Abstract This study evaluated the inhibitory effects of kolaviron, a biflavonoid from Garcinia kola seed, on benzoyl peroxide (BPO)-induced free radical generation in rat’s skin. Adult male rats were administered with Group I: 0.2 ml acetone per animal as control, Group II: 100 mg of kolaviron/kg b.wt./0.2 ml acetone, Group IlI: 20 mg BPO/0.2 ml acetone per animal, Group IV: 100 mg of kolaviron/kg b.wt./0.2 ml acetone plus 20 mg BPO/0.2 ml acetone per animal. Skin of all the animals were removed quickly and processed for biochemical analysis. Benzoyl peroxide-treated rats showed (P <0.05) decrease in vitamin C, E, glutathione (GSH) and total antioxidant capacity (TAC) but when it is co-administered with kolaviron the values of vit C, E, GSH and TAC significantly increases. The values of protein carbonyl (PC), lipid peroxide (LP), malondialdehyde (MDA), nitrite (NO2), conjugated diene (CD) and hydrogen peroxide generation (H2O2) in rats treated with Benzoyl peroxide (P < 0.05) increases significantly but decreases as kolaviron was co-treated (P < 0.05). Taken together, kolaviron inhibited the adverse effects of BPO induce free radical generation.