(+)-Aeroplysinin-1

(+)-Aeroplysinin-1 is a metabolite originally isolated from the marine sponge V. aerophoba with diverse biological activities.¹ (+)-Aeroplysinin-1 (0.25-0.5 μM) induces cell death in MCF-7 and ZR-75-1 human breast cancer cells in a time- and concentration-dependent manner but has no effect on normal human fibroblasts at concentrations up to 5 μM.² It also blocks EGF-induced endocytosis of the EGF receptor (EGFR) and EGF-dependent cell proliferation in MCF-7 cells. (+)-Aeroplysinin-1 inhibits bovine aortic endothelial (BAE) cell proliferation and cord formation in a Matrigel™ assay.³ It inhibits angiogenesis in a dose-dependent manner in a chick chorioallantoic membrane (CAM) assay when administered from 1.5 to 3 nmol per egg. (+)-Aeroplysinin-1 also has antibacterial activity against Gram-positive bacteria, including S. aureus, S. albus, and B. subtilis, but not Gram-negative bacteria and inhibits HIV-1 replication (IC₅₀ = 14.6 μM) via inhibition of HIV-1 reverse transcriptase.⁴

WARNING This product is not for human or veterinary use.

1. Fattorusso, E., Minale, L., and Sodano, G. Aeroplysinin-1, an antibacterial bromo-compound from the sponge Verongia aerophoba. J. Chem. Soc. Perkin 1 1, 16-18 (1972).

2. Kreuter, M.H., Leake, R.E., Müller-Klieser, W., et al. Inhibition of intrinsic protein tyrosine kinase activity of EGF-receptor kinase complex from human breast cancer cells by the marine sponge metabolite (+)-aeroplysinin-1. Comp. Biochem. Physiol. B 97(1), 151-158 (1990).

3. Rodríguez-Nieto, S., González-Iriarte, M., Carmona, R., et al. Antiangiogenic activity of aeroplysinin-1, a brominated compound isolated from a marine sponge. The FASEB Journal 16(2), 261-263 (2002).

4. García-Vilas, J.A., Martínez-Poveda, B., Quesada, A.R., et al. Aeroplysinin-1, a sponge-derived multi-targeted bioactive marine drug. Mar. Drugs 14(1), (2015).