Product name: Hamaudol
Synonym name: (3'S)-(-)-Hamaudol
Catalogue No.: BP2082
Cas No.: 735-46-6
Formula: C₁₅H₁₆O₅
Mol Weight: 276.288
Botanical Source: Saposhnikoviae Radix
Physical Description:
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.

HPLC of Hamaudol

HNMR of Hamaudol

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

Introduction/Overview

Hamaudol (CAS No.: 735-46-6) is a natural chromite compound isolated from the traditional Chinese medicinal herb Saposhnikovia divaricata. As one of the main active ingredients in saposhng, Hemaofen has attracted widespread attention for its significant anti-inflammatory effects and its inhibitory activity against cyclooxygenase (COX) enzymes. In recent years, as the incidence of inflammatory diseases continues to rise, the potential therapeutic value of Hemaofen in various chronic inflammatory diseases such as inflammatory bowel disease, rheumatoid arthritis, psoriasis, osteoarthritis, and gout has gradually been revealed. This paper aims to systematically review the chemical structure and physicochemical properties of Hymafen, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and clinical application prospects, providing theoretical basis and reference for research in the fields of natural product pharmacology and new drug development.

Chemical structure and physicochemical properties

Hemaofen is a typical chromone compound, with a molecular formula of C_16H_16O_5 and a molecular weight of 276.2880. Its structural features include a benzene ring with polyhydroxyl substitution and a chromone core structure, giving it strong biological activity. In terms of physicochemical properties, the LogP value of Hymafurol is 1.8048, indicating moderate lipid solubility, which is beneficial for cell membrane penetration and bioavailability. Its topological pole surface area (TPSA) is 79.9 Ų, indicating moderate polarity, which may affect its absorption and distribution characteristics. Low water solubility (0.1793 mg/mL) suggests limited solubility in the aqueous phase, suggesting that bioavailability may be improved through formulation techniques. The blood-brain barrier has a low penetration ability, reducing the risk of central nervous system side effects. The hERG channel inhibition test was negative, indicating a low risk of hemothol cardiotoxicity. The Ames test result was 0.6, indicating a low genotoxicity risk and meeting safety requirements.

Plant Origins and Extraction Methods

Hiphofen is mainly extracted from the roots of Saposhnikovia divaricata. Saposhnikovia is a plant in the Apiaceae family, widely distributed in Northeast and North China, and has long been used in traditional Chinese medicine to treat wind-cold colds, headaches, rheumatic pain, and other conditions. The extraction of Hemaofen is usually done using organic solvent extraction combined with chromatography separation technology. Specific methods include:

1. Raw material processing: Select dried windbreak roots and crush them to an appropriate particle size.
2. Solvent extraction using ethanol or methanol as solvent, with reflux or ultrasound-assisted extraction, generally taking 2-4 hours.
3. Crude extract concentration: Vacuum concentration removes most of the solvent to obtain concentrated extracts.
4. Separation and purification: Using silica gel column chromatography or high-performance liquid chromatography (HPLC) technology, combined with gradient elution, to separate and purify haimafen.
5. Structural identification: Confirm the structure using nuclear magnetic resonance (NMR), mass spectrometry (MS), and infrared spectroscopy (IR).

In recent years, supercritical CO_2 extraction and membrane separation technologies have also been attempted to improve extraction efficiency and purity, reduce solvent residues, and promote industrial production.

Pharmacological activity research

The pharmacological activity of Hemaofen mainly focuses on its anti-inflammatory and analgesic effects. Its inhibitory effect on cyclooxygenase (COX)-1 and COX-2 is central to its anti-inflammatory mechanism. Experimental data showed that the IC_50 of Hemaofen for COX-1 and COX-2 were 0.30 mM and 0.57 mM respectively, demonstrating effective inhibitory ability against both enzymes, with particularly strong selective inhibition of COX-1.

Anti-inflammatory effects

Both in vivo and in vitro experiments have confirmed that Hymaofen has significant anti-inflammatory effects. In the mouse acute inflammation model, haimaofol can significantly inhibit the release of inflammatory mediators, reducing tissue edema and infiltration of inflammatory cells. Its anti-inflammatory effects are not limited to inhibiting COX enzyme activity, but also involves regulation of various inflammatory signaling pathways.

Analgesic effect

Hemurofen exerts analgesic effects by inhibiting the synthesis of inflammatory mediators and reducing prostaglandin (PGs) levels. In animal experiments, Hemophenol significantly prolonged the latency period of pain caused by thermal and chemical stimuli, demonstrating good analgesic activity.

Other pharmacological effects

Some studies suggest that Hemaofen also has antioxidant and immunomodulatory effects, but the related mechanisms require further clarification.

Mechanism of action and molecular targets

The mechanism of action of Hemaofen is complex, involving multiple signaling pathways and molecular targets, and its regulatory role in inflammatory diseases is especially noteworthy.

Cyclooxygenase inhibition

Hemaofen inhibits prostaglandin synthesis and alleviates inflammatory responses by competitively binding to the active sites of COX-1 and COX-2. This mechanism is similar to nonsteroidal anti-inflammatory drugs (NSAIDs), but their lower hERG suppression and genotoxicity risk may provide better safety.

Regulation of inflammation-related signaling pathways

Hemaofen affects various inflammation-related targets, including key factors such as nuclear factor κB (NF-κB), signal transduction and transcription activator factor 3 (STAT3), tumor necrosis factor α (TNF-α), and interleukin 6 (IL-6). For example:

• Inflammatory bowel disease (IBD): Hemaofen regulates targets such as AMPK, NOTCH1, IDO1, TLR4, and STAT3, inhibits inflammatory cascades, and improves intestinal barrier function.
• Rheumatoid arthritis (RA): inhibits immune cell activation and the release of inflammatory mediators by regulating BCL2, TLR4, STAT3, ALOX5, and others.
• Psoriasis: Affects signaling pathways such as RARA, RARG, MAPK1, TNF, and NOS2, reducing epidermal cell proliferation and inflammation.
• Osteoarthritis and gout: regulates MMP1, PTGS1/2, NFKB1, IL6, IL1B, NLRP3, and inhibits joint inflammation and cartilage degradation.

Immune regulation and antioxidant effects

Hemaofen enhances cellular antioxidant capacity by activating the NFE2L2 (NRF2) signaling pathway, reducing tissue damage caused by oxidative stress. At the same time, its regulation of immune regulatory molecules helps restore immune homeostasis and reduce chronic inflammation.

Druggability evaluation and pharmacokinetics

The druggability parameters of Hymafure indicate that it has good drug development potential:

• The molecular weight (276.2880) is moderate, complying with the Lipinski rule, which is beneficial for oral absorption.
• LogP (1.8048) shows moderate lipid solubility, aiding membrane penetration.
• TPSA (79.9 Ų) indicates moderate polarity, which is beneficial for absorption and distribution.
• Low water solubility (0.1793 mg/mL) suggests the need for pharmacological methods to improve solubility and bioavailability.
• Blood-brain barrier penetration ability is low, reducing the risk of adverse reactions in the central nervous system.
• hERG channel inhibition negative, reducing the risk of cardiotoxicity.
• A negative Ames test (0.6) indicates a low genotoxicity risk.

Pharmacokinetics: Hemaofen is well absorbed orally, but due to water solubility, its bioavailability may be affected. Metabolism in the body mainly occurs through hepatic enzyme systems, and the safety of these metabolites still requires further research. The main excretory routes are the kidneys and bile.

Prospects and outlooks for clinical applications

As a natural chromotone-type anti-inflammatory active ingredient, Haimaofen has broad clinical application potential. Its targeted effects in various inflammatory diseases provide important clues for the development of novel anti-inflammatory drugs. The future clinical application prospects of Hemaofen are mainly reflected in the following aspects:

1. Development of anti-inflammatory and analgesic drugs: Based on its inhibition of COX enzyme and multi-target regulation, Hemaofen can serve as a candidate compound for novel nonsteroidal anti-inflammatory drugs (NSAIDs), especially suitable for adjunctive treatment of chronic inflammatory diseases.
2. Inflammatory bowel disease and autoimmune diseases: By regulating signaling pathways such as AMPK, STAT3, and TLR4, Hemaofen is expected to improve intestinal inflammation and immune imbalance, making it a potential therapeutic agent for inflammatory bowel disease and rheumatoid arthritis.
3. Treatment of skin diseases: For inflammatory skin diseases such as psoriasis, Hemaofen regulates various inflammatory factors and cell proliferation signals, showing potential for the development of topical formulations.
4. Combination Strategies: Hemaofen can be used in combination with other anti-inflammatory drugs to create synergistic effects, reducing single-agent dosage and side effects.

However, the clinical translation of Hemaofen still faces many challenges, including improvements in water solubility and bioavailability, systematic safety evaluation, pharmacokinetic optimization, and large-scale clinical trial validation. Future research should integrate modern medicinal chemistry, pharmaceutics, and molecular biology techniques to deeply reveal its mechanisms of action, optimize formulation design, and promote clinical application.

Conclusion

Hemaofen, a natural chromoketone compound derived from saposhnikola, shows broad application prospects in the treatment of inflammatory diseases due to its remarkable anti-inflammatory activity and multi-target regulatory effects. Its favorable druggability parameters and low safety risks provide favorable conditions for new drug development. In the future, through systematic pharmacological mechanism research, pharmacokinetic optimization, and clinical validation, Hemaofen is expected to become an important candidate for the development of natural anti-inflammatory drugs, promoting the application and development of natural medicines in modern medicine.