Description
(+)-Aeroplysinin-1 is a metabolite originally isolated from the marine sponge
V. aerophoba with diverse biological activities. (+)-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. 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. 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 (IC
50 = 14.6 μM)
via inhibition of HIV-1 reverse transcriptase.
References
[1] E FATTORUSSO G S L Minale. Aeroplysinin-1, an antibacterial bromo-compound from the sponge Verongia aerophoba.[J]. Journal of the Chemical Society. Perkin transactions 1, 1972, 1: 16-18. DOI:
10.1039/p19720000016[2] MATTHIAS-H. KREUTER . Inhibition of intrinsic protein tyrosine kinase activity of EGF-receptor kinase complex from human breast cancer cells by the marine sponge metabolite (+)-aeroplysinin-1[J]. Comparative Biochemistry and Physiology Part B: Comparative Biochemistry, 1990, 97 1: Pages 151-158. DOI:
10.1016/0305-0491(90)90194-x[3] SALVADOR RODRíGUEZ-NIETO. Antiangiogenic activity of aeroplysinin-1, a brominated compound isolated from a marine sponge[J]. FASEB Journal, 2001, 16 2: 1-27. DOI:
10.1096/fj.01-0427fje[4] JAVIER A. GARCíA-VILAS. Aeroplysinin-1, a Sponge-Derived Multi-Targeted Bioactive Marine Drug[J]. Marine Drugs, 2015, 14 1. DOI:
10.3390/md14010001
