Phloretin Explained

Phloretin is a dihydrochalcone, a type of natural phenol. It can be found in apple tree leaves[1] and the Manchurian apricot.[2]

Metabolism

In rats, ingested phlorizin is converted into phloretin by hydrolytic enzymes in the small intestine.[3] [4] Phloretin hydrolase hydrolyses phloretin into phloretic acid and phloroglucinol.

Pharmacological research

In an animal model, phloretin inhibited active transport of glucose into cells by SGLT1 and SGLT2, though the inhibition is weaker than by its glycoside phlorizin.[5] An important effect of this is the inhibition of glucose absorption by the small intestine[4] and the inhibition of renal glucose reabsorption.[3] Phloretin also inhibits a variety of urea transporters.[6] [7] It induces urea loss and diuresis 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.[8] Phloretin inhibits aquaporin 9 (AQP9) on mouse hepatocytes.[9]

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.[10]

Glycosides

See also

Notes and References

  1. 10.1021/jf00056a057 . Polyphenolic pattern in apple tree leaves in relation to scab resistance. A preliminary study . Picinelli A. . Dapena E. . Mangas J. J. . 1995 . Journal of Agricultural and Food Chemistry . 43 . 8 . 2273–2278.
  2. Web site: Manchurian Apricot (Prunus armeniaca var. mandshurica). North Dakota State University. January 30, 2014.
  3. Idris . I. . Donnelly . R. . 10.1111/j.1463-1326.2008.00982.x . Sodium-glucose co-transporter-2 inhibitors: An emerging new class of oral antidiabetic drug . Diabetes, Obesity and Metabolism . 11 . 2 . 79–88 . 2009 . 19125776. free .
  4. Crespy . V. . Aprikian . O. . Morand . C. . Besson . C. . Manach . C. . Demigné . C. . Rémésy . C. . Bioavailability of phloretin and phloridzin in rats . The Journal of Nutrition . 131 . 12 . 3227–3230 . 2001 . 11739871. 10.1093/jn/131.12.3227 . free .
  5. 0002-9513. 203. 6. 975–979. Chan. Stephen S.. William D. Lotspeich. Comparative effects of phlorizin and phloretin on glucose transport in the cat kidney. American Journal of Physiology. Legacy Content. 2012-10-21. 1962-12-01. 10.1152/ajplegacy.1962.203.6.975. 14019989.
  6. 10.1073/pnas.0401704101. 0027-8424. 101. 19. 7469–7474. Fenton. Robert A. . Chung-Lin Chou . Gavin S. Stewart . Craig P. Smith . Mark A. Knepper. Urinary concentrating defect in mice with selective deletion of phloretin-sensitive urea transporters in the renal collecting duct. Proceedings of the National Academy of Sciences of the United States of America. 2004-05-11. 15123796 . 409942. 2004PNAS..101.7469F. free.
  7. 1931-857X. 280. 3. F487–F494. Shayakul. Chairat. Hiroyasu Tsukaguchi. Urs V. Berger. Matthias A. Hediger. Molecular characterization of a novel urea transporter from kidney inner medullary collecting ducts. American Journal of Physiology. Renal Physiology. 2012-10-21. 2001-03-01. 10.1152/ajprenal.2001.280.3.f487. 11181411. 22143248. https://web.archive.org/web/20160304185109/http://ajprenal.physiology.org/content/280/3/F487. 2016-03-04. dead.
  8. Alsanea. Sary . Gao. Mingming . Liu. Dexi . May 2017 . Phloretin Prevents High-Fat Diet-Induced Obesity and Improves Metabolic Homeostasis . The AAPS Journal . 19 . 3 . 797–805 . 10.1208/s12248-017-0053-0 . 1550-7416 . 28197827. 3638970 .
  9. Fenton. Robert A.. Chou. Chung-Lin. Stewart. Gavin S.. Smith. Craig P.. Knepper. Mark A.. 2004-05-11. Urinary concentrating defect in mice with selective deletion of phloretin-sensitive urea transporters in the renal collecting duct. Proceedings of the National Academy of Sciences of the United States of America . en . 101 . 19 . 7469–7474 . 10.1073/pnas.0401704101 . 0027-8424 . 15123796 . 409942. 2004PNAS..101.7469F. free.
  10. Payne NJ, Badwaik VD, Waghwani HK, Moolani HV, Tockstein S, Thompson DH, Dakshinamurthy R . Development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity . International Journal of Nanomedicine . 13 . 1917–1926 . March 2018 . 10.2147/IJN.S143506 . 29636609 . 5880570 . free .

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