Product name: Hupehenine
Synonym name: Delavine
Catalogue No.: BP0739
Cas No.: 98243-57-3
Formula: C₂₇H₄₅NO₂
Mol Weight: 415.662
Botanical Source: Fritillaria thunbergii
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.




Chengdu Biopurify Phytochemicals Ltd. is a leading company in the research, development, manufacture and marketing of High Quality Phytochemicals and Extracts(especially Active Ingredients from Traditional Chinese Medicine，TCM), Natural Active Pharmaceutical Ingredients worldwide.
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
C. Custom synthesis and semi-synthesis for Natural Active Ingredients
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.

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

Introduction/Overview

Hupehenine (CAS No.: 98243-57-3) is a type of isosteroid alkaloid derived from the traditional Chinese medicinal material Fritillaria hupehensis. In recent years, it has attracted widespread attention due to its diverse pharmacological activities. As an orally effective natural product, Hubeijiasin not only has traditional antitussive and expectorant effects but also demonstrates significant anticancer, antiparasitic, and neuroprotective activities, showing unique potential in research on neurodegenerative diseases such as Parkinson's disease. This paper systematically reviews the chemical structure and physicochemical properties of Hu Celuophyllin, plant origins and extraction methods, pharmacological activity and mechanism of action, drug readability evaluation, pharmacokinetic characteristics, and clinical application prospects, aiming to provide scientific evidence for subsequent basic research and clinical development.

Chemical structure and physicochemical properties

Hubeijiasin is an isosteroid alkaloid compound, with a molecular formula of C_27H_43NO_3 and a molecular weight of 415.6620. Its structure is based on a typical steroid skeleton, containing nitrogen atoms that give it basic characteristics. The LogP value of Hubeijia hormone is 4.2778, indicating high lipid solubility, which facilitates its penetration of cell membranes and the blood-brain barrier (BBB). Its topological pole surface area (TPSA) is 43.7 Ų, making it a moderately polar molecule with a certain degree of water solubility (0.0408 mg/mL) and good membrane permeability. Notably, Hubeijiain has high blood-brain barrier permeability, suggesting its potential application in central nervous system diseases. Additionally, Hubeijiasin did not show hERG channel inhibitory activity, reducing the risk of cardiotoxicity, and the Ames-induced mutagenic test results were negative, indicating a low genotoxicity risk.

Plant Origins and Extraction Methods

Hupehensin is mainly isolated from fritillaria hupehensis. Chuan-beimu is a perennial herbaceous plant in the Liliaceae family, genus Fritillaria, widely distributed in central and southwestern China. Its dried bulbs are a traditional Chinese medicinal herb traditionally used to treat coughs, excessive phlegm, and lung diseases.

Traditional extraction methods mostly use alcohol extraction combined with acid-base separation technology. The specific process includes:

1. Crude extraction: After crushing dried fritillaria, reflux extraction is performed with 70% ethanol. The extraction time is generally 2-3 hours, repeating 2-3 times to improve extraction efficiency.
2. Liquid-liquid separation: After the extract is concentrated, adjust the pH to 3-4 with acidified aqueous solution, then separate it with organic solvents (such as chloroform or ethyl acetate) to remove non-alkaline impurities.
3. Alkaline withdrawal: The acidic aqueous phase is adjusted to alkali (pH 9-10), allowing the alkaloid to exist in the form of a free base, then extracted with an organic solvent to enrich the alkaloid components.
4. Purification: Further purification is performed using column chromatography (such as silica gel columns, C18 reversed-phase columns) or high-performance liquid chromatography (HPLC) to obtain high-purity lake formin.

In recent years, the introduction of ultrasound-assisted extraction, microwave-assisted extraction, and membrane separation technologies has improved extraction efficiency and purity, while reducing process costs.

Pharmacological activity research

Antitussive and expectorant activity

As an important active ingredient in traditional Chinese medicine Chuanbeimu, Hubeijia Su plays a key role in suppressing cough and resolving phlegm. In vivo and in vitro experiments have shown that Hubeijiain can effectively suppress the cough reflex, promote respiratory mucus secretion, dilute phlegm, enhance ciliary movement, and facilitate phlegm excretion. Its mechanism of action may be related to regulating airway smooth muscle tone and inhibiting the release of inflammatory mediators.

Anticancer activity

Hubeijiachin exhibits inhibitory effects on various tumor cells, especially prominent in liver cancer cell lines. In vitro experiments show that Hubeijiain can induce apoptosis of liver cancer cells and inhibit cell proliferation and migration. Its anticancer effects involve multiple signaling pathways and molecular targets, including:

• Inhibits the expression of the anti-apoptotic protein BCL2, promoting cell apoptosis.
• Inhibits the STAT3 signaling pathway, blocking tumor cell proliferation and immune escape.
• Regulates TOP1 and MAPK1-related pathways, intervening in cell cycle and stress responses.
• Inhibits tumor-related genes TERT and PIK3CA, affecting tumor cell proliferation and survival.
• Reduces MMP9 expression and inhibits tumor cell invasion and metastasis.
• Inhibits EGFR and PTGS2, blocking pro-inflammatory and growth-promoting signals in the tumor microenvironment.
• Promotes functional recovery of the tumor suppressor gene TP53 and enhances apoptosis.

Antiparasitic activity

Hu Meijia exhibits inhibitory effects on various parasites, especially effective against schistosomes and certain protozoa. Its antiparasitic mechanisms may involve disruption of parasitic energy metabolism and cell membrane disruption, which requires further research.

Neuroprotective effects

Recent studies have found that Hubeijiain can inhibit α-synuclein-induced fibrogenesis, reducing the accumulation of neurotoxicity in nerve cells, suggesting its potential application value in neurodegenerative diseases such as Parkinson's disease. Both in vitro cell models and animal experiments have confirmed its effects on neuronal protection and inflammation suppression.

Mechanism of action and molecular targets

The multi-target mechanism of Hubejiamin is the basis of its multiple pharmacological activities. Its main mechanisms of action include:

1. Regulates apoptosis and the cell cycle
   Hubeijiachin promotes mitochondrial pathway-mediated apoptosis by regulating the expression of BCL2 family proteins. At the same time, it affects the STAT3 and MAPK1 signaling pathways, blocks the cell cycle progression, and inhibits tumor cell proliferation.

2. Inhibits tumor invasion and metastasis
   By downregulating matrix metalloproteinase MMP9, Hubeijian reduces tumor cells' ability to degrade the matrix and inhibits tumor metastasis.

3. Anti-inflammatory and immunomodulatory
   Inhibits PTGS2 (COX-2) expression, reduces the production of pro-inflammatory mediators, and regulates the tumor microenvironment and neuroinflammatory response.

4. Neuroprotective mechanisms
   Inhibits abnormal aggregation of α-synuclein, reduces neurotoxicity, protects dopaminergic neurons, and delays neurodegenerative progression.

5. Antiparasitic mechanisms
   It may cause parasite death by interfering with parasitic metabolic enzyme activity and membrane structural stability.

These multi-target and multi-pathway synergistic effects give Hubeijia Extract broad pharmacological activity and application potential.

Druggability evaluation and pharmacokinetics

The druggability evaluation of Hubeijiasin shows it has promising potential for drug development:

• Molecular weight 415.6620, complies with Lipinski rules, suitable for oral administration.
• LogP 4.2778 shows good lipid solubility, facilitating cell membrane penetration and blood-brain barrier penetration.
• TPSA 43.7 Ų, moderate polarity, balancing water solubility and membrane permeability.
• Water solubility is 0.0408 mg/mL, which is not high but can be improved through salt formation or formulation techniques.
• The blood-brain barrier has high permeability, making it suitable for treating central nervous system diseases.
• No hERG channel suppression, reducing the risk of cardiotoxicity.
• Ames test is negative, with low genotoxicity risk.

Regarding pharmacokinetics, most existing studies are based on animal models, showing that Hubeijiasin is well absorbed orally and has a moderate plasma half-life, mainly metabolized by the liver, with excretion routes including bile and urine. Its high lipophilubility leads to its widespread distribution in tissues, especially brain tissue. Future research on human pharmacokinetics is needed to clarify bioavailability, metabolic pathways, and drug interactions.

Prospects and outlooks for clinical applications

As a versatile natural product, Lake Beijia Acid has broad clinical application potential:

1. Respiratory diseases
   Its cough-suppressing and expectorant effects make it suitable as an adjunct treatment for chronic bronchitis, asthma, and lung infections.

2. Tumor treatment
   By regulating tumor growth and metastasis through multiple targets, Hubeijiasin is expected to serve as an adjunct or combination therapy for liver cancer and other solid tumors. Combined with modern drug delivery systems, such as nanocarriers, it is expected to improve targeting and efficacy.

3. Neurodegenerative diseases
   The ability to counter α-synuclein aggregation offers new approaches for treating diseases such as Parkinson's disease. In the future, it can be combined with other neuroprotective drugs to conduct preclinical and clinical research.

4. Antiparasitic treatment
   In areas with high incidence of parasitic diseases, Hubeijiasu has promotional value as a natural antiparasitic drug.

Future research should focus on:

• Clarify the molecular targets and downstream signaling pathways of Hubejiain to reveal its network of action.
• Optimize extraction and purification processes to increase yield and purity.
• Develop novel delivery systems to improve bioavailability and targeting.
• Systematic toxicology and pharmacokinetic studies are conducted to ensure safety.
• Design clinical trials to verify efficacy and safety.

Conclusion

As an isosteroid alkaloid derived from fritillaria chuan, Hu Beijia Su shows broad research and application prospects due to its diverse pharmacological activities and good druggability. Its potential in cough suppression and expectoration, anti-cancer, antiparasitic properties, and neuroprotection is particularly notable in the treatment of liver cancer and Parkinson's disease. In the future, through in-depth mechanistic research, optimized formulation technology, and clinical validation, Hubeijiasu is expected to become an important representative of natural product drug development and contribute new treatment options to human health.