Phloridzin, a natural hydoxychalcone constituent obtained from fruit trees is an antidiabetic and antineoplastic agent. Phloridzin was first isolated, for clinical pharmaceutical usage, from the pear tree bark of <i>Pyrus communis</i> in 1838 as the first sodium-glucose linked transport 2 (SGLT2) inhibitor. Additionally, phloridzin is also reported to have antineoplastic activity. Phloridzin had to take an exit from the pharmaceutical market due to its side effects and poor bioavailability when compared to other antidiabetic drug competitors. This limit of phloridzin’s bioavailability is primary attributed to the degradation of the glyosidic bond of the drug to result in the formation of phloretin, the aglycone of pholoridzin. Phloretin displays a reduced capacity of SGLT2 inhibition, however this nutraceutical displays enhanced antineoplastic activity in comparison to phloridzin. Gold nanoparticles (AuNPs) have been studied for drug delivery applications for poorly bioavailable drugs. Hence, in order to tackle the bioavailability of these hydroxychalcones and study the unknown anticancer mechanism, we synthesized phloridzin and phloretin conjugated gold nanoparticles (Phl-AuNP and Pht-AuNP) in single step, rapid, biofriendly processes. The synthesized AuNPs morphology was characterized via transmission electron microscopy and UV-Vis spectroscopy. The presence of phloridzin or phloretin was confirmed using SEM-EDS. The percentage of organic component (phloridzin/phloretin) onto AuNPs surface was characterized using TGA. Assessment of the antineoplastic potency of the hydroxylchalcone conjugated AuNPs against cancerous cell lines was accomplished through monitoring via flow cytometry. We hypothesize that functionalization of these chalcones onto the gold nanoparticles’ surface may improve the pharmacokinetic profile of phloridzin and phloretin.

Novel self-patented gold nanoparticles for antineoplastic activity

251st National Meeting (2016)

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