An anti-Leishmania antimony derivative
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Sodium stibogluconate is a pentavalent antimony derivative that is highly active against Leishmania amastigotes in macrophages.1 Sodium stibogluconate has diverse effects on both this intracellular parasite and its host cell.2,3
1.Roberts, W.L., and Rainey, P.M.Antileishmanial activity of sodium stibogluconate fractionsAntimicrob. Agents Chemother.37(9)1842-1846(1993) 2.Frézard, F., Demicheli, C., and Ribeiro, R.R.Pentavalent antimonials: New perspectives for old drugsMolecules14(7)2317-2336(2009) 3.Singh, N., Kumar, M., and Singh, R.K.Leishmaniasis: Current status of available drugs and new potential drug targetsAsian Pac. J. Trop. Med.5(6)485-497(2012)
Cell experiment: |
Human myeloid cell line TF-1 is maintained in RPMI 1640 supplemented with 10% FCS and 40 ng/mL recombinant human GM-CSF. For cell proliferation assays, cells are washed in 10% FCS medium twice, resuspended in 10% FCS medium, incubated at 37°C for 16 h, and then cultured at 37°C in 10% FCS medium containing various amounts of cytokines, sodium stibogluconate, or potassium antimonyl tartrate for 3-6 days. The cell numbers in proliferation assays are determined by an MTT assay or by microscopic cell counting[1]. |
Animal experiment: |
BALB/c and athymic nude BALB/c mice are inoculated (s.c.) at the flanks with Renca cells (106 cells/site). Four days after inoculation, the mice are subjected to no treatment (control) or treatment with IL-2 (105 IU/day for 5 days i.p.), Stibogluconate sodium (12 mg/day i.m. at hip regions), or the combination of the two agents for 2 wk. Tumor volume is measured during the study period and calculated using the formula for a prolate spheroid[2]. |
参考文献: [1]. Pathak MK, et al. Sodium stibogluconate is a potent inhibitor of protein tyrosine phosphatases and augments cytokine responses in hemopoietic cell lines. J Immunol. 2001 Sep 15;167(6):3391-7. |
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