Amorfrutins are efficient modulators of peroxisome proliferator-activated receptor gamma (PPAR gamma) with potent antidiabetic and anticancer properties: a patent evaluation of WO2014177593 A1

摘要

Introduction: PPAR is an essential regulator of lipid, glucose, and insulin metabolism. PPAR full agonists, such as thiazolidinediones, are the mainstay drugs for the treatment of type 2 diabetes; however, undesirable clinical side effects have contributed to poor compliance with therapy and limited their full therapeutic potential. In the last few years, many efforts have been made in the discovery and development of selective PPAR modulators (SPPARMs) as safer alternatives to PPAR full agonists.Areas covered: This application claims the plant-derived amorfrutins or their synthetic analogs as SPPARMs with potential to exhibit glucose-lowering effects without provoking side effects associated with full PPAR activation. Specifically, the in vivo glucose-lowering properties of the high-affinity SPPARM amorfrutin B are described. Moreover, examples of this class of compounds exhibit interesting antiproliferative activities.Expert opinion: The patent (WO2014177593 A1) under discussion proposes enriching functional food products or phytomedical extracts with safe licorice extracts, containing sufficient amounts of amorfrutins, with the ultimate goal of inhibiting the early development of disorders such as insulin resistance. Interestingly, some example compounds show anticancer properties in colon, prostate, and breast malignancies. However, further in vivo investigations of the claimed compounds for these specific indications will be necessary to definitively support their clinical applications.