Bafilomycin A1

Bafilomycin A1

Bafilomycin A1 is a macrolide antibiotic derived from Streptomyces griseus. It is a specific inhibitor of vacuolar-type H+-ATPase (V-ATPase), a protein complex responsible for the acidification of intracellular compartments in eukaryotic cells.

Structure

Bafilomycin A1 is a 16-membered macrolide lactone with a unique 3,5-dihydroxy-3-methylglutaric acid (DMGA) side chain. The macrolide ring contains a conjugated system of double bonds, which is responsible for its strong absorbance in the UV region.

Mechanism of Action

Bafilomycin A1 inhibits V-ATPase by binding to the V0 subunit c, preventing proton translocation across the vesicular membrane. This results in the neutralization of the acidic environment within the vesicle, which can affect various cellular processes such as protein sorting, zymogen activation, receptor-mediated endocytosis and synaptic vesicle proton gradient generation.

Applications

Due to its ability to inhibit V-ATPase, Bafilomycin A1 has been used in research to study the role of this enzyme in various biological processes. It has also been used to investigate the mechanisms of diseases such as osteoporosis, cancer, and infectious diseases that involve the disruption of cellular pH homeostasis.

Toxicity

Bafilomycin A1 is toxic to eukaryotic cells due to its inhibition of V-ATPase. It can cause cell death by disrupting the cellular pH balance, leading to the dysfunction of various cellular processes.

See Also

• Macrolide
• Streptomyces griseus
• Vacuolar-type H+-ATPase
• Osteoporosis
• Cancer
• Infectious diseases

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