Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
130.6400
.1500
-.9700
No
No
No
No
Unknown
No
Unknown
Ajugasterone C is a natural steroid compound primarily isolated from the plant Leuzea carthamoids. As a member of the molting steroids, Caryophyllone C has attracted attention in traditional herbal medicine due to its potential anti-inflammatory and metabolic regulatory effects. In recent years, with the deepening of research on the pharmacological activity and molecular mechanism of natural products, Caryophyllone C has become a hot topic in the study of metabolic diseases and inflammation related diseases due to its significant biological activity and better safety characteristics. This article will provide a systematic review of the chemical structure, plant origin, pharmacological activity, mechanism of action, and pharmacological evaluation of Carnosterone C, and explore its potential and future development direction in clinical applications.
The molecular formula of Caryophyllone C is C27H40O8, with a molecular weight of 480.64, belonging to the family of ecdysteroids. Its structural features include a typical four ring steroid skeleton with multiple hydroxyl and ester modifications, giving it high polarity. The LogP value is 0.15, indicating strong hydrophilicity and good water solubility. Its topological polar surface area (TPSA) is 130.64 and the number of hydrogen bond acceptors is 7, indicating that the molecule has strong hydrogen bond forming ability, which is of great significance for its binding to biological targets. Caryophyllone C is not easily able to penetrate the blood-brain barrier, and has no hepatotoxicity, cardiotoxicity, or hERG channel inhibitory activity, demonstrating good safety characteristics.
The main source of Caryophyllone C is Leuzea carthamoides, a perennial herbaceous plant in the Asteraceae family, widely distributed in Siberia and Central Asia, Russia. Jin Gu Cao is used in traditional medicine as a medicinal herb to enhance physical strength, resist fatigue, and fight inflammation. As one of its main active ingredients, Caryophyllone C is usually obtained through solvent extraction and chromatographic separation techniques.
Common extraction methods include:
1. Solvent extraction Use polar organic solvents such as methanol, ethanol, or ethyl acetate to reflux or ultrasonically extract the dried powder.
2. Liquid liquid distribution By distributing solvents of different polarities, impurities are removed and the content of target compounds is increased.
3. Column chromatography separation Using silica gel or C18 reverse phase column for separation and purification, combined with high-performance liquid chromatography (HPLC) for component identification and purity detection.
In recent years, supercritical CO2 extraction and membrane separation technology have also been attempted to be applied to the extraction of Caryophyllum oxyphyllum ketone C, improving extraction efficiency and environmental friendliness.
Caryophyllone C exhibits various pharmacological activities, particularly outstanding in anti-inflammatory and metabolic regulation.
In vivo experiments, Carnosterone C at a dose of 100 mg/kg showed significant inhibitory effects on the carrageenan induced foot edema model in Sprague Dawley rats, indicating its good anti-inflammatory effect. This anti-inflammatory activity may be related to its regulation of inflammatory mediator release and inhibition of inflammatory signaling pathways.
Caryophyllone C has regulatory effects on various metabolic targets, including AMPK（PRKAA1）、PTPN1、STAT3、ABCB1、ALOX15、PRKCA、NFE2L2、SHBG、TOP1 And HIF1A, etc. By activating the AMPK signaling pathway, Carnosterone C can promote energy metabolism and lipid metabolism, and improve insulin resistance. Its inhibitory effect on PTPN1 (protein tyrosine phosphatase 1B) helps enhance insulin signaling and lower blood glucose levels. In addition, by regulating the NFE2L2 (nuclear factor erythroid 2-related factor 2) pathway, Caryophyllone C can enhance cellular antioxidant capacity and alleviate oxidative stress-related metabolic damage.
Caryophyllone C may also participate in the regulation of inflammation and tumor microenvironment by regulating transcription factors such as STAT3 and HIF1A, but related research is still in the preliminary stage and needs further clarification.
The mechanism of action of Caryophyllone C involves multiple signaling pathways and molecular targets, mainly including:
AMPK activation
AMPK, as a key regulatory factor in cellular energy metabolism, is activated by Carnosterone C, which promotes fatty acid oxidation and glucose uptake, and improves metabolic disorders.
PTPN1 inhibition
PTPN1 negatively regulates the insulin signaling pathway. Carnosterone C inhibits PTPN1 activity, enhances insulin sensitivity, and improves glucose metabolism abnormalities.
NFE2L2 regulation
NFE2L2 is a core transcription factor for antioxidant stress. Carnosterone C activates the NFE2L2 pathway, enhances cellular antioxidant defense, and reduces cellular damage caused by oxidative stress.
STAT3 and HIF1A regulation
STAT3 and HIF1A are involved in inflammatory and cellular adaptive responses, and Carnosterone C may exert anti-inflammatory and cell protective effects by regulating these transcription factors.
ABCB1 and TOP1 regulation
ABCB1 is a multidrug resistance related protein, TOP1 is a DNA topoisomerase, and the regulatory effect of Carnosterone C suggests its potential function in cell protection and drug metabolism.
The pharmacological parameters of Caryophyllone C show that it has good potential for drug development. The molecular weight of 480.64 conforms to Lipinski's rule, and a LogP value of 0.15 indicates good water solubility, which is beneficial for oral absorption. Although higher TPSA (130.64) and hydrogen bond acceptor numbers (7) may limit its membrane permeability, they also contribute to stable binding with the target.
In terms of safety, Caryophyllone C did not exhibit hepatotoxicity, cardiotoxicity, or hERG channel inhibition, reducing the risk of cardiovascular adverse reactions. It cannot penetrate the blood-brain barrier, reducing the possibility of central nervous system side effects. The results of Ames mutagenicity test are still unclear and require further testing.
In terms of pharmacokinetics, there is currently limited data on the absorption, distribution, metabolism, and excretion (ADME) of Carnosterone C. Preliminary studies indicate that its oral bioavailability is limited, which may be related to its high polarity and metabolic stability. In the future, its bioavailability needs to be improved through structural optimization and formulation improvement.
As a natural steroid with multi-target regulatory ability, Caryophyllone C has shown broad application prospects in metabolic diseases, inflammatory diseases, and related pathological states. Its anti-inflammatory effect provides a new idea for the treatment of chronic inflammatory diseases, and its metabolic regulation function is expected to be used as an adjuvant treatment for metabolic syndrome such as diabetes, obesity and fatty liver.
Future research should focus on the following directions:
In depth analysis of the mechanism
By utilizing modern molecular biology techniques, we aim to further elucidate the mechanism of action of Caryophyllone C in the cellular signaling network and clarify its interaction patterns with key targets.
Pharmacokinetic optimization
By improving drug design and formulation technology, we aim to enhance its oral bioavailability and in vivo stability, thereby increasing the feasibility of clinical applications.
Safety and Toxicological Assessment
The system conducts long-term toxicology and mutagenicity assessments to ensure its clinical safety and lay the foundation for clinical trials.
Clinical research advancement
Based on existing pharmacological evidence, design a reasonable clinical trial plan to verify its efficacy and safety in patients with metabolic and inflammatory diseases.
As a molting steroid derived from Leuzea carthamoids, Carnosteroid C has shown great potential for drug development due to its significant anti-inflammatory and metabolic regulatory activities. Its multi-target mechanism of action and superior safety characteristics provide theoretical basis and practical basis for its treatment in metabolic diseases and inflammation related diseases. Although the current research on its pharmacokinetics and clinical applications is not sufficient, with the advancement of related technologies and the deepening of research, Caryophyll C is expected to become an important research object and potential drug candidate molecule in the field of natural product pharmacology. Future interdisciplinary collaboration and systematic research will drive it from the laboratory to clinical practice, benefiting more patients.
