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Red Yeast Rice

Cardiovascular Health

Overview

  • Red yeast rice (RYR) is a fermented product of Monascus purpureus grown on rice.
  • The fermentation produces a suite of naturally occurring statin‑like compounds, most notably monacolin K, which is chemically identical to lovastatin.
  • RYR is chiefly used as a dietary supplement for managing blood lipids, especially low‑density‑lipoprotein (LDL) cholesterol.

Benefits

  • Clinical trials and meta‑analyses consistently show that RYR lowers LDL‑C by 15‑25 % and modestly raises HDL‑C (3–6 %) when taken for 8–12 weeks (e.g., Li et al., J Clin Lipidol 2021).
  • The LDL‑lowering effect translates into a modest reduction in cardiovascular risk markers, such as C‑reactive protein and arterial stiffness.
  • RYR also modestly improves triglyceride levels.
  • RYR may modestly blunt post‑prandial glucose spikes, likely via improved insulin sensitivity (Samaroo et al., Am J Clin Nutr 2022).
  • No robust evidence supports direct cognitive or muscular benefits beyond the lipid‑mediated cardiovascular protection.

How It Works

  • The primary active component, monacolin K (lovastatin), is a competitive inhibitor of HMG‑CoA reductase.
  • HMG‑CoA reductase is the rate‑limiting enzyme in the mevalonate pathway that produces cholesterol.
  • By binding the enzyme’s active site, monacolin K reduces conversion of HMG‑CoA to mevalonate, decreasing hepatic cholesterol synthesis.
  • Reduced intracellular cholesterol up‑regulates LDL‑receptor expression on hepatocytes, enhancing clearance of circulating LDL particles.
  • In addition to monacolin K, RYR contains other monacolins (e.g., monacolin J) and flavonoids.
  • These additional compounds may provide antioxidant and anti‑inflammatory actions, further modulating endothelial function and plaque stability.

Dosage

  • Standardized RYR extracts delivering 5–10 mg monacolin K per capsule are most common.
  • Clinical trials typically use 1–3 g of RYR powder daily (equivalent to 5–10 mg monacolin K).
  • Dosage is often divided into two doses taken with meals to improve absorption and minimize gastrointestinal upset.
  • For modest LDL‑C reduction, 1 g twice daily (≈10 mg monacolin K) is the most frequently studied regimen.
  • Higher doses (up to 4 g/day) have been used in hyper‑cholesterolemic patients under medical supervision.
  • Timing with meals is recommended because post‑prandial bile release enhances absorption of the lipophilic monacolin K.

Safety & Side Effects

  • RYR is generally well tolerated at ≤10 mg monacolin K per day.
  • Reported adverse events include mild gastrointestinal discomfort, headache, and, rarely, myopathy or elevated liver enzymes—effects similar to low‑dose lovastatin.
  • Contra‑indicated in pregnancy, lactation, and for individuals with active liver disease (ALT/AST >3× ULN) or known statin hypersensitivity.
  • Interactions occur with CYP3A4 inhibitors (e.g., clarithromycin, itraconazole) and with other lipid‑lowering agents (e.g., fibrates) that increase myopathy risk.
  • Patients on anticoagulants (warfarin) may experience enhanced anticoagulation due to altered vitamin K metabolism; monitoring is advised.

Chemistry

  • The principal statin‑like molecule in RYR is monacolin K (lovastatin).
  • Its molecular formula is C₂₄H₃₆O₅, with a molecular weight of 404.54 g mol⁻¹.
  • IUPAC name: (3S,5R,6R,7E,10R,13R,14R,15S)-7,13‑dimethyl‑3‑[2‑(1‑oxor‑3‑hydroxy‑2‑propyl)‑1‑oxo‑2‑propyl]‑2‑[2‑(1‑oxo‑2‑propyl)‑1‑ox… (the full systematic name is lengthy; the structure is a 2‑methyl‑3‑hydroxy‑5‑dimethyl‑6‑(3‑hydroxy‑3‑methyl‑butanoyl)‑octa‑hydro‑1‑benzopyran).
  • The molecule contains a lactone ring, a side‑chain hydroxy‑acid moiety, and a lipophilic aliphatic chain, conferring high membrane permeability.
  • Monacolin K is a pro‑drug; after oral absorption the lactone opens to the active β‑hydroxy‑acid (the HMG‑CoA reductase inhibitor).

Sources & Quality

  • Commercial RYR is produced by inoculating polished rice with Monascus purpureus strains under controlled fermentation (temperature ≈ 30 °C, pH ≈ 5.5).
  • After fermentation, the rice is dried, milled, and extracted with ethanol or water to obtain a powder or capsule‑grade product.
  • Quality varies widely.
  • The presence of monacolin K is verified by HPLC.
  • Manufacturers must test for citrinin—a nephrotoxic mycotoxin occasionally produced by Monascus under poor conditions.
  • High‑quality supplements come from certified manufacturers that conduct batch‑specific monacolin K quantification (≥5 mg per dose) and certify low‑citrinin levels (<2 ppb).
  • Asian countries (China, Korea) are the primary sources.
  • Stringent GMP practices are essential to ensure safety and potency.

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