Chirality has attracted increasing attentions in the pharmaceutical industry,owing to great differences in pharmacological,toxicological and/or metabolic activities of enantiomeric drugs in living systems.The development of diverse approaches for chiral separation of optically active compounds has become a growing focus of researches.The inherent chirality of biomacromolecules,involving DNA,RNA and proteins,has exhibited intriguing applications as chiral stationary phases for high-performance liquid chromatography and chiral selectors in membranes.Here introduce our works on enantioselective separation using biomolecular enantioselective recognition.1) Bovine serum albumin (BSA) anchored on the surface of magnetic Fe3O4 nanoparticles (MNPs) were prepared using electrostatic adsorption and studied as a new magnetic chiral selector for the separation of chiral drug enantiomers.It is indicated that the immobilized BSA molecules on the magnetic nanoparticles using electrostatic adsorption retain their stereoselective recognition with site II-binding drug ibuprofen at pH 7.0 and site I-binding drug ofloxacin at pH 9.0,with a optimal loading of 467 mg BSA per gram of MNPs.Depending upon the eutectic point of racemic compound,a hybrid process involving the enrichment of one enantiomer using BSA-PDDA-MNPs followed by subsequent crystallization is proposed to obtain the enantiomer with higher optical purity.2) We presented a novel and facile method to generate DNA-based selectors to discriminate enantiomers,of which the core is to construct chiral-recognition sites along the DNA helix structures via metal ion-coordination.The enantiomeric excess (e.e.) of the ofloxacin racemate solution,after being adsorbed by the RET-Cu(II) complex,can be increased up to 59% in R-enantiomer with the [Cu2+]/base ratio of 0.1,while under the same [Cu2+]/base ratio the highest e.e.value reaches 51% in case of VEGF and 48% for c-kit2 respectively (Table 1).