Development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity

Jason N Payne,1,2,* Vivek D Badwaik,3,* Hitesh K Waghwani,2,* Harsh V Moolani,2 Sarah Tockstein,2 David H Thompson,3 Rajalingam Dakshinamurthy1 1Department of Chemistry, Austin Peay State University, Clarksville, TN, USA; 2Department of Chemistry, Western Kentucky University, Bowling Green, KY, USA...

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Autores principales:	Payne JN, Badwaik VD, Waghwani HK, Moolani HV, Tockstein S, Thompson DH, Dakshinamurthy R
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	Gold Nanoparticles Cancer Phloretin Phloridzin Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/b1a38ae7299f4a259ab3bd175ecd70a1
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spelling	oai:doaj.org-article:b1a38ae7299f4a259ab3bd175ecd70a12021-12-02T04:20:41ZDevelopment of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity1178-2013https://doaj.org/article/b1a38ae7299f4a259ab3bd175ecd70a12018-03-01T00:00:00Zhttps://www.dovepress.com/development-of-dihydrochalcone-functionalized-gold-nanoparticles-for-a-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Jason N Payne,1,2,* Vivek D Badwaik,3,* Hitesh K Waghwani,2,* Harsh V Moolani,2 Sarah Tockstein,2 David H Thompson,3 Rajalingam Dakshinamurthy1 1Department of Chemistry, Austin Peay State University, Clarksville, TN, USA; 2Department of Chemistry, Western Kentucky University, Bowling Green, KY, USA; 3Department of Chemistry, Multi-disciplinary Cancer Research Facility, Bindley Bioscience Center, West Lafayette, IN, USA *These authors contributed equally to this work Background: Phloridzin, an antidiabetic and antineoplastic agent usually found in fruit trees, is a dihydrochalcone constituent that has a clinical/pharmaceutical significance as a sodium-glucose linked transport 2 (SGLT2) inhibitor. While the aglycone metabolite of phloridzin, phloretin, displays a reduced capacity of SGLT2 inhibition, this nutraceutical displays enhanced antineoplastic activity in comparison to phloridzin.Purpose: The objective of this study was to develop gold nanoparticle (AuNP) mediated delivery of phloridzin and phloretin and explore their anticancer mechanism through conjugation of the dihydrochalcones and the AuNP cores.Methods: Phloridzin and phloretin conjugated AuNPs (Phl-AuNP and Pht-AuNP) were synthesized in single-step, rapid, biofriendly processes. The synthesized AuNPs morphology was characterized via transmission electron microscopy and ultraviolet-visible spectroscopy. The presence of phloridzin or phloretin was confirmed using scanning electron microscopy-energy dispersive x-ray spectroscopy. The percentage of organic component (phloridzin/phloretin) onto AuNPs surface was characterized using thermogravimetric analysis. Assessment of the antineoplastic potency of the dihydrochalcones conjugated AuNPs against cancerous cell lines (HeLa) was accomplished through monitoring via flow cytometry.Results: The functionalized AuNPs were synthesized via a single-step method that relied only upon the redox potential of the conjugate itself and required no toxic chemicals. The synthesized Phl-AuNPs were found to be in the size range of 15±5 nm, whereas the Pht-AuNP were found to be 8±3 nm, placing both conjugated AuNPs well within the size range necessary for successful pharmaceutical applications. These assays demonstrate a significant increase in the cancerous cell toxicities as a result of the conjugation of the drugs to AuNPs, as indicated by the 17.45-fold increase in the efficacy of Pht-AuNPs over pure phloretin, and the 4.49-fold increase in efficacy of Phl-AuNP over pure phloridzin.Conclusion: We report a simple, biofriendly process using the reducing and capping potential of the dihydrochalcones, phloridzin and phloretin, to synthesize stable AuNPs that have promising futures as potential antineoplastic agents. Keywords: gold nanoparticles, cancer, phloretin, phloridzinPayne JNBadwaik VDWaghwani HKMoolani HVTockstein SThompson DHDakshinamurthy RDove Medical PressarticleGold NanoparticlesCancerPhloretinPhloridzinMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 1917-1926 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	Gold Nanoparticles Cancer Phloretin Phloridzin Medicine (General) R5-920
spellingShingle	Gold Nanoparticles Cancer Phloretin Phloridzin Medicine (General) R5-920 Payne JN Badwaik VD Waghwani HK Moolani HV Tockstein S Thompson DH Dakshinamurthy R Development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity
description	Jason N Payne,1,2,* Vivek D Badwaik,3,* Hitesh K Waghwani,2,* Harsh V Moolani,2 Sarah Tockstein,2 David H Thompson,3 Rajalingam Dakshinamurthy1 1Department of Chemistry, Austin Peay State University, Clarksville, TN, USA; 2Department of Chemistry, Western Kentucky University, Bowling Green, KY, USA; 3Department of Chemistry, Multi-disciplinary Cancer Research Facility, Bindley Bioscience Center, West Lafayette, IN, USA *These authors contributed equally to this work Background: Phloridzin, an antidiabetic and antineoplastic agent usually found in fruit trees, is a dihydrochalcone constituent that has a clinical/pharmaceutical significance as a sodium-glucose linked transport 2 (SGLT2) inhibitor. While the aglycone metabolite of phloridzin, phloretin, displays a reduced capacity of SGLT2 inhibition, this nutraceutical displays enhanced antineoplastic activity in comparison to phloridzin.Purpose: The objective of this study was to develop gold nanoparticle (AuNP) mediated delivery of phloridzin and phloretin and explore their anticancer mechanism through conjugation of the dihydrochalcones and the AuNP cores.Methods: Phloridzin and phloretin conjugated AuNPs (Phl-AuNP and Pht-AuNP) were synthesized in single-step, rapid, biofriendly processes. The synthesized AuNPs morphology was characterized via transmission electron microscopy and ultraviolet-visible spectroscopy. The presence of phloridzin or phloretin was confirmed using scanning electron microscopy-energy dispersive x-ray spectroscopy. The percentage of organic component (phloridzin/phloretin) onto AuNPs surface was characterized using thermogravimetric analysis. Assessment of the antineoplastic potency of the dihydrochalcones conjugated AuNPs against cancerous cell lines (HeLa) was accomplished through monitoring via flow cytometry.Results: The functionalized AuNPs were synthesized via a single-step method that relied only upon the redox potential of the conjugate itself and required no toxic chemicals. The synthesized Phl-AuNPs were found to be in the size range of 15±5 nm, whereas the Pht-AuNP were found to be 8±3 nm, placing both conjugated AuNPs well within the size range necessary for successful pharmaceutical applications. These assays demonstrate a significant increase in the cancerous cell toxicities as a result of the conjugation of the drugs to AuNPs, as indicated by the 17.45-fold increase in the efficacy of Pht-AuNPs over pure phloretin, and the 4.49-fold increase in efficacy of Phl-AuNP over pure phloridzin.Conclusion: We report a simple, biofriendly process using the reducing and capping potential of the dihydrochalcones, phloridzin and phloretin, to synthesize stable AuNPs that have promising futures as potential antineoplastic agents. Keywords: gold nanoparticles, cancer, phloretin, phloridzin
format	article
author	Payne JN Badwaik VD Waghwani HK Moolani HV Tockstein S Thompson DH Dakshinamurthy R
author_facet	Payne JN Badwaik VD Waghwani HK Moolani HV Tockstein S Thompson DH Dakshinamurthy R
author_sort	Payne JN
title	Development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity
title_short	Development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity
title_full	Development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity
title_fullStr	Development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity
title_full_unstemmed	Development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity
title_sort	development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/b1a38ae7299f4a259ab3bd175ecd70a1
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_version_	1718401329106255872

Development of dihydrochalcone-functionalized gold nanoparticles for augmented antineoplastic activity

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