Leaves and fruits of Horus nigra L. (Moraceae) are used for the treatment of wounds especially mouth sore in Turkish traditional medicine. The present study was designed to investigate wound healing activity of M. nigra by using incision and excision wound models. Furthermore, anti-inflammatory activity was assessed by Whittle method. Lyophilized fruit extract (MNF) displayed significant wound healing activity, while aqueous leaf extract of M nigra (MNL) did not. Through biological activity guided fractionation technique, MNF was subjected to successive solvent extraction. Among the subextracts obtained, n-butanol (MNF-nBuOH) subextract was found to possess wound healing activity. MNF-n-BuOH was subjected Sephadex LH-20 column chromatography to obtain three fractions, which then applied to the same biological activity tests. Compounds 1 and 2 were isolated from the active fraction and their structures were identified as quercetin-3-O-rutinoside and kaempferol-3-O-rutinoside, respectively. The isolates were investigated for their in vitro enzyme inhibitory activities.