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Phloretin Antioxidant in Apple Foliage

Phloretin Antioxidant in Apple Foliage

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Published by Rama Shakti
Phloretin Antioxidant in Apple Foliage
Phloretin Antioxidant in Apple Foliage

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Published by: Rama Shakti on Dec 25, 2013
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02/02/2014

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Phloretin
Phloretin is a plant-derived dihydrochalcone polyphenol primarily found in various species of apple (J. Nutr. 2005;1351!2-"# reportedly capa$le of demonstratin% antio&idant activity'.his flavonoid e&hi$its potent antio&idant activity in pero&ynitrite scaven%in% and in the suppression of lipid pero&idation ()iochem. )iophys. *es. +ommun. 2002;2,5,-13#. lon% ith its %lucoside phlorid/in' phloretin is $elieved to $e an important contri$utor to the health $enefits of apples (J. %ric. ood +hem. 2003;513!-53#.Phloretin also has $een identified in tomatoes' and is considered an important source of dietary flavonoids (J. %ric. ood +hem. 200";523-1#. n addition' it as once used as a su$stitute for 4uinine.*esearch on the potential cutaneous $enefits of phloretin $e%an more than 20 years a%o' hen to $otanically derived flavonoids - phloretin and the structurally related compound nordihydro%uaiaretic acid - ere found to stron%ly inhi$it eratinocyte %roth. he investi%ators su%%ested that the compounds $e considered antipsoriatic a%ents (nt. J. 6ermatol. 1,"!;20-#.
Heightened Permeation
Nine years a%o' phloretin as evaluated for its potential to enhance the transdermal penetration of lidocaine hydrochloride. nvesti%ators treated e&cised human sin samples ith a methanolic solution of phloretin 12 hours $efore lidocaine application' at p7 .0 and !.0. t a p7 of .0' a 3.2-fold increase in total permeation as seen' compared ith control samples after 2 hours.n a su$se4uent test' unilamellar phosphatidylcholine liposomes ere used as a vehicle for phloretin' and a 5.-fold %reater permeation of lidocaine as o$served in pretreated sin' compared ith control sin after 2 hours. he investi%ators concluded that phloretin indeed demonstrated potential as a transdermal penetration enhancer for lidocaine (J. Pharm. 8ci. 2001;,0"5-,2#.n 2003' uner et al. shoed that permeation of porcine sin ith phloretin and -etocholestanol prior to treatment ith 5-aminolevulinic acid increased acid diffusion (the permeation of hich as enhanced $y cetylpyridinium chloride and $en/alonium chloride# at p7 !.0 appro&imately 1.!-fold (nt. J. Pharm. 2003;25510,-1#.n an e&periment also pu$lished in 2003' the same team studied the same compounds - phloretin and -etocholestanol included in unilamellar liposomes - for their via$ility in enhancin% the transport of sodium fluorescein across rat' porcine' and human sin. Phloretin as found to have a si%nificant positive effect on sodium fluorescein diffusion in rat and porcine sin after 30 hours $ut no influence on human sin as compared to control' hereas -etocholestanol e&hi$ited a positive effect on all sin types (J. +ontrol. *elease 2003;",321-"#.
 
)y usin% various methods to evaluate mem$rane interactions' some of the same investi%ators su$se4uently determined that phloretin and -etocholestanol interact ith the lipid layer and alter the structure' renderin% a %reater fluidity in the mem$rane (9ur. J. Pharm. )iopharm. 200;5!32,-3#.n the same issue of the 9uropean Journal of Pharmaceutics and )iopharmaceutics in hich these findin%s ere pu$lished' uner and :alenta pu$lished a study on the effects of phloretin on the topical permeation of lidocaine usin% one hydrophilic and three lipophilic delivery systems. he researchers conducted standard diffusion e&periments ith ran/ diffusion cells throu%h porcine sin' and found that phloretin enhanced lidocaine permeation 1.3,-fold in the hydrophilic formulation and 1.25- to 1.!-fold in the lipophilic formulations (9ur. J. Pharm. )iopharm. 200;5!30!-12#.ore recently' uner et al. shed li%ht on the mechanisms of action of phloretin and -etocholestanol. n increase in intercellular lipid $ilayer fluidity in the stratum corneum is thou%ht to confer the o$served penetration-enhancin% effects associated ith these compounds. 9valuation of the effects of these compounds on phase transition and enthalpy revealed that $oth compounds decrease the diffusional resistance of the stratum corneum to dru%s ith a hydrophilic-lipophilic e4uili$rium (nt. J. Pharm. 2005;2,1,-55#.
Antioxidant Actions
*esearchers evaluated the contri$ution of the ma<or phenolic phytochemicals in apples to the total antio&idant capacity of the fruit usin% a 2'2=-a/ino-$is(3-ethyl$en/othia/oline--sulfonic acid# radical scaven%in% assay. hey found a linear relationship $eteen phenolic concentration and total antio&idant activity' and estimated that the %reatest phenolic contri$ution to the total antio&idant capacity of apples as derived from 4uercetin' folloed in order $y epicatechin' procyanidin )(2#' phloretin' and chloro%enic acid' ith the contri$ution from vitamin + fallin% <ust ahead of that of phloretin (J. %ric. ood +hem. 2003;5151-20#.Phloretin has also recently $een studied in a com$ination solution. n a paper no under revie for pu$lication' >resa%o et al. evaluated the effects of a topical antio&idant formulation containin% phloretin' vitamin +' and ferulic acid in miti%atin% ultraviolet (?:#-induced harm. )iomarers of cutaneous dama%e' includin% the formation of sun$urn cells and thymine dimers' and the e&pression of matri& metalloproteinase-, and p53' ere assessed in 10 normal healthy volunteers. Pretreatment ith the antio&idant mi&ture effectively inhi$ited the deleterious effects of ?: irradiation and also prevented ?: e&posure from inducin% immunosuppressive effects.he investi%ators concluded that the dual role of phloretin' as a stron% antio&idant and penetration enhancer' helps to au%ment the availa$ility of the other antio&idants to the sin (>resa%o +' et al. Photoprotective effects of a topical antio&idant mi&ture containin% vitamin +' ferulic acid' and phloretin a%ainst ?:-induced o&idative stress in human sin. 8u$mitted for pu$lication' 2010#.
Skin Care Potential
n 200!' @in et al. isolated and identified 13 compounds from the ormosan apple (alus doumeri var. formosana#' a native aianese $otanical. he compounds' hich included 3-hydro&yphloretin' demonstrated potent antio&idant and cellular tyrosinase-reducin% activities in human epidermal melanocytes.
 
n addition' 3-hydro&yphloretin as found to $e one of the to most active constituents' alon% ith catechol' also e&hi$itin% activity as a competitive inhi$itor in a inetic analysis of mushroom tyrosinase. he investi%ators concluded that $oth compounds have potential as cosmetic a%ents (Phytochemistry 200!;"11",-,,#. he tyrosinase-reducin% activities of phloretin also su%%est intri%uin% potential as a sin-li%htenin% a%ent.8everal of the same investi%ators previously reported on seven phenolic compounds isolated from the ormosan apple that ere assessed for their potential application in sin care. he researchers found that the compounds 3-hydro&yphlorid/in' 3-hydro&yphloretin' and 4uercetin shoed the most potent free radical-scaven%in% properties a%ainst 1'1-diphenyl-2-picrylhydra/yl (6PP7# and supero&ide radicals. he phloretin compounds (phlorid/in is the %lucosidic form# also e&hi$ited inhi$itory activity a%ainst &anthine o&idase and elastase.n addition' these compounds inhi$ited matri& metalloproteinase-1 synthesis in human fi$ro$last cells. he results are si%nificant $ecause these en/ymes $rea don ey dermal constituents' contri$utin% to cutaneous a%in%. he team concluded that the phloretin e&tracts as ell as 4uercetin sho potential for use in antia%in% or other cosmetic formulations ()iol. Pharm. )ull. 200;2,!0-5#.ore recently' investi%ators e&amined the phytochemicals in apples and apple <uices to ascertain the compounds= relative contri$utions to potential chemopreventive properties. he researchers fractionated a polyphenol-enriched apple <uice e&tract and measured antio&idant effects' modulation of carcino%en meta$olism' anti-inflammatory and antihormonal activities' and antiproliferative potential. Phloretin and epicatechin ere identified as the stron%est inhi$itors of cycloo&y%enase-1' hich could contri$ute to an anti-inflammatory effect (ol. Nutr. ood *es. 200";52(81#82"-8#. he researchers concluded that the com$ination of various constituents e&hi$itin% complementary properties may lead to increased total chemopreventive $enefits.Nota$ly' phloretin has also $een found to inhi$it the %roth of several cancer cells and to induce apoptosis of )1 melanoma' 7@0 human leuemia cells' and 7-2, human colon cancer cells. n an investi%ation of the effects of the flavonoid on human colon cancer cells' Par et al. speculated that the inhi$itory effects may $e mediated via mitochondrial mem$rane permea$ility alterations and activation of caspase pathays (J. ed. ood 200!;105"1-#.
Conclusions
he 4uantity of research thus far conducted on phloretin' a phenolic compound found most a$undantly in various species of apples and pears' is relatively modest. Nevertheless' evidence su%%ests that phloretin e&hi$its antio&idant activity and e&erts a potentially si%nificant influence on the sin' particularly in enhancin% the permeation of other in%redients.lthou%h much more research is necessary' particularly randomi/ed controlled trials' this $otanical in%redient is an intri%uin% addition to the ever-e&pandin% roster of naturally derived in%redients ith the potential to impart si%nificant health $enefits to the sin. t is found in Phloretin + (8in+euticals nc.#.

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