Several natural and synthetic flavone derivatives have been reported to inhibit formation of amyloid fibrils or to remodel existing fibrils. These studies suggest that the numbers and positions of hydroxyl groups on the flavone rings determine their effectiveness as amyloid inhibitors. In many studies the primary method for determining the effectiveness of inhibition is measuring Thioflavin T (...

High blood cholesterol has been associated with cardiovascular diseases. The enzyme HMG CoA reductase (HMGCR) is responsible for cholesterol synthesis, and inhibitors of this enzyme (statins) have been used clinically to control blood cholesterol. Sterol regulatory element binding protein (SREBP) -2 is a key transcription factor in cholesterol metabolism, and HMGCR is a target gene of SREBP-2. ...

Most anticancer drugs have their origin in traditional medicinal plants. We describe here a flavone, 5,3'-dihydroxy-3,6,7,8,4'-pentamethoxyflavone (PMF), from the leaves of the Thai plant Gardenia obtusifolia, that has anti-inflammatory and anticancer potential. Because the nuclear factor-κB (NF-κB) pathway is linked to inflammation and tumorigenesis, we investigated the effect of PMF on this p...

Flavonoids are a class of dietary phytochemicals that modulate various biological activities. The effects of flavone and five hydroxylated derivatives on the methoxyresorufin O-demethylase activity catalyzed by cDNA-expressed human cytochromes P450 (CYP)1A1 and 1A2 were examined. Flavone was a less potent inhibitor of CYP1A1 (IC50 = 0.14 microM) than CYP1A2 (IC50 = 0.066 microM). Four hydroxyla...

We describe here the isolation of three flavone 6-C-glycosides from the leaves of Anthurium andraeanum, The two new flavones were identified through detailed spectroscopic analysis as 4"'-(3,4-dimethoxycinnamoyl)-embinin (2) and 4"'-ferruloyl-embinin (3).

The flavone backbone is a well-known pharmacophore present in a number of substrates and inhibitors of various P450 enzymes. In order to find highly potent and novel P450 family I enzyme inhibitors, an acetylene group was incorporated into six different positions of flavone. The introduction of an acetylene group at certain locations of the flavone backbone lead to time-dependent inhibitors of ...

Natural products have been studied to provide alternative treatments against human diseases as they various medicinal properties. One of these natural is substances in the class flavonoids. These bioactive molecules antioxidant, anti-inflammatory and antitumor activities. The number studies focusing on increasing discover new therapeutic agents such cancer. We aimed determine in-vitro anticance...

A new digalacturonide flavone, luteolin 7-O-beta-galacturonyl-(2 --> 1)-O-beta-galacturonide (1), was isolated along with nine known flavone glycosides from the aqueous methanolic extract of Lantana camara (L.) flowers. Their structures were determined on the basis of the spectral data. The extract of L. camara was evaluated for antioxidant and hepatoprotective properties in the acetaminophen-i...

Four dihydroxy flavone derivatives viz 5,3′-, 7,3′-, 2′,3′and 2′,4′-dihydroxy flavones were evaluated for their antinociceptive response in doses ranging from 3 to 200 mg/kg (s.c). Antinociception in mice was studied employing acetic acid induced abdominal constrictions, formalin induced nociception and tail immersion assay procedures. Involvement of opioid mechanism in the antinociceptive acti...

Modified flavone derivatives show diverse pharmacological effects, which may be attributed to their interaction with lipid membranes. We have studied the interaction of Chrysin (C) and some novel flavone derivatives, 4 ́–methoxyflavone (C1), 4 ́– chloroflavone (C2) and 4 ́–nitroflavone (C3) with dipalmitoylphosphatidylcholine (DPPC) using molecular dynamic (MD) simulation, differential scanning ca...