Pro-inflammatory and toxicological evaluation of Hepacare(®) in mice.

OBJECTIVES: Hepacare(®) is a widely marketed herbal formulation in Nigeria for treating chronic liver ailments. This study evaluated the safety, as well as pro-inflammatory and genotoxicity effects, of Hepacare(®) in mice. METHODS: The effect of the formulation was estimated in a 28-day study where 25 mice were divided into five groups, and Hepacare(®) was orally administered at 250, 500, 750 and 2500 mg/kg body weight. The biochemical and haematological parameters were determined, organ weights were estimated and histopathology was also conducted. mRNA expression of the pro-inflammatory cytokines, TNF-α and IL-6 was estimated by RT-PCR in acute toxicity experiments. RESULTS: The LD(50) was calculated at 3807.89 mg/kg body weight in mice. There was a significant increase (p < 0.05) in the ALP activity in the 750 mg/kg treated group, while the 2500 mg/kg group exhibited significant increases in their AST, ALT, ALP, total bilirubin and total protein levels compared with the control group. However, there was a significant dose related increase in monocytes counts in the groups treated with 750 and 2500 mg/kg. There was no significant difference (p > 0.05) in TNF-α and IL-6 mRNA expression in the genotoxicity studies in all of the treatment groups compared with the control. However, several hepatic and nephro-pathological derangements were observed in the groups treated with higher doses of the formulation. CONCLUSIONS: The study established that the herbal formulation may not induce significant pro-inflammatory toxic responses and genotoxic effects, but prolonged intake of higher doses may cause severe biochemical and clinical abnormalities.