Aaptamine

Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects^{[1][2][3][4][5][6][7]}. In Vitro:Aaptamine (10 μM) can shift the dose-response curve of norepinephrine to the right in a parallel manner in isolated rabbit aorta and renal artery, without affecting the curves of histamine or potassium chloride^[1].
Aaptamine (30 μg/mL; 0-48 h) can increase the expression of p21 and induce cell cycle arrest in MG63 cells^[2].
Aaptamine (3 days) is cytotoxic to HeLa cells, with an IC₅₀ of 15 μg/mL^[3].
Aaptamine (50-100 μM; 6-24 h) can activate AP-1- and NF-κB-dependent transcriptional activity in JB6 Cl41 cells^[4].
Aaptamine (5-55 µg/mL; 24 h) has an inhibitory effect on ESBL-producing Gram-negative uropathogenic bacteria^[6]. In Vivo:Aaptamine (5-100 μg; intrathecal injection; single dose) has an analgesic effect in a rat model of chronic constriction injury (CCI)-induced peripheral neuropathy^[7].