Previously, anthocyanins were successfully acylated with lauric acid using Novozym 435 lipase, and the corresponding products were confirmed to have higher stability. As novel synthetic compounds, their toxicological safety has not been evaluated. Therefore, acute, subacute and subchronic toxicities of anthocyanin-lauric acid derivatives (ALDs) were investigated while their antioxidant activities were also evaluated in vitro. The acute toxicity results showed that the 50% lethal dose (LD50) of ALDs in mice was >10 g kg-1. Subsequently, the subacute toxicity test was conducted by oral administration of ALDs at doses of 0.63, 1.25 and 2.50 g kg-1 for 28 days. No adverse effect of ALDs on body weight, food/water intake, organ coefficient and histology was observed. Though there were some fluctuations in AST and ALT, the tested biochemical parameters were maintained within the normal ranges. The subchronic toxicity test results demonstrated that less than 0.60 g of ALDs per kg BW intake did not affect mortality, body weight, food/water intake, gross pathology, histology, hematology and serum biochemistry. Furthermore, cyanidin-3-(6''-dodecanoyl)-glucoside, the main component of ALDs, had a beneficial reducing power and a strong DPPH˙, ABTS+˙, and O2-˙ scavenging activity. This study provides an imperative reference to the safety of ALDs, suggesting their application as novel colorants or antioxidants in food and therapeutics.