The flower of Syringa pubescens Turcz. is a Chinese folk medicine and also used as flower tea for healthcare. The effects of five drying methods on the active compound contents, the antioxidant abilities, anti-inflammatory properties and enzyme inhibitory activities were evaluated. The plant materials were treated using shade-drying, microwave drying, sun-drying, infrared drying and oven drying. The seven active compounds were simultaneously determined by an HPLC method. Furthermore, the chemicals differences were assessed using Scanning electron microscopy, UV spectroscopy and infrared spectroscopy. The antioxidant capacities and protective effects on L02 cells induced by hydrogen peroxide were measured. The anti-inflammatory effects on lipopolysaccharide-induced RAW264.7 cells were investigated. The enzyme inhibitory activities were determined against α-amylase, α-glucosidase cholinesterases and tyrosinase. The results indicated that drying methods had significantly influences on the active compound contents and biological properties. In consideration of the contents of bioactive compound, the suitable drying methods were SHD, SD, OD and MD. The SHD sample exhibited stronger radical scavenging ability on DPPH, ABTS, hydroxyl and superoxide anions and higher reducing power compared with other samples prepared by SD, OD, MD and IRD. Moreover, SHD sample had strong protective effects against L02 cells damage induced by H2O2. SPF samples, especially SHD sample, significantly inhibited inflammatory factor secretion in LPS-stimulated RAW 264.7 cell. All studied SPF sample exhibited evidently inhibitory effects on the four enzymes. SHD sample possessed the highest inhibitory activity on α-glucosidase and α-amylase. While SHD and SD samples had the potential inhibitory effects on cholinesterases and tyrosinase. In consideration of active compound contents and biological activities, it was recommended that SHD and SD were applied for drying SPF at an industrial scale.