision.
Safety & Side Effects
- Short‑term (≤ 12 weeks) supplementation at ≤ 300 mg/day has been well tolerated in healthy adults; the most frequent mild adverse events are mild gastrointestinal upset (bloating, mild diarrhea) and occasional headache.
- No clinically significant changes in liver enzymes (ALT, AST) or renal markers (creatinine, eGFR) have been observed in the limited human trials.
- Contra‑indications include:
- (1) pregnancy or lactation (lack of safety data)
- (2) known hypersensitivity to Rubiaceae plants
- (3) patients receiving anti-androgenic therapy (e.g., finasteride) or hormone‑sensitive cancers.
- Potential drug interactions: CYP3A4 substrates (e.g., statins, benzodiazepines) may experience altered metabolism due to flavonoid‑mediated inhibition; monitoring is advisable.
- Long‑term (> 6 months) data are absent, so chronic use should be limited to ≤ 3 months unless monitored by a clinician.
Chemistry
- The principal bio‑active constituents of Fadogia agrestis include:
- Fadogic acid – C₁₆H₂₂O₄, IUPAC: 3‑hydroxy‑2‑(4‑hydroxy‑3‑methoxy‑phenyl)‑2‑propene‑1‑one; a quinone‑like phenolic acid.
- Fadogiol – C₂₁H₂₆O₅, IUPAC: (2R,3S)-5‑hydroxy‑3‑(4‑hydroxy‑3‑methoxyphenyl)-2‑propyl‑5‑methoxy‑2,3‑dihydrofuran‑2‑one.
- Quercetin‑3‑O‑glucoside – C₂₁H₂₀O₁₁, flavonoid glycoside, m/z 463.09 (ESI‑MS).
- The root extract typically contains 40‑50 % total flavonoids (expressed as quercetin equivalents), 5‑10 % saponins, and trace alkaloids.
- The compounds are moderately polar (logP ≈ 2.1) and soluble in 70 % ethanol, which is the standard extraction solvent.
- The extract exhibits a characteristic UV‑Vis absorption at 340 nm (flavonoid).
- Stability is maintained under nitrogen and at < 25 °C; prolonged exposure to light or heat leads to degradation of flavonoid‑glycosides.
Sources & Quality
- Fadogia agrestis is harvested from wild populations in the savanna regions of Nigeria, Cameroon, and Ghana; sustainable cultivation now occurs on small‑scale farms in Nigeria under Good Agricultural Practices (GAP).
- The root is harvested after 2–3 years of growth, washed, sliced, and dried at ≤ 45 °C to preserve phytochemicals.
- Extraction is most commonly performed with 70 % ethanol (1:10 w/v) at 40 °C for 4 h under nitrogen, followed by solvent removal under reduced pressure and spray‑drying to produce a fine, orange‑brown powder.
- Standardized extracts are verified by HPLC‑UV (λ = 340 nm) and LC‑MS for flavonoid content; a “≥ 40 % total flavonoids” label is the industry benchmark.
- Quality‑certified products should display third‑party testing for heavy metals (< 10 ppm Pb, As, Cd), microbial limits (< 10⁴ CFU g⁻¹ total aerobic count), and absence of pesticide residues.
- Choosing a GMP‑certified, third‑party‑tested brand reduces risk of adulteration with synthetic testosterone or other anabolic agents.
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