YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Synthesis and Biological Activity of 5-S-GAD(N-${\beta}$-alanyl-5-S-glutathionyl-3,4-dihydroxyphenylalanine), a Novel Antibacterial Substance

신규 항균물질 5-S-GAD(N-${\beta}$-alanyl-5-S-glutathionyl-3,4-dihydroxyphenylalanine)의 합성 및 생리활성

  • Leem, Jae-Yoon (Korea Research Institute of Bioscience and Biotechnology, KIST) ;
  • Park, Ho-Yong (Korea Research Institute of Bioscience and Biotechnology, KIS) ;
  • Natori, Shunji (Faculty of Pharmaceutical Sciences, University of Tokyo)
  • Published : 1998.06.01
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Abstract

We had already reported that we purified N-${\beta}$-alanyl-5-S-glutathionyl-3,4-dihydroxyphenylalanine (5-S-GAD), a novel antibacterial substance from the immunized adult Sarcoph aga peregrina (Flesh fly). We found that the antibacterial activity of synthetic 5-S-GAD is equal to that of authentic 5-S-GAD without a specificity of antibacterial activity against Gram positive and Gram negative. Significant synergism was detected between 5-S-GAD and streptomycin against streptomycin resistant strain E.coli K12 594. It has an antitumor activity against several tumor cell lines at a concentration of $100{\mu}M$. However, no cytotoxic activity against murine macrophage was detected at a concentration of $500{\mu}M$. Furthermore, haemolytic activity against sheep erythrocytes was not detected at the same concentration. We suggest that the S-conjugation of glutathion with dihydroxyphenylalanine might be important to increase antibacterial activity of dihydroxyphenylalanme.

Keywords

References

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