Paxilline: Difference between revisions

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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.
{{DISPLAYTITLE:Paxilline}}


== History ==
== Overview ==
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.
'''Paxilline''' is a naturally occurring indole-diterpene alkaloid that is produced by certain species of fungi, particularly those in the genus ''[[Penicillium]]''. It is known for its role as a potent blocker of large-conductance calcium-activated potassium channels (BK channels), which are important in various physiological processes.


== Structure and Synthesis ==
== Chemical Structure and Biosynthesis ==
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.
[[File:Paxiline_biosynthesis.svg|thumb|right|300px|Biosynthesis pathway of Paxilline]]
Paxilline is characterized by its complex polycyclic structure, which includes an indole moiety fused to a diterpene skeleton. The biosynthesis of paxilline involves several enzymatic steps starting from simple precursors such as [[geranylgeranyl pyrophosphate]] and [[tryptophan]]. The pathway includes cyclization, oxidation, and methylation reactions that lead to the formation of the final paxilline structure.


== Biological Activity ==
== 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.
Paxilline is primarily known for its ability to inhibit BK channels, which are found in various tissues including the [[nervous system]], [[muscle]], and [[endocrine glands]]. By blocking these channels, paxilline can affect muscle contraction, neurotransmitter release, and hormone secretion. This makes it a valuable tool in research for studying the physiological roles of BK channels.


== Toxicity ==
== Applications in Research ==
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.
In the field of [[neuroscience]], paxilline is used to investigate the function of BK channels in neuronal excitability and synaptic transmission. It is also employed in [[cardiovascular research]] to study the role of these channels in regulating vascular tone and blood pressure.


== References ==
== Safety and Toxicity ==
<references />
While paxilline is a useful research tool, it is important to handle it with care due to its potential toxicity. Ingestion or improper handling can lead to adverse effects, and it should be used in controlled laboratory settings.


== See Also ==
== Related Pages ==
* [[Mycotoxin]]
* [[Indole alkaloid]]
* [[Diterpene]]
* [[Potassium channel]]
* [[Penicillium]]
* [[Penicillium]]
* [[Potassium channel]]
* [[BK channel]]
* [[Indole]]
* [[Diterpene]]
* [[X-ray crystallography]]
* [[Nonribosomal peptide synthetase]]
* [[Cytochrome P450]]
* [[Neuronal excitability]]
* [[Smooth muscle]]
* [[Intracellular calcium]]


[[Category:Alkaloids]]
[[Category:Ion channel blockers]]
[[Category:Mycotoxins]]
[[Category:Mycotoxins]]
[[Category:Indole diterpenes]]
[[Category:Potassium channel blockers]]
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Latest revision as of 11:05, 15 February 2025


Overview[edit]

Paxilline is a naturally occurring indole-diterpene alkaloid that is produced by certain species of fungi, particularly those in the genus Penicillium. It is known for its role as a potent blocker of large-conductance calcium-activated potassium channels (BK channels), which are important in various physiological processes.

Chemical Structure and Biosynthesis[edit]

Biosynthesis pathway of Paxilline

Paxilline is characterized by its complex polycyclic structure, which includes an indole moiety fused to a diterpene skeleton. The biosynthesis of paxilline involves several enzymatic steps starting from simple precursors such as geranylgeranyl pyrophosphate and tryptophan. The pathway includes cyclization, oxidation, and methylation reactions that lead to the formation of the final paxilline structure.

Biological Activity[edit]

Paxilline is primarily known for its ability to inhibit BK channels, which are found in various tissues including the nervous system, muscle, and endocrine glands. By blocking these channels, paxilline can affect muscle contraction, neurotransmitter release, and hormone secretion. This makes it a valuable tool in research for studying the physiological roles of BK channels.

Applications in Research[edit]

In the field of neuroscience, paxilline is used to investigate the function of BK channels in neuronal excitability and synaptic transmission. It is also employed in cardiovascular research to study the role of these channels in regulating vascular tone and blood pressure.

Safety and Toxicity[edit]

While paxilline is a useful research tool, it is important to handle it with care due to its potential toxicity. Ingestion or improper handling can lead to adverse effects, and it should be used in controlled laboratory settings.

Related Pages[edit]