Signaling pathways and proteins targeted by antidiabetic chalcones.

Chalcones have shown a broad spectrum of biological activities with clinical potential against various diseases. The biological activities are mainly attributed to the presence of α, ß-unsaturated carbonyl system, perceived as potential Michael acceptors. In this review, we discussed the antioxidant potential of chalcones and elucidated the mechanisms of pathways and proteins such as carbohydrate digestive enzymes (α-amylase and α-glucosidase), aldose reductase, SGLT-2, and Nrf2 that are targeted by antidiabetic chalcones. In addition to their insulin mimetic potential, we explore the major molecular targets of chalcones and discuss the biochemical and therapeutic implication of modulating these targets. Finally, we dwell on the opulence of the literature and envisage how RNA interference-mediated gene silencing technique and in silico molecular docking could be exploited in the search for novel and more efficacious antidiabetic chalcones.

Syhthesis and antitumor activity of alkoxylbiphenyl/curcumine conjugates / 国际药学研究杂志

Objecti ve To design and synthesize conjugates of alkoxylbiphenyl/C5-curcumine with antitumor activities. Methods Bicyclol,acetone and benzaldehyde with various substituents were used as raw materials. The target compounds were obtained by oxidizing and Aldol condensation reaction. And their antitumor activities were evaluated by MTS assay in the parental sensitive K562 and drug-resistant K562/A02 cell lines. Results Twelve alkoxylbiphenyl/C5-curcumine conjugates were prepared. Conclusion The synthetic procedure of the target compounds is simple,and the yield is high. Compound 3b could significantly inhibit K562 and drug-resistant K562/A02 cell proliferation,and the IC50 is 5.38 and 3.60μmol/L,respectively.