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The rhizoma of <i>Ligusticum sinense</i>, a Chinese medicinal plant, has long been used as a cosmetic for the whitening and hydrating of the skin in ancient China. In order to investigate the antimelanogenic components of the rhizoma of <i>L. sinense</i>, we performed an antimelanogenesis assay-guided purification using semi-preparative HPLC accompanied with spectroscopic analysis to determine the active components. Based on the bioassay-guided method, 24 compounds were isolated and identified from the ethyl acetate layer of methanolic extracts of <i>L. sinense</i>, and among these, 5-[3-(4-hydroxy-3-methoxyphenyl)allyl]ferulic acid (<b>1</b>) and <i>cis</i>-4-pentylcyclohex-3-ene-1,2-diol (<b>2</b>) were new compounds. All the pure isolates were subjected to antimelanogenesis assay using murine melanoma B16-F10 cells. Compound <b>1</b> and (3<i>S</i>,3a<i>R</i>)-neocnidilide (<b>8</b>) exhibited antimelanogenesis activities with IC₅₀ values of 78.9 and 31.1 &#956;M, respectively, without obvious cytotoxicity. Further investigation showed that compound <b>8</b> demonstrated significant anti-pigmentation activity on zebrafish embryos (10‒20 &#956;M) compared to arbutin (20 &#956;M), and without any cytotoxicity against normal human epidermal keratinocytes. These findings suggest that (3<i>S</i>,3<i>aR</i>)-neocnidilide (<b>8</b>) is a potent antimelanogenic and non-cytotoxic natural compound and may be developed potentially as a skin-whitening agent for cosmetic uses.