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23 avril 2011 6 23 /04 /avril /2011 09:10
Z Naturforsch C. 2008 May-Jun;63(5-6):366-70.

Coumarin, anthroquinone and stilbene derivatives with anticholinesterase activity.

Source

Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, 06330 Ankara, Turkey. iorhan@gazi.edu.tr

Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are the key enzymes in pathogenesis of Alzheimer's disease (AD), which is characterized by a deficit in central cholinergic transmission.


In the current study, AChE and BChE inhibitory activities of seven coumarin derivatives

[umbelliferone (1),

4-methylumbelliferone (2),

4-hydroxycoumarin (3),

scopoletin (4),

8-methoxypsoralen (5),

bergapten (6), and

iso-bergapten (7)],

a furanocoumarin mixture obtained from Heracleum crenatifolium Boiss. (Umbelliferae), as well as of two anthroquinone derivatives [rhein (8)

and aloe-emodine (9)]

and one stilbene, rhapontin (10),

were tested by the spectrophotometric method of Ellman using an ELISA microplate-reader at 1 mg mL(-1).

Among them, the furanocoumarin mixture [(68.8 +/- 0.76)%], bergapten [(62.4 +/- 0.74)%], aloe-emodine [(57.2 +/- 1.32)%], scopoletin [(53.1 +/- 0.83)%], and 4-methylumbelliferone [(62.3 +/- 1.03)%] showed over 50% inhibition against AchE, while umbelliferone [(54.3 +/- 0.23)%], 4-methylumbelliferone [(80.9 +/- 1.17)%], scopoletin [(73.5 +/- 1.01)%], 8-methoxypsoralen [(67.1 +/- 0.98)%], as well as the furanocoumarin mixture [(76.7 +/- 0.95)%] had a notable anti-BChE effect.

PMID:
 
18669022
 
[PubMed - indexed for MEDLINE]

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