Verruculogen Explained

Verruculogen is a mycotoxin produced by certain strains of aspergillus that belongs to a class of naturally occurring 2,5-diketopiperazines.[1] It is an annulated analogue of cyclo(L-Trp-L-Pro) which belongs to the most abundant and structurally diverse class of tryptophan-proline 2,5-diketopiperazine natural products. It produces tremors in mice due to its neurotoxic properties. It also tested positive in a Salmonella/mammalian microsome assay and was shown to be genotoxic. It is a potent blocker of calcium-activated potassium channels.[2]

Synthesis

Both verruculogen and its isoprenyl derivative fumitremorgin A belong to the only family of alkaloids with an eight-membered endoperoxide ring, and both have been synthesised involving ligand-controlled C–H borylation.[3]

Notes and References

  1. 2,5-Diketopiperazines: Synthesis, Reactions, Medicinal Chemistry, and Bioactive Natural Products . Borthwick AD . Chemical Reviews . 2012 . 112 . 7 . 3641–3716 . 10.1021/cr200398y . 22575049.
  2. Web site: Verruculogen from Penicillium verruculosum. sigmaaldrich.com. 25 September 2023.
  3. Feng Y, Holte D, Zoller J, Umemiya S, Simke LR, Baran PS . Total Synthesis of Verruculogen and Fumitremorgin A Enabled by Ligand-Controlled C–H Borylation . Journal of the American Chemical Society . 137 . 32 . 10160–10163 . August 2015. 26256033 . 10.1021/jacs.5b07154 . 4777340 .