包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
25mg | 电议 |
Cell lines | Vero E6 and Calu-3 |
Preparation Method | Vero E6 and Calu-3 cells were preincubated for 30 min with 2-fold serial dilutions of a starting concentration of 200 μM Suramin hexasodium salt and subsequently infected with 2 × 104PFU of SARS-CoV-2 (MOI of 1 on Vero E6 cells) in 50 μl medium with compound. |
Reaction Conditions | 200μM for 16 hours or 21 hours |
Applications | RT-qPCR revealed that the SARS-CoV-2 RNA levels decreased upon Suramin hexasodium salt treatment in a dose-dependent manner, showing a 3-log reduction at the highest concentration tested (200 μM) |
Animal models | C57BL/6JNarl (B6) mice |
Preparation Method | Suramin hexasodium salt was diluted in normal saline, and indicated doses were administered at 4 h pre-infection, 1day post-infection or/and 3day post-infection (dpi) via the intraperitoneal (ip) route. Specifically, each dose comprised 0, 0.25, 0.5, 1 or 2 mg suramin hexasodium salt. |
Dosage form | Intraperitoneal injection, 0, 0.25, 0.5, 1 or 2 mg |
Applications | Viral loads in sera of mock-treated mice infected with the 0810bTw, 0611aTw and 0706aTw CHIKV strains at the 2 dpi peak were 5.8, 3 and 4.2 Log10 CCID50/ml, respectively (Fig. 2A). To parallel, viral titers of suramin hexasodium salt-treated sera after received two doses (pre 4 h and 1 dpi) were 5, 2.5 and 3.8 Log10 CCID50/ml for 0810bTw, 0611aTw and 0706aTw strains, respectively. |
产品描述 | Suramin hexasodium salt is a polysulfonated naphthylurea with various biological activities. Suramin hexasodium salt is a DNA topoisomerase II inhibitor with an IC50of 5 μM[1]. Suramin hexasodium salt at 300–600 μg/ml significantly inhibited HO-8910 PM and HeLa cell growth at 24 h, in both a time-dependent and dose-dependent manner, with an IC50of 320 μg/ml and 475 μg/ml, respectively. Suramin hexasodium salt at 300 μg/ml significantly decreased the expression of Hpa mRNA (P < 0.005) and protein (P < 0.005) in both HO-8910 PM and HeLa cells at 48 h[2]. Suramin hexasodium salt shows antiviral activity against the newly emerged virus strain SARS-CoV-2[3,4].Solution based assays of RdRp inhibition determined that the half-maximal inhibition concentration (IC50) of suramin hexasodium salt is 0.26 μM, Cell-based experiments indicated that suramin hexasodium salt was able to inhibit SARS-CoV-2 duplication in Vero E6 cells with a half-maximal effective concentration (EC50) of roughly 2.9 μM[3].Suramin hexasodium salt treatment of infected Vero E6 cells led to a reduction in extracellular viral RNA levels of up to 3 log. The highest concentration of compound that was used proved harmless to the cells; also, cytotoxicity was observed previously only above 5 mM. Suramin hexasodium salt also displayed antiviral efficacy in a human lung epithelial cell line, and we observed a >2 log reduction in levels of infectious virus progeny in suramin hexasodium salt -treated cells (CC50/EC90 = >55)[4]. Suramin hexasodium salt has therapeutic effects on CHIKV-infected mice. Suramin hexasodium salt treatment ameliorated foot swelling and reduced inflammatory infiltration, which corresponded to reduced viremia and viral antigen expression in infected tissues. Suramin hexasodium salt induces a dose-dependent reduction in foot swelling in CHIKV 0810bTw-infected mice, and the vary degrees of decreased viremia that was detected in suramin hexasodium salt -treated mice further confirmed therapeutic effects of this drug. In the time-related assay, a single dose of 2 mg suramin hexasodium salt (at 4 h pre-infection) or double doses of 2 mg suramin hexasodium salt (at 1 dpi and 3 dpi) significantly decreased disease score and viremia compared to mock-treated mice. References: |