Sipjundaebo-tang was a well-known restorative traditional herbal prescription that used to treat anemia, anorexia, fatigue and inflammation. In this study, we examined the bioconversion of compounds in the Sipjundaebo-tang (SJ) and fermented Sipjundaebo-tang with Lactobacillus fermentum KFRI 164 (FSJ) using established HPLC-DAD method. The chromatogram of FSJ has shown that the contents of six bioactive compounds 5-HMF, paeoniflorin, ferulic acid, cinnam aldehyde, decursin, glycyrrhizin in SJ has decreased. And the contents of unknown compounds (1), (2), (3), (4) and (5) in FSJ were higher than each contents of SJ. The antioxidant activities of SJ and FSJ were conducted by DPPH free radical and Hydrogen peroxide ($H_2O_2$) scavenging assay. Electron donating activity (EDA, %) value of FSJ has shown higher than 21.9% and 14.5% at a concentration of 0.5 mg/ml for DPPH radical scavenging activity and $H_2O_2$ scavenging activity, respectively. Also, the neuroprotective activities of SJ and FSJ against glutamate-induced oxidative stress in a mouse hippocampal cell line (HT22) were evaluated by MTT assay. As a result, FSJ has shown higher neuroprotective activity than 56.5% comparing with SJ. In conclusion, the fermented SJ using microorganism could convert compounds in SJ and enhance antioxidant activity and neuroprotective activity.