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                同义名:
                    
                        
                            黄芪皂苷 IV
                            
                             / AS-IV; AST-IV
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
Astragaloside IV是一种从黄芪中分离的活性皂苷类物质,能抑制 ERK1/2 和 JNK 的激活,并能下调 MDA-MB-231 乳腺癌细胞中的基质金属蛋白酶 MMP-2 和 MMP-9 的表达,具有抗肿瘤活性。
 
                                 
                                
                            

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| 描述 | Astragaloside IV(AS-IV) is a saponin from Astragalus membranaceus. Oral administration of AS-IV (10 and 20 mg/kg) significantly attenuated memory impairment and neuroinflammation[3]. High-dose astragaloside IV has a significant protective effect against D-GalN/LPS-induced (D-galactosamine/lipopolysaccharide-induced ) acute liver injury in mice [4]. High doses of astragaloside IV (10, 20, 40 ng/ml) inhibited NSCLC (non-small cell lung cancer ) cell growth[5]. Astragaloside IV inhibited the viability and invasive potential of MDA-MB-231 breast cancer cells, suppressed the activation of the mitogen activated protein kinase (MAPK) family members ERK1/2 and JNK, and downregulated matrix metalloproteases (MMP)-2 and -9[6]. | 
| 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. | 
| 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. | 
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 | 
| NCT01553643 | Intracranial Arterial Stenosis | Phase 4 | Unknown | - | Taiwan ... 展开 >> China Medical University Hospital Recruiting Taiching, Taiwan Contact: Chung Hsiang Liu, MD. 收起 << | 
| 计算器 | ||||
| 存储液制备 |  | 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 | |
| CAS号 | 84687-43-4 | 
| 分子式 | C41H68O14 | 
| 分子量 | 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 | 
| MDL No. | MFCD16036240 | 
| 别名 | 黄芪皂苷 IV ;AS-IV; AST-IV | 
| 运输 | 蓝冰 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, room temperature | 
| 溶解方案 | DMSO: 105 mg/mL(133.76 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
 
 
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