Product name: Yixingensin
Synonym name: Ombuin 3-O-β-D-glucopyranoside; Ombuin-3-O-β-D-glucoside; Ombuin-3-O-glucoside
Catalogue No.: BP2269
Cas No.: 158642-42-3
Formula: C₂₃H₂₄O₁₂
Mol Weight: 492.433
Botanical Source:
Type of Compound: Flavonoids

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.

NMR of Yixingensin

HPLC of Yixingensin

Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃

Introduction/Overview

Yixingensin, also known as Phytolacca 3-glucoside, is a natural flavonoid compound derived from the traditional Chinese medicinal plant Phytolacca acinosa Roxb. Its molecular formula is C_24H_28O_11, CAS number 158642-42-3, and it has attracted widespread attention in recent years due to its potential pharmacological activity, especially its value in respiratory diseases. As a chronic inflammatory disease of the airways, asthma involves multiple inflammatory mediators and signaling pathways, seriously affecting patients' quality of life. Crocoticin exhibits significant antiasthmatic activity by regulating various inflammation-related targets, making it a hot topic in natural product pharmacological research.

This paper systematically reviews the pharmacological activity, mechanism of action, and molecular targets of cocoticuloflavin, focusing on its chemical structure, physicochemical properties, plant origins, and extraction methods. Combining druggability evaluation and pharmacokinetic data, it explores its clinical application prospects, aiming to provide theoretical basis and research directions for the development of natural anti-asthma drugs.

Chemical structure and physicochemical properties

Fluxanthin belongs to the flavonoid class, specifically the 3-position glucoside derivative of Phytolacin xanthus. Its molecular weight is 492.4330, and its molecular structure contains multiple hydroxyl groups and glycosyl groups, giving it high polarity and water solubility. The LogP value was 0.3433, indicating strong hydrophilicity, which is beneficial for distribution but may limit its ability to penetrate lipid membranes. The topological pole surface area (TPSA) is 188.5100, indicating high polarity and is usually negatively correlated with the molecule's ability to pass through the cell membrane.

Water solubility is 1.4148, supporting its good solubility in the aqueous phase, which is beneficial for the development of oral formulations. The low permeability of the blood-brain barrier suggests its effect is mainly limited to peripheral tissues, reducing the risk of central nervous system side effects. The hERG channel inhibition test was negative, indicating a low risk of coraciflavin cardiotoxicity. The Ames test result was 0.6, indicating a low genotoxicity risk and good safety.

Plant Origins and Extraction Methods

Oxanthin is mainly found in the roots and fruits of Phyloca plants. Pollack pokeweed is a perennial herbaceous plant widely distributed in southern China and Southeast Asia. In traditional Chinese medicine, it is used to clear heat, detoxify, reduce swelling, and disperse nodules. Its roots are rich in active ingredients such as flavonoids, saponins, and polysaccharides.

Common methods for extracting flavonoids include:

1. Solvent extraction method: Using ethanol or methanol as extraction solvents, with reflux or ultrasound assistance, can effectively extract flavonoid components. The extract is purified through concentration, separation, and column chromatography to obtain high-purity xoryfroxin.

2. Supercritical fluid extraction: Using supercritical CO_2 as the solvent combined with ethanol assistance, it offers high extraction efficiency and environmental friendliness, suitable for industrial production.

3. High-Performance Liquid Chromatography (HPLC) Purification: Extracts are separated and purified to ensure the purity and structural integrity of rhinocerosin.

In recent years, combining modern extraction technologies and separation methods, the extraction efficiency and purity of cocoticlastin have significantly improved, laying a foundation for its pharmacological research and clinical application.

Pharmacological activity research

Cocotaxanthin exhibits significant anti-inflammatory, antioxidant, and immunomodulatory activities in various in vitro and in vivo models, with particular attention for its role in respiratory diseases such as asthma.

Anti-asthmatic activity

The pathological features of asthma include airway hyperresponsiveness, chronic inflammation, and airway remodeling. Cocoscarflavin reduces airway inflammation and allergic reactions by regulating various inflammatory mediators and signaling pathways.

1. Inhibition of inflammatory factor expression: Chycofrexanthin significantly downregulates Th2 cell-related cytokines such as IL-4, IL-5, and IL-13, reducing airway eosinophil infiltration and suppressing IgE-mediated allergic reactions.

2. Regulates immune cell function: By acting on the FCER1A receptor, it regulates the activation of mast cells and basophils, reduces histamine release, and relieves airway spasms.

3. Antioxidant effect: By scavenging free radicals, it reduces oxidative stress damage to airway epithelial cells, protecting airway structural integrity.

4. Improves airway hyperresponsiveness: acts on ADRB2 receptors, regulates smooth muscle relaxation, and relieves airway spasms.

Other potential pharmacological effects

Besides anti-asthma, cocoslavin also exhibits certain anti-tumor, antibacterial, and neuroprotective effects, but related research is still in its early stages and requires further validation.

Mechanism of action and molecular targets

The mechanism of action of coco-regulated multi-target flavonoids mainly involves immune regulation, inflammation suppression, and airway smooth muscle relaxation, among other aspects.

Main molecular targets

• CHRM3 (M3-type cholinergic receptor): regulates airway smooth muscle contraction; cocoslavin relieves airway spasms by antagonizing CHRM3.

• ADRB2 (β2 adrenergic receptor): promotes relaxation of airway smooth muscle; cocochlostlavin can enhance ADRB2 signaling and improve airway patency.

• HRH1 (Histamine H1 receptor): mediates allergic reactions; cocochoflavin inhibits HRH1 activity and reduces histamine-induced airway inflammation.

• IL4, IL5, IL13: Key Th2 cell secretion factors that drive asthma inflammation. Crochetin downregulates the expression of these cytokines and inhibits the inflammatory cascade.

• FCER1A (high-affinity IgE receptor α chain): regulates mast cell activation; cocoticsulfanin blocks FCER1A-mediated signaling, reducing allergic reactions.

• IL17A, PTGDR2, IL25: Involved in airway inflammation and immune regulation, cococarflin's regulation of these targets helps suppress chronic inflammation and airway remodeling.

Signal path regulation

Cocofrexanthin reduces the release of inflammatory mediators and lowers airway inflammatory responses by inhibiting the NF-κB and MAPK signaling pathways. At the same time, it regulates the JAK/STAT pathway, inhibits Th2 cell differentiation, and restores immune balance.

Druggability evaluation and pharmacokinetics

The druggability parameters of cocoflavin indicate that it has good potential for drug development.

• Molecular weight and polarity: molecular weight 492.4330, TPSA 188.5100. Although relatively high, it is suitable for lung-targeted administration to reduce systemic side effects.

• Water solubility and lipid solubility: Good water solubility (1.4148), LogP 0.3433, beneficial for formulation design and in vivo absorption.

• Low blood-brain barrier permeability: reduces the risk of central nervous system toxicity, suitable for treating peripheral diseases.

• Safety: hERG channels have no inhibitory effect; Ames test results show low genotoxicity and relatively high safety.

Pharmacokinetics, cocoflavin is absorbed orally relatively quickly, and its bioavailability is limited by the hydrolysis and metabolism of glycoside structures. Its distribution in the body is mainly concentrated in the lungs and liver, with metabolic pathways primarily being hepatic enzymatic hydrolysis and glucosidase action, and excretion primarily via the kidneys. Moderate half-life and supports routine dosing regimens.

Prospects and outlooks for clinical applications

With deeper understanding of asthma pathogenesis, natural products have become drug candidates with multiple targets and multiple pathways, demonstrating unique advantages. With its remarkable anti-inflammatory, immunomodulatory, and airway protective effects, cocoslavin has the potential to become a new anti-asthma medication.

Future clinical application prospects include:

1. Adjunctive asthma therapy: serves as a supplement to traditional hormones and β2 agonists, reducing drug side effects and resistance risks.

2. Chronic airway inflammatory diseases: For chronic obstructive pulmonary disease (COPD), the anti-inflammatory effects of coracin are also applicable.

3. Combination Medication Strategy: Combine with existing drugs to achieve synergistic effects and improve treatment outcomes.

4. New dosage form development: inhalation formulations, nanocarrier systems, etc., to improve lung targeted drug delivery efficiency.

However, the clinical translation of coflavin still faces challenges, such as pharmacokinetic optimization, dose safety evaluation, and large-scale clinical trials, all requiring multidisciplinary collaboration.

Conclusion

As a natural flavonoid compound with multi-target regulatory capabilities, cocosulfurin shows broad application prospects in the treatment of asthma and related respiratory diseases. Its excellent safety and druggability parameters lay the foundation for subsequent drug development. In the future, combining modern medicinal chemistry, molecular biology, and clinical research, in-depth elucidation of the mechanisms of action and pharmacokinetic characteristics of cocofilavin will help promote its transition from the laboratory to clinical practice, benefiting a wide range of patients. The ongoing development of natural product pharmacology will provide more innovative treatment options for complex diseases such as asthma.