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Chemical Structure| 84687-43-4 Chemical Structure| 84687-43-4

Structure of Astragaloside IV
CAS No.: 84687-43-4

Chemical Structure| 84687-43-4

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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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Product Details of Astragaloside IV

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

Safety of Astragaloside IV

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • JNK

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. J Neuroinflammation. 2020 Apr 6;17(1):105.
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. Chin Med J (Engl). 2022 May 5;135(9):1099-1101.
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. J Transl Med. 2024 Apr 30;22(1):406.
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 Neural Regen Res. 2018 Jun;13(6):1081-1086.
Bone marrow-derived macrophages (BMDMs) 100 µM 24 hours AS-IV significantly suppressed pro-inflammatory macrophage subsets and promoted pro-resolving macrophage subsets. Front Immunol. 2021 Sep 13;12:740565.
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 Int J Mol Med. 2021 Aug;48(2):164.
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. Int J Biol Sci. 2021 Apr 24;17(7):1821-1836.
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. Int J Biol Sci. 2021 Apr 24;17(7):1821-1836.
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. J Exp Clin Cancer Res. 2018 Aug 29;37(1):207.
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. J Exp Clin Cancer Res. 2018 Aug 29;37(1):207.
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. Cell Prolif. 2023 Nov;56(11):e13485.
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. Cell Prolif. 2023 Nov;56(11):e13485.
TM3 cells 100 µM 3 days AS.IV effectively reduced mutant myocilin associated ER stress Int J Mol Sci. 2021 Nov 19;22(22):12508.
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. J Cell Mol Med. 2018 Sep;22(9):4354-4365.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
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. Chin Med J (Engl). 2022 May 5;135(9):1099-1101.
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. J Neuroinflammation. 2020 Apr 6;17(1):105.
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. J Transl Med. 2024 Apr 30;22(1):406.
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. Int J Biol Sci. 2021 Apr 24;17(7):1821-1836.
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. Cell Prolif. 2023 Nov;56(11):e13485.
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. J Exp Clin Cancer Res. 2018 Aug 29;37(1):207.
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 Int J Mol Med. 2021 Aug;48(2):164.
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. Front Immunol. 2021 Sep 13;12:740565.
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. Ann Med. 2023 Dec;55(1):2216942
C57BL/6 mice Total-body irradiation-induced aging model Oral gavage 50 mg/kg Once daily for 2 weeks To evaluate the improvement effect of CAG on age-related symptoms, results showed that CAG significantly alleviated aging phenotypes (e.g., grayed fur, osteoporosis) and improved behavioral performance in aged mice. Additionally, CAG reduced the expression of senescence markers (e.g., P53, P21, and P16) and decreased the production of SASP factors. Int J Mol Sci. 2023 Mar 31;24(7):6554.

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 <<

Protocol

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

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