Paxilline

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Paxilline is a mycotoxin that is produced by the fungus Penicillium paxilli. It is a potent potassium channel blocker, specifically inhibiting the BK channel (big potassium channel). Paxilline has been used in scientific research to help understand the function and behavior of BK channels.

History

Paxilline was first isolated from Penicillium paxilli in 1973 by Cole and Cox. Since then, it has been used in various studies to investigate the role of BK channels in different physiological processes.

Structure and Synthesis

Paxilline is a complex indole diterpene compound. Its structure was determined using X-ray crystallography and includes a unique 6-5-6-5 tetracyclic ring system. The biosynthesis of paxilline in Penicillium paxilli involves a number of enzymatic steps, including the action of a nonribosomal peptide synthetase and several cytochrome P450 enzymes.

Biological Activity

Paxilline is a potent inhibitor of BK channels, which are large conductance, voltage and calcium-activated potassium channels. These channels are involved in a wide range of physiological processes, including neuronal excitability, smooth muscle contraction, and intracellular calcium signaling. By blocking these channels, paxilline can affect these processes.

Toxicity

As a mycotoxin, paxilline can be harmful if ingested or inhaled. It has been shown to cause tremors and other neurological symptoms in livestock that have consumed contaminated feed. However, the exact mechanism of its toxicity is not fully understood.

References

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