Phloretin is a
dihydrochalcone, a type of natural phenol. It can be found in apple tree leaves and the
Manchurian apricot.
Metabolism
In rats, ingested
phlorizin is converted into phloretin by hydrolytic enzymes in the small intestine.
hydrolyses phloretin into
phloretic acid and
phloroglucinol
Phloroglucinol is an organic compound with the formula C6H3(OH)3. It is a colorless solid. It is used in the synthesis of pharmaceuticals and explosives. Phloroglucinol is one of three isomeric benzenetriols. The other two isomers are hydroxyqu ...
.
Pharmacological research
In an animal model, phloretin inhibited
active transport
In cellular biology, ''active transport'' is the movement of molecules or ions across a cell membrane from a region of lower concentration to a region of higher concentration—against the concentration gradient. Active transport requires cellul ...
of glucose into cells by
SGLT1
Sodium/glucose cotransporter 1 (SGLT1) also known as solute carrier family 5 member 1 is a protein in humans that is encoded by the gene which encodes the production of the SGLT1 protein to line the absorptive cells in the small intestine and th ...
and
SGLT2
The sodium/glucose cotransporter 2 (SGLT2) is a protein that in humans is encoded by the (solute carrier family 5 (sodium/glucose cotransporter)) gene.
Function
SGLT2 is a member of the sodium glucose cotransporter family, which are sodium-d ...
, though the inhibition is weaker than by its
glycoside
In chemistry, a glycoside is a molecule in which a sugar is bound to another functional group via a glycosidic bond. Glycosides play numerous important roles in living organisms. Many plants store chemicals in the form of inactive glycoside ...
phlorizin. An important effect of this is the inhibition of glucose absorption by the small intestine
[ and the inhibition of ]renal glucose reabsorption Renal glucose reabsorption is the part of kidney (renal) physiology that deals with the retrieval of filtered glucose, preventing it from disappearing from the body through the urine.
If glucose is not reabsorbed by the kidney, it appears in the u ...
.[ Phloretin also inhibits a variety of ]urea transporter
A urea transporter is a membrane transport protein, transporting urea. Humans and other mammals have two types of urea transport proteins, UT-A and UT-B. The UT-A proteins are important for renal urea handling and are produced by alternative spl ...
s. It induces urea loss and diuresis
Diuresis () is increased urination (polyuria) or, in the related word senses more often intended, the physiological process that produces such an increase or the administration of medications to encourage that process. It involves extra urine pr ...
when coupled with high protein diets. Phloretin has been found to inhibit weight gain and improve metabolic homeostasis in mice fed with high-fat diet. Phloretin inhibits aquaporin 9 (AQP9) on mouse hepatocyte
A hepatocyte is a cell of the main parenchymal tissue of the liver. Hepatocytes make up 80% of the liver's mass.
These cells are involved in:
* Protein synthesis
* Protein storage
* Transformation of carbohydrates
* Synthesis of cholesterol, ...
s.
Nanoparticle Synthesis
Phloretin functionalized gold-nanoparticles (Pht-GNPs) were synthesized using a single-step synthesis method and tested for its anticancer activity. Pht-GNPs showed significant cancer cell toxicities compared to free phloretin.
Glycosides
* Phlorizin is the 2'- glucoside of phloretin
* Naringin dihydrochalcone is a diglycoside of phloretin
See also
* Phloretin-glucosidase
References
{{Sodium-glucose transporter modulators
Dihydrochalcones
3-Hydroxypropenals
Resorcinols