Studies on the Structure and Biological Activity of Microcystins Produced from Korean Cyanobacteria, Microcystis Species

한국산 남조류 Microcystis로부터 생산된 microcystin 구조와 생물활성에 관한 연구

  • Choi, Byoung Wook (Department of Industrial Chemistry, Taejon Natl. Univ. of Technology) ;
  • Noh, Young Ho (Department of Industrial Chemistry, Taejon Natl. Univ. of Technology) ;
  • Lee, Jong-Soo (College of Fisheries, Gyeongsang Natl. Univ.)
  • 최병욱 (대전산업대학교 공업화학과) ;
  • 노영호 (대전산업대학교 공업화학과) ;
  • 이종수 (경상대학교 수산대학 수산가공과)
  • Received : 1997.03.06
  • Accepted : 1997.05.29
  • Published : 1997.08.10

Abstract

Hepatotoxic cyanobacteria, Microcystis species, were collected from the Nakdong River and we could isolate hepatotoxins, microcystin-LR and microcystin-RR, which are also strong inhibitors of protein phosphatase 1 and 2A. From the microcystins, several microcystin derivatives were synthesized and tested on the mouse toxicity in order to establish the structure-activity relationship. Esterification od carboxyl groups of Glu and MeAsp residue produced nontoxic compounds. However, when we reduced the Mdha residue with sodium borohydride into Ala residue, toxicity was still maintained. Also, the change of guanidyl moiety of Arg residue in microcystin-LR into dimethylpyrimidyl moiety did not change the toxicity of microcystins as well. Thus the carboxyl groups seem to play important roles in binding with protein phosphatase 1 and 2A, whereas Mdha residue and the guanidyl moiety of Arg residue do not.

Keywords

Acknowledgement

Supported by : 한국학술진흥재단

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