ChemInform Abstract: Marine AChE Inhibitors Isolated from Geodia barretti: Natural Compounds and Their Synthetic Analogues.

ChemInform ◽  
2016 ◽  
Vol 47 (24) ◽  
Author(s):  
Elisabeth K. Olsen ◽  
Espen Hansen ◽  
Lindon W. K. Moodie ◽  
Johan Isaksson ◽  
Kristina Sepcic ◽  
...  
2021 ◽  
Author(s):  
Manuela Oliverio ◽  
Monica Nardi ◽  
Maria Luisa Di Gioia ◽  
Paola Costanzo ◽  
Sonia Bonacci ◽  
...  

Semi-synthesis is an effective strategy to obtain both natural and synthetic analogues of the olive secoiridoids, starting from easy accessible natural compounds.


Marine Drugs ◽  
2021 ◽  
Vol 19 (2) ◽  
pp. 55
Author(s):  
Synthia Michon ◽  
Florine Cavelier ◽  
Xavier J. Salom-Roig

Aurilides are a class of depsipeptides occurring mainly in marine cyanobacteria. Members of the aurilide family have shown to exhibit strong cytotoxicity against various cancer cell lines. These compounds bear a pentapeptide, a polyketide, and an α-hydroxy ester subunit in their structure. A large number of remarkable studies on aurilides have emerged since 1996. This comprehensive account summarizes the biological activities and total syntheses of natural compounds of the aurilide family as well as their synthetic analogues.


2020 ◽  
Vol 18 (8) ◽  
pp. 696-719
Author(s):  
Speranta Avram ◽  
Maria Mernea ◽  
Carmen Limban ◽  
Florin Borcan ◽  
Carmen Chifiriuc

Background: Alzheimer’s disease (AD) is considered a severe, irreversible and progressive neurodegenerative disorder. Currently, the pharmacological management of AD is based on a few clinically approved acethylcholinesterase (AChE) and N-methyl-D-aspartate (NMDA) receptor ligands, with unclear molecular mechanisms and severe side effects. Methods: Here, we reviewed the most recent bioinformatics, cheminformatics (SAR, drug design, molecular docking, friendly databases, ADME-Tox) and experimental data on relevant structurebiological activity relationships and molecular mechanisms of some natural and synthetic compounds with possible anti-AD effects (inhibitors of AChE, NMDA receptors, beta-secretase, amyloid beta (Aβ), redox metals) or acting on multiple AD targets at once. We considered: (i) in silico supported by experimental studies regarding the pharmacological potential of natural compounds as resveratrol, natural alkaloids, flavonoids isolated from various plants and donepezil, galantamine, rivastagmine and memantine derivatives, (ii) the most important pharmacokinetic descriptors of natural compounds in comparison with donepezil, memantine and galantamine. Results: In silico and experimental methods applied to synthetic compounds led to the identification of new AChE inhibitors, NMDA antagonists, multipotent hybrids targeting different AD processes and metal-organic compounds acting as Aβ inhibitors. Natural compounds appear as multipotent agents, acting on several AD pathways: cholinesterases, NMDA receptors, secretases or Aβ, but their efficiency in vivo and their correct dosage should be determined. Conclusion: Bioinformatics, cheminformatics and ADME-Tox methods can be very helpful in the quest for an effective anti-AD treatment, allowing the identification of novel drugs, enhancing the druggability of molecular targets and providing a deeper understanding of AD pathological mechanisms.


2016 ◽  
Vol 14 (5) ◽  
pp. 1629-1640 ◽  
Author(s):  
Elisabeth K. Olsen ◽  
Espen Hansen ◽  
Lindon W. K. Moodie ◽  
Johan Isaksson ◽  
Kristina Sepčić ◽  
...  

Barettin, 8,9-dihydrobarettin, bromoconicamin and a novel brominated marine indole were isolated from Geodia barretti and evaluated as inhibitors of electric eel acetylcholinesterase together with synthetic analogs.


Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
H Derendorf
Keyword(s):  

Planta Medica ◽  
2013 ◽  
Vol 79 (13) ◽  
Author(s):  
C Si ◽  
L Wu ◽  
S Liu ◽  
G Xu ◽  
X Ren ◽  
...  

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