Melanogenesis inhibitors from the rhizoma of ligusticum sinense in B16-f10 melanoma cells in vitro and zebrafish in vivo

Min Chi Cheng, Tzong Huei Lee, Yi Tzu Chu, Li Ling Syu, Su Jung Hsu, Chia Hsiung Cheng, Jender Wu, Ching Kuo Lee

Research output: Contribution to journalArticlepeer-review

15 Citations (Scopus)


The rhizoma of Ligusticum sinense, 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 L. sinense, 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 L. sinense, and among these, 5-[3-(4-hydroxy-3-methoxyphenyl)allyl]ferulic acid (1) and cis-4-pentylcyclohex-3-ene-1,2-diol (2) were new compounds. All the pure isolates were subjected to antimelanogenesis assay using murine melanoma B16-F10 cells. Compound 1 and (3S,3aR)-neocnidilide (8) exhibited antimelanogenesis activities with IC50 values of 78.9 and 31.1 µM, respectively, without obvious cytotoxicity. Further investigation showed that compound 8 demonstrated significant anti-pigmentation activity on zebrafish embryos (10-20 µM) compared to arbutin (20 µM), and without any cytotoxicity against normal human epidermal keratinocytes. These findings suggest that (3S,3aR)-neocnidilide (8) is a potent antimelanogenic and non-cytotoxic natural compound and may be developed potentially as a skin-whitening agent for cosmetic uses.

Original languageEnglish
Article number3994
JournalInternational Journal of Molecular Sciences
Issue number12
Publication statusPublished - Dec 1 2018


  • Antimelanogenesis
  • B16-F10 melanoma cell
  • Ligusticum sinense
  • Pigmentation
  • Rhizoma
  • Zebrafish

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry


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