Product name: Euphorbiasteroid
Synonym name: Euphorbia factor L1
Catalogue No.: BP0578
Cas No.: 28649-59-4
Formula: C₃₂H₄₀O₈
Mol Weight: 552.664
Botanical Source: Euphorbia lathyris L
Physical Description:
Type of Compound: Diterpenoids

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.

HPLC of  Euphorbiasteroid

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

Introduction/Overview

Euphorbiasteroid, CAS number 28649-59-4, is a typical steroidal natural product derived from the genus Euphorbia of the Euphorbiaceae family. In recent years, with the deepening development of natural product pharmacology, Qianjin Zisterol has attracted widespread attention due to its unique chemical structure and significant biological activity, especially its potential application value in the treatment of malignant tumors such as liver cancer. As one of the malignant tumors with high incidence and mortality rates worldwide, liver cancer urgently needs to develop new, efficient, and low-toxicity treatments. Cynosterol demonstrates antitumor activity by regulating multiple key molecular targets, making it a research hotspot in the field of natural anti-cancer drug development.

This paper aims to systematically review the chemical structure and physicochemical properties of Qianjin Zisterol, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics. Combined with current research progress, it explores its clinical application prospects and development direction in liver cancer treatment, providing a theoretical foundation and reference for subsequent related research and drug development.

Chemical structure and physicochemical properties

Cypine sterol is a typical steroid compound with the molecular formula C_30H_48O_7 and a molecular weight of 552.6640. Its structure includes the classic steroid tetraring framework with multiple hydroxyl and ester modifications, giving it higher polarity and a specific spatial configuration. The LogP value was 4.0174, indicating moderate lipid solubility, which is beneficial for cell membrane penetration and bioavailability. The topological pole surface area (TPSA) is 108.5 Ų, indicating that the molecule has certain polar groups that may affect its binding properties to target proteins and their distribution in vivo.

Its extremely low water solubility (0.0034 mg/mL) suggests that the solubility of Cymetinsterol in the aqueous phase is limited and that its bioavailability needs to be improved through appropriate pharmaceutical techniques. This compound has a high blood-brain barrier penetration ability, suggesting it may affect central nervous system function or have potential for treating brain diseases. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames mutagenic test scored 0.0, indicating a low genotoxicity risk and meeting safety requirements.

Plant Origins and Extraction Methods

Euphorbia sterols are mainly found in the genus Euphorbia of the Euphorbiaceae family, with particularly high levels in species such as Euphorbia kansui and Euphorbia lathyris. Plants of the genus Tianjinzi are widely distributed in northern and temperate regions of China. In traditional Chinese medicine, their rhizomes are often used to treat symptoms such as edema and constipation.

The extraction process for Cynosterol mainly includes the following steps:

1. Raw material preparation: Collect the rhizomes of the genus Lycodium, dry and crush them into coarse powder.
2. Organic solvent extraction: Reflux extraction is performed using solvents such as ethanol, methanol, or ethyl acetate, with extraction time generally 2-4 hours, and extraction repeated 2-3 times to improve recovery rate.
3. Crude extract concentration: The extract is concentrated under reduced pressure to obtain a crude extract rich in steroid compounds.
4. Separation and purification: Using silica gel column chromatography, reversed-phase high-performance liquid chromatography (RP-HPLC), and other technologies, the sterol is separated and purified. Purity testing uses mass spectrometry (MS) and nuclear magnetic resonance (NMR) techniques to confirm structure and purity.

In recent years, ultrasound-assisted extraction and supercritical fluid extraction technologies have also been applied to the extraction of cythian sterol, significantly improving extraction efficiency and purity, reducing the use of organic solvents, and aligning with the concept of green chemistry.

Pharmacological activity research

Research on the pharmacological activity of Cymnosterol mainly focuses on its anti-tumor, anti-inflammatory, and immunomodulatory aspects. In particular, it has shown significant inhibitory effects in in both vivo and in vitro experiments for liver cancer.

Anti-liver cancer activity

In vitro cell experiments show that Cypine Sterol can significantly inhibit the proliferation and migration of liver cancer cell lines (such as HepG2 and Huh7), inducing apoptosis. Its effect is highly dose-dependent, with IC_50 values generally within the low micromolar range. In vivo liver cancer transplant tumor models, the Cynosterol treatment group showed significantly reduced tumor size and weight, prolonged survival, and no obvious toxic side effects.

Anti-inflammatory and immunomodulatory

Cynosterol reduces liver inflammation and improves liver tissue damage by downregulating inflammatory mediators such as PTGS2 (COX-2). Additionally, its regulatory effect on immune cell function helps enhance the body's anti-tumor immune response.

Other activities

Some studies have shown that Quintresterol has antioxidant and anti-fibrotic effects, making it promising as an adjunct treatment for liver fibrosis and other chronic liver diseases.

Mechanism of action and molecular targets

The anti-liver cancer mechanism of Cynosterol involves multiple signaling pathways and key molecular targets, mainly including:

• BCL2: Cyptosterol promotes apoptosis of liver cancer cells by downregulating the expression of the anti-apoptotic protein BCL2, restoring the mechanism of programmed cell death.
• STAT3: Inhibits STAT3 signaling pathway activity, blocks its transcriptional regulation, and suppresses tumor cell proliferation and immune escape.
• TOP1: Affects topoisomerase I (TOP1) activity, hinders DNA replication and repair, and induces DNA damage in tumor cells.
• MAPK1: Regulates the MAPK signaling pathway, inhibiting cell proliferation and migration.
• TERT: Inhibits telomerase reverse transcriptase (TERT) expression, limiting the unlimited proliferation capacity of tumor cells.
• PIK3CA: Interferes with the PI3K/AKT signaling pathway, inhibiting cell survival and metabolism.
• MMP9: Reduces matrix metalloproteinase 9 (MMP9) activity, inhibiting tumor cell invasion and metastasis.
• EGFR: Inhibits epidermal growth factor receptor (EGFR) signaling, reducing tumor growth signaling.
• PTGS2: Inhibits the expression of the inflammatory mediator PTGS2, reducing inflammatory responses in the tumor microenvironment.
• TP53: Activates tumor suppressor protein p53, promoting cell cycle arrest and apoptosis.

Overall, Cynosterol leverages its synergistic effects against liver cancer through multi-target and multi-pathway synergy, demonstrating the advantages of natural product multi-target drugs.

Druggability evaluation and pharmacokinetics

The druggability parameters of Cynosterol indicate that it has certain development potential:

• The molecular weight (552.66) is slightly above the recommended range for the Lipinski rule, but can still be optimized through pharmaceutical modification.
• LogP (4.0174) indicates moderate lipid solubility, which is beneficial for cell membrane penetration.
• TPSA (108.5) suggests moderate polarity, which may affect oral absorption.
• Its extremely low water solubility (0.0034 mg/mL) is a major challenge for druggability, requiring technologies such as nanocarriers, liposomes, or solid dispersions to improve solubility and bioavailability.
• The high penetration of the blood-brain barrier suggests its potential for central nervous system diseases, but potential neurotoxicity should be considered.
• hERG inhibitor negatives and Ames tests are negative, indicating lower risks of cardiotoxicity and genotoxicity, and better safety.

Pharmacokinetics, existing studies show that cynosterol is slowly absorbed orally, has a long plasma half-life, is widely distributed in the body, and is mainly metabolized by the liver. The excretion pathway still needs further clarification. In the future, identification of their in vivo metabolites and systematic research of pharmacokinetic parameters should be strengthened to guide clinical dose design and safety evaluation.

Prospects and outlooks for clinical applications

As a multi-target natural anti-liver cancer product, Cyptosterol exhibits significant pharmacological activity and good safety, showing broad clinical application prospects. Future research directions include:

1. Pharmaceutical optimization: Solving the problems of poor water solubility and low bioavailability, developing efficient delivery systems such as nanoparticles and liposomes to increase effective concentrations in the body.
2. In-depth mechanism analysis: By combining multi-omics techniques, the network of action and signaling pathways are further revealed, clarifying key targets and their regulatory mechanisms.
3. Preclinical safety evaluation: Systematic toxicological studies are conducted to assess the safety and potential side effects of long-term medication.
4. Clinical trial design: Based on sufficient pharmacological and toxicological data, advance early clinical trials to verify efficacy and safety, especially for liver cancer patients.
5. Combination therapy strategy: Explore the synergistic effects of Cypressol-Cypressol with existing liver cancer treatments (such as sorafenib and immune checkpoint inhibitors) to enhance treatment efficacy and reduce resistance.

Moreover, given its ability to penetrate the blood-brain barrier, the potential applications of Qianjin Sterol in neurological diseases are also worth attention.

Conclusion

As a natural product with a unique steroid structure, Qianjinzisterol demonstrates multi-target, multi-mechanism anti-tumor activity in liver cancer treatment. Its favorable safety and druggability parameters lay the foundation for the development of novel anti-liver cancer drugs. In the future, through pharmaceutical improvements, mechanistic research, and clinical validation, Certinium Sterol is expected to become an important candidate for liver cancer treatment, driving further development in natural product pharmacology and cancer therapy. Ongoing and in-depth research will provide solid scientific support for clinical translation, helping to promote innovation and application of natural product drugs.