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Suramin hexasodium salt
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Suramin hexasodium salt图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
25mg电议

产品介绍
苏拉明六钠盐(Suramin hexasodium salt)是一种可逆的竞争性蛋白酪氨酸磷酸酶(PTPases)抑制剂。

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:
[1]. Bojanowski K, et al. Suramin is an inhibitor of DNA topoisomerase II in vitro and in Chinese hamster fibrosarcomacells. Proc Natl Acad Sci U S A. 1992 Apr 1;89(7):3025-9.
[2]. Li, H.; Li, H.; Qu, H.; et al. Suramin inhibits cell proliferation in ovarian and cervical cancer by downregulating heparanase expression. Cancer Cell Int. 2015, 15, 1–11
[3]. Yin, W. et al. Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin. Nat. Struct. Mol. Biol. 28, 319–325 (2021).
[4]. Salgado-Benvindo, C., Thaler, M., Tas, A., Ogando, N. S., et al. Suramin inhibits SARS-CoV-2 infection in cell culture by interfering with early steps of the replication cycle. 2020. Antimicrob. Agents Chemother. 20, DOI: 10.1128/AAC.00900-20
[5]. Kuo SC, Wang YM, Ho YJ, Chang TY, Lai ZZ, Tsui PY, Wu TY, Lin CC. 2016. Suramin treatment reduces chikungunya pathogenesis in mice. Antiviral Res 134:89–96.