This study was conducted for the purpose of examining the anti-wrinkle, whitening, astringent effect, and antioxidant activities of Smilacis rhizoma, Smilax china roots, as a cosmeceutical, viz. SRW; water extract, SRE; 80% ethanol extract, SRHW; hot water extract. The highest content of flavonoid compound was 6.19 mg·QC/g in SRE, and that for the polyphenol compound was 291.58 291.58 mg·TA/g in SRHW. In the analysis of anti-wrinkle activity at 2,000 ㎍/ mL, the highest results for collagenase and elastase inhibition were53.28% in SRE and 9.42% in SRW. The result for tyrosinase inhibition activity was 32.84~36.49% and the astringent effect was less than 9%. The highest DPPH radical scavenging ability was 96.04% in SRE. With an ABTS radical scavenging ability of 500 ㎍/mL, greater than 90% was detected for all extracts, and, in particular, 98.14% activity was detected for SHRW at 250 ㎍/mL. The highest SOD-like activity was 20.08% for SHRW at 2,000 ㎍/mL. The highest nitrite scavenging capacity for pH 1.2 was 96.21% in SRHW at 2,000 ㎍/mL, and the highest condition for pH 3.0 was 54.12% in SRE. In RAW264.7 macrophages, a decrease in SRHW of approximately 10% was observed at a concentration of 200 ㎍/mL, and SRE decreased by 13%. These results demonstrated that S. china roots can differ depending on the extraction solvent and method, and that extract from S. china roots may be useful for extraction using hot water-soluble and 80% ethanol solvent due to its exceptional anti-wrinkle, whitening, astringent effect, and DPPH and ABTS radical scavenging activity. And S. china roots is believed to be a natural resource that can be used as a cosmeceutical material.