Natural and synthetic xanthones as monoamine oxidase inhibitors: Biological assay and 3D-QSAR

• Type: Article in International Scientific Journal
• Date: 2001

Authors

Gnerre, C (Author) Other; Thull, U (Author) Other; Gaillard, P (Author) Other; Carrupt, PA (Author) Other; Testa, B (Author) Other; Fernandes, E (Author) FFUP; Silva, F (Author) Other; Pinto, M (Author) Other; Pinto, MMM (Author) FFUP; Wolfender, JL (Author) Other; Hostettmann, K (Author) Other; Cruciani, G (Author) Other

Journal

Title: Helvetica Chimica Acta

Vol. 84

Pages: 552-570

ISSN: 0018-019X

Publisher: Wiley-Blackwell

Indexing

ISI Web of Knowledge - 61 Citations

Scopus - 67 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

Other information

Authenticus ID: P-000-X5H

DOI: 10.1002/1522-2675(20010321)84:3<552::aid-hlca552>3.0.co;2-x

Abstract (EN): Fifty-nine xanthones (= 9H-xanthen-9-ones) of natural or synthetic origin were investigated for their inhibitory activity toward monoamine-oxidase A (MAO-A) and MAO-B. The compounds demonstrated reversible. time-independent activities, with selectivity toward MAO-A. The most active inhibitor had an IC50 of 40 nM. Electron absorption spectroscopy revealed the formation of a 1:1 charge-transfer complex between lumiflavine and xanthones. 3D-QSAR Studies according to the CoMFA/GOLPE procedure provided information on the relationship between steric and electrostatic fields and MAO-A inhibition. The ALMOND procedure yielded additional topographical information on structural factors favoring activity.

Language: English

Type (Professor's evaluation): Scientific