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The Pharmaceutical Society of Korea (대한약학회)
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Alaternin and Emodin with Hydroxyl Radical inhibitory and／or Scavenging Activities and Hepatoprotective Activity on Tacrine-Induced Cytotoxicity in HepG2 Cells

  • Jung, Hyun-Ah (Research Institute of Marine Science and Technology, Korea Maritime University) ;
  • Chung, Hae-Young (College of Pharmacy, Pusan National University) ;
  • Takaka, Yokezawa (Institute of Natural Medicine, Toyama Medical and Pharmaceutical University) ;
  • Kim, Youn-Chul (College of Pharmacy, Wonkwang University) ;
  • Hyun, Sook-Kyung (Faculty of Food Science and Biotechnology, Pukyong National University) ;
  • Choi, Jae-Sue (Faculty of Food Science and Biotechnology, Pukyong National University)
  • Published : 2004.09.01
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Abstract

The antioxidative and hepatoprotective potentials of two anthraquinones, alaternin (2-hydroxy-emodin) and emodin, to scavenge and/or inhibit hydroxyl radicals generated by the Fenton reaction and to protect tacrine-induced cytotoxicity in human liver derived HepG2 cells were evaluated, respectively. The inhibitory activity on hydroxyl radical generated in a cell-free chemical system (FeSO$_4$/$H_2O$$_2$) was investigated by a fluorescence spectrophotometer using a highly fluorescent probe, 2$^1$,7$^1$-dichlorofluorescein. The hydroxyl radical scavenging activity was determined by electron spin resonance spectroscopy using 5,5-dimethy-1-pyrroline-N-oxide as hydroxyl radicals trapping agents. Tacrine-induced HepG2 cell toxicity was determined by a 3-［4,5-dimethylthiazole-2yl］-2,5-diphenyltertrazolium bromide assay. Although the scavenging activity of alaternin on hydroxyl radical was similar to that of emodin in dose-dependent pat-terns, the inhibitory activity exhibited by the former on hydroxyl radical generation was stron-ger than that of the latter, with $IC_{50}$/ values of 3.05$\pm$0.26 $\mu$M and 13.29$\pm$3.20 $\mu$M, respectively. In addition, the two anthraquinones, alaternin and emodin showed their hepatoprotective activ-ities on tacrine-induced cytotoxicity, and the EC$_{50}$ values were 4.02 11M and 2.37 $\mu$M, respec-tively. Silymarin, an antihepatotoxic agent used as a positive control exhibited the EC$_{50}$ value of 2.00 $\mu$M. These results demonstrated that both alaternin and emodin had the simultaneous antioxidant and hepatoprotective activities.ies.

Keywords

References

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