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Product name: Asperosaponin VI
Synonym name: Akebia saponin D
Catalogue No.: BP0207
Cas No.: 39524-08-8
Formula: C47H76O18
Mol Weight: 929.107
Botanical Source: Present in Akebia quinata, Lonicera nigra, Patrinia and Phytolacca spp.
Physical Description: Powder
Type of Compound: Triterpenoids
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, up to kilograms
Inquire for bulk scale.
Descriptions:
Asperosaponin VI (ASA VI) is a kind of saponin in the medicinal herb Dipsacus asper Wall which has long been used as an antiosteoporosis drug, exhibits a significant induction of proliferation, differentiation and mineralization in MC3T3-E1 and primary osteoblastic cells, it may induce osteoblast maturation and differentiation, and then increase bone formation via increasing BMP-2 synthesis, and activating p38 and ERK1/2.[1]
Asperosaponin VI, a triterpene saponin isolated from Dipsacus asper Wall, plays protective roles on acute myocardial infarction in rats.[2]
Asperosaponin VI has protective effect against hypoxia-induced cardiomyocytes apoptosis probably by activating the PI3K/Akt and CREB pathways.[3]
References:
[1] Yinbo Niu ?, Yuhua Li ?, Huang H, et al. Phytothe Res , 2011, 25(11):1700-6.
[2] Li C, Liu Z J, Li G, et al. Eur J Pharmacol, 2010, 217(Pt 23):4123-31.
[3] Li C, Tian J, Li G, et al. Eur J Pharmacol, 2010, 649(1-3):100-7.
[4] Shan X, Wang J, Wu A. China Pharmacist, 2013, 16(03):388-90.
HPLC of Asperosaponin VI
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
304.7200
-3.0000
-2.5000
No
No
No
No
No
No
No
Asperosaponin VI (CAS No.: 39524-08-8) is derived from the traditional Chinese medicine Dipsacus asper Wall. ex Henry). As a commonly used herb in traditional Chinese medicine for nourishing the liver and kidneys and strengthening muscles and bones, Chuanxudan has long been used to treat osteoporosis, rheumatoid arthritis, and bruises. In recent years, with the development of modern pharmacology and molecular biology technologies, Chuanxuduan Saponin VI has attracted attention due to its multi-target and multi-pathway pharmacological activity, especially showing significant biological effects in regulating bone metabolism, protecting myocardium, preventing depression, and promoting wound healing. This paper aims to systematically review the chemical structure and physicochemical properties of Chuanxudan saponin VI, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation and pharmacokinetic characteristics, explore its clinical application potential and future research directions, and provide a reference for the field of natural product pharmacology.
Chuanxudan saponin VI belongs to the triterpene saponin class of compounds, with a molecular formula of C_42H_68O_18 and a molecular weight of 896.10. Its structural core is a pentacyclic triterpene backbone, connecting multiple glycosyl residues to form a typical saponin structure. The LogP value of Chuanxuan saponin VI is about -3.0, indicating strong hydrophilicity. The TPSA (Topological Polar Surface Area) reaches 304.72 Ų, and the number of hydrogen bond acceptors reaches 18, demonstrating strong polarity and hydrogen bonding ability. These physicochemical properties suggest that the compound's absorption in the body may be limited, while its polar structure facilitates stable binding with various biological macromolecule targets.
Chuanxuan saponin VI is not easily crossed by the blood-brain barrier (BBB), which is closely related to its high polarity and large molecular weight. In terms of safety, Chuanxuduan saponin VI showed no hepatotoxicity, cardiotoxicity, or hERG channel inhibition, and the Ames-induced mutagenic test was negative, indicating good safety and suitability for further drug development.
Chuanxudan saponin VI is mainly found in the roots of Chuanxudan. Chuanxudan is a perennial herbaceous plant of the Caprifoliaceae family, genus Chuanxudan, widely distributed in central-southern China and southwest China. Its root has been a traditional Chinese medicinal herb since ancient times, with effects such as nourishing the liver and kidneys, strengthening muscles and bones, and dispelling wind and dampness.
The extraction of Chuanxudan saponin VI is usually done by the water extraction alcohol precipitation method. The specific steps include: crushing the dried Rhizome roots, reflux extraction with water or 70%-80% ethanol, then adding ethanol to precipitate and remove impurities. Subsequently, the saponin was separated and purified by multi-stage column chromatography (such as silica gel columns and reversed-phase C18 columns), ultimately yielding high-purity Chuanxuan saponin VI. In recent years, modern technologies such as ultrasound-assisted extraction and microwave-assisted extraction have also been applied to improve extraction efficiency and purity. In addition, high-performance liquid chromatography (HPLC) combined with mass spectrometry (LC-MS) technology is widely used for qualitative and quantitative analysis.
Chuanxuan saponin VI has been studied most deeply in the field of bone metabolism. Multiple in vitro and in vivo experiments have shown that Chuanxudan saponin VI can significantly promote osteoblast differentiation (such as the MC3T3-E1 cell line) and enhance alkaline phosphatase (ALP) activity and mineralization capacity. Its mechanism of action mainly involves activating the bone morphogenetic protein-2 (BMP-2)-mediated signaling pathway, which further activates the p38 and ERK1/2 MAPK pathways, promoting the expression of osteogenic-related genes such as Runx2 and Osterix, which in turn promotes bone formation.
In addition, Chuanxuan saponin VI demonstrated significant bone protective effects in osteoporosis animal models, increasing bone density, improving bone microstructure, inhibiting bone resorption, and demonstrating good anti-osteoporosis potential.
Research on Chuanxuan saponin VI in the cardiovascular field shows that it has a significant protective effect against hypoxia-induced cardiomyocyte apoptosis. Mechanistically, Chuanxuan saponin VI activates the PI3K/Akt signaling pathway, promoting cell survival signaling and activating the cAMP reactive element-binding protein (CREB) pathway, inhibiting the expression of apoptosis-related proteins, reducing hypoxia-reperfusion injury, and protecting myocardial cell function.
Chuanxuan saponin VI has certain central nervous system regulatory effects, especially demonstrating antidepressant activity. Animal model studies have shown that Kawasudan saponin VI can regulate neurotransmitter levels and improve depressive-like behaviors. Its mechanism of action may involve regulating the neuroendocrine axis and anti-inflammatory effects, reducing neuroinflammation, and promoting neuroprotection.
Chuanxuduan saponin VI also shows promise in wound healing. In vitro experiments have shown that it can promote fibroblast proliferation and migration, accelerating wound closure. Mechanistically, it may be related to promoting extracellular matrix synthesis and regulating local inflammatory responses, helping to accelerate tissue regeneration and repair.
In addition to the main activities mentioned above, Chuanxudan saponin VI has also been reported to regulate hyperglycemia-related targets such as EHMT2, AMPK, and SGLT2, suggesting its potential for application in metabolic diseases. However, related research is still in its early stages and requires further validation.
The multi-target mechanism of Chuanxudan saponin VI reflects its complex pharmacological network regulatory characteristics.
BMP-2/p38 and ERK1/2 signaling pathways: Chuanxuan saponin VI induces BMP-2 expression, activates downstream p38 and ERK1/2 MAPK pathways, promotes osteoblast differentiation and mineralization, upregulates key transcription factors Runx2 and Osterix, and enhances bone formation.
PI3K/Akt and CREB pathways: In cardiomyocyte protection, chuanxuan saponin VI activates PI3K/Akt signaling, promotes cell survival, and inhibits apoptotic protein expression; At the same time, CREB activates, regulates the expression of anti-apoptotic genes, and alleviates hypoxia injury.
Metabolic Targets: Chuanxuduan saponin VI may regulate hyperglycemia-related targets such as AMPK (energy metabolism regulator), SGLT2 (sodium-glucose cotransporter 2), and EHMT2 (histone methyltransferase), suggesting potential roles in glucose metabolism and insulin sensitivity regulation.
Neuroprotective and antidepressant mechanisms: Chuanxuan saponin VI may exert antidepressant effects by regulating neurotransmitter systems and inflammatory factors, improving the neural environment.
Wound healing mechanisms: promotes fibroblast proliferation and migration, regulates extracellular matrix synthesis, modifies local inflammatory responses, and promotes tissue repair.
These diverse signaling pathways and regulatory targets reflect the broad pharmacological activity basis of Chuanxuduan saponin VI across various disease models.
Druggability evaluation of Chuanxuduan saponin VI showed good safety, with no hepatotoxicity, cardiotoxicity, or hERG channel inhibition, and the Ames-induced mutagenic test was negative, indicating a low genotoxicity risk. However, due to its large molecular weight (896.10 Da), high polarity (LogP approximately -3.0), and high TPSA (304.72 Ų), the oral bioavailability of Trancon Saponin VI may be limited, poorly absorbed in the body, and difficult to cross the blood-brain barrier.
Currently, pharmacokinetic research on Chuanxuan Saponin VI is relatively limited. Preliminary animal experiments indicate that this compound is widely distributed in the body, mainly metabolized through the liver, and its excretion pathway remains unclear. Research on its metabolites and metabolic enzyme systems still requires further research to clarify its in vivo kinetic characteristics and potential drug interaction risks.
To improve the bioavailability of Kawasuduan saponin VI, future strategies such as nanocarriers, liposome encapsulation, or structural modification may be considered to optimize its pharmacokinetic properties.
Chuanxudan Saponin VI, as the main active ingredient of Chuanxudan, demonstrates broad clinical application potential due to its multiple pharmacological activities such as promoting bone formation, myocardial protection, antidepressant, and wound healing assistance.
Osteoporosis and Fracture Repair: Chuanxuandan Saponin VI promotes osteoblast differentiation and bone formation, providing new therapeutic approaches for osteoporosis and fracture healing. In the future, it can be developed as a bone metabolism regulator or a bone repair adjunct drug.
Cardiovascular diseases: Its protective effect on hypoxic myocardial cells suggests potential application value in myocardial protection after ischemic heart disease and myocardial infarction.
Neuropsychiatric Disorders: Antidepressant activity may provide the potential for the adjunctive treatment of trangent saponin VI in depression and related neuropsychiatric disorders.
Wound repair: Its role in promoting wound healing gives it promising development in the treatment of trauma and skin diseases.
Nevertheless, the clinical translation of Chuanxudan Saponin VI still faces many challenges, including low bioavailability, complex metabolism in vivo, and lack of systematic clinical trial data. Future research should focus on:
Systematic research on pharmacokinetics and pharmacodynamics to clarify their in vivo behavior and dose-effect relationships.
Structural optimization and formulation development to enhance oral absorption and targeted delivery capabilities.
Multicenter, randomized, double-blind clinical trials to verify its safety and efficacy.
In-depth analysis of the mechanisms of multi-target action provides a theoretical foundation for precision therapy.
Combination drug strategies, exploring synergistic effects with existing drugs to expand their application scope.
Chuanxudan saponin VI, as an important active triterpene saponin in Chuanxudan, demonstrates significant therapeutic potential in bone metabolism regulation, myocardial protection, antidepressant, and wound healing due to its multi-target and multi-pathway pharmacological activity. Its excellent safety profile lays the foundation for subsequent drug development. However, due to poor pharmacokinetic properties and a lack of systematic clinical data, the clinical application of Chuanxuduan Saponin VI still requires further in-depth research. In the future, through structural optimization, formulation innovation, and clinical validation, Chuanxuduan Saponin VI is expected to be developed into a novel natural drug, providing effective pharmacological solutions for the treatment of related diseases.
Shenshuai
Wenjing
Hedandan
