1574306-31-2Relevant academic research and scientific papers
Analogues of the marine alkaloids oroidin, clathrodin, and hymenidin induce apoptosis in human HepG2 and THP-1 cancer cells
Tomai, Tihomir,Nabergoj, Dominik,Vrbek, Sanja,Zidar, Nace,Jakopin, iga,ula, Ale,Hodnik, iga,Juki, Marko,Anderluh, Marko,Ila, Janez,Dolenc, Marija Sollner,Peluso, Jean,Ubeaud-Squier, Genevive,Muller, Christian D.,Mai, Lucija Peterlin,Kikelj, Danijel
, p. 105 - 110 (2015/02/05)
The marine alkaloids clathrodin, oroidin, and hymenidin, which were isolated from Agelas sponges, possess diverse biological activities. Herein, we describe the design of a library of their analogues and the evaluation of their apoptosis-inducing activities against the human hepatocellular carcinoma HepG2 and acute monocytic leukaemia THP-1 cell lines. The screening of the complete library of 96 compounds using the HepG2 cell line allowed us to determine key structural elements and physicochemical properties that are responsible for the apoptosis-inducing activity. The indole-based compounds 24c, 28c, 29c, and 34c were found to be the most potent inducers of apoptosis in HepG2 and THP-1 cell lines with EC50 values in the low micromolar range. Cell cycle analysis assays confirmed that compounds 24c, 28c, 29c, and 34c induce the apoptosis of THP-1 cells at 25 μM, which highlights these oroidin analogues as interesting candidates for further evaluation of their anticancer activity. This journal is
Substituted 4-phenyl-2-aminoimidazoles and 4-phenyl-4,5-dihydro-2- aminoimidazoles as voltage-gated sodium channel modulators
Zidar, Nace,Jakopin, ?iga,Madge, David J.,Chan, Fiona,Tytgat, Jan,Peigneur, Steve,Dolenc, Marija Sollner,Toma?i?, Tihomir,Ila?, Janez,Ma?i?, Lucija Peterlin,Kikelj, Danijel
, p. 23 - 30 (2014/02/14)
Voltage-gated sodium channels play an integral part in neurotransmission and their dysfunction is frequently a cause of various neurological disorders. On the basis of the structure of marine alkaloid clathrodin, twenty eight new analogs were designed, sy
Antimicrobial activity of the marine alkaloids, clathrodin and oroidin, and their synthetic analogues
Zidar, Nace,Montalv?o, Sofia,Hodnik, ?iga,Nawrot, Dorota A.,?ula, Ale?,Ila?, Janez,Kikelj, Danijel,Tammela, P?ivi,Ma?i?, Lucija Peterlin
, p. 940 - 963 (2014/03/21)
Marine organisms produce secondary metabolites that may be valuable for the development of novel drug leads as such and can also provide structural scaffolds for the design and synthesis of novel bioactive compounds. The marine alkaloids, clathrodin and oroidin, which were originally isolated from sponges of the genus, Agelas, were prepared and evaluated for their antimicrobial activity against three bacterial strains (Enterococcus faecalis, Staphylococcus aureus and Escherichia coli) and one fungal strain (Candida albicans), and oroidin was found to possess promising Gram-positive antibacterial activity. Using oroidin as a scaffold, 34 new analogues were designed, prepared and screened for their antimicrobial properties. Of these compounds, 12 exhibited >80% inhibition of the growth of at least one microorganism at a concentration of 50 μM. The most active derivative was found to be 4-phenyl-2-aminoimidazole 6h, which exhibited MIC90 (minimum inhibitory concentration) values of 12.5 μM against the Gram-positive bacteria and 50 μM against E. coli. The selectivity index between S. aureus and mammalian cells, which is important to consider in the evaluation of a compound's potential as an antimicrobial lead, was found to be 2.9 for compound 6h.
