Asperosaponin VI

Phytother Res. 2011 Nov;25(11):1700-6.

Asperosaponin VI, a saponin component from Dipsacus asper wall, induces osteoblast differentiation through bone morphogenetic protein-2/p38 and extracellular signal-regulated kinase 1/2 pathway.[Pubmed: 21452371 ]

Osteoporosis is a reduction in skeletal mass because of the loss of osteoblastic activity or an increase in osteoclastic activity. The survival of osteoblast cells plays a crucial role in the development of osteoporosis.
METHODS AND RESULTS:
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. The assay of cell proliferation, alkaline phosphatase (ALP) activity and measurement of mineralized matrix, showed that ASA VI exhibited a significant induction of proliferation, differentiation and mineralization in MC3T3-E1 and primary osteoblastic cells. Induction of differentiation by ASA VI was associated with increased bone morphogenetic protein-2 (BMP-2), indicating that BMP-2 is essential in ASA VI to mediate osteoblast maturation and differentiation. In addition, ASA VI may induce differentiation by increasing the activity of p38 and ERK1/2.
CONCLUSIONS:
In conclusion, ASA VI may induce osteoblast maturation and differentiation, and then increase bone formation via increasing BMP-2 synthesis, and activating p38 and ERK1/2.

Eur J Pharmacol. 2010 Feb 10;627(1-3):235-41.

Protective roles of Asperosaponin VI, a triterpene saponin isolated from Dipsacus asper Wall on acute myocardial infarction in rats.[Pubmed: 19909736 ]

Asperosaponin VI is a saponin of the medicinal herb Dipsacus asper (Xuduan), and no pharmacological activity has been reported yet. In this study, we investigated the anti-myocardial ischemia effects of Asperosaponin VI (ASA VI) both in vivo and in vitro.
METHODS AND RESULTS:
An animal model of myocardial ischemia(MI) injury was induced by coronary occlusion, pretreatment with ASA VI (10 and 20mg/kg, i.v.) could protect the heart from ischemia injury by decreasing the levels of creatine kinase-MB (CK-MB), lactate dehydrogenase (LDH), glutamic oxalacetic transaminase (GOT) and cardiac troponin T (cTnT) in serum, increasing the levels of catalase, glutathione peroxidase (GSH-Px) and superoxide dismutase (SOD) levels in heart, and decreasing that of malondialdehyde (MDA) level in acute MI rats. ASA VI also raised the activities of mitochondrial enzymes (succinate dehydrogenase (SDH), isocitrate dehydrogenase (ICDH), malate dehydrogenase (MDH) and alpha-ketoglutarate dehydrogenase (alpha-KGDH)) and those of adenosine triphosphate (ATP) content, but lowered Ca(2+) level. Electrocardiograph parameters and histopathological observations demonstrated the same protective effects. In vitro experiment, neonatal rat cardiomyocytes were incubated to test the direct cytoprotective effect of ASA VI against H(2)O(2) exposure. Pretreatment with ASA VI (30 and 60 microg/ml) prior to H(2)O(2) exposure increased cell viability and inhibited H(2)O(2)-induced reactive oxygen species increase. ASA VI (15, 30 and 60 microg/ml) also increased the activities of LDH in the cultured supernatant and SOD in cardiomyocytes, but decreased the cardiomyocytes MDA level.
CONCLUSIONS:
Our results suggested that ASA VI could provide significant cardioprotective effects against acute MI in rats. The mechanisms might be attributed to scavenging lipid peroxidation products and reactive oxygen species, increasing antioxidant defense enzymes and preventing mitochondrial damage.

Eur J Pharmacol. 2010 Dec 15;649(1-3):100-7.

Asperosaponin VI protects cardiac myocytes from hypoxia-induced apoptosis via activation of the PI3K/Akt and CREB pathways.[Pubmed: 20863824 ]

Cardiomyocyte apoptosis plays a critical role in the progress of heart diseases. Asperosaponin VI (ASA VI), a triterpene saponin isolated from Dipsacus asper Wall, has shown cardioprotective effects in vivo. However, whether ASA VI has a protective effect against cardiomyocyte apoptosis is poorly understood.
METHODS AND RESULTS:
The present study was aimed to investigate the cardioprotective role of ASA VI and the underlying mechanisms in hypoxia-induced cardiomyocyte apoptosis. Cardiomyocytes were exposed to hypoxic condition for 6 h and then cell viability markedly decreased, lactate dehydrogenase (LDH) and creatine phosphokinase (CK) activities in the culture supernatant significantly increased. Hypoxia-activated apoptosis were confirmed by Hoechst 33258 nuclear staining and Annexin V-FITC staining. These changes were associated with the decrease of the Bcl-2/Bax ratio, active caspase-3 expression, phosphorylations of Akt and cAMP response element-binding protein (CREB). Moreover, ASA VI significantly attenuated increased LDH and CK activities, and increased cell viability in hypoxia treated myocytes in a dose-dependent fashion. Hoechst 33258 nuclear staining and Annexin V-FITC staining observations demonstrated the same protective effects. ASA VI treatment inhibited apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB. Furthermore, the protective effects of ASA VI were prevented by phosphatidylinositol-3-kinase (PI3K) inhibitor LY294002 treatment.
CONCLUSIONS:
In consequence, we demonstrated that ASA VI had protective effect against hypoxia-induced cardiomyocytes apoptosis probably by activating the PI3K/Akt and CREB pathways.

Nat Prod Commun. 2014 Jun;9(6):773-8.

Chromatographic fingerprint combined with content of asperosaponin VI and antioxidant activity for quality evaluation of wine-fried Dipsaci Radix.[Pubmed: 25115076]

Dipsaci Radix, the dry root of Dipsacusasper Wall. ex Henry, is a commonly used traditional Chinese medicine (TCM).
METHODS AND RESULTS:
A novel comprehensive method was proposed for quality evaluation of wine-fried Dipsaci Radix by an integrated data including three aspects of information: high performance liquid chromatography (HPLC) fingerprint, Asperosaponin VI content and antioxidant activity (AA). Various indicators including fingerprint similarity, Asperosaponin VI content and AA were respectively employed for quality assessment of processed Dipsaci Radix samples. Results showed that considerable differences existed in quality of processed samples with different processing conditions according to three indicators. Among the factors affecting quality of wine-fried Dipsaci Radix, heating temperature was the most influential factor based on analysis of variance (ANOVA), and should be cautiously controlled. The three evaluation indicators respectively used for optimization of processing technology suggested different optimal conditions of wine-frying. Therefore, a combined indicator based on three evaluation indicators was used for determination of optimal processing condition. Multivariate statistical methods such as Hierarchical Clustering Analysis (HCA) and Principal Components Analysis (PCA) were both employed to classify the processed samples for quality evaluation.
CONCLUSIONS:
To more comprehensively evaluate the quality of wine-fried Dipsaci Radix, HPLC fingerprint combined with content of Asperosaponin VI and AA may be a reasonable and practical approach.