In this study, we investigated the contents of total polyphenol (TP), total flavonoid, and absorbance at 475 nm (OD475) which may produced in solid-fermented leaf of Smilax china L. by Aspergillus oryzae as a new functional components with reddish brown color, contents of water soluble substance (WSS), electron donating ability (EDA), Hunter L*, a*, b* values, sensory overall acceptability (OA) and also, the inhibitory activities (XOI and AOI) against partial purified xanthine oxidase (XO) and aldehyde oxidase (AO) from rabbit liver which were well known to relate the gout, and alcoholic liver disease, respectively in order to optimize water extraction using response surface methodology (RSM). All the R 2 values of the second-order polymonials ranged from 0.85 to 0.98, except for the EDA (0.69) and the XOI (0.78). However, the activities of the EDA and XOI were relatively high in the lower concentration of the fermented Smilax china L. leaf. The effects on the water extraction were highest in the concentration, among the dependent variables, and showed significant differences at the 1% level in the TP, TF and WSS contents and the a*, b* and OD475 values, but the OA showed significant differences at the 5% level. The optimal values of AOI, which was the most important functionality in the Smilax china L. that was predicted via RSM, were 59.48% at the 2.19% concentration, a 90.02°C extraction temperature and a 4.03 minute extraction time (R 2 : 0.93, p<0.007). The ranges of all the dependent variables of the optimal water extraction were 1.6~1.8% for the concentration, 83~93°C for the temperature and 3.4~4.4 minutes for the extraction time; and the optimal water extraction conditions were a 1.7% concentration, an 88°C extraction temperature and a 3.9-min extraction time. Key words:Smilax china L., Aspergillus oryzae, response surface methodology, water extraction conditions, xanthine and aldehyde oxidase.