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An aporphine alkaloid with diverse biological activities
Remerin is an aporphine alkaloid that has been found in N. nucifera and has diverse biological activities.1,2,3,4 It selectively binds to the serotonin (5-HT) receptor subtype 5-HT2A over 5-HT1A and dopamine D1 and D2 receptors (Kis = 0.0621, 1.17, 1.4, and 22.6 ?M, respectively).2 Remerin is active against C. albicans as well as chloroquine-resistant and -sensitive strains of P. falciparum with IC50 values of 4.5, 0.4, and 0.2 ?g/ml, respectively.1 It enhances cytotoxicity induced by vinblastine in multidrug-resistant KB-V1 oral epidermoid carcinoma cells.3 Remerin (20 mg/kg) improves survival in a mouse model of sepsis induced by methicillin-resistant S. aureus (MRSA).4
1.Agnihotri, V.K., ElSohly, H.N., Khan, S.I., et al.Constituents of Nelumbo nucifera leaves and their antimalarial and antifungal activityPhytochem. Lett.1(2)89-93(2008) 2.Munusamy, V., B.K., Y., Buckle, M.J.C., et al.Structure-based identification of aporphines with selective 5-HT2A receptor-binding activityChem. Biol. Drug Des.81(2)250-256(2012) 3.You, M., Wickramaratne, D.B.M., Silva, G.L., et al.(?)-Roemerine, an aporphine alkaloid from Annona senegalensis that reverses the multidrug-resistance phenotype with cultured cellsJ. Nat. Prod.58(4)598-604(1995) 4.Yin, S., Rao, G., Wang, J., et al.Roemerine improves the survival rate of septicemic BALB/c mice by increasing the cell membrane permeability of Staphylococcus aureusPLoS One10(11)e0143863(2015)
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