Dietary triacylglycerols and cholesterol esters (TAG and CE)

Dietary triacylglycerols and cholesterol esters are the predominant forms of fat consumed in the human diet, serving as vital energy sources and precursors for cellular components (StatPearls, 2023). In the gastrointestinal tract, these lipids are emulsified by bile salts and hydrolyzed by enzymes such as pancreatic lipase and cholesterol esterase into smaller molecules like fatty acids and free cholesterol for absorption (PubMed, 2021). This absorption process is a key physiological step, but when excessive, it leads to metabolic disorders including obesity and hyperlipidemia, which are major risk factors for cardiovascular disease (NIH, 2022). While these lipids are not therapeutic targets in the traditional sense of being proteins, they are the substrates for enzymes and transporters that are targeted by drugs. For instance, orlistat inhibits the lipases required for triacylglycerol breakdown, while ezetimibe targets the NPC1L1 transporter to reduce cholesterol absorption (StatPearls, 2023).

Other names

Dietary fatsIntestinal lipidsNeutral lipidsExogenous lipidsLuminal triacylglycerols and cholesterol esters

Inhibition of gastrointestinal lipases (e.g., pancreatic lipase) to prevent triacylglycerol hydrolysis, or inhibition of sterol transporters (e.g., NPC1L1) to prevent cholesterol absorption (StatPearls, 2023).