Transcript Acetylcholinesterase inhibitory activity of thio-avarol derivatives

Serbia - Italia
Bilateral Cooperation
ACETYLCHOLINESTERASE
INHIBITORY ACTIVITY OF
THIO-AVAROL DERIVATIVES
25th and 26th June, 2012
Beograd
Pozzuoli - Napoli
The Sponges
Dysidea avara
Dr. Salvatore De Rosa
Dirigente di Ricerca
National Research Council of Italy
Institute of Biomolecular Chemistry
CNR-ICB
E-mail: [email protected]
Dr. Giuseppina Tommonaro
Ricercatore
National Research Council of Italy
Institute of Biomolecular Chemistry
CNR-ICB
E-mail: [email protected]
Mr. Carmine Iodice
CollaboratoreTecnico ente di Ricerca
National Research Council of Italy
Institute of Biomolecular Chemistry
CNR-ICB
E-mail: [email protected]
Avarol is a marine sesquiterpene
hydroquinone possesing a rearanged
drimane skeleton.
Avarone is the quinone form of avarol.
Avarol
Avarone
Avarol was found to have
anti-inflammatory
antipsoriatic
antioxidant
antitumor
antiplatelet
analgesic
anti-HIV
activities.
Of particular interest is
acetylcholinesterase inhibitory
activity of thio-avarol derivatives with a
carboxylic group in the molecule,
such as
avarol-3‘-thiobenzoate
avarol-3‘–thiolactate
avarol-4‘–thiolactate
TLC bioautographic assay
(white spot on a purple background)
1 μg
Galanthamine was used a positive control.
O
O
N
H
HO
Galanthamine 0.01 μg
Dr. Pietro Amodeo
I Ricercatore
National Research Council of Italy
Institute of Biomolecular Chemistry
CNR-ICB
E-mail: [email protected]
Dr. Rosa Maria Vitale
Ricercatore
National Research Council of Italy
Institute of Biomolecular Chemistry
CNR-ICB
E-mail: [email protected]
Binding properties of avarol and its
inhibitory derivatives to the enzyme
have been characterising by computational
approach.
This research aims to design new avarol
derivatives which better inhibit
acetylcholinesterase.
Serbia - Italia
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