Xanthohumol, a prenylated chalcone from hop, is an inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2 and shows chemopreventive effects.
Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities. Xanthohumol significantly attenuates ADP-induced blood platelet aggregation, and significantly reduces the expression of fibrinogen receptor (activated form of GPIIbIIIa) on platelets' surface[3]. 5-50 nM xanthohumol reduced the frequency of spontaneously occurring Ca2+ sparks (>threefold) and Ca2+ waves in control myocytes and in cells subjected to Ca2+ overload caused by the following: 1) exposure to low K+ solutions, 2) periods of high frequency electrical stimulation, 3) exposures to isoproterenol, or 4) caffeine. At room temperatures, 50-100 nM xanthohumol reduced the rate of relaxation of electrically- or caffeine-triggered Ca2+transients, without suppressing ICa, but this effect was small and reversed by isoproterenol at physiologic temperatures. Xanthohumol also suppressed the Ca2+ content of the SR and its rate of recirculation[4]. The anti-angiogenic activity of XN was more potent than epigallocatechin-3-gallate (EGCG). Treatment of endothelial cells with XN led to increased AMPK (5' adenosine monophosphate-activated protein kinase) phosphorylation and activity[5]. XN significantly reduced cell viability and induced apoptosis via pro-caspase-3/8 cleavage and poly(ADP ribose) polymerase (PARP) degradation[6]. In addition, a xanthohumol-enriched hop extract displayed a weak to moderate antiviral activity against BVDV (bovine viral diarrhea virus) (therapeutic index (TI)=6.0), HSV-2 (TI=>5.3), Rhino (TI=4.0) and HSV-1 (TI=>1.9) with IC(50) values in the low microg/ml range. Xanthohumol accounted for the antiviral activity observed in the xanthohumol-enriched hop extract against BVDV, HSV-1 (herpes simplex virus type 1) and HSV-2. Xanthohumol also showed antiviral activity against CMV (cytomegalovirus), suggesting that it might have a generalized anti-herpesvirus antiviral activity. Again, superior antiviral activity was observed with the xanthohumol isomer against CMV[7].
Portugal
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Recruiting
Porto, Portugal, 4200-319
Contact: Raquel Soares, PhD (+351)225513624 raqsoa@med.up.pt 收起 <<
Portugal
... 展开 >> Medical Faculty of University of Porto
Recruiting
Porto, Portugal, 4200-319
Contact: Raquel Soares, PhD (+351)225513624 raqsoa@med.up.pt 收起 <<
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