01932nam a2200241Ia 4500 MX-MdCICY 20260521091411.0 CICY B-14134 Xanthones with neuraminidase inhibitory activity from the seedcases of Garcinia mangostana Bioorganic & medicinal Chemistry, 18(17), p.6258-6264, 2010 This study was designed to gain deeper insights into the molecular properties of natural xanthones as neuraminidase inhibitors. A series of xanthones 1-12 was isolated from the seedcases of Garcinia mangostana and evaluated for bacteria neuraminidase inhibitory activity. Compounds 11 and 12 emerged to be new xanthones (mangostenone F, mangostenone G)which we fully spectroscopically characterized. The IC(50)values of compounds 1-12 were determined to range between 0.27-65.7 microM. The most potent neuraminidase inhibitor 10 which has an IC(50)of 270 nM features a 5,8-diol moiety on the B ring. Interestingly, structure-activity studies reveal that these xanthones show different kinetic inhibition mechanisms depending upon the arrangement of hydroxyl groups in the B ring. Compound 6 possessing a 6,7-diol motif on the B-ring operated under the enzyme isomerization model (k(5)=0.1144 microM(-1)s(-1), k(6)=0.001105 s(-1), and K(i)(app)=7.41 microM), whereas compound 10 possessing a 5,8-diol unit displayed simple reversible slow-binding inhibition (k(3)=0.02294 microM(-1)s(-1), k(4)=0.001025 s(-1), and K(i)(app)=0.04468 microM). Ryu, H. W. Curtis-Long, M. J. Jung, S. Jin, Y. M. Cho, J. K. Ryu, Y. B. Park, K. H https://drive.google.com/file/d/1lubyBvrFeQMv_fU5apI-rEwi5ypDSG6g/view?usp=drivesdk Para ver el documento ingresa a Google con tu cuenta: @cicy.edu.mx Loc REF1 250602s9999 xx |||||s2 |||| ||und|d 24268 24268 0 0 Loc 0 0 F1 CICY CICY RE 2025-06-25 0 B-14134 2025-06-25 15:39:35 2025-06-25 REF1