New apratoxins of marine cyanobacterial origin from Guam and Palau

Bioorg Med Chem. 2002 Jun;10(6):1973-8. doi: 10.1016/s0968-0896(02)00014-7.

Abstract

Two collections of the marine cyanobacterium Lyngbya sp. from Guam and Palau that both afforded the potent cytotoxin apratoxin A (1) each yielded different structural analogues with lower degrees of methylation. The new apratoxins, termed apratoxins B (2) and C (3), were evaluated for their in vitro cytotoxicity along with semisynthetic E-dehydroapratoxin A (4) to identify key structural elements responsible for the cytotoxicity and to initiate SAR studies on this novel family of depsipeptides. All analogues 2-4 displayed weaker cytotoxicity than 1, but to different extents. While compound 3 closely approached the cytotoxicity of 1, compounds 2 and 4 exhibited significantly reduced activity, possibly also related to a conformational change. The 16S rRNA genes of the different apratoxin producers have partially been sequenced and compared, and other genetic differences are currently being revealed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Cyanobacteria / chemistry*
  • Cyanobacteria / classification
  • Cyanobacteria / genetics
  • Cytotoxins / chemistry
  • Cytotoxins / isolation & purification*
  • Cytotoxins / toxicity*
  • Depsipeptides*
  • Guam
  • Humans
  • Inhibitory Concentration 50
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Oceans and Seas
  • Palau
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / isolation & purification*
  • Peptides, Cyclic / toxicity*
  • Phylogeny
  • Protein Conformation
  • RNA, Ribosomal, 16S / genetics
  • Seawater / microbiology*
  • Tumor Cells, Cultured

Substances

  • Cytotoxins
  • Depsipeptides
  • Peptides, Cyclic
  • RNA, Ribosomal, 16S
  • apratoxin B
  • apratoxin C
  • dehydroapratoxin A