Product name: Casuarictin
Synonym name: 1(β)-O-Galloylpedunculagin；a-Glucosidase inhibitor CB-3
Catalogue No.: BP5066
Cas No.: 79786-00-8
Formula: C₄₁H₂₈O₂₆
Mol Weight: 936.649
Botanical Source:
Type of Compound: Phenols

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.

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

Introduction/Overview

Casuarictin tannin is a natural polyphenolic compound with significant biological activity, belonging to the tannin family. Its molecular structure is complex, containing multiple phenolic hydroxyl groups, giving it excellent antioxidant and enzyme-inhibiting activities. In recent years, with in-depth research into the pharmacological effects of natural products, Casuarina Tanting, due to its potential application value in diabetes, neurodegenerative diseases, and antiviral fields, has gradually become a hot topic in pharmacology and drug development. This paper will systematically review the chemical structure, physicochemical properties, plant origin, and extraction methods of Casuarina tannin, focusing on its pharmacological activity, mechanism of action, and molecular targets. Combined with druggability evaluation and pharmacokinetic data, it explores its clinical application prospects and future research directions.

Chemical structure and physicochemical properties

The molecular formula of Casuarina tanning is C41H28O26, with a molecular weight of 936.6490, making it a high-molecular-weight polyphenolic compound. Its structural core is the typical polyphenol cyclic framework of tannins, containing multiple phenolic hydroxyl and ester bonds, giving it high polarity and rich hydrogen bond donor/acceptor properties. The LogP value is 1.7369, indicating moderate lipophilicity, which facilitates interaction with biofilms. Its topological pole surface area (TPSA) reaches as high as 444.18 Ų, reflecting strong polarity and extremely low water solubility (0.0009), which significantly affects its bioavailability and in vivo distribution. Casuarina tanning does not easily cross the blood-brain barrier, suggesting that its direct role in the central nervous system may be limited. Additionally, the hERG channel inhibition test results were negative, indicating a low risk of cardiotoxicity; The Ames test result was 0.6, indicating a low genotoxicity risk.

Plant Origins and Extraction Methods

Casuarina tanning is mainly found in the bark, leaves, and fruits of various plants, with abundant content especially in plants of the Casuarinaceae family. Common source plants include Casuarina spp. and plants with higher tannin content. The extraction method typically uses a mixed solvent system of polar solvents such as methanol, ethanol, or water, and produces crude extracts through ultrasound-assisted extraction, reflux extraction, or Soxhlet extraction. Subsequently, purification is performed using liquid-liquid partitioning, column chromatography (such as silica gel, C18 reversed-phase column), and high-performance liquid chromatography (HPLC), ultimately obtaining high-purity casuarina tanning pavilions. Identification methods mainly rely on modern analytical techniques such as mass spectrometry (MS), nuclear magnetic resonance (NMR), and infrared spectroscopy (IR) to ensure structural accuracy and purity.

Pharmacological activity research

α-glucosidase inhibitory activity

Casuarina tanning showed strong and competitive α-glucosidase inhibitory effects, with an IC50 value of 0.21 μg/mL, significantly outperforming many traditional inhibitors. This activity gives it potential value in diabetes treatment, as it can delay the digestion and absorption of carbohydrates, reduce postprandial blood sugar peaks, and thus improve blood sugar control.

Neuroprotection and Alzheimer's disease

As a prosento-aging stabilizing factor-like protein (PSFL) inhibitor, Casuarina Tanting demonstrates unique pharmacological potential in the field of neurodegenerative diseases. PSFL protein is closely related to neuropathological processes associated with Alzheimer's disease (AD), and its inhibition helps slow neuronal degeneration and cognitive decline. Casuarina tannin may intervene in the pathological progression of AD by regulating PSFL protein, making it a candidate molecule for neuroprotectants.

Anti-HIV activity

Casurina tanning exhibits inhibitory activity against various HIV-related targets, including the two main viral co-receptors CCR5 and CXCR4, as well as HIV1 protease (HIV1-PR), integrase, reverse transcriptase (RT), and the viral envelope protein gp120. Its multi-target inhibitory properties offer new ideas for anti-HIV drug development, especially with potential advantages in treating resistant strains.

Mechanism of action and molecular targets

Casuarina tanning has diverse mechanisms, mainly reflected in the following aspects:

1. Enzyme inhibition: By competitively binding to the active site of α-glucosidase, it blocks substrate binding, inhibits enzyme activity, and slows carbohydrate metabolism.

2. Protein-protein interaction regulation: As a PSFL protein inhibitor, Casurina tannin may stabilize neuronal function and slow neurodegenerative changes by directly binding to or modulating related signaling pathways.

3. Multi-target antiviral mechanism: Casuarina tanning inhibits multiple stages of the HIV replication cycle by interfering with viral entry to receptors (CCR5, CXCR4), inhibiting key viral enzymes (HIV1-PR, Integrase, RT), and blocking the binding of viral envelope protein gp120 to host cells.

4. Antioxidant and anti-inflammatory effects: Its rich phenolic hydroxyl structure endows it with powerful free radical scavenging ability, reduces oxidative stress, inhibits the release of inflammatory mediators, and protects cells from damage.

Druggability evaluation and pharmacokinetics

The large molecular weight (936.65 Da) and high polarity (TPSA 444.18 Ų) limit its oral bioavailability and membrane permeability. Water solubility is extremely low (0.0009), which may cause poor absorption in the body. Its moderate LogP value (1.7369) indicates certain lipid solubility, which is beneficial for cell membrane penetration, but overall excessive polarity remains a limiting factor. Low blood-brain barrier penetration capacity suggests that the central nervous system's efficacy may depend on indirect mechanisms or require special delivery system assistance.

In terms of safety, negative hERG channel inhibition reduces the risk of cardiotoxicity, and Ames trial results show a lower genotoxicity risk, meeting the safety requirements for early drug development. In the future, further in vivo pharmacokinetic (ADME) studies are needed to clarify its metabolic pathways, half-life, and tissue distribution, providing a basis for dosage formulation design and clinical application.

Prospects and outlooks for clinical applications

As a versatile natural product, Casuarina tanning has broad clinical application potential:

1. Diabetes Treatment: Its potent α-glucosidase inhibitory activity makes it an ideal candidate for controlling postprandial hyperglycemia. Through structural optimization and formulation improvement, it is expected that new oral hypoglycemic drugs will be developed.

2. Neurodegenerative diseases: PSFL protein inhibition targeting Alzheimer's disease provides new targets for neuroprotection. Combined with modern drug delivery technologies, such as nanocarrier systems, it can enhance intracranial delivery efficiency and improve treatment outcomes.

3. Anti-HIV drug development: The multi-target inhibitory properties offer new ideas for antiviral drug design, especially offering potential advantages in treating resistant strains. Can be used in combination with existing antiviral drugs to achieve synergistic effects.

4. Antioxidant and anti-inflammatory applications: Its natural antioxidant properties make it suitable for development as an adjunct therapy to alleviate oxidative stress and inflammatory responses related to chronic diseases.

Future research should focus on pharmacokinetic optimization, structural modification, formulation innovation, and preclinical safety evaluation of Casuarina tanning to promote clinical translation. In addition, it delves into the mechanisms of molecular action and its interactions with targets, providing a theoretical foundation for precision therapy.

Conclusion

As a natural polyphenolic compound with multiple pharmacological activities, Casuarina Tanting shows broad application prospects in diabetes, neurodegenerative diseases, and antiviral fields. Its unique chemical structure endows it with significant enzyme inhibition and multi-target regulation capabilities, making it an important subject for pharmacological research of natural products. Although its druggability faces certain challenges, through optimization of modern medicinal chemistry and pharmaceutics, Casuarina Tanning Pavilion is expected to develop into a new generation of functional drugs. Future systematic research will further reveal its mechanism of action, promote its clinical translation and drive innovative development of natural product drugs.