Structure of Astragaloside IV
CAS No.: 84687-43-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Astragaloside IV, an active component isolated fromAstragalus membranaceus, suppresses the activation ofERK1/2andJNK/b> , and downregulates matrix metalloproteases (MMP)-2, (MMP)-9in MDA-MB-231 breast cancer cells.
Synonyms: AS-IV; AST-IV
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CAS No. : | 84687-43-4 |
Formula : | C41H68O14 |
M.W : | 784.97 |
SMILES Code : | O[C@H]([C@H]([C@@H]([C@@H](CO)O1)O)O)[C@@H]1O[C@@H]2[C@@]3([H])C(C)(C)[C@@H](O[C@H]4[C@@H]([C@H]([C@@H](CO4)O)O)O)CC[C@]3(C5)[C@]65CC[C@]7(C)[C@]([C@](C)(O8)CC[C@H]8C(C)(O)C)([H])[C@@H](O)C[C@](C)7[C@]6([H])C2 |
Synonyms : |
AS-IV; AST-IV
|
MDL No. : | MFCD16036240 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
Astrocytes | 1, 10, 50, 100, 200 μM | 10 days | AS-IV inhibited astrocyte replicative senescence, evidenced by decreased senescence-associated β-galactosidase activity and expression of senescence marker p16, increased nuclear level of lamin B1, and reduced pro-inflammatory senescence-associated secretory phenotype. | PMC7137443 |
H9C2 cells | 50 µM or 100 µM | 24 hours | AS-IV reversed the Dox-induced apoptosis and necrosis of H9C2 cells in a dose-dependent manner. | PMC9276071 |
Caco-2 cells | 150 µM | 24 hours | To evaluate the inhibitory effect of Astragaloside IV on LPS-induced inflammation in Caco-2 cells, the results showed that Astragaloside IV significantly reversed the inhibition of cell viability by LPS and reduced the production of inflammatory cytokines. | PMC11061986 |
RGC-5 cells | 100 mg/L | 24 hours | To investigate the protective effect of Astragaloside IV on H2O2-induced oxidative stress injury in RGC-5 cells, the results showed that Astragaloside IV increased cell survival rate, decreased apoptotic cell number, reduced H2O2-induced reactive oxygen species levels, inhibited the decrease of mitochondrial membrane potential, reduced cytochrome c release, inhibited Bax and caspase-3 expression, and increased Bcl-2 expression | PMC6022471 |
Bone marrow-derived macrophages (BMDMs) | 100 µM | 24 hours | AS-IV significantly suppressed pro-inflammatory macrophage subsets and promoted pro-resolving macrophage subsets. | PMC8473681 |
mouse podocytes | 10 µM, 20 µM, 40 µM | 24 hours | To evaluate the protective effects of Astragaloside IV on high glucose-induced podocyte injury, the results showed that Astragaloside IV significantly improved the expression levels of NLRP3, pro-caspase-1 and caspase-1, and inhibited the decrease in cell viability | PMC8262660 |
BMSCs cells | 0-80 μM | 24, 48, 72 hours | Astragaloside IV significantly enhanced the cell viability of BMSCs at 40 μM, while a further increase in concentration attenuated this effect. | PMC8120474 |
RAW264.7 cells | 10 μM, 40 μM, 80 μM | 4 days | Astragaloside IV promoted osteoclast differentiation at low concentrations (10 μM), while osteoclastogenesis was inhibited at higher concentrations with a reduction in the osteoclast area and accumulation of preosteoclasts. | PMC8120474 |
THP-1 monocytes | 80 nM | 48 hours | Astragaloside IV significantly inhibited IL-4 and IL-13-induced M2 polarization, as shown by reduced expression of CD206 and M2-associated genes. | PMC6116548 |
A549 and H1299 lung cancer cells | 80 nM | 48 hours | Astragaloside IV suppressed M2-CM-induced invasion, migration, and angiogenesis of A549 and H1299 cells. | PMC6116548 |
Human bone marrow mesenchymal stem cells (BMSCs) | 5 μM, 20 μM, 50 μM, 100 μM | To evaluate the effect of AS-IV on BMSCs proliferation, results showed that AS-IV (50 μM) significantly increased BMSCs proliferation. | PMC10623974 | |
Human umbilical vein endothelial cells (HUVECs) | 5 μM, 20 μM, 50 μM, 100 μM | To evaluate the effect of AS-IV on HUVECs proliferation, migration, and tube formation ability, results showed that AS-IV (50 μM) significantly promoted HUVECs proliferation, migration, and tube formation ability. | PMC10623974 | |
TM3 cells | 100 µM | 3 days | AS.IV effectively reduced mutant myocilin associated ER stress | PMC8619727 |
A549 cells | 100 μg/mL | 48 hours | To investigate the effect of Astragaloside IV on TGF-β1-induced epithelial-mesenchymal transition (EMT). Results showed that Astragaloside IV significantly reversed TGF-β1-induced EMT, inhibited α-SMA expression, and increased E-cadherin expression. | PMC6111865 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
C57BL/6J mice | Lewis lung cancer model | Intragastric administration | 40 mg/kg | Once daily for 21 days | Astragaloside IV significantly inhibited the growth and metastasis of Lewis lung cancer and reduced the percentage of M2 macrophages in tumor tissue. | PMC6116548 |
Wistar rats | Dox-induced heart failure model | intraperitoneal injection | 1.0 mg/kg | once daily for 9 weeks | AS-IV treatment significantly increased the ejection fraction in heart failure rats, reduced cardiomyocyte apoptosis, and reversed the abnormal expression of DRP1 and mitofusin. | PMC9276071 |
Mice | MPTP-induced Parkinson's disease model | Intraperitoneal injection | 100 mg/kg | Every 12 hours for 5 weeks | AS-IV protected against the loss of dopamine neurons and behavioral deficits in the mouse model of PD, accompanied by reduced accumulation of senescent astrocytes in substantia nigra compacta. | PMC7137443 |
SD rats | Distraction osteogenesis model | Intragastric administration | 20 mg/kg/day | Once daily for 4 weeks | Astragaloside IV accelerated bone regeneration during DO by enhancing osteogenesis and preosteoclast-induced angiogenesis simultaneously, partially through AKT/GSK-3β/β-catenin signaling. | PMC8120474 |
C57BL/6 mice | DSS-induced colitis model | Oral gavage | 100 mg/kg | Once daily for 10 days | To evaluate the therapeutic effect of Astragaloside IV on DSS-induced colitis in mice, the results showed that Astragaloside IV significantly alleviated inflammation, improved intestinal barrier function, and acted by inhibiting the PI3K/AKT signaling pathway. | PMC11061986 |
C57BL/6J mice | DSS-induced colitis model | Oral | 50 or 100 mg/kg | Once daily for 10 days | AS-IV attenuated the inflammatory progression of DSS-induced colitis and promoted the phenotypic transition of macrophages from pro-inflammatory to pro-resolving macrophages. | PMC8473681 |
Sprague-Dawley rats | Glucocorticoid-induced avascular necrosis of the femoral head model | Oral gavage | 20 mg/kg/day | Once daily for 6 weeks | To evaluate the protective effect of AS-IV on glucocorticoid-induced avascular necrosis of the femoral head, results showed that AS-IV promoted osteogenesis and angiogenesis via the Akt/Runx2 and Akt/HIF-1α/VEGF pathways, respectively, and suppressed apoptosis and oxidative stress via the Akt/Bad/Bcl-2 and Akt/Nrf2/HO-1 pathways, respectively. | PMC10623974 |
Mice | db/db mice | intragastric administration | 40 mg/kg | once daily for 12 weeks | To evaluate the protective effects of Astragaloside IV on diabetic nephropathy in db/db mice, the results showed that Astragaloside IV significantly reduced weight gain, hyperglycemia and serum triglyceride levels, improved renal function and podocyte injury, and inhibited NLRP3 inflammasome-mediated inflammation | PMC8262660 |
Kunming mice | Acute alcohol-induced liver injury model | Oral | 50, 150, and 500 mg/kg | Once daily for 7 days | Astragaloside IV ameliorates acute alcohol-induced liver injury by modulating gut microbiota and inhibiting NLRP3/Caspase-1 signaling pathway. | PMC10228327 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT01553643 | Intracranial Arterial Stenosis | Phase 4 | Unknown | - | Taiwan ... More >> China Medical University Hospital Recruiting Taiching, Taiwan Contact: Chung Hsiang Liu, MD. Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.27mL 0.25mL 0.13mL |
6.37mL 1.27mL 0.64mL |
12.74mL 2.55mL 1.27mL |
Tags: Astragaloside IV | MMP | ERK | JNK | Matrix metalloproteinases | Extracellular signal regulated kinases | c-Jun N-terminal kinase | Extracellular Signal-Regulated Kinase 1 | Extracellular Signal-Regulated Kinase 2 | Nuclear factor erythroid 2-related factor 2 | Antioxidant Response Element | cytokine production | antioxidant | extracellular matrix remodeling | 84687-43-4
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