This study evaluated the phytochemistry, male sexual function (MSF)-enhancing and toxicity potentials of aqueous root extract of G. erubescens (AREGE). For the MSF test, 30 rats were randomly divided into groups A, B, C, D, E and F, each group containing 5 rats. Group A represented the control and received only distilled water. Sexual dysfunction was induced in rats of groups B-F by orally administering clonidine (0.5 mg/kg body weight [BW]). Rats in groups B-F were thereafter treated with distilled water, 13.43 mg/kg BW Kongy [standard drug], AREGE [50 mg/kg BW], AREGE [100 mg/kg BW] and AREGE [200 mg/kg BW] respectively. Rats were treated for 7 days, sacrificed and their blood, penises and testes collected for analysis of selected MSF-associated biochemical parameters. For the toxicity study, 40 rats were randomly divided into groups W, X, Y and Z of 10 rats each and administered distilled water, AREGE [50 mg/kg BW], AREGE [100 mg/kg BW] and AREGE [200 mg/kg BW] respectively. Five rats per group were sacrificed 24 h after treatment for 1 day while the rest were sacrificed 24 h after treatment for 21 days. Their blood, livers and kidneys were collected for liver/kidney function indices determination. Extract contains alkaloids, flavonoids, steroids, iron, zinc, selenium, glutamic acid, arginine, phenylalanine, tryptophan and tyrosine among others. Clonidine reduced testosterone, luteinizing hormone (LH), dihydrotestosterone (DHT), nitric oxide (NO) and prolactin levels. The extract significantly increased (p < 0.05) testosterone, serum LH, DHT, prolactin and penile NO concentrations when compared with the clonidine and distilled water-treated group. Extract also significantly increased (p < 0.05) serum gammaglutamyl transferase (GGT), sodium, phosphate, creatinine, urea, liver/serum aspartate aminotransferase (AST) and alanine aminotransferase (ALT) but reduced kidney GGT and alkaline phosphatase (ALP) and serum total protein levels when compared with the control. Available results show that AREGE possesses MSF-enhancing activity but poses a threat to the normal functioning of the liver and kidney.