To investigate the effect of blood-activating Chinese medicinal compounds and water-draining Chinese medicinal compounds on tumor necrosis factor alpha (TNF-alpha) and nuclear factor kappaB (NF-kappa B) expressions in rats with intracerebral hemorrhage (ICH) at the acute stage, and to monitor their therapeutic effect and mechanism of action on inflammation and cerebral edema. A rat model of cerebral hemorrhage was achieved by injecting autologous arterial blood into the caudate nucleus. A total of 168 rats were randomly divided into 4 groups: blood-activating medicine group (n=42), water-draining medicine group (n=42), sham operated group (n=42), and the model group (n=42). A series of brain samples were obtained at days 1, 3 and 5 after ICH from rats in all groups. Protein expression levels of TNF-alpha and NF-kappa B were measured by immunohistochemical staining and gene expression levels of TNF-alpha and NF-kappa B were measured by real-time fluorescent PCR. Compared to the sham operated group, protein expression levels of TNF-alpha and NF-kappa B in the model group significantly increased (P < 0.01). Protein and gene expressions of TNF-alpha from the blood-activating medicine group and water-draining medicine group significantly decreased when compared to those in the model group P < 0.05). Meanwhile, compared to the model group, the expression of NF-kappa B in the blood-activating medicine group significantly decreased (P < 0.05), while expression of NF-kappa B in the water-draining medicine group did not differ (P > 0.05). Blood-activating Chinese medicinal compounds and water-draining Chinese medicinal compounds can alleviate inflammation of peripheral tissue and cerebral edema. However, the blood-activating Chinese medicinal compounds were more effective than the water-draining Chinese medicinal compounds. The possible effective mechanism may be by means of inhibiting the activation of NF-kappa B so as to suppress the transcription of target genes including gene expression of TNF-alpha.