This study investigated the biochemical and histopathological testicular dysfunctions following subacute toxic exposure to malathion; and the potential counteracting effects of N-acetyl cysteine (NAC) and Silymarin against these induced toxic effects. The study was carried out on 48 Sprague-Dawley males, rats were divided into six equal groups, drugs were given by gastric gavage daily for 30 days as follow; control group: received distilled water, the group I: rats were treated with NAC at a dose 200 mg/kg/day; group II: rats were treated with Silymarin at a dose 200 mg/kg/day; group III: rats were given malathion at a dose of 200 mg/kg/day; group IV: rats were given malathion plus NAC; group V: rats were given malathion plus Silymarin. Significant reductions in the testicular weights were observed in malathion exposed rats. Malathion caused significant reductions in hormonal assay including follicle –stimulating hormone (FSH), luteinizing hormone (LH) and testosterone, butyryl cholinesterase activity as well, sperm counts and motility with significant increases in abnormal sperm morphology. The histopathological findings showed diffusely necrotic seminiferous tubules and arrested spermatogenesis. Administration of NAC and Silymarin improved the biochemical and histopathological alterations in the testes induced by malathion. However, NAC was much better than Silymarin for inducing these protective effects.