Planta Med 2014; 80 - PG16
DOI: 10.1055/s-0034-1382605

Chaetomin a new calmodulin inhibitor from Chaetomium globosum

J Rivera-Chávez 1, M González-Andrade 1, G García-Aguirre 2, R Mata 1
  • 1Facultad de Química
  • 2Instituto de Biología, Universidad Nacional Autónoma de México, Mexico City 04510, Mexico

Bioassay-guided fractionation of the active organic extract of Chaetomium globosum, a fungus isolated from maize, led to the separation of one epipolythiodioxopiperazine, which was identified as chaetomin (1). Compound 1 binds to the new human calmodulin (hCaM) biosensor hCaM M124C-A350, with a k d value in the nM order (kd=57 nM), eleven-fold higher than trifluoroperazine (TFP) used as positive control. Molecular docking predicted that 1 interacts with CaM in a similar site as KAR-2 (a vinblastine derivative) compound does. In conclusion, compound 1 binds to CaM with a higher affinity, which might explain its cytotoxic effect against some cancer cell lines.

Fig. 1