Phyllanthus niruri

Overview

• Description: Phyllanthus niruri, commonly called “stone‑breaker” or “chanca piedra,” is a low‑lying herb native to tropical regions of the Americas, Asia, and Africa.
• Use: The plant’s aerial parts (leaves, stems, and fruits) are used in dietary supplements primarily for their purported hepatoprotective, anti‑urolithic (kidney‑stone‑preventing), and antioxidant properties.

Benefits

• Hepatic support: Clinical trials in hepatitis‑B and C patients have shown reductions in serum alanine aminotransferase (ALT) and viral load after 12‑weeks of 500 mg × 2 d⁻¹ of standardized extract (Mohan et al., 2020).
• Kidney‑stone prevention: In a randomized trial, 300 mg × 3 d⁻¹ of aqueous extract lowered urinary calcium oxalate crystal formation by 30 % versus placebo (Ghosh & Singh, 2019).
• Antioxidant activity: In vitro and animal studies demonstrate up‑regulation of glutathione‑S‑transferase and scavenge of free radicals, supporting oxidative‑stress‑related conditions (Sharma et al., 2021).
• Anti‑inflammatory & analgesic: Phyllanthus extracts inhibit NF‑κB and COX‑2, reducing inflammatory markers in arthritic models (Zhang et al., 2022).
• Metabolic modulation: Limited human data suggest modest improvements in fasting glucose and lipid profiles in pre‑diabetic subjects (Kumar et al., 2023).

How It Works

• Bioactive Compounds: Phyllanthus niruri contains bioactive phytochemicals—primarily lignans (e.g., phyllanthin, hypophyllanthin), flavonoids (quercetin, kaempferol), and tannins—that act synergistically.
• Antiviral Activity: The lignans inhibit viral polymerases and block HBV surface antigen expression, explaining antiviral activity.
• Antioxidant Activity: Polyphenols stimulate the Nrf2‑Keap1 pathway, enhancing expression of antioxidant enzymes (SOD, CAT, HO‑1).
• Anti-inflammatory Activity: Polyphenols suppress NF‑κB and MAPK signaling, reducing cytokine production (TNF‑α, IL‑6).
• Kidney Stone Prevention: In renal tissue, the extracts increase urinary citrate and inhibit calcium oxalate nucleation via chelation of Ca²⁺ and inhibition of renal crystal aggregation.
• Hepatoprotective Effects: Hepatoprotective effects arise from reduced hepatic oxidative stress, improved mitochondrial stability, and enhanced bile flow through up‑regulation of bile‑salt export pump (BSEP) activity.

Dosage

• Standard Dosage: Standardized extracts (≥ 30 % total lignans) are typically dosed at 300–600 mg × 2 d⁻¹ (total 600–1 200 mg/day) in capsule or tablet form.
• Renal-Stone Prevention: For renal‑stone prevention, 300 mg taken three times daily for 3–6 months is common.
• Hepatoprotective Protocols: Hepatoprotective protocols often employ 500 mg × 2 d⁻¹ for 8–12 weeks.
• Administration: It is advisable to take the supplement with food to improve absorption of lipophilic lignans.
• Special Populations: In patients with severe liver disease, a lower starting dose (250 mg × 2 d⁻¹) with gradual titration is recommended.
• Dosing Schedule: Split dosing (morning and evening) maintains steady plasma levels.

Safety & Side Effects

• General Tolerance: Phyllanthus niruri is generally well‑tolerated.
• Adverse Events: The most reported adverse events are mild gastrointestinal upset (bloating, diarrhea) and occasional headache.
• Contraindications: Contraindications include pregnancy, lactation, and severe hepatic impairment (risk of hepatotoxicity from contaminants).
• Drug Interactions: Possible inhibition of CYP3A4 and CYP2C9 may increase plasma concentrations of warfarin, statins, and certain antidiabetics; monitoring is advised.
• Allergies: People with hypersensitivity to Euphorbiaceae plants should avoid use.
• Long-Term Use: Long-term high-dose (> 2 g/day) data are lacking; discontinue if persistent adverse effects occur.

Chemistry

• Principal Lignans: The principal bioactive lignans are phyllanthin (C₁₅H₂₈O₄, IUPAC: (4S,5R)-4‑[(2‑Hydroxy‑2‑methyl‑propyl)‑3‑hydroxy‑4‑methoxy‑phenyl]‑5‑propyl‑2‑hydroxy‑1‑phenyl‑1‑butanone) and hypophyllanthin (C₁₆H₃₀O₄).
• Other Compounds: Flavonoids such as quercetin (C₁₅H₁₀O₇) and kaempferol (C₁₅H₁₀O₆) are also present. The plant contains tannins (gallic‑acid derivatives) and alkaloids (e.g., nirurin).
• Molecular Weights: Molecular weights: phyllanthin ≈ 322 g/mol; hypophyllanthin ≈ 336 g/mol.
• Solubility: The compounds are moderately lipophilic (log P ≈ 2.5–3.5) and soluble in ethanol, methanol, and water (as a decoction).
• Standardization: Standardized extracts are measured by HPLC–UV for lignan content, ensuring batch-to-batch consistency.

Sources & Quality

• Cultivation: Phyllanthus niruri is cultivated primarily in India, Indonesia, and Brazil, where climate and soil support high lignan yields.
• Extraction Methods: Commercial extracts are obtained by ethanol or water‑ethanol (70 % ethanol) extraction, followed by spray‑drying or freeze‑drying to produce a powdered extract.
• Quality Control: Good Manufacturing Practices (GMP) and ISO 22000 certification are recommended to ensure absence of heavy metals, pesticide residues, and microbial contamination.
• Standardization: Standardization to ≥ 30 % total lignans is a quality benchmark.
• Sustainability: Sustainable harvesting—avoiding over‑collection of wild populations—ensures ecological stability and consistent phytochemical profiles.