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Steve Peigneur Ale? ?ula Nace Zidar Fiona Chan-Porter Robert Kirby David Madge Janez Ila? Danijel Kikelj Jan Tytgat 《Marine drugs》2014,12(4):2132-2143
Clathrodin is a marine alkaloid and believed to be a modulator of voltage-gated sodium (NaV ) channels. Since there is an urgent need for small molecule NaV channel ligands as novel therapeutics, clathrodin could represent an interesting lead compound. Therefore, clathrodin was reinvestigated for its potency and NaV channel subtype selectivity. Clathrodin and its synthetic analogues were subjected to screening on a broad range of NaV channel isoforms, both in voltage clamp and patch clamp conditions. Even though clathrodin was not found to exert any activity, some analogues were capable of modulating the NaV channels, hereby validating the pyrrole-2-aminoimidazole alkaloid structure as a core structure for future small molecule-based NaV channel modulators. 相似文献
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Nace Zidar Sofia Montalv?o ?iga Hodnik Dorota A. Nawrot Ale? ?ula Janez Ila? Danijel Kikelj P?ivi Tammela Lucija Peterlin Ma?i? 《Marine drugs》2014,12(2):940-963
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. 相似文献
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The objectives of this experiment were to determine the chloroplast pigments dynamics of soybean leaves during the growth stages under different tillage systems, which can be a major factor limiting yield of soybean. The greatest differences between the photosynthetic productivity parameters of the investigated soybean were determined from reproductive stages (R2 and R3?–?4). The chlorophyll a, chlorophyll a/b and carotenoids content under CT, DH and NT were greater in the reproductive stages (R2 and R3?–?4) than in the early stages (V3?–?4 and R1). The concentration dynamics of chlorophyll b and chlorophyll a/b was very similar in all growth stages and under all tillage systems in the 2-yr average. The increased drought stress in 2003 was likely critical in the observed lower seed yields in 2003. The yield of soybean was significantly lower under NT than CT and DH treatments in both years. The relationship between the soybean yield and chloroplast pigments concentration is strongly influenced by external factors. In the 2-yr average the soybean yield was considerably affected by the years and tillage systems. Statistical analysis showed a very significant relationship between chlorophyll pigments content, but photosynthetic parameters investigated did not correlate with soybean yield. 相似文献
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Prevalence and effects of the cymothoid isopod (Ceratothoa oestroides,Risso 1816) on cultured meagre (Argyrosomus regius,Asso 1801) in the Eastern Adriatic Sea 
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下载免费PDF全文 Slavica Čolak Matko Kolega Danijel Mejdandžić Ivan Župan Tomislav Šarić Edi Piplović Bosiljka Mustać 《Aquaculture Research》2018,49(2):1001-1007
Meagre (Argirosomus regius) is a relatively new farmed fish species in Croatian mariculture. This study is the first attempt to determine the prevalence of cymothoid isopod parasite Ceratothoa oestroides and its effects on cultured meagre in the Mediterranean area. When analysing growth of meagre at two sites in the central part of the Eastern Adriatic Sea, the greatest difference in total fish length was recorded in March 2016, when fish with parasites were 33% smaller than fish without parasites (24.47 ± 3.29 vs. 16.28 ± 1.01 cm; p < .001). The largest difference in mass was also recorded during sampling in March, when parasitized fish was 74% lighter than the unparasitized fish (171.75 ± 72.96 vs. 44.77 ± 6.57 g; p < .001). The presence of the cymothoid isopod in the buccal cavity was observed, and caused fish deformation throughout the entire duration of the study. Also, female parasites with pulli II in marsupium were found. Based on the determined prevalence and effects on production and health status, monitoring of the interaction between C. oestroides and meagre should be considered in future management plans for cultivation of this promising species for Mediterranean aquaculture. 相似文献
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