We present the inhibitory properties of the Solanum nigrescens anthocyanin fraction (SNAF) and its major constituents on alpha‐glucosidase (AG), pancreatic lipase (PL), HMG‐CoA reductase, and ornithine decarboxylase (ODC). The effect of SNAF was simultaneously evaluated in ICR male mice exposed to triglyceride charge test (TCT). HPLC‐MS profiling revealed the presence cyanidin‐3‐O‐rutinoside‐5‐glucoside (CRG), delphinidin‐3‐(p‐coumaroyl)‐rutinoside‐5‐glucoside (DCRG), and petunidin‐3‐(cis‐p‐coumaroyl)‐rutinoside‐5‐glucoside (PCRG) as major constituents of the fraction. SNAF, CRG, and specially PCRG, induced strong non‐competitive inhibition on PL (IC50, 33‐86 µg mL‐1). The results of TCT confirmed their capacity to ameliorate (p < 0.001) hypertriglyceridemia during postprandial and interdigestive stages. SNAF, CRG, DCRG, and PCRG caused negligible growth inhibition (MIC > 600 µg mL‐1) on beneficial bacteria whereas SNAF and DCRG exerted inhibitory activity on Helicobacter pylori ATCC25922 (MIC,187‐64 µg mL‐1). Additional exploration revealed that SNAF and DCRG produced non‐competitive activity on H. pylori urease, which facilitates bacterial growth under acidic conditions.