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Phloretin, as a Potent Anticancer Compound: From Chemistry to Cellular Interactions

Phloretin is a natural dihydrochalcone found in many fruits and vegetables, especially in apple tree leaves and the Manchurian apricots, exhibiting several therapeutic properties, such as antioxidant, antidiabetic, anti-inflammatory, and antitumor activities. In this review article, the diverse aspe...

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Autores principales: Tuli, Hardeep Singh, Rath, Prangya, Chauhan, Abhishek, Ramniwas, Seema, Vashishth, Kanupriya, Varol, Mehmet, Jaswal, Vivek Sheel, Haque, Shafiul, Sak, Katrin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9787340/
https://www.ncbi.nlm.nih.gov/pubmed/36557950
http://dx.doi.org/10.3390/molecules27248819
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author Tuli, Hardeep Singh
Rath, Prangya
Chauhan, Abhishek
Ramniwas, Seema
Vashishth, Kanupriya
Varol, Mehmet
Jaswal, Vivek Sheel
Haque, Shafiul
Sak, Katrin
author_facet Tuli, Hardeep Singh
Rath, Prangya
Chauhan, Abhishek
Ramniwas, Seema
Vashishth, Kanupriya
Varol, Mehmet
Jaswal, Vivek Sheel
Haque, Shafiul
Sak, Katrin
author_sort Tuli, Hardeep Singh
collection PubMed
description Phloretin is a natural dihydrochalcone found in many fruits and vegetables, especially in apple tree leaves and the Manchurian apricots, exhibiting several therapeutic properties, such as antioxidant, antidiabetic, anti-inflammatory, and antitumor activities. In this review article, the diverse aspects of the anticancer potential of phloretin are addressed, presenting its antiproliferative, proapoptotic, antimetastatic, and antiangiogenic activities in many different preclinical cancer models. The fact that phloretin is a planar lipophilic polyphenol and, thus, a membrane-disrupting Pan-Assay Interference compound (PAIN) compromises the validity of the cell-based anticancer activities. Phloretin significantly reduces membrane dipole potential and, therefore, is expected to be able to activate a number of cellular signaling pathways in a non-specific way. In this way, the effects of this minor flavonoid on Bax and Bcl-2 proteins, caspases and MMPs, cytokines, and inflammatory enzymes are all analyzed in the current review. Moreover, besides the anticancer activities exerted by phloretin alone, its co-effects with conventional anticancer drugs are also under discussion. Therefore, this review presents a thorough overview of the preclinical anticancer potential of phloretin, allowing one to take the next steps in the development of novel drug candidates and move on to clinical trials.
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spelling pubmed-97873402022-12-24 Phloretin, as a Potent Anticancer Compound: From Chemistry to Cellular Interactions Tuli, Hardeep Singh Rath, Prangya Chauhan, Abhishek Ramniwas, Seema Vashishth, Kanupriya Varol, Mehmet Jaswal, Vivek Sheel Haque, Shafiul Sak, Katrin Molecules Review Phloretin is a natural dihydrochalcone found in many fruits and vegetables, especially in apple tree leaves and the Manchurian apricots, exhibiting several therapeutic properties, such as antioxidant, antidiabetic, anti-inflammatory, and antitumor activities. In this review article, the diverse aspects of the anticancer potential of phloretin are addressed, presenting its antiproliferative, proapoptotic, antimetastatic, and antiangiogenic activities in many different preclinical cancer models. The fact that phloretin is a planar lipophilic polyphenol and, thus, a membrane-disrupting Pan-Assay Interference compound (PAIN) compromises the validity of the cell-based anticancer activities. Phloretin significantly reduces membrane dipole potential and, therefore, is expected to be able to activate a number of cellular signaling pathways in a non-specific way. In this way, the effects of this minor flavonoid on Bax and Bcl-2 proteins, caspases and MMPs, cytokines, and inflammatory enzymes are all analyzed in the current review. Moreover, besides the anticancer activities exerted by phloretin alone, its co-effects with conventional anticancer drugs are also under discussion. Therefore, this review presents a thorough overview of the preclinical anticancer potential of phloretin, allowing one to take the next steps in the development of novel drug candidates and move on to clinical trials. MDPI 2022-12-12 /pmc/articles/PMC9787340/ /pubmed/36557950 http://dx.doi.org/10.3390/molecules27248819 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Tuli, Hardeep Singh
Rath, Prangya
Chauhan, Abhishek
Ramniwas, Seema
Vashishth, Kanupriya
Varol, Mehmet
Jaswal, Vivek Sheel
Haque, Shafiul
Sak, Katrin
Phloretin, as a Potent Anticancer Compound: From Chemistry to Cellular Interactions
title Phloretin, as a Potent Anticancer Compound: From Chemistry to Cellular Interactions
title_full Phloretin, as a Potent Anticancer Compound: From Chemistry to Cellular Interactions
title_fullStr Phloretin, as a Potent Anticancer Compound: From Chemistry to Cellular Interactions
title_full_unstemmed Phloretin, as a Potent Anticancer Compound: From Chemistry to Cellular Interactions
title_short Phloretin, as a Potent Anticancer Compound: From Chemistry to Cellular Interactions
title_sort phloretin, as a potent anticancer compound: from chemistry to cellular interactions
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9787340/
https://www.ncbi.nlm.nih.gov/pubmed/36557950
http://dx.doi.org/10.3390/molecules27248819
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