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Astragaloside IV (AS-IV), the primary active ingredient in Astragalus membranaceus, has a wide range of potential applications, particularly in cancer, digestive disorders, cardiovascular diseases, and other contemporary high incidence, high-risk diseases. It may also be developed as a medication. Astrageloside IV has been shown to have protective effects on the immune, digestive, nervous, and cardiovascular systems. The action mechanisms were linked to the control of calcium balance, anti-oxidants, anti-apoptosis, antivirus software, and other factors.
| Targets |
MMP-2; MMP-9; ERK1; ERK2; JNK
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|---|---|
| ln Vitro |
Astragaloside IV (10, 20, 40 ng/mL) inhibits NSCLC cell growth, whereas low concentrations of astragaloside IV (1, 2.5, 5 ng/mL) has no obvious cytotoxicity on cell viability. Additionally, astragaloside IV combined therapy significantly raises the chemosensitivity of NSCLC cells to cisplatin. When cisplatin is present, astragaloside IV co-treatment significantly reduces the mRNA and protein levels of B7-H3[2]. Astragaloside IV reduces the activity of the matrix metalloproteases (MMP)-2 and -9, suppresses the activation of the mitogen activated protein kinase (MAPK) family members ERK1/2 and JNK, and inhibits the viability and invasive potential of MDA-MB-231 breast cancer cells[4].
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| ln Vivo |
Astragaloside IV (10, 20 mg/kg, p.o.) exhibits a potent ability to prevent cognitive deficits brought on by transient cerebral ischemia and reperfusion. In comparison to the Model group, Astragaloside IV (10 mg/kg) and Astragaloside IV (20 mg/kg) can significantly lower these cytokine levels. It is possible that both MyD88-dependent and -independent pathways are crucial for Astragaloside IV's anti-inflammatory effects given that it significantly reduces the level of TLR4 and its downstream proteins. In addition to lowering the expression of Iba1 protein, astragaloside IV also inhibits the expression of NLRP3 and cleaved-caspase-1.
In the mouse model, the high-dose astragaloside IV group significantly improved the 48-hour survival rate [60% (9/15) vs 13.3% (2/15), P < 0.05], significantly decreased serum ALT and AST levels (P < 0.01), significantly decreased liver histopathological indices and the degree of hepatocyte apoptosis (P < 0.01), significantly increased SOD activity (P < 0.01), and significantly decreased the content of MDA.
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| Enzyme Assay |
In a nutshell, MDA-MB-231 cells treated as advised or tumor tissues are harvested and lysed in Mg2+ lysis buffer containing 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.5 M NaCl, and protease inhibitor cocktail. Equal amounts of lysates are incubated with PAK-PBD beads at 4°C for one hour. Centrifugation is used to pellet PAK-PBD beads, which are then washed in a solution of 25 mM Tris (pH 7.5), 30 mM MgCl2, and 40 mM NaCl. Western blotting is used to find active Rac1.
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| Cell Assay |
The CCK-8 assay is used to determine cell viability. In a nutshell, 4×104 (cells/well) of cultured NSCLC cells are seeded into 96-well plates. Then, for an additional 2 hours at 37°C in the dark, a 10 µL/well CCK8 solution is added. The wavelength of 490 nm is used to calculate absorbance.
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| Animal Protocol |
BCCAO is used to prepare transient cerebral ischemia and reperfusion because it is regarded as the best model for studying the injury-mediated inflammatory response to transient cerebral ischemia and reperfusion. The Sham, Model, Astragaloside IV (10 mg/kg), and Astragaloside IV (20 mg/kg) treatment groups are randomly assigned to mice. The IV astragaloside treatment groups begin 7 days prior to surgery and end on the day of sacrifice by intragastric administration. 2 hours before ischemia on the day of surgery, astragaloside IV is administered. Distilled water is used to treat the groups that operated as a sham and the model. The bilateral common carotid arteries are exposed and delicately separated with a small ventral neck incision after the mice have been given an intraperitoneal injection of chloral hydrate (350 mg/kg) to induce anesthesia. With a few minor modifications from the previous description, the common carotid arteries are then twice (20 min each) occluded with ligated surgical silk. Between each of the two occlusion periods (ischemia 20 min, reperfusion 10 min, ischemia 20 min), there is a 10 min reperfusion period. The same surgical procedure is performed on mice who underwent a sham operation without the surgical silk ligation. Heaters are used to keep the mouse's body temperature at 370±5°C throughout the procedure and until the animal wakes up from the anesthesia.
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| References |
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| Molecular Formula |
C41H68O14
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|---|---|
| Molecular Weight |
784.9702
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| Exact Mass |
784.46
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| Elemental Analysis |
C, 62.73; H, 8.73; O, 28.54
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| CAS # |
84687-43-4
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| Related CAS # |
84687-43-4
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| Appearance |
solid powder
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| SMILES |
C[C@]12CC[C@@]34C[C@@]35CC[C@@H](C([C@@H]5[C@H](C[C@H]4[C@@]1(C[C@@H]([C@@H]2[C@]6(CC[C@H](O6)C(C)(C)O)C)O)C)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O)O)O)(C)C)O[C@H]8[C@@H]([C@H]([C@@H](CO8)O)O)O
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| InChi Key |
QMNWISYXSJWHRY-YLNUDOOFSA-N
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| InChi Code |
InChI=1S/C41H68O14/c1-35(2)24(54-33-29(48)26(45)20(44)17-51-33)9-11-41-18-40(41)13-12-37(5)31(39(7)10-8-25(55-39)36(3,4)50)19(43)15-38(37,6)23(40)14-21(32(35)41)52-34-30(49)28(47)27(46)22(16-42)53-34/h19-34,42-50H,8-18H2,1-7H3/t19-,20+,21-,22+,23-,24-,25-,26-,27+,28-,29+,30+,31-,32-,33-,34+,37+,38-,39+,40-,41+/m0/s1
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| Chemical Name |
(2R,3R,4S,5S,6R)-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-6-[(2S,3R,4S,5R)-3,4,5-trihydroxyoxan-2-yl]oxy-9-pentacyclo[9.7.0.01,3.03,8.012,16]octadecanyl]oxy]-6-(hydroxymethyl)oxane-3,4,5-triol
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| Synonyms |
Astragaloside IV
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~127.4 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (3.18 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (3.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2739 mL | 6.3697 mL | 12.7393 mL | |
| 5 mM | 0.2548 mL | 1.2739 mL | 2.5479 mL | |
| 10 mM | 0.1274 mL | 0.6370 mL | 1.2739 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.
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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