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Product name: Ankaflavin
Synonym name: Ankaflavine
Catalogue No.: BP4056
Cas No.: 50980-32-0
Formula: C23H30O5
Mol Weight: 386.48
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 Ankaflavin
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
69.6700
3.9669
2.2683
.0094
2.5510
23.6515
High
90.3314
4.4643
No
Yes
No
No
No
Yes
0.0
No
Yes
No
Yes
Ankaflavin (CAS No.: 50980-32-0) is a natural product extracted from red rice fermented by Monascus spp., and is an important member of the Monascus pigment family. In recent years, with the deepening study of pharmacological activity of natural products, red yeast xianthuan has attracted widespread attention due to its unique biological activity, especially its potential applications in metabolic disease and tumor treatment. As an orally active peroxisome proliferator-activated receptor γ (PPARγ) agonist, red yeast xiantin exhibits multi-target, multi-mechanism pharmacological properties, including anti-inflammatory, anticancer, anti-atherosclerosis, and lipid-lowering effects. This paper aims to systematically review the chemical structure, origin, extraction methods, pharmacological activity, and mechanism of action of red yeast fluxanthin, combining druggability evaluation and pharmacokinetic characteristics to explore its clinical application prospects and challenges, providing a theoretical basis for subsequent research and development.
The molecular formula of red yeast rice flavonin is C_24H_34O_4, with a molecular weight of 386.4880, and structurally, it belongs to the polyhydroxypolyene compounds. Its chemical structure features include a polyene chain and multiple hydroxyl substituents, giving it certain polarity and lipid solubility. The LogP value of red yeast fluxanthin was 3.9669, indicating good lipid solubility, which facilitates cell membrane penetration and distribution in vivo. Its topological pole surface area (TPSA) is 69.67 Å^2, indicating moderate polarity that facilitates oral absorption. Its low water solubility (0.0094 mg/mL) suggests limited solubility in the aqueous phase, but this poses certain challenges for oral formulation design. Erythrosqlavin can effectively cross the blood-brain barrier (BBB), which opens up potential applications in central nervous system diseases. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames-induced mutagenic test result was 0.0, indicating low genotoxicity risk and good safety.
Monascus spp. mainly comes from red rice fermented by Monascus spp. Monascus is a traditional class of fermenting microorganisms widely used in the food industry, especially in fermented food production in East Asia. Monasoxanthin is a secondary metabolite produced during the metabolic process of Monascus and has significant physiological activity.
The process for extracting Monascus yeast rice flavonoids typically includes the following steps: First, solid or liquid fermentation techniques are used to cultivate Monascus monascus. After fermentation, the fermented product is extracted using organic solvents (such as ethanol, methanol, or ethyl acetate). Subsequently, high-purity red yeast yeast flavin is obtained through separation and purification techniques such as liquid-liquid partitioning, silica gel column chromatography, and reversed-phase high-performance liquid chromatography (RP-HPLC). In recent years, green extraction technologies such as ultrasound-assisted extraction and supercritical fluid extraction have also been applied to efficiently extract red yeast xilavin, improving yield and purity while reducing the use of organic solvents.
As a PPARγ agonist, red yeast rice flavin can regulate the expression of genes related to lipid metabolism, promote β-oxidation of fatty acids, and lower plasma levels of triglycerides and low-density lipoprotein cholesterol (LDL-C). Its targets involve key proteins 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 lysosozyme 9 (PCSK9), apolipoprotein E (APOE), and peroxisome proliferator-activated receptor α (PPARA). By modulating these targets, red yeast rice flavonin not only lowers blood lipids but also improves lipid metabolism disorders, possessing potential anti-atherosclerotic effects.
Monasluxlavin can significantly inhibit the release of inflammatory mediators, reduce the expression of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1β, and alleviate inflammatory responses. Its anti-inflammatory mechanism mainly regulates the NF-κB signaling pathway and the MAPK pathway, inhibiting the transcriptional activity of inflammation-related genes, thereby protecting tissues and alleviating chronic inflammation.
Monascus flantin exhibits selective cytotoxicity and can induce apoptosis in various cancer cell lines. Its mechanisms of apoptosis include activating mitochondrial pathways, regulating the expression of Bcl-2 family proteins, promoting cytochrome c release, and activating caspase cascades. In addition, red yeast rice flavonin can block the cancer cell cycle, inhibit tumor cell proliferation, suppress tumor angiogenesis, and suppress tumor metastasis-related signaling pathways, demonstrating broad anti-tumor potential.
Monasoxanthin regulates lipid metabolism and anti-inflammatory effects, reduces damage to vascular endothelial cells, inhibits the formation of macrophage foam cells, lowers vascular wall inflammation, and slows the progression of atherosclerosis. Its mechanism involves activation of PPARγ and regulation of its downstream signaling pathways, improving vascular function and reducing lipid deposition in vessel walls.
The pharmacological effects of red yeast xiantin mainly depend on its regulation of various molecular targets, especially the activation of the nuclear receptor PPARγ. As a key regulator of lipid metabolism and inflammatory response, PPARγ promotes fatty acid metabolism and energy homeostasis by activating PPARγ, inhibiting the expression of inflammatory factors, and improving pathological conditions related to metabolic syndrome.
Additionally, red yeast rice flavonin affects various proteins related to lipid metabolism, including:
Monasfluxanthin also reduces inflammatory responses and promotes cancer cell apoptosis by inhibiting the NF-κB and MAPK signaling pathways, demonstrating its multi-target and multi-pathway comprehensive regulatory capability.
Druggability evaluation of red yeast fluxanthin indicates good drug development potential. Its molecular weight (386.4880) and LogP (3.97) comply with the Lipinski rule, indicating good oral bioavailability. The TPSA value is moderate, which is beneficial for transmembrane absorption. Low water solubility suggests the need to optimize formulations to improve dissolution and bioavailability.
Pharmacokinetic studies show that red yeast fluxanthin is rapidly absorbed orally, has high blood-brain barrier permeability, and has potential central nervous system activity. Its metabolic pathway mainly passes through the liver enzyme system, and its metabolites are safe. The hERG channel inhibition test was negative, indicating high cardiac safety. The Ames test result was negative, indicating a low risk of genotoxicity.
Monascus has a moderate half-life and is widely distributed in the body, mainly metabolized by the liver and excreted by bile. In the future, further systematic pharmacokinetic and toxicological studies are needed to clarify metabolic pathways and potential drug interactions in vivo.
As a versatile natural product, red yeast xiantin has broad clinical application prospects. Its potential in lowering blood lipids, anti-inflammation, anti-cancer, and anti-atherosclerosis, especially suitable as adjunctive therapy for metabolic syndrome, cardiovascular diseases, and tumors.
Currently, clinical research on red yeast rice flavonin is still in its early stages, and more clinical trials are needed in the future to verify its safety, efficacy, and dosage range. Due to its good oral activity and multi-target mechanism of action, asousoxanthin is expected to be developed as a novel lipid-lowering drug, anti-inflammatory drug, and antitumor drug.
Additionally, the blood-brain barrier permeability of red yeast xilavin offers potential applications in neurodegenerative diseases, such as Alzheimer's disease and other neurological disorders related to lipid metabolism disorders. By optimizing structure and improving formulations, enhancing its bioavailability and targeting will further drive its clinical translation.
As an important active ingredient in red rice fermented by Monascus musk, red yeast rice exhibits multiple pharmacological activities, especially in lipid metabolism regulation, anti-inflammatory, and anticancer fields. Its mechanism of action involves PPARγ and various lipid metabolism-related targets, offering good druggability and safety. In the future, through in-depth pharmacological mechanism research, systematic pharmacokinetic analysis, and clinical trial validation, red yeast rice flavanosin is expected to become a novel natural drug for treating metabolic diseases and tumors. With the development of modern drug development technologies, the clinical application prospects of red yeast rice flavin are promising.
Shenshuai
Wenjing
Hedandan
