brefeldin a

Brefeldin A is a lactone macrolide natural product originally isolated from the fungus Penicillium brefeldianum. It is primarily used as a research tool rather than as an approved pharmaceutical. Mechanistically, it blocks Sec7 domain-containing guanine nucleotide exchange factors (GEFs), which are necessary for activation of ADP-ribosylation factor 1 (Arf1), thereby preventing COP-I coat assembly on Golgi membranes and disrupting vesicular trafficking. This leads to rapid tubulation and fusion of the Golgi with the ER and inhibits secretion in eukaryotic cells[1][5][6]. Brefeldin A also induces apoptosis in certain cell types and has been shown to inhibit intracellular collagen degradation and apical sodium channels in epithelia[5][6]. While initially investigated for antiviral activity due to its broad antibiotic properties—including antifungal and antitumor effects—its poor efficacy limited clinical development; it remains widely used in cell biology research for studying membrane traffic dynamics[1][2].

Other names

(+)-brefeldin Aascotoxincyaneindecumbinnectrolidesynergisidin