Lysophospholipids (LPLs), including glycerolysophospholipids and lysosphingolipids, constitute a group of important lipid mediators. What is more, dietary LPLs have a positive impact towards health, apparently without meaningful side effects. Since the total chemical synthesis of fully active, enantiomerically pure LPLs is a very complicated challenge, the present review is devoted to biotransformations based on the action of various phospholipases and lipases that additionally fully meet the green chemistry concept. We also discuss the benefficial effects of bioactive lysophospholipids, focusing on lysophosphatidic acid, lysophosphatidylcholine, lysophosphatidylglycerol, sphingosylphosphorylcholine, lysophosphatidylinositol, lysophosphatidylserine, lysophosphatidylethanolamine, cyclic phosphatidic acid, and sphingosine- 1-phosphate. Besides, we detail their structure, enzymatic routes of in vivo generation, the main routes of enzymatic digestion in the gut and isolation of phospholipids from natural sources with carbon dioxide supercritical extraction-based processes. Keywords: Beneficial effects, digestion, extraction, lipases, lysophospholipids, phospholipases.
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