title: Amorfrutins are efficient modulators of peroxisome proliferator-activated receptor gamma (PPARγ) with potent antidiabetic and anticancer properties: a patent evaluation of WO2014177593 A1.
abstract: BACKGROUND
  PPARγ is an essential regulator of lipid, glucose, and insulin metabolism. PPARγ 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 PPARγ modulators (SPPARγMs) as safer alternatives to PPARγ full agonists.
  
  
  METHODS
  This application claims the plant-derived amorfrutins or their synthetic analogs as SPPARγMs with potential to exhibit glucose-lowering effects without provoking side effects associated with full PPARγ activation. Specifically, the in vivo glucose-lowering properties of the high-affinity SPPARγM amorfrutin B are described. Moreover, examples of this class of compounds exhibit interesting antiproliferative activities.
  
  
  CONCLUSIONS
  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.
authors.affiliation: a University of Naples Federico II, Department of Pharmacy, "Drug Discovery" Laboratory , Via D. Montesano 49, Naples, Italy +39 081 678 613 ; +39 081 678 012 ; antonio.lavecchia@unina.it.
authors.forename: Antonio
authors.initials: A
authors.lastname: Lavecchia
authors.affiliation: a University of Naples Federico II, Department of Pharmacy, "Drug Discovery" Laboratory , Via D. Montesano 49, Naples, Italy +39 081 678 613 ; +39 081 678 012 ; antonio.lavecchia@unina.it.
authors.forename: Carmen
authors.initials: C
authors.lastname: Di Giovanni
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy / Q000473:pathology; D006801:Humans; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D047495:PPAR gamma / Q000187:drug effects* / Q000378:metabolism; D010330:Patents as Topic; D012459:Salicylates / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D007004:Hypoglycemic Agents; D047495:PPAR gamma; D012459:Salicylates; C582540:amorfrutin B
keywords: anticancer; diabetes; insulin resistance; natural product; peroxisome proliferator-activated receptor; selective PPARγ modulators