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Product name: Monascin
Synonym name: Monascoflavin
Catalogue No.: BP4055
Cas No.: 21516-68-7
Formula: C21H26O5
Mol Weight: 358.434
Botanical Source: Monascus
Physical Description:
Type of Compound: Miscellaneous
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.
The product could be supplied from milligrams to grams
Inquire for bulk scale.
For Reference Standard and R&D, Not for Human Use Directly.
HPLC of Monascin
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
69.6700
3.0551
1.4527
.0207
3.0008
25.4528
High
85.9728
4.5412
No
Yes
No
No
No
Yes
0.0
No
Yes
No
Yes
Monascin is a nitrogen heterogeneous pigment isolated from the traditional fermented red yeast rice (Monascus spp.). Due to its unique biological activity and potential medicinal value, it has attracted widespread attention in the field of natural product pharmacology in recent years. As a long-established fermented food, red yeast rice has been widely studied for containing various bioactive components. Among them, red yeast rice, as one of its main secondary metabolites, exhibits significant anti-tumor, anti-inflammatory, and lipid-regulating effects. Monasto not only has oral activity but can also regulate various cellular signaling pathways, especially as an Nrf2 activator and PPARγ agonist, giving it unique advantages in the prevention and treatment of metabolic and inflammation-related diseases.
This paper will systematically review the chemical structure and physicochemical properties of monascus, plant origin and extraction methods, pharmacological activity studies, mechanisms of action and molecular targets, druggability evaluation, and pharmacokinetic characteristics, and finally explore its clinical application prospects and future research directions, aiming to provide theoretical basis and research references for the drug development of monascus.
The chemical structure of red yeast is a polyphenolic pigment containing nitrogen heterocyclic rings, with a molecular formula C21H26O5N and a molecular weight of 358.4340. Its structure includes a pyranan ring with a conjugated system and a nitrogen heterocycle, giving it unique spectral properties and biological activity. The LogP value of red yeast acid is 3.0551, indicating moderate lipid solubility, which facilitates membrane penetration and distribution in the body. The polar surface area (TPSA) is 69.6700, indicating moderate molecular polarity and conducive to oral absorption.
Monasto has low water solubility (0.0207 mg/mL), which to some extent limits its solubility and bioavailability in the aqueous phase, but its high lipid solubility and good blood-brain barrier permeability (BBB) offer potential applications in central nervous system diseases. Notably, red yeast acid does not show hERG channel inhibitory activity, suggesting a low risk of cardiotoxicity, and the Ames test result is 0.0, indicating no significant mutagenicity.
Monascus is mainly derived from red yeast rice, a traditional food made by fermenting rice from Monascus purpureus and related Monascus strains. During fermentation, Monascus synthesizes various pigment compounds through secondary metabolic pathways, with Monascus being one of the main nitrogen heterocolorants.
Traditional methods for extracting red yeast rice include solvent extraction and chromatographic separation. Generally, ethanol or methanol is used as the extraction solvent, combined with ultrasound-assisted extraction or reflux extraction techniques to improve extraction efficiency. The extract is concentrated and separated for purification. Common separation methods include silica gel column chromatography and reversed-phase high-performance liquid chromatography (RP-HPLC). In recent years, supercritical CO2 extraction and membrane separation technologies have also been introduced to improve purity and yield.
The optimization of extraction processes mainly focuses on improving the yield and purity of red yeast rice, while reducing the coexistence of other impurities such as red yeast toxins, ensuring the safety and biological activity of the extract.
Erygatin exhibits significant inhibitory effects in various tumor cell lines, including liver cancer, breast cancer, and colorectal cancer. Its antitumor mechanism involves inducing apoptosis, blocking the cell cycle, and inhibiting tumor cell migration and invasion. In vivo experiments have shown that red yeast acid can significantly inhibit tumor growth and reduce tumor burden.
Monasto yeast exerts its anti-inflammatory effect by inhibiting the production and release of inflammatory mediators. It can downregulate the expression of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1β, inhibiting activation of the NF-κB signaling pathway and thereby reducing inflammatory responses. In various inflammation models, red yeast rice shows good anti-inflammatory effects.
Monasto has shown potential in regulating lipid metabolism. It regulates lipid metabolism-related targets such as cholesterol ester transfer protein (CETP), 3-hydroxy-3-methylglutaryl-CoA reductase (HMGCR), low-density lipoprotein receptor (LDLR), apolipoprotein B (APOB), proproprotein converting enzyme Kexin 9 (PCSK9), apolipoprotein E (APOE), and peroxisome proliferator-activated receptor α (PPARA), thereby regulating plasma lipid levels. Lowering serum total cholesterol and low-density lipoprotein cholesterol (LDL-C), and increasing high-density lipoprotein cholesterol (HDL-C), help prevent and treat atherosclerosis and related cardiovascular diseases.
Monkeast can inhibit the activation of NORs (Nitric Oxide Radicals, active nitrogen radicals), reduce oxidative stress damage, protect cells from oxidative damage, and further support its anti-inflammatory and anti-tumor effects.
The biological activity of red yeast is closely related to its regulation of multiple signaling pathways, mainly including:
As an activator of Nrf2 (nuclear factor red 2-related factor 2), red yeast xi promotes the transfer of Nrf2 from the cytoplasm to the nucleus, inducing the expression of antioxidant and detoxifying enzymes such as glutathione peroxidase (GPx), superoxide dismutase (SOD), and heme oxygenase-1 (HO-1). This enhances the cells' antioxidant capacity, reduces cellular damage related to oxidative stress, and is one of the key mechanisms for their anti-inflammatory and anti-tumor effects.
Monasto yeast is an agonist of the peroxisome proliferator-activated receptor γ (PPARγ), regulating lipid metabolism, glucose metabolism, and inflammatory responses. Activation of PPARγ promotes the oxidation and storage of fatty acids, improves insulin sensitivity, inhibits the expression of pro-inflammatory factors, and co-regulates metabolic homeostasis and immune responses, playing a key role in lowering blood lipids and anti-inflammation.
Monasto also regulates key lipid metabolism-related targets such as CETP, HMGCR, LDLR, APOB, PCSK9, APOE, and PPARA, comprehensively modulating cholesterol synthesis, transport, and clearance, lowering blood lipid levels, and preventing cardiovascular diseases.
Additionally, red yeast rice inhibits the NF-κB signaling pathway, reduces the expression of pro-inflammatory factors, and alleviates inflammatory responses; Regulation of apoptosis-related proteins such as Bax, Bcl-2, and the Caspase family promotes tumor cell apoptosis.
The molecular weight of red yeast is 358.4340, which complies with Lipinski's "drug similarity rule," and the LogP is 3.0551, indicating moderate lipid solubility and favorable oral absorption. Its TPSA is 69.6700, indicating good membrane permeability. Low water solubility (0.0207 mg/mL) may limit its bioavailability, but it can be improved through formulation optimization.
Monasto has excellent blood-brain barrier penetration ability, making its application possible in central nervous system diseases. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames test is non-mutagenic and relatively safe.
Pharmacokinetic studies show that red yeast extract is rapidly absorbed orally and widely distributed, with main metabolic pathways including phase I and phase II metabolism in the liver. It has a moderate half-life and a reasonable clearance rate in the body, making it suitable for oral drug development. Further research is needed in the future on the activity and toxicological characteristics of its metabolites.
As a natural product, red yeast rice shows broad application prospects in the treatment of anti-tumor, anti-inflammatory, and metabolic diseases, thanks to its advantages of multi-target and multi-pathway regulation. Especially in the lipid-lowering field, red yeast rice can become an ideal candidate for treating hyperlipidemia and atherosclerosis, by regulating key targets such as CETP, HMGCR, and PCSK9. Additionally, its dual functions as an Nrf2 activator and a PPARγ agonist offer new approaches for the treatment of metabolic syndrome, diabetes, and related chronic inflammatory diseases.
Currently, clinical research on red yeast extract is still in its early stages. In the future, it is necessary to strengthen systematic evaluation of its pharmacokinetics, toxicology, and clinical safety, optimize formulation processes, and improve bioavailability. At the same time, combining modern drug design technologies to develop erythrocylin derivatives or combination drug strategies is expected to enhance therapeutic efficacy and application range.
Moreover, the potential of red yeast in central nervous system diseases is worth further exploration, especially for its good blood-brain barrier permeability, which may provide new drug candidates for interventions in neurodegenerative diseases.
As an important active ingredient in red yeast rice, red yeast rice demonstrates broad medicinal value due to its unique chemical structure and diverse pharmacological activities. Its multiple mechanisms of anti-tumor, anti-inflammatory, and lipid-lowering provide valuable examples for pharmacological research of natural products. Druggability evaluations show that red yeast rice has promising potential for drug development, but issues such as water solubility and bioavailability still need to be addressed.
In the future, by integrating modern drug development technologies, in-depth exploration of the mechanism of action of red yeast rice and optimizing its pharmacokinetic properties will help promote its clinical translation, develop safe and effective new natural drugs, and contribute new strength to human health.
Shenshuai
Wenjing
Hedandan
