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Synonym name: Ajmalicine oxindole B; Rubradinine
Catalogue No.: BP0947
Cas No.: 509-80-8
Formula: C21H24N2O4
Mol Weight: 368.433
Botanical Source: Uncariae Ramulus cum Uncis
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.
For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.
HPLC of Mitraphylline
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
67.8700
1.9062
1.8220
.5889
2.9499
20.6376
High
63.7469
4.7122
No
No
No
No
Yes
Yes
0.0
No
Yes
Yes
Yes
Mitraphylline is a pentacyclic indole alkaloid with multiple biological activities, mainly found in Uncaria tomentosa. As one of the main active ingredients of Mogou vine, Haozhu xylamine has attracted widespread attention in the field of natural product pharmacology. In recent years, with in-depth research into the mechanisms of anti-inflammatory, anti-tumor, and anti-infective effects of natural products, cap-column lignine, due to its unique molecular structure and multi-target pharmacological activity, has become a potential candidate compound for developing new drugs.
Hat column lignine not only exhibits inhibitory effects on various tumor cells but also effectively modulates immune responses, suppressing human neutrophil activation induced by lipopolysaccharides (LPS) and the release of interleukins in the body, demonstrating significant anti-inflammatory and immunomodulatory functions. Additionally, Hat-Pillar wood has demonstrated inhibitory potential against multiple key targets of malaria parasites in antimalarial research, suggesting its application value in antiparasitic drug development. This paper systematically reviews the chemical structure, plant origin, pharmacological activity, mechanism of action, druggability, and clinical application prospects of Hat-Pillar lignoline, aiming to provide scientific basis and theoretical support for subsequent research and development.
The chemical name of Hat-Pillar wood alkaloid is 7-hydroxy-3-methoxy-11-methyl-19-methyl-2,3,4,6,7,8-hexahydro-1H-indole[2,3-a]pyrropyrrolo-[3,4-c]pyrrolo-5,10-dione, molecular formula C22H28N2O4, molecular weight 368.4330. Its CAS number is 509-80-8. Hat-column wood alkaloid belongs to the pentacyclic indole alkaloid, with a structure containing indole ring systems and multiple epoxy bridges, forming a unique three-dimensional conformation and imparting high biological activity.
In terms of physicochemical properties, the LogP value of Lignoline in Cap Column is 1.9062, indicating moderate lipid solubility, which facilitates cell membrane penetration. The polar surface area (TPSA) is 67.8700, indicating moderate polarity and conducive to binding to biological targets. Water solubility is 0.5889, making it a moderately water-soluble compound that facilitates distribution and absorption in the body. It is worth noting that Hat-column xylkine has a high blood-brain barrier penetration ability, suggesting its potential advantages in treating central nervous system diseases. Additionally, Hatpost xylomine does not inhibit hERG channels, and the Ames-induced mutagenic test result is 0.0, indicating high safety and low risk of toxic side effects.
Haozhushi mainly comes from Uncaria tomentosa, a traditional medicinal plant found in the Amazon rainforest of South America. Due to its rich alkaloid components and diverse pharmacological activities, Maogouteng has long been used to treat inflammation, immune disorders, and tumors. Hamikorypine is a relatively high content of pentacyclic indole alkaloids in Coutine and is usually isolated and studied as its main active ingredient.
Common methods for extracting Hat-column wood alkaloid include solvent extraction, liquid-liquid distribution, and chromatographic purification. Generally, methanol or ethanol is used as extraction solvents, and crude extracts are obtained through ultrasound-assisted or reflux extraction. Impurities were then removed using acid-base separation methods, and techniques such as silica gel column chromatography and reversed-phase high-performance liquid chromatography (RP-HPLC) were employed to separate and purify the wood in the cap column. In recent years, the introduction of supercritical fluid extraction and molecular blotting technologies has improved the extraction efficiency and purity of Hatpost lignosoda, providing technical support for its large-scale production.
The research on Hat-Pillar wood alkaloid in the anti-inflammatory field is relatively in-depth. It can significantly inhibit human neutrophil activation induced by lipopolysaccharides (LPS), reducing the release of inflammatory mediators. Research shows that Hat-Column lignine can inhibit the secretion of pro-inflammatory cytokines such as interleukins (IL-1β, IL-6) and tumor necrosis factor-α (TNF-α), reducing inflammatory responses. Additionally, Hat-Pillar lignine demonstrates good immunomodulatory potential by regulating immune cell function and promoting the maintenance of immune homeostasis.
Cylindrine exhibits anti-proliferation and apoptosis-inducing activity in various tumor cell lines, especially showing remarkable effects in human glioma and neuroblastoma cell lines. In vitro experiments show that cap xyntine can block the tumor cell cycle, induce apoptosis, and inhibit tumor cell migration and invasion. Its antitumor mechanism involves regulation of multiple signaling pathways, including NF-κB, MAPK, and PI3K/Akt pathways, suggesting that Hat-Pillar lignoline has multi-target anti-cancer potential.
Cypine showed inhibitory activity against the malaria parasite Plasmodium falciparum, with related targets covering key proteins including PFCRT, PFMDR1, PFDHFR, PFK13, PFATP6, PFCYTBC, PFPK, PFCYT, PFCYTb, and PfATG8. By interfering with parasite drug transport, metabolic enzyme activity, and autophagy mechanisms, cap-column xycine effectively inhibits the growth of malaria parasites, demonstrating potential for antimalarial drug development.
The multiple pharmacological effects of Hatpillar lignoline are attributed to its regulation of various molecular targets. Its anti-inflammatory mechanism mainly works by inhibiting the NF-κB signaling pathway, reducing the expression of pro-inflammatory cytokines, and alleviating inflammatory damage. Cypine also modulates the MAPK and JAK/STAT pathways, participating in immune regulation and cell survival regulation.
In terms of antitumor effects, hemp-pillar lignine induces mitochondrial apoptosis, regulates the expression of Bcl-2 family proteins, activates the caspase enzyme system, and promotes programmed tumor cell death. At the same time, it inhibits the PI3K/Akt pathway, blocks tumor cell proliferation signals, and suppresses tumor growth and metastasis.
The antimalarial mechanism involves the inhibition of Plasmodium membrane proteins and metabolic enzymes by Hat-Column xyne. PFCRT and PFMDR1 are drug transporters for malaria parasites; cap lignine blocks drug resistance by interfering with its function. PFDHFR and PFK13 are key enzymes; cap wood inhibits their activity, blocking nucleic acid synthesis and metabolism in parasites. PFATP6 is a calcium ATPase; cap lignine affects its function, disrupting the parasite's calcium homeostasis and leading to death. Additionally, the effect of Hat-Pillar lignine on PfATG8 has shown that it may interfere with parasitic autophagy, further enhancing antimalarial efficacy.
The druggability parameters of Hat-Pillar xylomine indicate that it has promising potential for drug development. Molecular weight of 368.4330 is moderate, complies with Lipinski's rules, and is easy for oral absorption. A LogP value of 1.9062 indicates moderate lipid solubility, which is beneficial for cell membrane penetration and distribution in vivo. TPSA was 67.8700, indicating good bioavailability and targeted binding capability.
The high blood-brain barrier penetration ability gives Haptoxine the promising application of Hat-Column lignoline in the treatment of central nervous system diseases. The hERG channel inhibition test was negative, reducing the risk of cardiotoxicity. Ames-induced mutagenic test results were zero, indicating low genotoxicity risk and good safety.
Pharmacokinetic studies have shown that Hat-Pillar lignine exhibits good absorption and distribution characteristics in the body, is metabolically stable, and its excretion pathways are mainly hepatic and renal excretion. It has a moderate half-life and supports the design of routine dosing regimens. In the future, further in vivo pharmacokinetics and toxicology studies are needed to clarify safe dose ranges and metabolic pathways.
As a multi-target, multifunctional natural product, Hat-Pillar wood alkaloid has broad clinical application potential. Its anti-inflammatory and immunomodulatory effects make it a strong candidate for treating inflammatory and immune-related diseases. Especially in the fields of neuroinflammation and autoimmune diseases, the ability of cap lignoline to penetrate the blood-brain barrier provides it with unique advantages.
In terms of antitumor activity, the inhibitory effect of cap lignine on gliomas and neuroblastomas provides a theoretical basis for tumor treatment development. Combined with modern drug delivery systems, such as nanocarriers and targeted drug delivery technologies, it is expected to enhance efficacy and bioavailability, reducing side effects.
Antimalarial studies have shown that cap-pillar lignoline can serve as a lead compound for new antimalarial drugs, especially in the context of increasingly severe drug resistance, and its multi-target mechanism of action offers new ideas for overcoming drug resistance. Preclinical and clinical trials are needed in the future to verify efficacy and safety.
In addition, structural modification and derivative design of Hatpost wood alkali are also key research areas for future research. By chemically modifying and optimizing their pharmacokinetic properties and targeted selectivity, drug molecules with greater clinical value are developed.
As the main pentacyclic indole alkaloid in Maogupeng, Hamikou Ligus demonstrates broad medicinal value due to its unique chemical structure and multi-target pharmacological activity. Its multiple biological functions—anti-inflammation, anti-tumor, and antimalarial effects—provide valuable resources for the development of natural product drugs. Druggability evaluation shows that cap-pillar lignoline has good drug development potential, high safety, and outstanding blood-brain barrier penetration.
In the future, by integrating modern medicinal chemistry, molecular biology, and pharmacological technologies, the mechanism of action of Hat-Column wood can be deeply analyzed, its drug properties optimized, and systematic preclinical and clinical studies will be conducted, laying a solid foundation for its transformation into clinical applications. Hat-pillar lignoline is expected to become a new natural medicine for treating various complex diseases, promoting the development and innovation of natural product pharmacology.
Shenshuai
Wenjing
Hedandan
