In this work, a [Cu(mal)(bpy)] center dot H2O (mal, L-(-)-malic acid; bpy, 4,4 '-bipyridyl) homochiral metal-organic frameworks (MOFs) was synthesized and used for modifying the inner walls of capillary columns by utilizing amido bonds to form covalent links between the MOFs particles and capillary inner wall. The synthesized [Cu(mal)(bpy)] center dot H2O and MOFs-modified capillary column were characterized by X-ray diffraction, thermogravimetric analysis, particle size distribution analysis, nitrogen absorption characterization, FTIR spectroscopy, SEM, and energy-dispersive X-ray spectroscopy (EDX). The MOFs-modified capillary column was used for the stereoisomer separation of some drugs. The LODs and LOQs of six analytes were 0.1 and 0.25 mu g/mL, respectively. The linear range was 0.25250 mu g/mL for ephedrine, 0.25-250 mu g/mL for pseudoephedrine, 0.25-180 mu g/mL for Dpenicillamine, 0.25-120 mu g/mL for L-penicillamine, 0.25-180 mu g/mL for D-phenylalanine, and 0.25-160 mu g/mL for L-phenylalanine, all with R-2 > 0.999. Finally, the MOFs-modified capillary column was applied for the analysis of active ingredients in a real sample of the traditional Chinese medicine ephedra.