Merocyclophanes A and B, antiproliferative cyclophanes from the cultured terrestrial Cyanobacterium Nostoc sp

Phytochemistry. 2012 Jul:79:109-15. doi: 10.1016/j.phytochem.2012.03.005. Epub 2012 May 7.

Abstract

The cell extract of a cultured terrestrial Nostoc sp. (UIC 10062), obtained from a sample collected at Grand Mere State Park in Michigan, displayed antiproliferative activity against the HT-29 human colon cancer cell line. Bioactivity-guided fractionation of the cell extract, combined with LC-MS analysis, led to the isolation of two cyclophanes, named merocyclophanes A and B (1 and 2). Their structures were determined by various spectroscopic techniques including HRESIMS, and 1D and 2D NMR analyses. The stereoconfiguration was assigned on the basis of X-ray crystallographic and CD analyses. The structures of merocyclophanes A and B (1 and 2) established a hitherto unknown [7.7]paracyclophane skeleton in nature, as characterized by α-branched methyls at C-1/14. Merocyclophanes A and B (1 and 2) displayed antiproliferative activity against the HT-29 human colon cancer cell line with IC₅₀ values of 3.3 and 1.7 μM, respectively.

Publication types

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

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / isolation & purification
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Culture Techniques
  • Cyanobacteria / chemistry*
  • Cyanobacteria / classification
  • Cyanobacteria / genetics
  • Cyanobacteria / growth & development
  • Cycloparaffins / chemistry*
  • Cycloparaffins / isolation & purification
  • Cycloparaffins / pharmacology*
  • HT29 Cells
  • Humans
  • Inhibitory Concentration 50
  • Phylogeny
  • RNA, Bacterial / genetics
  • RNA, Ribosomal, 16S / genetics
  • Stereoisomerism

Substances

  • Antineoplastic Agents
  • Cycloparaffins
  • RNA, Bacterial
  • RNA, Ribosomal, 16S