Cell protection against different noxious stimuli like oxidative stress or chemical toxins plays a central role in the treatment of many diseases. The inducible heme oxygenase isoform, heme oxygenase-1 (HO-1), is known to protect cells against a variety of harmful conditions including apoptosis. Because a number of medium strong electrophiles from a series of α-X-substituted 2',3,4,4'-tetrameth...

The action of β-secretase (BACE1) is strongly correlated with the onset of Alzheimer's disease (AD). Aminochalcone derivatives were examined for their ability to inhibit BACE1. Parent aminochalcones showed two digit micromolar IC(50)s against BACE1. Potency was enhanced 10-fold or more by introducing benzenesulfonyl derivatives to the amino group: 1 (IC(50) = 48.2 μM) versus 4a (IC(50) = 1.44 μ...

An effective method has been developed for the preparation of novel chiral chalcone derivatives under mild conditions from the easily accessible starting materials nitromethane and chalcone derivatives 2. The corresponding products were obtained in moderate yields with excellent enantioselectivities (up to 99%).

Hymenoclea salsola, Asteraceae, Resin Flavonoids, 2',4',6 'OH Chalcone Hymenoclea salsola (Asteraceae), a dominant shrub of the desert areas of California and Baja California, Mexico, secretes high amounts of resin on the leaf surface. Chemi­ cal analysis of the resin revealed the presence of a complex mixture of flavonoid aglycones. Among the compounds identified is the rare 2',4',6'-OH chalco...

Background The flavonoids, naringenin-chalcone and narigenin, are intermediates in phenylpropanoid metabolism in plants, occupying the central position as primary intermediates in flavonoid biosynthesis and are synthesized by chalcone synthase (CHS) and chalcone isomerase (CHI) respectively.[1] It has been reported that supplementation of narigenin-chalcone and narigenin can inhibit the activit...

When chalcone and trans-4-phenyl-3-buten-2-one (PBO) were incubated with liver microsomes of untreated rats in the presence of NADPH, 4-hydroxychalcone and trans-4-(4-hydroxyphenyl)-3buten-2-one (4-OH-PBO), respectively, were formed as major metabolites. Two minor metabolites of chalcone, 4 -hydroxychalcone and 2-hydroxychalcone, were also observed. The oxidase activity affording 4-hydroxychalc...