Phloretin
Wikipedia:
A dihydrochalcone, a type of natural phenols. It can be found in apple tree leaves and the Manchurian apricot.
Pharmacology
Phloretin inhibits the active transport of glucose into cells by SGLT1 and SGLT2, though the inhibition is weaker than by its glycoside phlorizin. Orally consumed phlorizin is nearly entirely converted into phloretin by hydrolytic enzymes in the small intestine.An important effect of this is the inhibition of glucose absorption by the small intestine and the inhibition of renal glucose reabsorption.Phloretin also inhibits a variety of urea transporters. It induces urea loss and diuresis when coupled with high protein diets.
Phloretin has been found to inhibit GLUT2 and aquaporin 9 (AQP9) on mouse hepatocytes.
Metabolism
Phloretin hydrolase uses phloretin and water to produce phloretate and phloroglucinol.
Glycosides
- Phlorizin is the 2'-glucoside of phloretin.
- Naringin dihydrochalcone is a diglycoside of phloretin.
ARTICLES/STUDIES
Aflatoxin
Allergies
Anti-Inflammatory
- Phloretin promotes lipolysis and inhibit inflammation in mouse 3T3-L1 cells.
- Phloretin attenuates the inflammatory and oxidative stress pathways that accompany lung injury in mice.
- Phloretin inhibits interleukin-1β-induced COX-2 and ICAM-1 in human lung epithelial cells.
- The molecular pharmacology of phloretin: anti-inflammatory mechanisms of action.
Antimicrobial
- Biochemical and antimicrobial activity of phloretin.
- Phloretin might have a potential application in the development of treatment for MRSA infections.
- Phloretin also acts as an inhibitor of E. coli O157:H7 biofilm formation as well as an anti-inflammatory agent in inflammatory bowel diseases.
- Phloretin attenuate the virulence of S. typhimurium and can protect against S. typhimurium infection.
- Antimicrobial and anti-Inflammatory activity of apple polyphenol phloretin on respiratory pathogens.
- Phloretin potentiates polymyxin E activity against gram-negative bacteria.
- Phloretin is protective in a murine salmonella enterica serovar typhimurium infection model.
Arthritis
Cancer
- These results demonstrate that phloretin exerts potent chemo-preventive activity in human glioblastoma cells through the generation of ROS.
- Phloretin, as a potent anticancer compound: from chemistry to cellular interactions.
- Phloretin is a promising anticancer therapeutic agent.
- Phloretin suppresses metastasis by targeting protease and inhibits cancer stemness and angiogenesis in human cervical cancer cells.
- Phloretin from crab-apple showed significant positive anticancer activities against several human cancer cell lines.
- Phloretin has possible chemopreventive role in which modulating the antioxidant and detoxification enzyme status.
- A review of the induced cytoprotective effects of Phloretin on mammalian cells.
- Phloretin can enhance the killing effect of γδ T cells on SW-1116 cells.
- Phloretin exhibits an anticancer effect and enhances the anticancer ability of cisplatin on non-small cell lung cancer cell lines.
- Phloretin (Ph), a natural product found in apples and pears, inhibits liver cancer cells.
- Phloretin is able to inhibit NSCLC A549 cell growth by inducing apoptosis.
- Phloretin inhibits phorbol ester-induced tumor promotion and expression of cyclooxygenase-2 in mouse skin.
- The combination of HSP70 with phloretin could be a novel treatment for efficient immunotherapy of intractable cancers such as skin melanoma.
- The apple polyphenol phloretin inhibits colorectal cancer cell growth.
- Apple polyphenol phloretin complexed with ruthenium is capable of reprogramming the breast cancer microenvironment.
- Phloretin induces G2/M arrest and apoptosis by suppressing the β-catenin signaling pathway in colorectal carcinoma cells.
BPH
- Phloretin ameliorates testosterone-induced benign prostatic hyperplasia.
- Phloretin in benign prostate hyperplasia and prostate cancer.
Cardiovascular
- The flavonoid phloretin suppresses stimulated expression of endothelial adhesion molecules and reduces activation of human platelets
- Phloretin would be a potent agent preventing thrombosis and atherosclerosis.
- Phloretin may have potential as a treatment against atherosclerosis and restenosis after vascular injury.
- Phloretin alleviates arsenic trioxide-induced apoptosis of H9c2 cardiomyoblasts.
Cerebrovascular
COPD
Depression
Diabetes
- Phloretin is a strong α-glucosidase inhibitor, thus could be contribute to the improvement of diabetes mellitus.
- Phloretin either alone or in combination with duloxetine alleviates the STZ-induced diabetic neuropathy in rats
Hepatoprotective
- Phloretin has hepatoprotective effects in mice.
- Phloretin attenuation of hepatic steatosis via an improvement of mitochondrial dysfunction.
Immunosuppressive
Insulin Sensitivity / Insulin Resistance
- Phloretin and phloridzin improve insulin sensitivity and enhance glucose uptake.
- Phloretin might be able to increase insulin sensitivity and alleviate the metabolic diseases
- Phloretin and phlorizin mitigates inflammatory stress and alleviate adipose and hepatic insulin resistance.
Neuroprotective
- Phloretin attenuates behavior deficits and neuroinflammatory response in MPTP induced Parkinson's disease in mice.
- The effect of phloretin on synaptic proteins and adult hippocampal neurogenesis in Aβ (1-42)-injected male Wistar rats
- Neuroprotective effect of phloretin in rotenone-induced mice model of Parkinson's disease.
- Phloretin enhances remyelination by stimulating oligodendrocyte precursor cell differentiation.
Obesity / Overweight
Osteoarthritis
Osteopenia/Osteoporosis
- Phloretin was effective in preventing estrogen deficiency-induced osteoclastogenic resorption.
- Phloretin may be a potential therapeutic agent targeting osteoclast differentiation and bone resorption in skeletal diseases such as osteoporosis.
Nootropic / Neuroprotective
- Phloretin has nootropic, neuroprotective and neurotrophic activities in scopolamine induced memory impaired mice.
- Phloretin has neuroprotective effects on rotenone-induced toxicity in human SH-SY5Y neuronal-like cells.