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

Department of Herbal Crop Research, National Institute of Horticultural and Herbal Science, RDA, Eumseong 27709, Korea
YD Life Science Research Institutes, YD Life Science Co., Ltd., Seongnam 13235, Korea
Department of Food Science & Biotechnology, Chungbuk National University, Cheongju 28644, Korea
Authors to whom correspondence should be addressed.
Academic Editors: Maurizio Battino and Masatoshi Maki
Int. J. Mol. Sci. 2016, 17(8), 1350;
Received: 21 June 2016 / Revised: 24 July 2016 / Accepted: 12 August 2016 / Published: 18 August 2016
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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, 13C, 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. View Full-Text
Keywords: Lithospermi radix; nuclear magnetic resonance (NMR); pseudoshikonin I; matrix-metalloproteinase (MMPs) Lithospermi radix; nuclear magnetic resonance (NMR); pseudoshikonin I; matrix-metalloproteinase (MMPs)

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Lee, D.Y.; Choi, S.-I.; Han, S.H.; Lee, Y.-J.; Choi, J.-G.; Lee, Y.-S.; Choi, J.H.; Lee, S.-E.; Kim, G.-S. Potential of Pseudoshikonin I Isolated from Lithospermi Radix as Inhibitors of MMPs in IL-1β-Induced SW1353 Cells. Int. J. Mol. Sci. 2016, 17, 1350.

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