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Extracts of the bulbs of Italian ecotypes of Allium sativum were analysed to determine their phenolic profiles, antioxidant activities, ascorbic acid and allicin content, and in vitro antibacterial and anti-proliferative activities. Ultra performance liquid chromatography with diode array detector (UPLC-DAD) was used to detect and quantify gallic acid, chlorogenic acid, caffeic acid, epicatechin, hyperoside, ferulic acid, apigenin, p-coumaric acid and allyl isothiocyanate. All extracts exhibited antioxidant activity with concentrations necessary to inhibit the activity of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical by 50% (EC50) ranging from 60 to 114 mg. Ascorbic acid and allicin ranged between 0.268 and 0.658 mg/g, and between 0.411 and 1.105%, respectively. Extracts exhibited antimicrobial activity against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa more so than against Bacillus cereus. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays demonstrated that the extracts inhibited the proliferation of the human epithelial colorectal adenocarcinoma (Caco-2) cells in time- and dose-dependent manners.