squalamine

Squalamine is a synthetic aminosterol originally isolated from the tissues of the spiny dogfish shark (Squalus acanthias), now produced in the laboratory. It exhibits broad-spectrum antimicrobial and antiangiogenic activity. Mechanistically, squalamine binds to cell membranes and inhibits sodium-hydrogen exchanger NHE3 in endothelial cells. This leads to altered intracellular pH and disruption of signaling pathways induced by angiogenic growth factors such as VEGF. The result is inhibition of key steps in angiogenesis including actin polymerization and endothelial cell proliferation[3][5]. Squalamine also demonstrates bactericidal and fungicidal effects[1][2][3], enhances antibiotic efficacy when combined with standard antibiotics[3], reduces aggregation of alpha-synuclein (implicated in Parkinson’s disease)[10], and has shown antiviral properties[8]. It has been investigated for use in cancer (lung, ovarian), age-related macular degeneration, diabetic eye disease (retinopathy), Parkinson’s disease-related constipation (as ENT-01), among others[4][5][10].

Brand names

OHR-102OHR102OHR 102

Other names

squalamine lactate(3β,5α,7α)-3-[[3-((4-Aminobutyl)amino)propyl]amino]cholestane-7,24-diol-24-hydrogen sulfate