Novel marine-derived halogen-containing gramine analogues induce vasorelaxation in isolated rat aorta

Bromoageliferin and dibromoageliferin, secondary metabolites from the marine sponge Agelas conifera, inhibit voltage-operated, but not store-operated calcium entry in PC12 cells

“…Recently, several authors described that brominated alkaloids from marine organisms induce vasorelaxation or influence ionic membrane channels (Iwata et al, 2001;Peters et al, 2002;Bickmeyer et al, 2004). The potency of pyrrole alkaloids to inhibit voltage-dependent calcium elevation increased with the number of bromine atoms associated within the pyrrole moiety and with the presence of an imidazole group (present work, Bickmeyer et al, 2004).…”

Indole derivatives inhibited the formation of bacterial biofilm and modulated Ca2+ efflux in diatom

“…The report about the cytotoxic mechanisms of gramine substances showed that indole derivatives 5,6-dibromo-1,2-dimehtylgramine evoked Ca 2+ release from skeletal muscle Sarcoplasmic reticulum through ryanodine receptors and indicated that gramine derivatives were useful tools for the investigation of Ca 2+ release from Sarcoplasmic reticulum (Nakahata et al, 1999). Iwata et al (2001) also reported that gramine derivatives 2, 5, 6-tribromo-1-methylgramine and 5, 6-dibromo-1, 2-dimethylgramine decreased cytosolic Ca 2+ level by inhibiting the transient increase in isolated rat aorta. Gramine derivatives reduced intracellular Ca 2+ abundance in animal cells, which might contribute to their inhibitory effects on the growth.…”

Gramine Derivatives Targeting Ca2+ Channels and Ser/Thr Phosphatases: A New Dual Strategy for the Treatment of Neurodegenerative Diseases

“…52 Indeed, some of its brominated derivatives have been described as Ca 2+ channels blockers. 53 In our laboratory, we observed that 1 protected SH-SY5Y neuroblastoma cells against the toxic stimulus generated by OA in a wide range of concentrations. We wondered whether such huge neuroprotective effect was, at least in part, due to the activation of PPP enzymes.…”