Synonym name: Paclitaxel Related Compound A
Catalogue No.: BP0332
Cas No.: 71610-00-9
Formula: C₄₅H₅₃NO₁₄
Mol Weight: 831.912
Botanical Source: Alkaloid from Taxus wallichiana, the bark of Taxus yunnanensis and Cephalotaxus mannii

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 Cephalomannine

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

Introduction/Overview

Cephalomannine (CAS No.: 71610-00-9), a natural paclitaxel alkaloid, has attracted widespread attention in the field of anti-tumor drug development in recent years. This compound is mainly isolated and extracted from the genus Taxus (Taxus spp.) plants. Its structure is similar to the classic paclitaxel, showing significant anticancer activity, especially in the treatment of malignant tumors such as leukemia, showing potential clinical value. Tricanal not only possesses oral bioactivity, but also, due to its unique molecular structure and mechanism of action, is an important candidate for chemotherapy drug development.

This paper aims to systematically review the chemical structure and physicochemical properties, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics of Tricarpine, combined with its molecular targets in leukemia and other tumor diseases, to explore its clinical application prospects and development trends, and to provide theoretical basis and research reference for the development of natural product pharmacology and antitumor drugs.

Chemical structure and physicochemical properties

Tricanine alkali is a complex taxane diterpene alkaloid with a molecular formula of C47H51NO14 and a molecular weight of 847.90. Its chemical structure is highly similar to taxel, both containing a unique paclitaxane framework and multiple hydroxyl and ester groups, which impart its distinctive pharmacological activity. The LogP value of trisalinal soda is about 2.8, indicating moderate lipid solubility, which facilitates cell membrane penetration and oral absorption.

The molecular surface area (TPSA) reaches 239.36 Ų, with 14 hydrogen bond receptors, indicating high molecular polarity, which may affect its ability to cross the cell membrane and pharmacokinetic behavior. The blood-brain barrier has a relatively low penetration capacity, suggesting limited distribution in the central nervous system and potentially reducing the risk of CNS toxicity. Current research on its hepatotoxicity, cardiotoxicity, and hERG channel inhibition is still insufficient, and Ames-induced mutagenic assay results are unclear, requiring further systematic evaluation of its safety.

Plant Origins and Extraction Methods

Taxus cuspidata is mainly found in Taxus chinensis, Taxus cuspidata, and others. Tricarpus plants are an important natural source of antitumor drugs due to their abundant taxane diterpene alkaloids. Traditionally, the extraction of Tripitan Azine soda has been achieved using organic solvent extraction combined with multi-stage chromatography separation and purification technology.

Common extraction processes include: crushing dried Tridentium wood and extracting it using polar solvents such as methanol, ethanol, or ethyl acetate; Subsequently, impurities are removed through liquid-liquid distribution; Separation and purification were performed using silica gel column chromatography, reversed-phase high-performance liquid chromatography (RP-HPLC), and other technologies; Ultimately, high-purity trijun nimbal alkali is obtained. In recent years, green extraction technologies such as supercritical CO2 extraction and microwave-assisted extraction have gradually been applied to the extraction of trichistan alkali, improving extraction efficiency and reducing environmental pollution.

Pharmacological activity research

Trisalinaline, as a paclitaxel analog, mainly stabilizes microtubule structures, blocks cell mitosis, inhibits tumor cell proliferation, and exerts anti-tumor effects. It exhibits significant cytotoxicity across various tumor cell lines, especially high sensitivity in leukemia cells.

In vitro experiments show that tricycleline can induce tumor cell cycle stagnation at the G2/M phase, promoting apoptosis. Animal model studies have also confirmed its effectiveness in inhibiting tumor growth and prolonging survival. Compared to taxane, tricapsheline has better oral activity and shows potential clinical advantages.

In addition, tricarcenine aline also has a certain inhibitory effect on multidrug-resistant (MDR) tumor cells, possibly by inhibiting the drug efflux mechanism mediated by P-glycoprotein (P-gp), increasing intracellular accumulation of chemotherapy drugs and enhancing efficacy.

Mechanism of action and molecular targets

The antitumor mechanism of tritaxine mainly relies on its binding and stabilizing effects on tubulins, preventing microtubule depolymerization and leading to cell division arrest and apoptosis. In addition, for hematological malignancies such as leukemia, tritaxannine alkaloid involves regulation of several key molecular targets:

• AMPK (PRKAA1): As a cellular energy sensor, AMPK activation helps regulate the metabolic state of tumor cells. Tricarpinin alkali may inhibit tumor cell proliferation by modulating the AMPK signaling pathway.
• MCL1 and BCL2: Downregulation of these two anti-apoptotic proteins promotes tumor cell apoptosis. Tricycleline induces programmed cell death by regulating its expression levels.
• NOTCH1: As an important regulator of cell differentiation and proliferation, inhibition of the NOTCH1 signaling pathway helps block abnormal proliferation of leukemia cells.
• STAT3: This transcription factor is abnormally activated in various tumors. Tritaxannine blocks tumor cells' ability to survive and invade by inhibiting STAT3 signaling.
• MAPT: a microtubule-associated protein tau, involved in microtubule stability; tricapeline may influence microtubule dynamics through interaction with MAPT.
• IDH1: The metabolic enzyme isocitrate dehydrogenase 1, mutated in is related to tumor metabolic reprogramming. Tricycleline may affect its function and regulate tumor metabolism.
• NFE2L2: Encodes the transcription factor Nrf2, regulating cellular antioxidant responses. Tricanine may enhance tumor cells' sensitivity to oxidative stress by modulating Nrf2 signaling.
• TOP1: Topoisomerase I, involved in DNA uncycling; tricapsine alkaloids may synergistically inhibit TOP1 activity and enhance DNA damage.
• SIRT1: Deacetylase, regulates cell survival and metabolism. Trisalquinine may modulate tumor cell fate by affecting SIRT1.

In summary, Sanjianxinine aline exerts its anti-tumor effects through multi-target and multi-pathway synergistic effects, especially demonstrating unique molecular mechanism advantages in leukemia treatment.

Druggability evaluation and pharmacokinetics

Tritaxannine alkaloid has a large molecular weight (847.90 Da) and high polarity (TPSA 239.36 Ų), posing challenges to its pharmacokinetic properties. Its moderate lipophilic solubility (LogP 2.8) favors membrane penetration, but its high number of hydrogen bond receptors may limit its oral absorption and bioavailability.

Current research shows that tricadanenine has good oral activity, which is rare among paclitaxel compounds, possibly due to its structural modification and metabolic stability. The blood-brain barrier has a low penetration capacity, reducing the risk of central nervous system toxicity but also limiting its therapeutic potential for brain tumors.

In terms of safety, the hepatotoxicity, cardiotoxicity, and hERG channel inhibition effects of tricyclaxannine alkaloid are not yet clear, requiring systematic toxicology and safety evaluation. Pharmacokinetic studies show that trijunanine alkaloid is metabolized in the body in the body quite complexly, mainly through hepatic enzyme systems, with a moderate half-life and a certain degree of in vivo stability.

In the future, it is necessary to integrate drug delivery systems to optimize its in vivo distribution, enhance bioavailability and targeting, reduce potential toxic side effects, and promote clinical translation.

Prospects and outlooks for clinical applications

As a powerful supplement to paclitaxel antitumor drugs, tricyclasel alkaloid shows broad application prospects, especially in the treatment of hematological malignancies such as leukemia. Its oral activity provides patients with a more convenient route of administration, improving the limitations of traditional intravenous prilitaxel.

With deeper analysis of its molecular targets and mechanisms of action, tricanal aline is expected to be combined with other targeted drugs and immunotherapy drugs to achieve synergistic effects. Moreover, based on its structural characteristics, the development of medicinal chemical modifications and nanocarrier technology will further enhance its pharmacokinetic performance and tumor targeting potential.

Future research should focus on:

• Systematic evaluation of the safety and toxicological characteristics of tricyclaxenine;
• Optimizing dosage forms and administration regimens to improve clinical efficacy and patient compliance;
• Exploring its application potential across various tumor types, especially drug-resistant tumors;
• Developing molecular target-based precision therapy strategies to advance personalized medicine.

Conclusion

Tricanal alkalis, as a natural compound with significant antitumor activity, holds significant research value and application potential in the field of anticancer drug development due to its unique chemical structure and multi-target mechanism. Although current understanding of its pharmacokinetics and safety is not yet comprehensive, its good oral activity and therapeutic potential for tumors such as leukemia provide a solid foundation for clinical translation.

In the future, by integrating modern medicinal chemistry, molecular biology, and drug delivery technologies, Tricapsal Taxane is expected to become a new generation of highly effective, low-toxicity anti-tumor drugs, bringing new hope for cancer patients. Ongoing and in-depth basic and clinical research will be key to advancing its clinical application.