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The Pharmaceutical Society of Korea (대한약학회)
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Anti-Complementary Activity of Protostane-Type Triterpenes from Alismatis Rhizoma

  • Lee, Sang-Myung (Laboratory of Immunomodulator, Korea Research Institute of Bioscience, Biotechnology) ;
  • Kim, Jung-Hee (Laboratory of Immunomodulator, Korea Research Institute of Bioscience, Biotechnology) ;
  • Zhang, Ying (Yan Bian Institute for Drug Contro) ;
  • An, Ren-Bo (Laboratory of Immunomodulator, Korea Research Institute of Bioscience, Biotechnology, Yan Bian Institute for Drug Control) ;
  • Min, Byung-Sun (Laboratory of Immunomodulator, Korea Research Institute of Bioscience, Biotechnology) ;
  • Joung, Hyouk (Laboratory of Immunomodulator, Korea Research Institute of Bioscience, Biotechnology) ;
  • Lee, Hyeong-Kyu (Laboratory of Immunomodulator, Korea Research Institute of Bioscience, Biotechnology)
  • Published : 2003.06.01
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Abstract

Four protostane-type triterpenes, alisol B 23-acetate (1a), alisol C 23-acetate (2a), alisol B(3a), and alisol A 24-acetate (4a), were isolated from the rhizome of Alismatis plantago-aquatica L. var. orientale Samuelson (Alismataceae) and eleven protostane derivatives (compounds 1-11) were obtained by selective modification from alisol B 23-acetate (1a). These compounds were investigated for their anti-complement activity against the classical pathway of the complement system. Alisol B (3a) and alisol A 24-acetate (4a) exhibited anti-complement activity with $IC_{50} values of 150 and 130 \mu$ M. Among the synthetic derivatives, the tetrahydroxylated protostane triterpene (9) showed moderate inhibitory activity with $IC_{50} value of 97.1 \mu$ M. Introduction of an aldehyde group at C-23 (10; $IC_{50} value, 47.7 \mu$ M) showed the most potent inhibitory effect on the complement system in vitro.

Keywords

References

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