School of Food Science and Technology, School of Chemical Engineering, Hubei University of Arts and Science, Xiangyang, Hubei 441053, China.
School of Life Science, Northwest University, Xi'an, Shaanxi 710069, China.
Curr Med Chem. 2020;27(19):3168-3186. doi: 10.2174/0929867326666190121143252.
Rhaponticin is a stilbenoid glucoside compound, 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 intracellular Reactive Oxygen Species (ROS), the 1,1-Diphenyl-2-Picrylliydrazyl (DPPH) radical, and Hydrogen Peroxide (H2O2). Meanwhile, RHAG exhibited the inhibitory activity for the 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.
瑞香素是一种二苯乙烯苷类化合物，存在于药用大黄的根茎中。瑞香素苷元（RHAG）是瑞香素的二苯乙烯苷元代谢物，具有多种生物活性，包括抗癌活性，可作为潜在的人细胞色素 P450 抑制剂、抗高血脂作用、抗过敏作用、抗氧化和抗菌活性。此外，它还被报道能清除细胞内活性氧（ROS）、1,1-二苯基-2-苦基肼基（DPPH）自由基和过氧化氢（H2O2）。同时，RHAG 对 DNA、RNA 和蛋白质的合成表现出抑制活性，并且还呈现出诱导白色念珠菌形态变化和凋亡的能力。在这里，瑞香素及其代谢物 RHAG 的结构、药代动力学、药理作用以及作用机制已经被广泛综述。本综述将为开发瑞香素或 RHAG 的治疗药物提供一定的参考价值。
