Potential of Pseudoshikonin I Isolated from Lithospermi Radix as Inhibitors of MMPs in IL-1β-Induced SW1353 Cells

Int J Mol Sci. 2016 Aug 18;17(8):1350. doi: 10.3390/ijms17081350.


Pseudoshikonin I, the new bioactive constituent of Lithospermi radix, was isolated from this methanol extract by employing reverse-phase medium-pressure liquid chromatography (MPLC) using acetonitrile/water solvent system as eluents. The chemical structure was determined based on spectroscopic techniques, including 1D NMR (¹H, (13)C, DEPT), 2D NMR (gCOSY, gHMBC, gHMQC), and QTOF/MS data. In this study, we demonstrated the effect of pseudoshikonin I on matrix-metalloproteinase (MMPs) activation and expression in interleukin (IL)-1β-induced SW1353 chondrosarcoma cells. MMPs are considered important for the maintenance of the extracellular matrix. Following treatment with PS, active MMP-1, -2, -3, -9, -13 and TIMP-2 were quantified in the SW1353 cell culture supernatants using a commercially available ELISA kit. The mRNA expression of MMPs in SW1353 cells was measured by RT-PCR. Pseudoshikonin I treatment effectively protected the activation on all tested MMPs in a dose-dependent manner. TIMP-2 mRNA expression was significantly upregulated by pseudoshikonin I treatment. Overall, we elucidated the inhibitory effect of pseudoshikonin on MMPs, and we suggest its use as a potential novel anti-osteoarthritis agent.

Keywords: Lithospermi radix; matrix-metalloproteinase (MMPs); nuclear magnetic resonance (NMR); pseudoshikonin I.

MeSH terms

  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Humans
  • Interleukin-1beta / pharmacology*
  • Lithospermum / chemistry*
  • Magnetic Resonance Spectroscopy
  • Matrix Metalloproteinase 1 / metabolism
  • Matrix Metalloproteinase 13 / metabolism
  • Matrix Metalloproteinase 3 / metabolism
  • Matrix Metalloproteinase 9 / metabolism
  • Matrix Metalloproteinase Inhibitors / chemistry
  • Matrix Metalloproteinase Inhibitors / pharmacology*
  • Matrix Metalloproteinases / metabolism*
  • Molecular Structure
  • Tissue Inhibitor of Metalloproteinase-2 / metabolism


  • Interleukin-1beta
  • Matrix Metalloproteinase Inhibitors
  • Tissue Inhibitor of Metalloproteinase-2
  • Matrix Metalloproteinase 13
  • Matrix Metalloproteinases
  • Matrix Metalloproteinase 3
  • Matrix Metalloproteinase 9
  • Matrix Metalloproteinase 1