Synonym name:
Catalogue No.: BP0123
Cas No.: 18642-44-9
Formula: C₃₇H₅₆O₁₁
Mol Weight: 676.844
Botanical Source: Actaea racemosa (Cimicifuga racemosa) and Cimicifuga spicata

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 Actein

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

Introduction/Overview

Actein (CAS No. 18642-44-9) is a triterpene glycoside natural product derived from the rhizome of the traditional Chinese medicinal material Cimicifuga (Cimicifuga foetida). In recent years, it has attracted widespread attention due to its diverse biological activities. As a natural triterpenoid compound with significant pharmacological activity, Cimicifugal Pavilion not only shows potential therapeutic value in bone metabolism regulation, anti-tumor effects, and antioxidant effects, but also involves regulatory mechanisms of various signaling pathways, indicating its promising application in osteoporosis, tumors—especially breast and bladder cancers—as well as liver cirrhosis. This paper systematically reviews the chemical structure and physicochemical properties of Cimicifuga Pavilion, plant origin and extraction methods, pharmacological activity, and mechanism of action. Combined with druggability evaluation and pharmacokinetic data, it explores its clinical application potential and future development directions.

Chemical structure and physicochemical properties

Cimicifuga Ting belongs to the triterpene glycoside class of compounds, with a molecular weight of 660.8 and a LogP value of about 3.5, indicating moderate lipid solubility. Its molecular structure contains multiple hydroxyl and glycoside groups, with a TPSA (topological polar surface area) of 180 and 11 hydrogen bond acceptors, suggesting high molecular polarity that may affect bioavailability and membrane permeability. The chemical structure of the Cimicifuga Pavilion is complex, containing a typical triterpene skeleton linked to glycosides, giving it unique biological activity.

In terms of physicochemical properties, Cimicifuga Pavilion has moderate solubility in water and organic solvents, good stability, and is suitable for various extraction and purification processes. The combination of its LogP value and TPSA value showed that the cimicifuguga pavilion has a lower ability to penetrate the blood-brain barrier (Low), which somewhat limits its application in central nervous system diseases but helps reduce CNS toxicity.

Plant Origins and Extraction Methods

Cimicifuga is mainly isolated from the rhizome of Cimicifuga foetida. Cimicifuga, a plant of the Ranunculaceae family, is widely distributed in Northeast and North China. In traditional Chinese medicine, it is used to relieve exterior symptoms, clear heat, and relieve pain. As one of the main active ingredients of Cimicifuga, the extraction and purification processes of Cimicifuga Pavilion are already quite mature.

Common extraction methods include alcohol extraction (such as ethanol or methanol extraction), binder-liquid separation, and column chromatography separation. The typical process is: crush dried cimicifuga rhizomes and extract them by reflux with 70% ethanol; after concentration, distribute them with solvents such as ethyl acetate, followed by silica gel column chromatography or high-performance liquid chromatography (HPLC) for purification. In recent years, new technologies such as ultrasound-assisted extraction and supercritical fluid extraction have also been applied to the extraction of the Cimimagina Pavilion, improving extraction efficiency and purity.

Pharmacological activity research

Cimimifuga Pavilion has a wide range of pharmacological activities, including bone metabolism regulation, anti-tumor, antioxidant, and anti-fibrotic properties.

1. Bone metabolism and osteoporosis

Cimimifuga Pavilion has a significant osteogenesis-promoting effect on osteoblasts, stimulating their proliferation and differentiation, and facilitating the synthesis of bone matrix. Research shows that Cimimuga Pavilion can prevent oxidative damage to osteoblasts in osteoporosis patients and slow down bone loss, demonstrating its potential value in osteoporosis prevention and treatment. By regulating intracellular redox status, it protects osteoblasts from oxidative stress damage, promotes bone formation, and has a good protective effect on bone.

2. Antitumor activity

Cimicifuga Pavilion exhibits activity in various tumor cell lines that inhibit proliferation, induce apoptosis, and induce autophagy. Especially in breast and bladder cancer cells, the Cimicifuga Pavilion exerts its anti-cancer effects through multiple signaling pathways. Its mechanisms include:

• By regulating ER-Sarcoplasmic Reticulum (ER-IP3) receptor and Na,K-ATPase activity, intracellular calcium ion release is induced, affecting the cell cycle and apoptosis.
• Inhibits NF-κB and MEK signaling pathways, reducing tumor cell proliferation and invasion capacity.
• It promotes activation of the ROS/JNK pathway, inhibits the AKT signaling pathway, and induces autophagy and apoptosis in bladder cancer cells.
• It has low toxicity in the body and demonstrates good safety.

3. Antioxidant and anti-fibrotic

Cimicifuga Pavilion activates the NFE2L2 (Nrf2) pathway, enhancing cellular antioxidant capacity and reducing oxidative stress-related cell damage. Additionally, Cimicifuga Pavilion shows potential protective effects against fibrotic diseases such as cirrhosis, possibly inhibiting fibrosis and improving liver function by regulating key targets like STAT3, MMP2, and HIF1A.

Mechanism of action and molecular targets

The multi-target mechanism of Cimicifuga Pavilion is the foundation for its multiple biological activities. The main targets and signaling pathways involved are as follows:

• Calcium signaling regulation: Cimicifuga Pavilion can induce intracellular calcium ion release by altering the activities of ER-IP3 receptors and Na,K-ATPase, regulating intracellular calcium homeostasis, and affecting osteoblast function as well as tumor cell proliferation and apoptosis.
• NF-κB and MEK/ERK pathway: Cimicifugethethillescent inhibits the NF-κB signaling pathway, reduces inflammatory responses and tumor cell survival signals, while regulating the MEK/ERK pathway, affecting cell proliferation and differentiation.
• ROS/JNK and AKT pathway: Cimicifuga pavilion activates the JNK pathway by promoting ROS production, inhibiting AKT signaling, inducing autophagy and apoptosis in tumor cells, and exerting anticancer effects.
• Antioxidant-related target: Cimicifuga Pavilion activates NFE2L2 (Nrf2) transcription factor, enhancing cellular antioxidant defenses and protecting osteoblasts and hepatocytes from oxidative damage.
• Cirrhosis-related targets: including STAT3, MMP2, HIF1A, SIRT1, etc. Cimicifuga Pavilion inhibits liver fibrosis and improves the liver microenvironment by modulating these targets.

Druggability evaluation and pharmacokinetics

The druggability parameters of the Cimicifuga Pavilion indicate that it has certain development potential. The molecular weight is 660.8, TPSA is 180, and the number of hydrogen bond acceptors is 11, indicating strong polarity and possibly affecting oral bioavailability. A LogP value of 3.5 indicates moderate lipid solubility, which is beneficial for cell membrane penetration. Low blood-brain barrier permeability reduces the risk of central nervous system side effects.

In toxicological evaluation, Cimicifuga Pavilion did not show significant cardiotoxicity or hERG channel inhibition, suggesting good cardiovascular safety. Hepatotoxicity and Ames-related mutagenicity remain unclear and require further systematic study.

Pharmacokinetics, existing literature reports are limited, but preliminary studies show that Cimicifugal Pavilion is widely distributed in the body, has stable metabolism, and low toxicity, making it suitable for further drug development. In the future, further research is needed on its absorption, distribution, metabolism, and excretion (ADME) characteristics to optimize administration methods and formulations.

Prospects and outlooks for clinical applications

As a multifunctional natural triterpene glycoside, Cimicifugating shows broad clinical application prospects due to its remarkable activity in bone metabolism regulation, anti-tumor, and anti-fibrotic effects.

• Osteoporosis Treatment: Cimimifuga Pavilion promotes osteoblast bone formation and provides antioxidant protection, offering new approaches for osteoporosis prevention and treatment, especially suitable for the elderly and patients with bone metabolism disorders.
• Tumor adjuvant therapy: Cimimifuga Pavilion exhibits antiproliferative and apoptotic effects in various tumor cells such as breast and bladder cancer, showing promise as an adjunct to anticancer drugs, enhancing chemotherapy efficacy and reducing side effects.
• Liver fibrosis and cirrhosis: By regulating multiple fibrosis-related targets, Cimimifuga Pavilion may become a potential therapeutic agent for cirrhosis and related liver diseases.
• Safety advantages: Cimifuga Pavilion has low toxicity in the body, with low risks of cardiotoxicity and mutagenicity, making it suitable for long-term use.

Future research should focus on systematic preclinical pharmacokinetics and toxicology of Cimicifuga Pavilion, clarify the molecular mechanisms of its targets, and conduct clinical trials to verify its safety and efficacy. At the same time, by integrating modern medicinal chemistry and formulation, the properties and administration methods of the drugs are being optimized, promoting Cimimagining Pavilion from the laboratory to clinical applications.

Conclusion

As a natural triterpene glycoside derived from Cimicifuga, Cimicifugal Pavilion, with its multi-target and multi-mechanism pharmacological activity, shows broad application prospects in the treatment of diseases such as osteoporosis, tumors, and liver fibrosis. Its unique chemical structure and physicochemical properties provide the basis for its biological activity, while extensive pharmacological research reveals its complex mechanisms of action. Although clinical data on Cimicifuga Pavilion are currently insufficient, its good safety and diverse therapeutic potential make it a research hotspot in the field of natural product pharmacology. In the future, through in-depth mechanistic research and clinical validation, Cifa Pavilion is expected to become an important candidate for natural drug development, providing new therapeutic strategies for the prevention and treatment of related diseases.