Product name: Pellitorine
Synonym name:
Catalogue No.: SBP02918
Cas No.: 18836-52-7
Formula: C₁₄H₂₅NO
Mol Weight: 223.36
Botanical Source:
Type of Compound:

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

Pellitorine (CAS No.: 18836-52-7) is a natural amide compound originally isolated from various plants, attracting attention for its unique structure and diverse biological activities. In recent years, with the deepening development of natural product pharmacology, wall-me-straw aline has demonstrated significant pharmacological potential in multiple fields, including anti-inflammatory, anti-pain, cognitive function improvement, antithrombotic effects, anti-cancer, and anti-infection. Its mechanism of action involves multiple signaling pathways and molecular targets, with outstanding performance in its antagonism of TRPV1 receptors, activation of the BDNF-ERK1/2-CREB pathway, and regulation of the Nrf2-HO-1 antioxidant defense system. Additionally, wall-patch aline plays a role in sepsis and antithrombosis by regulating HMGB1, RAGE/TLR4, and coagulation factor activities, demonstrating broad clinical application prospects. This paper will systematically review the chemical structure, plant origin, pharmacological activity, mechanism of action, druggability evaluation, and future development direction of Wallgrass alkaloid, aiming to provide theoretical basis and reference for research and development in related fields.

Chemical structure and physicochemical properties

Wall-grass aline is a natural amide compound with a molecular formula of C15H27NO and a molecular weight of 223.36. Its structural feature is a long-chain fatty amide backbone, containing a fatty acid side chain connected to an amino group, making it a natural product of the fatty amide class. The LogP value of wall-grass aline is 3.98, indicating good lipid solubility and facilitating cell membrane penetration; the polar surface area (TPSA) is 38.33 Ų, with 2 hydrogen bond receptors, indicating moderate polarity and potentially affecting bioavailability and targeting. Although it has high lipid solubility, its ability to penetrate the blood-brain barrier is relatively low, suggesting that its direct effect in the central nervous system may be limited. Druggability evaluations showed that wall-to-bark aline had no significant hepatotoxicity, cardiotoxicity, or hERG channel inhibitory effects, and its safety was good. However, Ames' mutagenicity remains unclear and requires further toxicological research support.

Plant Origins and Extraction Methods

Pellionia mainly comes from various traditional medicinal plants, especially Pellionia and its related species. Common plants include Pellionia repens and plants of the Pepper family. Traditionally, these plants have been used in folk remedies for pain relief, anti-inflammation, and anti-infection.

The extraction method typically uses organic solvent extraction combined with column chromatography for separation. The specific steps include:
1. Using ethanol or methanol as solvent for reflux extraction of dried plant materials;
2. After the crude extract is concentrated by rotary evaporation, purification is performed using silica gel column chromatography or high-performance liquid chromatography (HPLC);
3. Confirm the structure using techniques such as mass spectrometry (MS) and nuclear magnetic resonance (NMR).

In recent years, the application of ultrasound-assisted extraction (UAE) and supercritical fluid extraction (SFE) technologies has improved the extraction efficiency and purity of wallgrass alkaloids, laying the foundation for its large-scale production.

Pharmacological activity research

Anti-chronic pain effects

Wallgrass can competitively antagonize the transient receptor potential vanillate receptor 1 (TRPV1), blocking capsaicin-induced receptor activation and reducing pain signal transmission. TRPV1 is an important ion channel for sensing heat pain and inflammatory pain. Wallgrassine regulates it and demonstrates significant analgesic effects. Additionally, wall-tizine promotes neural plasticity and pain regulation by upregulating brain-derived neurotrophic factor (BDNF), activating mitogen-activated protein kinase 1/2 (ERK1/2) and cyclic adenosine phosphate reactive element binding protein (CREB) signaling pathways, thereby alleviating chronic pain symptoms.

Improves cognitive impairment

In cognitive dysfunction models, wall-me-l'azine promotes neuronal survival and synapse formation by activating the BDNF-ERK1/2-CREB pathway, thereby improving learning and memory abilities. At the same time, wall-clown upregulated nuclear factor E2-related factor 2 (Nrf2) and its downstream antioxidant enzyme Heme oxygenase 1 (HO-1), enhancing cellular antioxidant capacity and reducing oxidative stress damage. It regulates glutathione peroxidase 4 (GPX4) and dihydroolactyl acid dehydrogenase (DHODH), effectively inhibiting lipid peroxidation, combating ferroptosis, and providing a molecular basis for neuroprotection.

Anti-inflammatory and anti-septic effects

Wall-bare blocks activation of downstream nuclear factor κB (NF-κB) signaling pathway by inhibiting the release of high-mobility group protein B1 (HMGB1) and its receptors RAGE (AGER) and Toll-like receptor 4 (TLR4), reducing the secretion of pro-inflammatory factors such as tumor necrosis factor α (TNF-α) and interleukin-6 (IL-6), significantly alleviating inflammatory responses. This mechanism is particularly prominent in sepsis models. Wallgrass aline regulates immune inflammatory responses and reduces the risk of multi-organ injury, offering potential clinical value.

Antithrombotic effect

Wallgrass aline can prolong clotting time, inhibit key coagulation factors (such as thrombin F2, factor Xa F10) and the platelet glycoprotein IIb/IIIa complex (ITGA2B/ITGB3), blocking platelet aggregation and fibrin formation. At the same time, its regulation of plasminogen activator inhibitor-1 (SERPINE1) and angiotensin-converting enzyme (ACE) further exerts antithrombotic effects, suggesting its potential in the prevention and treatment of thrombosis-related diseases.

Anticancer and antibacterial activities

Wallgrass alkaloid exhibits inhibitory effects on various tumor cell lines, especially showing significant cell proliferation inhibition and apoptosis induction effects in leukemia and breast cancer cells. Its anti-cancer mechanisms involve cell cycle arrest, activation of apoptotic signaling, and regulation of antioxidant defense systems. Additionally, wall-bladderine exhibits antibacterial activity against various bacteria, possibly by disrupting cell membrane integrity and suppressing key enzyme activities.

Kills Aedes aegypti larvae

Wallgrass alkaloid disrupts ion ion balance and water regulation in Aedes mosquito larvae by inhibiting V-type H⁺-ATPase and Aaqueductin 4 (Aaqpop4), thereby exerting insecticidal effects and providing new ideas for mosquito-borne disease control.

Mechanism of action and molecular targets

The multi-target mechanism of wall-cut alkaloid reflects its broad pharmacological activity:

• TRPV1 receptor: Wall-methyl alkaloid acts as a competitive antagonist, blocking capsaicin-induced ion channel activation and reducing pain signaling.
• BDNF-ERK1/2-CREB pathway: promotes neuronal survival and synaptic plasticity, improving cognitive function.
• Nrf2-HO-1 antioxidant pathway: enhances cellular antioxidant capacity, reducing oxidative stress and inflammatory damage.
• HMGB1-RAGE/TLR4-NF-κB signaling axis: inhibits pro-inflammatory factor expression, exerting anti-inflammatory and anti-sepsis effects.
• Coagulation factors and platelet glycoprotein complexes: inhibit coagulation cascades and prevent thrombosis.
• GPX4 and DHODH: Inhibit lipid peroxidation, resist ferroptosis, and protect nerve cells.
• V-type H⁺-ATPase and AaAQP4: disrupt mosquito ion and water homeostasis, achieving insecticidal effects.

In addition, wall-patch aline also exhibits certain inhibitory activity against malaria-related targets such as PFCRT, PFMDR1, and PFDHFR, suggesting its potential application in the antimalarial field.

Druggability evaluation and pharmacokinetics

Wallazine has a moderate molecular weight (223.36), high lipid solubility (LogP=3.98), and moderate polarity, which facilitates cell membrane penetration and distribution in vivo. Its low permeability to the blood-brain barrier may limit its direct effect in the central nervous system, but it can still exert cognitive and analgesic effects by modulating peripheral nerves and indirect signaling pathways. It is relatively safe in vivo, with no significant hepatotoxicity, cardiotoxicity, or hERG channel inhibition, reducing the risk of cardiovascular adverse reactions.

Currently, pharmacokinetic data on wall-based line are limited. Preliminary studies show that its oral bioavailability is moderate, and its metabolism mainly occurs through hepatic enzyme systems. The metabolites and excretion pathways still need further clarification. In the future, systematic ADME (Absorption, Distribution, Metabolism, Excretion) studies and toxicological evaluations are needed to support clinical development.

Prospects and outlooks for clinical applications

With its multi-target and multi-pathway pharmacological properties, wall-patched alkaloid demonstrates broad application potential in chronic pain, cognitive dysfunction, inflammatory diseases, thrombosis, and tumor treatment. Especially in current chronic pain management and neurodegenerative disease treatment, wall-me-l'azine offers a new therapeutic strategy as a TRPV1 antagonist and neurotrophic factor modulator.

In addition, the effects of wall-on-the-wall alkaloid in antiseptic and antithrombotic effects make it possible for adjunctive treatment in critically ill patients. Its anticancer and antibacterial activities also lay the foundation for the development of novel anti-tumor and anti-infective drugs. Combined with its ability to kill Aedes aegypti larvae, wall-grass aline may also be applied in vector control in public health.

Future research should focus on:
1. Systematic evaluation of the pharmacokinetics and toxicology of wall-me-gum;
2. Structural optimization and derivative design to improve bioavailability and targeting;
3. In-depth analysis of multi-target mechanisms to reveal their synergistic effects;
4. Preclinical and clinical trials to verify safety and efficacy.

Through interdisciplinary collaboration, wall-and-stone is expected to develop into a versatile natural drug candidate molecule to meet diverse clinical needs.

Conclusion

As a natural amide compound with rich biological activity, wall-based soda has demonstrated unique research value and application prospects in the field of natural product pharmacology. Its multi-target, multi-mechanism pharmacological effects offer new approaches for treating chronic pain, cognitive impairment, inflammation, thrombosis, and tumors. Although pharmacokinetics and clinical research on wall-me-l'aline are still in their early stages, its good safety and broad pharmacological activity make it a natural drug candidate worthy of further development. In the future, through systematic mechanistic research and clinical validation, wall-based sinline is expected to become an important representative in the development of natural product drugs, contributing new treatment options to human health.