The cape myrtle,Myrsine africanaL., is a widely used medicinal plant, which has not been well investigated. We assessed thein vivohepatoprotective andin vitroantiproliferative and antioxidant effects of leaf extracts ofM. africanachemically profiled using high-performance liquid chromatography. Three flavonoids were quantified, and gas chromatography–mass spectrometry analysis revealed the presence of common fatty acids. The animal study was conducted on mice treated with CCl4, using three doses each of the methanol and chloroform extract (100, 200 and 300 mg/kg b.w.),with silymarin as a positive control. Hepatoprotective effects were determined by analyzing blood for liver marker and antioxidant enzymes, direct bilirubins and total proteins. The methanol extract (300 mg/kg b.w.) showed the strongest hepatoprotective effects against abnormalities produced by CCl4. Thein vivohepatoprotective effects correlated well with thein vitroantioxidant and antiproliferative activities and with high levels of flavonoids in the extracts. Finally, molecular docking studies of the constituent quercetin were undertakenin silicoand several sites of binding to human estrogen receptor (ER) protein, linked with alkaline phosphatase, identified.