Haskap (Lonicera caerulea L.), an emerging commercial fruit crop in North America, has been known for its medicinal benefits amongst the people of Russia, Japan, and Northeastern China for centuries. The vitamin C content in haskap berries, ranging between 29 and 187 mg/100 g, is significantly higher than in other vitamin C-rich sources such as oranges, strawberries, and raspberries. Cyanidin-3-O-glucoside (C3G) is the major anthocyanin present in haskap comprising about 79–92% of its total anthocyanin content and over 60% of the total polyphenols. Considerable evidence shows significant antioxidant, cardio-protective, anti-inflammatory, neuroprotective, anticancer, and anti-diabetic properties of C3G-rich haskap preparations and C3G alone both in vitro and in vivo. This review broadly discusses the in vitro and pre-clinical significance of haskap-mediated cytoprotection and disease prevention; thereby, we strongly suggest further exploration of C3G-rich haskap preparations as potential functional food, dietary antioxidant supplements as well as natural health products targeting specific chronic and metabolic diseases.