Oxophenarsine (hydrochloride)

Oxophenarsine hydrochloride is an anti-syphilitic agent, and also has non-classical applications including treating chronic discoid lupus erythematosus, inhibiting HIV-1 protein synthesis, and prolonging the duration of insulin action. Oxophenarsine hydrochloride forms an unstable insulin complex via sulfhydryl groups or free amino groups, thereby prolonging the hypoglycemic effect of insulin. Oxophenarsine hydrochloride inhibits HIV-1-specific protein synthesis and virus production^[1][2][3]. In Vitro:Oxophenarsine hydrochloride (18 h) forms an unstable complex with purified Lilly Isletin insulin, and this complex reverts to unmodified insulin after 2 weeks of storage at low temperature^[1].
Oxophenarsine (0.15-12 μg/mL; 4-12 days) shows no cytotoxicity against H9 T cells and PHA-stimulated peripheral blood lymphocytes at concentrations up to 6.0 μg/mL, and toxicity is only observed at concentrations of 12 μg/mL and above^[2].
Oxophenarsine (0.038-6.0 μg/mL; 12 days) potently suppresses acute HIV-1 infection in PHA-stimulated peripheral blood lymphocytes and H9 T cells. After 12 days of incubation, concentrations of 0.15 μg/mL and above achieve over 5 log₁₀ inhibition^[2].
Oxophenarsine (0.06-60 μg/mL) does not inhibit the activity of purified HIV-1 reverse transcriptase even at concentrations as high as 60 μg/mL^[2].
Oxophenarsine (0.006-6.0 μg/mL; 4 weeks) completely inhibits HIV-1 production by lymphocytes from HIV-1 seropositive subjects that are co-cultured with PHA-stimulated peripheral blood lymphocytes for 4 weeks at concentrations of 0.6 μg/mL and above^[2].
Oxophenarsine (0.6-6.0 μg/mL; 0-40 days) potently inhibits HIV-1 production in H9-HIV-1 persistently infected cells at concentrations of 0.6 μg/mL and above, eliminates detectable viral p24, reverse transcriptase activity and infectious virus within 4-7 days, and the inhibitory effect is reversible after drug withdrawal^[2].
Oxophenarsine (0.6-6.0 μg/mL; 10 days) inhibits the synthesis of HIV-1-specific proteins in acutely infected H9 cells at concentrations of 0.6 μg/mL and higher, without affecting viral DNA or RNA levels^[2].
Oxophenarsine (0.6-6.0 μg/mL; 20 days) inhibits the synthesis of HIV-1-specific proteins in H9-HIV-1 persistently infected cells at concentrations of 0.6 μg/mL and above, without affecting viral DNA or RNA levels^[2].