The fabulous story of glyphozines.
DOI:
https://doi.org/10.56867/Keywords:
Diabetes mellitus, History, Sodium-Glucose Transporter 2 Inhibitors, Heart Failure, Renal Insufficiency, Chronic.Abstract
Introduction: The surprising history of gliflozins begins with the phlorizin-induced renal diabetes model and culminates with synthesizing the C glycosides derived from phloridzin: gliflozins. These drugs, specifically SGLT2 inhibitors, constitute a new class of oral antidiabetics with unsuspected beneficial effects on cardiovascular and
renal levels.
Objective of the review: The aim of the present historical narrative review of the events related to developing
glyphozins from phlorizin.
Essential points of the review:
• Phloridzin or phlorizin, a natural O-glucoside, was discovered in 1835 by two Belgian chemists: Laurent Guillaume de Koninck (1809-1887) and Jean Servais Stas (1813-1891).
• Joseph von Mering described in 1883 the glucosuric effects of phlorizin, first in dogs, then in humans,
which will lead to a model of nephrogenic diabetes.
• In the 1950s, phlorizin was observed to block glucose transport in different epithelia, including the kidney
and intestine.
• Today, phlorizin is known to be a nonspecific antagonist of glucose (GLUT) receptors. We also owe a lot
to patients with congenital glycosuria, in whom inactivating mutations of GLUT receptors were identified.
Conclusion: The fabulous fate of gliflozins illustrates the relevance of the history of medicine and translational
research that allowed significant therapeutic advances for many diabetic, renal, and cardiac patients.

Downloads
Published
Issue
Section
License
Copyright (c) 2023 Hernán Valdés Socin, Miguel Vanoni Patiño (Author)

This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License.