Product name: Allocryptopine
Synonym name: Thalictrimine; alpha-Fagarine; γ-Homochelidonine; Beta-Homochelidonine
Catalogue No.: BP0143
Cas No.: 485-91-6
Formula: C₂₁H₂₃NO₅
Mol Weight: 369.417
Botanical Source: Macleaya cordata (Willd.) R. Br.
Physical Description:
Type of Compound: Alkaloids

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.




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The main services:
A. Supply active ingredients and reference standards of TCM, from mgs to kgs scale
B. Custom extraction and purification, target Herb Active Ingredients
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D. CR(contract research), CM(contract manufacture) and PD(process development) services from lab scale, pilot scale to commercial scale(GMP is also available)
E. TCM compounds library for drug screen,more than 3000 compounds available, many of them are rare and unique.

HPLC of Allocryptopine

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

Introduction/Overview

Allocryptopine, CAS number 485-91-6, is a natural alkaloid with multiple biological activities, mainly extracted from the genus Macleaya (Macleaya cordata) of the papavery family. As a derivative of corydalisin, albinepinine has attracted widespread attention in the field of natural product pharmacology due to its potential therapeutic value in liver protection, cardiovascular regulation, and neurological diseases. In recent years, with in-depth research into its molecular mechanisms, albinepinine has demonstrated unique pharmacological properties, especially in its anti-liver fibrosis, antiarrhythmia, and central nervous system regulation effects, providing a theoretical foundation and experimental basis for the development of novel natural drugs.

This paper will systematically review the chemical structure and physicochemical properties of biylinpine, plant origin, and extraction methods, elaborate on its pharmacological activity and mechanism of action, and, combined with druggability evaluation and pharmacokinetic data, explore its prospects and challenges in clinical application, aiming to provide comprehensive reference for further research and drug development of this natural product.

Chemical structure and physicochemical properties

Beneginine is an aromatic ether type of organic heterotetracyclic compound with a complex chemical structure, including the dibenzoazate alkaloid backbone, cyclic ketones, tertiary amino groups, and cyclic acetals, among other functional groups. Its molecular formula is C21H21NO5, molecular weight is 369.41, and LogP value is about 3.0, indicating moderate lipid solubility that facilitates cell membrane penetration. The topological pole surface area (TPSA) is 61.38 Ų, and the number of hydrogen bond acceptors is 6, indicating that it possesses certain affinity and selectivity when binding to biological macromolecules.

Structurally, the dibenzoazide skeleton of Altegeline endows it with stable aromatics and a distinctive spatial configuration, while cyclone and cyclic acetal groups provide potential reactive sites. The presence of tertiary amino groups allows them to form diverse binding patterns with target proteins in organisms via hydrogen and ionic bonds. Additionally, the structural characteristics of alloreginine give it good modifiability in drug design, making it easy to optimize its efficacy and pharmacokinetic properties through chemical synthesis.

Plant Origins and Extraction Methods

Binepinine mainly originates from Macleaya cordata (South China Corydalis) and its related species within the genus Corydalisa of the Papaveraceae family. Macleaya cordata is a perennial herbaceous plant widely distributed in southern China and Southeast Asia. In traditional Chinese medicine, its rhizome and whole plant are often used medicinally, with effects of promoting blood circulation, removing blood stasis, relieving pain, and reducing swelling.

Traditional methods for extracting Alzine typically use alcohol solvents (such as ethanol, methanol) to extract dried plant material by reflux or ultrasound, followed by acid-base extraction, liquid-liquid distribution, and column chromatography for separation and purification. Modern extraction technologies such as supercritical CO₂ extraction and high-performance liquid chromatography (HPLC) purification have been applied to improve extraction efficiency and purity.

The specific steps include:

1. Sample pretreatment: collect Macleaya cordata, dry it, and crush it.
2. Solvent extraction: 70% ethanol reflux extraction is used, with extraction time generally 2-4 hours.
3. Liquid-liquid distribution: Adjust pH with acidic aqueous solution to separate alkaline components.
4. Column chromatography purification: Separation is performed using silica gel or a C18 reversed phase column, combined with gradient elution to enrich the alkaloid alkalis.
5. Crystallization or freeze-drying: Obtain high-purity allequinine powder.

This method offers mature processes, moderate costs, and suitability for large-scale production, providing a stable material foundation for subsequent pharmacological research and drug development.

Pharmacological activity research

Liver-protective effects

Numerous in vivo and in vitro experiments have shown that alznine has a significant anti-injury effect on hepatocytes. Its main mechanisms are improving liver function indicators, reducing hepatocyte necrosis and inflammatory responses, and inhibiting the process of liver fibrosis. The study found that alkaloids can reduce collagen deposition in the liver and lower the expression of fibrosis-related factors such as α-SMA and TGF-β, suggesting that it exerts anti-fibrotic effects by regulating the activation of hepatic stellate cells.

Additionally, alkaloids are independent of the aromatic hydrocarbon receptor (AhR) pathway, significantly upregulating cytochrome P450 1A (CYP1A) mRNA levels in human hepatocytes and HepG2 cells, enhancing the liver's detoxification and metabolism capacity, and reducing hepatotoxic damage.

Cardiovascular system function

Benehipinine has antiarrhythmic effects, mainly by blocking the potassium channel of hERG (human ether-a-go-go related gene). hERG channels play a key role in cardiac repolarization, and their dysfunction is the pathological basis for various arrhythmias. Binazine effectively inhibits hERG currents, extends the duration of action potentials, stabilizes the electrical activity of myocardial cells, and thus reduces the occurrence of arrhythmias.

Additionally, alzine promotes ileal smooth muscle relaxation by inhibiting phosphodiesterase (PDE) activity, increases intracellular cAMP levels, and regulates bladder contraction responses mediated α by adrenergic receptors, demonstrating its potential in regulating smooth muscle function and vasomotor contraction.

Activities related to the nervous system and psychiatric disorders

Allotropine has potential interactions with various neurotransmitter receptors and transporters, including SIGMAR1, acetylcholinesterase (ACHE), 5-hydroxytryptamine receptor 2B (HTR2B), dopamine receptor D1 (DRD1), 5-hydroxytryptamine receptor 7 (HTR7), cholinergic receptors M1 and M3 (CHRM1, CHRM3), dopamine transporter (SLC6A3), and 5-hydroxytryptamine transporter (SLC6A4). These targets are closely related to depressive disorders and other mental illnesses, suggesting that allohepine may exert antidepressant or neuroprotective effects by modulating the neurotransmitter system.

Currently, related research is still in its early stages, and future studies will need to be conducted in depth using cell and animal models to explore its effects and mechanisms on the central nervous system.

Mechanism of action and molecular targets

The multi-target mechanism of Beneginine reflects its complex pharmacological characteristics. Its main targets and mechanisms include:

1. CYP1A induction: Beneginine can independently induce CYP1A gene expression independently of the AhR pathway, enhance hepatocyte metabolic enzyme activity, promote metabolism and detoxification of harmful substances, and reduce liver damage.

2. PDE inhibition and cAMP regulation: By inhibiting phosphodiesterase activity, algenopyringine increases intracellular cAMP levels, regulates smooth muscle cell function, promotes ileal dilation and bladder contraction, and demonstrates its role in smooth muscle physiological regulation.

3. hERG channel blockade: Benehipinine effectively blocks human hERG potassium channels expressed in HEK293 cells, delaying cardiomyocyte repolarization and exerting antiarrhythmic effects.

4. Regulation of neurotransmitter receptors and transporters: Beneginine interacts with various neural targets such as SIGMAR1, ACHE, 5-HT receptors, dopamine receptors, and transporters, potentially affecting neurotransmitter synthesis, release, and reuptake, regulating neural function, and possessing potential antidepressant and neuroprotective effects.

The diversity of these mechanisms makes allogemine a versatile natural drug candidate with broad clinical application potential.

Druggability evaluation and pharmacokinetics

The molecular weight (369.41) and LogP (3.0) of allohipinine both met the Lipinski rule, suggesting good oral bioavailability potential. Its TPSA (61.38 Ų) is moderate, which helps penetrate cell membranes and certain biological barriers.

However, key druggability indicators for allolinine—such as blood-brain barrier permeability, hepatotoxicity, cardiotoxicity (including safety related to hERG inhibition), and mutagenicity (Ames assay)—remain unclear, limiting the progress of clinical development. In particular, although hERG channel blockade has antiarrhythmic effects, excessive blocking may cause cardiotoxicity, so the safe dose window should be carefully evaluated.

Regarding pharmacokinetics, there are few existing literature reports and a lack of systematic data on absorption, distribution, metabolism, and excretion (ADME). Future in vivo pharmacokinetic studies are needed to clarify the bioavailability, half-life, metabolic pathways, and excretion mode of alloglidine, providing a basis for clinical dosage formulation design and administration regimens.

Prospects and outlooks for clinical applications

As a multifunctional natural alkaloid, Beneginine has significant potential applications in liver diseases, cardiovascular diseases, and central nervous system disorders. Its anti-fibrosis and liver-protective effects offer new treatment approaches for chronic liver disease patients, especially in reversing liver fibrosis and improving liver function. The pharmacological activity of antiarrhythmic drugs offers patients with arrhythmic potential natural drug options, especially when traditional antiarrhythmic drugs have significant side effects, where alzinepine may serve as an adjunctive therapy.

In the field of neuropsychiatric disorders, albinoids demonstrate potential antidepressant and neuroprotective effects by modulating multiple neurotransmitter system targets, and are expected to become new targets for drug development for mental disorders in the future.

However, the clinical translation of albinein still faces many challenges, including insufficient safety evaluation, lack of pharmacokinetic data, dosage form development, and clinical trial design. Future research should focus on:

• Systematic toxicological and safety assessments, especially cardiac toxicity and hepatotoxicity.
• Pharmacokinetics and pharmacokinetic studies clarify the relationship between in vivo behavior and dose-response.
• Structural modification and drug design optimize efficacy and safety.
• In-depth analysis of multi-target mechanisms combined with modern molecular pharmacology and systems biology methods.
• Preclinical and clinical studies to verify its therapeutic efficacy and safety.

In summary, as a natural product with multiple pharmacological activities, alleginine has broad prospects for drug development, but requires multidisciplinary collaboration to realize its clinical application value.

Conclusion

As a typical alkaloid extracted from Macleaya cordata, Benehipine demonstrates its potential in liver protection, cardiovascular regulation, and the treatment of neurological diseases due to its unique chemical structure and diverse pharmacological activities. Its multi-target mechanism of action provides important evidence for the development of novel natural drugs. Although there are still shortcomings in druggability, safety, and pharmacokinetics, with deeper research and technological advancements, alzine is expected to become a star molecule in the field of natural product pharmacology, driving progress in related disease treatments.

In the future, multidisciplinary research combining modern medicinal chemistry, molecular biology, and clinical medicine will provide a solid scientific foundation for the drug development and clinical application of allogemine, promoting its transition from the laboratory to clinical practice and contributing new natural drug resources to human health.