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Summary This work investigates the antiradical capacity and potential of Garcinia kola extracts to improve the biochemical markers associated with erectile function and its possible application in clinical treatment. Inhibitory properties of aqueous extract of G. kola on phosphodiesterase-5 (PDE-5), arginase, angiotensin I –converting enzyme (ACE), and acetylcholinesterase (AChE) in rat’s genitals tissues were evaluated. Likewise, G. kola extract was explored for reducing power (FRAP) and 1.1-diphenyl-2-picryl-hydrazil (DPPH) radical scavenging abilities. G. kola extract exhibited greater PDE-5 (IC50 = 47.52 ± 0.01 μg/mL), ACE (IC50 = 46.90 ± 0.87 μg/mL), AChE (IC50 = 44.85 ± 1.33 μg/mL) and arginase (IC50 = 47.71 ± 0.25 μg/mL) inhibitory activity in the corpus cavernosum tissue than PDE-5 (IC50 = 75.58 ± 2.04 μg/mL), ACE (IC50 = 53.00 ± 0.30 μg/mL), AChE (IC50 = 54.57 ± 1.50 μg/mL) and arginase (IC50 = 69.68 ± 2.42 μg/mL) inhibitory activity in the testicular tissue homogenate. Furthermore, G. kola exhibited radical scavenging abilities against FRAP and DPPH* radicals. Hence, our results revealed that G. kola extracts are good sources for the development of nutraceuticals and pharmacological properties with attributes to enhance erectile performance.