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Isolation and 5-Demethylation of Tangertin from Chen-Pi and Their Inhibitory Effect on Hepatic Stellate Cell LX-2

XU Lanying1, ZHAO Hui2, ZHANG Ting1, WU Lun1, LONG Tao1,*, LI Shiming1,*   

  1. 1. Hubei Key Laboratory for Processing and Application of Catalytic Materials, College of Chemical Technology, Huanggang Normal University, Huanggang 438000, China; 2. Tianjin Key Laboratory of Food Biotechnology, College of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin 300134, China
  • Online:2015-12-15 Published:2015-12-24

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Abstract:

An efficient and large-scale isolation method for tangeretin from Chen-Pi (aged tangerine peels) has been
developed successfully. The transformation of tangeretin to 5-demethyltangeretin was performed in acidified alcohol solution
with high conversion efficiency. The structures of both isolated tangeretin and 5-demethyltangeretin were confirmed by MS
and 1H NMR. Both compounds exhibited strong inhibitory activity against LX-2 human hepatic stellate cells, with an IC50
of 150 μmol/L for tangeretin and 12.5 μmol/L for 5-demethyltangeretin, indicating the increased potency via the conversion
from tangeretin to 5-demethyltangeretin.

Key words: tangeretin, 5-demethyltangeretin, polymethoxyflavones, hepatic stellate cell LX-2

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