Glycerophospholipids are the main components of all biological cell membranes,which play a very important physiological role in many life activities,including serving as an extracellular mediator in induction of cellular proliferation,involving in the development of nervous and vascular systems,intracellular signaling,and suppression of apoptosis.It is a great challenge for the identification and quantitative analysis of phospholipids due to the variety of glycerophospholipid species,their occurrence at low concentrations in biological samples,matrix effects and the lack of easily ionized groups in their chemical structures.Effective approach has been employed to improve their ionization efficiency,chromatographic resolution,and significantly increase the sensitivity of mass spectrometry(MS) detection by modifying the chemical structures of glycerophospholipids through derivatization technique.The integration of MS with derivatization has been widely used in proteomics,glyconics,metabolite analysis and many other applications.In recent years,this strategy has been gradually applied in lipidomics.An overview on derivatization in MS-based strategy for lipidomic analysis over the last decade is presented in this review,and glycerophospholipids which are relatively important lipids in biological systems are mainly focused.