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Synonym name: Leukamenin F; Wangzaozin B
Catalogue No.: BP0674
Cas No.: 79498-31-0
Formula: C20H28O4
Mol Weight: 332.44
Botanical Source: Rabdosia umbrosa, Isodon amethystoides and Rabdosia japonica
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 glaucocalyxin A
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
74.6000
1.9198
1.9199
.1695
2.8731
15.0203
High
61.3944
5.7919
No
No
No
No
Yes
No
0.0
Yes
No
Yes
Yes
Glaucocalyxin A (CAS No.: 79498-31-0) is a natural product with significant biological activity, mainly derived from diterpenes of the Lamiaceae plant Rabdosia japonica var. As a class of natural products with diverse structures and broad pharmacological activity, diterpenoids demonstrate unique potential in anti-tumor, anti-inflammatory, antibacterial, and metabolic disease fields. Due to its unique chemical structure and multi-target regulatory capability, Blue Calyx Methyl has attracted significant attention in pharmacological research in recent years, especially demonstrating good antitumor activity in the treatment of malignant tumors such as osteosarcoma.
This review aims to systematically summarize the chemical structure and physicochemical properties of Blue Calyx Methylene, plant origins and extraction methods, deeply explore its pharmacological activity and mechanism of action, evaluate its druggability and pharmacokinetic characteristics, look ahead to its clinical application prospects, and strive to provide theoretical basis and research directions for subsequent basic and translational research.
Blue calyx diterpenoid belongs to the labdane diterpenoid class of compounds and has a typical diterpene skeleton structure. Its molecular formula is C20H28O4, and its molecular weight is 332.44. The structure of blue calyx methyl contains multiple unsaturated bonds and functional groups such as hydroxyl and ester groups, giving it certain polarity and biological activity.
In terms of physicochemical properties, the LogP value of blue calyx methyl acid is 1.9198, indicating moderate lipid solubility, which facilitates cell membrane penetration and distribution in vivo. Its topological pole surface area (TPSA) is 74.6 Ų, indicating a good polarity distribution that facilitates binding with biological macromolecules. Low water solubility (0.1695 mg/mL), which somewhat limits oral absorption but can be improved through formulation optimization. The blood-brain barrier has high penetration, indicating potential risks of central nervous system activity or side effects. The hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity. The Ames test result was 0, indicating that blue calyx methyl acid has no significant genotoxicity.
Blue calyx japonica is mainly found in Rabdosia japonica var. (Blue Sepal Grass), a plant widely distributed in East Asia. In traditional Chinese medicine, it is used to clear heat, detoxify, activate blood circulation, and relieve pain. As one of the main active ingredients of this plant, Blue Calyx Methyl Extract has been purified in recent years through various extraction and separation techniques.
Common extraction methods include organic solvent extraction (such as ethanol and methanol extraction), bind-liquid separation, and column chromatography separation. The typical process is: after crushing dried plants, reflux extraction with 70% ethanol, concentration followed by ethyl acetate distribution, followed by further purification by silica gel column chromatography or reversed-phase high-performance liquid chromatography (RP-HPLC) to obtain blue calyx methylene. In recent years, supercritical CO2 extraction technology and microwave-assisted extraction technology have also been applied to improve extraction efficiency and purity.
The optimization of the extraction process not only increased the yield of Blue Ephesal Methyl Extract but also laid the foundation for subsequent pharmacological research and formulation development.
The most well-known pharmacological effect of Lancalyxin is its antitumor activity. Multiple in vitro and in vivo studies have shown that blue calyxin can significantly inhibit the proliferation, migration, and invasion of various tumor cells, with particularly prominent performance in osteosarcoma cell lines. Its antitumor effects mainly work by inducing apoptosis, blocking cell cycle progression, and inhibiting tumor-related signaling pathways.
Research shows that blue calyx methyl can induce apoptosis in osteosarcoma cells by regulating the PI3K/Akt signaling pathway, inhibiting the nuclear translocation of the transcription factor GLI1. GLI1 is a key transcription factor in the Hedgehog signaling pathway, involved in tumor cell proliferation and survival. This mechanism of action of blue calyxin provides the molecular basis for its anti-osteosarcoma properties.
In addition, blue calyx methylene has been reported to have certain inhibitory effects on other tumor types such as breast cancer and lung cancer, indicating a broad anti-tumor spectrum.
Although Blue Calyx Methyl Extract mainly focuses on antitumor research, its regulatory potential for hyperglycemia-related targets is also gaining attention. Relevant targets include EHMT2, UBP2, PAI1, AMPK, SGLT2, GCK, APP, BACE1, CES1, and PTPN1, which play important roles in glucose metabolism, insulin signaling, and diabetic complications.
Blue Calyx Methyl may regulate the AMPK signaling pathway, promote glucose metabolism and energy balance, inhibit SGLT2, thereby reducing renal glucose reabsorption and improving hyperglycemic status. Additionally, its effects on epigenetic and signal regulatory factors such as EHMT2 and PTPN1 suggest that blue calyx methyl acid may have the potential to regulate the expression of genes related to glucose metabolism.
Although related research is still in its early stages, Blue Elyx Methyl Extract, as a multi-target regulator, has development prospects worthy of further exploration in the field of metabolic diseases.
In addition to anti-tumor and anti-hyperglycemic properties, Lycasterin also exhibits certain anti-inflammatory and antioxidant activities, helping to alleviate inflammation-related diseases. It reduces inflammatory responses and protects tissue cells by inhibiting the NF-κB signaling pathway and regulating intracellular redox status.
The pharmacological mechanism of blue calyxin is complex, involving multiple signaling pathways and molecular targets. Its antitumor effect mainly depends on regulation of the PI3K/Akt signaling pathway. The PI3K/Akt pathway is an important regulatory axis for cell proliferation, survival, and metabolism, with abnormal activation commonly seen in various tumors. Blue calyxin inhibits PI3K activity, blocks Akt phosphorylation, thereby suppressing downstream GLI1 transcription factor nuclear translocation and inducing tumor cell apoptosis.
GLI1, as a key effector molecule in the Hedgehog signaling pathway, plays an important role in tumor development and development. The inhibition of GLI1 by blue calyxin reveals its molecular basis for anti-tumor effects.
In terms of metabolic regulation, blue calyx methylene acts on various targets:
Additionally, the effects of blue calyxin on APP and BACE1 suggest its potential role in neurodegenerative diseases such as Alzheimer's, especially considering its good blood-brain barrier penetration.
The druggability parameters of Lancalyxin indicate good drug compatibility and safety. The molecular weight of 332.44 meets Lipinski's "drug similarity rule," and LogP (1.9198) indicates moderate lipid solubility, favorable for oral absorption. TPSA is 74.6 Ų, indicating moderate polarity that facilitates biofilm penetration.
Low water solubility (0.1695 mg/mL) may limit its oral bioavailability, but it can be effectively improved through pharmaceutical techniques such as nanocarriers and solid dispersions. High blood-brain barrier penetration offers potential therapeutic possibilities for central nervous system diseases, but central toxicity risks must also be considered.
The hERG channel inhibition test was negative, reducing the risk of cardiotoxicity. The Ames test showed no mutagenicity, indicating a low risk of genotoxicity.
Currently, pharmacokinetic studies of Lanca Methrin are relatively limited. Preliminary data show that its metabolism in the body mainly occurs through hepatic enzyme systems, with excretion routes including bile and urine. The half-life is moderate, suggesting that effective plasma concentrations can be maintained through a rational dosing regimen. In the future, further systematic pharmacokinetic and toxicological evaluations are needed to provide a basis for clinical translation.
As a natural product with multiple targets and multiple mechanisms, Lan Ca Metin demonstrates strong anti-tumor potential, especially in the field of osteosarcoma treatment, offering unique advantages. By regulating the PI3K/Akt-GLI1 signaling pathway, it induces tumor cell apoptosis, providing new ideas for targeted therapy of malignant tumors such as osteosarcoma.
Additionally, the regulatory potential of blue calyxin for hyperglycemia-related targets suggests its promising application in the treatment of diabetes and metabolic syndrome. Combined with its anti-inflammatory and antioxidant multiple pharmacological activities, Blue Calyx Methyl is expected to become a candidate molecule for multifunctional drug development.
Future research should focus on the following aspects:
As a natural product of the lauryl diterpene derived from Rabdosia japonica var., blue calyx methyl shows broad application prospects in anti-tumor and metabolic disease fields due to its unique chemical structure and multi-target regulatory capabilities. By modulating the PI3K/Akt-GLI1 signaling pathway to induce apoptosis in osteosarcoma cells, it offers a new strategy for tumor treatment. At the same time, the potential regulatory effect of blue calyxin on hyperglycemia-related targets provides a theoretical basis for its development in metabolic disease treatment.
Although current research on Lanca Methyl Extract is still in the basic and early stages of transformation, its excellent druggability parameters and safety evaluation have laid a solid foundation for subsequent clinical application. In the future, through multidisciplinary collaborative research, Lanca Methyl Acid is expected to become an important representative of natural product drug development, promoting the widespread application of natural products in modern medicine.
Shenshuai
Wenjing
Hedandan
