- Synthesis of alkaloid pulmonarin B and its application in the prevention and control of plant viruses and mycosis
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The present invention relates to the efficient synthesis of the alkaloid pulmonarin B and its application in the prevention and control of plant viruses and pathogenic diseases, the present invention is based on the systematic research literature, drawing
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Paragraph 0020
(2022/01/20)
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- Total synthesis of pulmonarin B and design of brominated phenylacetic acid/tacrine hybrids: Marine pharmacophore inspired discovery of new CHE and Aβ aggregation inhibitors
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A marine natural product, pulmonarin B (1), and a series of related tacrine hybrid analogues were synthesized and evaluated as cholinesterase (ChE) inhibitors. The in vitro ChE assay results revealed that 1 showed moderate dual acetylcholinesterase (AChE)/ butyrylcholinesterase (BChE) inhibitory activity, while the hybrid 12j proved to be the most potent dual inhibitor among the designed derivatives, being almost as active as tacrine. Molecular modeling studies together with kinetic analysis suggested that 12j interacted with both the catalytic active site and peripheral anionic site of AChE. Compounds 1 and 12j could also inhibit self-induced and AChE-induced Aβ aggregation. In addition, the cell-based assay against the human hepatoma cell line (HepG2) revealed that 1 and 12j did not show significant hepatotoxicity compared with tacrine and donepezil. Taken together, the present study confirmed that compound 1 was a potential anti-Alzheimer’s disease (AD) hit, and 12j could be highlighted as a multifunctional lead compound for anti-AD drug development.
- Cheng, Zhi-Qiang,Song, Jia-Li,Zhu, Kongkai,Zhang, Juan,Jiang, Cheng-Shi,Zhang, Hua
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- Isolation and synthesis of pulmonarins A and B, acetylcholinesterase inhibitors from the colonial ascidian Synoicum pulmonaria
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Pulmonarins A and B are two new dibrominated marine acetylcholinesterase inhibitors that were isolated and characterized from the sub-Arctic ascidian Synoicum pulmonaria collected off the Norwegian coast. The structures of natural pulmonarins A and B were tentatively elucidated by spectroscopic methods and later verified by comparison with synthetically prepared material. Both pulmonarins A and B displayed reversible, noncompetitive acetylcholinesterase inhibition comparable to several known natural acetylcholinesterase inhibitiors. Pulmonarin B was the strongest inhibitor, with an inhibition constant (K i) of 20 μM. In addition to reversible, noncompetitive acetylcholinesterase inhibition, the compounds displayed weak antibacterial activity but no cytotoxicity or other investigated bioactivities.
- Tadesse, Margey,Svenson, Johan,Sepcic, Kristina,Trembleau, Laurent,Engqvist, Magnus,Andersen, Jeanette H.,Jaspars, Marcel,Stensvaisg, Klara,Haug, Tor
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p. 364 - 369
(2014/03/21)
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