Structure–activity analysis of 2′-modified cinnamaldehyde analogues as potential anticancer agents

Characterization of the role of COP9 signalosome in regulating cullin E3 ubiquitin ligase activity

“…clones and subcloned into modified pcDNA3.1 with N-terminal FLAG tag. FLAG-CSN5 was subsequently transferred into the puro-MaRX retroviral expression vector (a kind gift from David Beach) and used to generate a stable FLAG-CSN5–expressing HEK293T cell line, as previously described (Gan et al , 2009). For DNA transfections, subconfluent cells were transfected using Genejuice (Novagen, San Diego, CA) according to the manufacturer's instructions.…”

Antioxidative Activities of Natural Hydroxy-Bearing Cinnamaldehydes and Cinnamic Acids: A Comparative Study

“…Cinnamaldehydes are more fatsoluble than their corresponding acids, so it is easier for cinnamaldehydes to adhere to the lipid part of erythrocytes than their corresponding acids, and thus cinnamaldehydes showed stronger hemolysis inhibitory activities than their corresponding acids. Certain phenolic compounds may incorporate into the hydrophobic core of the membrane bilayer, causing a reduction in membrane fluidity [17][18][19] [9,11,12,14], such as antimicrobial, anti-inflammatory, and as a good candidate for cancer therapy. Another possible cause for the higher activities of aldehydes is that the carbonyl group of cinnamaldehydes can easily combine with the residual amino group of the protein of RBCs forming reversible imine structure [20].…”

“…Some hydroxybearing cinnamaldehydes, such as ocoumaraldehyde from bark of cinnamon，p-coumaraldehyde， ferulaldehyde，and caffeic aldehyde have been widely studied and found to be good bioactive compounds. Much attention has been paid to their antioxidative activities [8][9][10][11][12][13][14]. But the comparative studies on the antioxidative effects of the hydroxy-bearing cinnamaldehydes with their corresponding acids are few.…”

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“…The study of structure-activity analysis to define structural features which is vital to cinnamaldehyde analogues activity of defining molecular drug targets for promising class of potential anticancer agents have been performed. The result reveal the propenal group and as well as the functional group in the 2'-position of cinnamaldehyde structure possesses anti-cancer activity 16,55 .…”

“…Proliferation, invasion, and tumor growth were inhibited in a murine A375 model (rats and mice) of human melanoma (skin cancer), though only at high doses of cinnamaldehyde 55 . However such effects were not achievable on dietary intake.…”