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Pentosan Polysulfate Sodium has been shown to inhibit HIV-1 activity with an ED ₅₀ of 0.19 μg/mL in MT-4 cells. It inhibits HIV-1 antigen expression in HUT-78 cells at an ED ₅₀ of 0.02 μg/mL, and complete inhibition of HIV-1 antigen expression is obtained at a concentration of 4.0 μg/mL.
Pentosan Polysulfate Sodium suppresses NF-κB, decreases the proinflammatory actions of TNFα, and decreases high glucose and advanced glycation end products (AGEs) stimulated MCP-1 production.

Pentosan Polysulfate Sodium has been shown to decreases interstitial inflammation and glomerulosclerosis in 5/6 nephrectomized rats. Pentosan polysulfate treatment preserves renal function, significantly reduces albuminuria, and markedly decreases the severity of renal lesions, including tubulointerstitial inflammation. Pentosan Polysulfate Sodium also reduces upregulation of TNFα and proinflammatory genes in aging diabetic kidneys.