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Astragaloside II (Astrasieversianin VIII)

Alias: Astrasieversianin VIIIAstragaloside II
Cat No.:V29119 Purity: ≥98%
Astragaloside II is a natural compound extracted from Astragalus membranaceus.
Astragaloside II (Astrasieversianin VIII)
Astragaloside II (Astrasieversianin VIII) Chemical Structure CAS No.: 84676-89-1
Product category: Disease Research Fields
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Astragaloside II is a natural compound extracted from Astragalus membranaceus.
Astragaloside II (Astrasieversianin VIII) (CAS 84676-89-1) is a triterpenoid saponin and an effective MDR reversal agent. It can downregulate the expression of P-gp and mdr1 genes, suppress phosphorylation of extracellular signal regulated kinase 1/2, p38, and c-Jun N-terminal kinase. Astragaloside II has immunomodulating activity and can trigger T cell activation through regulation of CD45 protein tyrosine phosphatase activity. It induces osteogenic activities of osteoblasts through the bone morphogenetic protein-2/MAPK and Smad1/5/8 pathways. It also has cardioprotective effects and causes improvement in cognitive function.
Biological Activity I Assay Protocols (From Reference)
Targets
Astragaloside II targets multiple pathways. It downregulates the expression of P-gp and mdr1 genes. It suppresses phosphorylation of extracellular signal regulated kinase 1/2, p38, and c-Jun N-terminal kinase. It regulates CD45 protein tyrosine phosphatase activity. It induces osteogenic activities through the bone morphogenetic protein-2/MAPK and Smad1/5/8 pathways. It serves as an autophagy inhibitor which restores chemosensitivity of anticancer agent cisplatin and enhances tumor cell death.
ln Vitro
In vitro, Astragaloside II can trigger T cell activation through regulation of CD45 protein tyrosine phosphatase activity. It increases CD45-mediated IL-2 and IFN-γ secretion and upregulates the mRNA levels of IFN-γ and T-bet in primary splenocytes and CD4+ T cells. It induces osteogenic activities of osteoblasts through the BMP-2/MAPK and Smad1/5/8 pathways. It downregulates the expression of P-gp and mdr1 gene.
ln Vivo
In vivo, Astragaloside II is a potent multidrug resistance (MDR) reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. It has cardioprotective effects as well as causing improvement in cognitive function. It is used in the prevention of cardio-cerebral vascular diseases. It also stimulates osteoblast differentiation.
Enzyme Assay
For cell-free assays, the inhibitory activity of Astragaloside II on P-gp can be assessed using ATPase activity assays or membrane vesicle transport assays. Its effect on ERK1/2, p38, and JNK phosphorylation can be studied using kinase activity assays with purified enzymes. Its immunomodulatory activity can be assessed by measuring its effect on CD45 phosphatase activity using a phosphatase assay with a chromogenic substrate.
Cell Assay
For in vitro cellular assays, the MDR reversal activity of Astragaloside II is assessed in drug-resistant cancer cell lines (e.g., hepatic cancer cells overexpressing P-gp). Cells are treated with Astragaloside II in combination with chemotherapeutic agents (e.g., cisplatin). Cell viability is measured using MTT or SRB assays. The expression of P-gp and mdr1 is assessed by Western blot or qPCR. Apoptosis is assessed by flow cytometry. Its immunomodulatory activity is assessed in primary splenocytes or CD4+ T cells by measuring cytokine secretion and T cell activation markers.
Animal Protocol
For in vivo studies, Astragaloside II could be administered orally or intraperitoneally in mouse xenograft models of drug-resistant hepatic cancer. It is used in combination with cisplatin or other chemotherapeutic agents. Tumor volume is measured periodically. MDR reversal is assessed by measuring the accumulation of chemotherapeutic agents in tumor tissue. Its immunomodulatory effects can be studied in models of immune-related diseases.
ADME/Pharmacokinetics
Astragaloside II (CAS 84676-89-1) has a molecular formula of C43H70O15 and a molecular weight of 827.02 g/mol. It is also known as Astrasieversianin VIII. Purity is typically >98% for research use. Solubility: soluble in DMSO and other organic solvents. For in vitro studies, stock solutions are prepared in DMSO. For in vivo administration, it can be formulated in suitable vehicles. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. ADMET properties: Caco-2 permeability -5.966, MDCK permeability -5.224, PAMPA +++, HIA, VDss -0.474.
Toxicity/Toxicokinetics
No detailed toxicity data is publicly available. As a natural saponin from Astragalus membranaceus, it is generally considered to have low toxicity, but standard toxicological studies would be required for drug development. In vitro cytotoxicity assays in various cell lines are typically performed alongside efficacy studies to confirm that observed effects are not due to a general reduction in cell viability.
References

[1]. Astragaloside II induces osteogenic activities of osteoblasts through the bone morphogenetic protein-2/MAPK and Smad1/5/8 pathways. Int J Mol Med. 2012 Jun;29(6):1090-8.

[2]. Reversal of P-glycoprotein-mediated multidrug resistance of human hepatic cancer cells by Astragaloside II. J Pharm Pharmacol. 2012 Dec;64(12):1741-50.

[3]. Astragaloside II triggers T cell activation through regulation of CD45 protein tyrosine phosphatase activity. Acta Pharmacol Sin. 2013 Apr;34(4):522-30.

Additional Infomation
Astragaloside II is a triterpenoid saponin whose cyclic astragalool is glycosylated at positions 3 and 6 by 2-O-acetyl-β-D-xylose and β-D-glucosyl residues, respectively. It is a plant metabolite. It is a β-D-glucosinolate, a monosaccharide derivative belonging to the oxacyclopentane class of compounds, a pentacyclic triterpenoid, and also a triterpenoid saponin. Functionally, it is related to cyclic astragalool. Astragaloside II has been reported in Astragalus hoantchy, Astragalus lepsensis, and other organisms with relevant data. See also: Root (part) of the closely related Astragalus propinquus.
Astragaloside II is a research-grade compound and is not approved for therapeutic use. It serves primarily as a pharmacological tool for studying MDR reversal, immunomodulation, and osteogenesis. Its mechanism of action involves downregulation of P-gp and mdr1 genes, suppression of MAPK phosphorylation, and regulation of CD45 phosphatase activity. It is a natural product from Astragalus membranaceus. No clinical trials have been reported.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C₄₃H₇₀O₁₅
Molecular Weight
827.01
Exact Mass
826.471
CAS #
84676-89-1
PubChem CID
13996693
Appearance
White to off-white solid powder
Density
1.4±0.1 g/cm3
Boiling Point
896.9±65.0 °C at 760 mmHg
Flash Point
265.3±27.8 °C
Vapour Pressure
0.0±0.6 mmHg at 25°C
Index of Refraction
1.615
LogP
0.8
Hydrogen Bond Donor Count
8
Hydrogen Bond Acceptor Count
15
Rotatable Bond Count
9
Heavy Atom Count
58
Complexity
1580
Defined Atom Stereocenter Count
21
SMILES
CC(=O)O[C@@H]1[C@H]([C@@H](CO[C@H]1O[C@H]2CC[C@]34C[C@]35CC[C@@]6([C@H]([C@H](C[C@]6([C@@H]5C[C@@H]([C@H]4C2(C)C)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O)O)O)C)O)[C@]8(CC[C@H](O8)C(C)(C)O)C)C)O)O
InChi Key
AYWNHWGQTMCQIV-PENCHUSISA-N
InChi Code
InChI=1S/C43H70O15/c1-20(45)54-32-28(48)22(47)18-53-36(32)57-26-10-12-43-19-42(43)14-13-39(6)33(41(8)11-9-27(58-41)38(4,5)52)21(46)16-40(39,7)25(42)15-23(34(43)37(26,2)3)55-35-31(51)30(50)29(49)24(17-44)56-35/h21-36,44,46-52H,9-19H2,1-8H3/t21-,22+,23-,24+,25-,26-,27-,28-,29+,30-,31+,32+,33-,34-,35+,36-,39+,40-,41+,42-,43+/m0/s1
Chemical Name
[(2S,3R,4S,5R)-4,5-dihydroxy-2-[[(1S,3R,6S,8R,9S,11S,12S,14S,15R,16R)-14-hydroxy-15-[(2R,5S)-5-(2-hydroxypropan-2-yl)-2-methyloxolan-2-yl]-7,7,12,16-tetramethyl-9-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-pentacyclo[9.7.0.01,3.03,8.012,16]octadecanyl]oxy]oxan-3-yl] acetate
Synonyms
Astrasieversianin VIIIAstragaloside II
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~150 mg/mL (~181.38 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (3.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.2092 mL 6.0459 mL 12.0918 mL
5 mM 0.2418 mL 1.2092 mL 2.4184 mL
10 mM 0.1209 mL 0.6046 mL 1.2092 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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