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Current Medicinal Chemistry 2019-Jan

Metabolism of Rhaponticin and Activities of Its Metabolite, Rhapontigenin: A Review.

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Dan Chen
Jing-Ru Liu
Yanjin Cheng
Hua Cheng
Ping He
Yang Sun

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Rhaponticin is a stilbenoid glucoside compound, can be found in medicinal plant of rhubarb rhizomes. Rhapontigenin (RHAG), the stilbene aglycone metabolite of rhaponticin, has shown various biological activities including anticancer activities to act a potential human cytochrome P450 inhibitor, antihyperlipidemic effect, anti-allergic action, antioxidant and antibacterial activities. Moreover, it was reported to scavenge intravellular reactive oxygen species (ROS), the 1,1-diphenyl-2-picrylliydrazyl (DPPH) radical, and hydrogen peroxide (H2O2). Meanwhile, RHAG exhibited the inhibitory activity for synthesis of DNA, RNA and protein, and also presented the capacity of inducing morphological changes and apoptosis of C. albicans. Here, the structure, pharmacokinetics, pharmacological effects as well as underlying mechanisms of rhaponticin and its metabolite, RHAG, have been extensively reviewed. This review will provide a certain reference value for developing the therapeutic drug of rhaponticin or RHAG.

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