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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. 0ood +hem. 2003;51 132!-53#. Phloretin also has $een identified in tomatoes' and is considered an important source of dietary flavonoids (J. -%ric. 0ood +hem. 200";51 223121#. 3n addition' it .as once used as a su$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 5eratinocyte %ro.th. (he investi%ators su%%ested that the compounds $e considered antipsoriatic a%ents (3nt. J. 6ermatol. 1,"!;21 110-1#.
Nine years a%o' phloretin .as evaluated for its potential to enhance the transdermal penetration of lidocaine hydrochloride. 3nvesti%ators treated e&cised human s5in samples .ith a methanolic solution of phloretin 12 hours $efore lidocaine application' at p7 2.0 and !.0. -t a p7 of 2.0' a 3.2-fold increase in total permeation .as seen' compared .ith control samples after 22 hours.
3n a su$se4uent test' unilamellar phosphatidylcholine liposomes .ere used as a vehicle for phloretin' and a 5.2-fold %reater permeation of lidocaine .as o$served in pretreated s5in' compared .ith control s5in after 22 hours. (he investi%ators concluded that phloretin indeed demonstrated potential as a transdermal penetration enhancer for lidocaine (J. Pharm. 8ci. 2001;,0 2"5-,2#.
3n 2003' -uner et al. sho.ed that permeation of porcine s5in .ith phloretin and 1-5etocholestanol prior to treatment .ith 5-aminolevulinic acid increased acid diffusion (the permeation of .hich .as enhanced $y cetylpyridinium chloride and $en/al5onium chloride# at p7 !.0 appro&imately 1.!-fold (3nt. J. Pharm. 2003;255 10,-11#.
3n an e&periment also pu$lished in 2003' the same team studied the same compounds - phloretin and 1-5etocholestanol included in unilamellar liposomes - for their via$ility in enhancin% the transport of sodium fluorescein across rat' porcine' and human s5in. Phloretin .as found to have a si%nificant positive effect on sodium fluorescein diffusion in rat and porcine s5in after 30 hours $ut no influence on human s5in as compared to control' .hereas 1-5etocholestanol e&hi$ited a positive effect on all s5in 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 1-5etocholestanol interact .ith the lipid layer and alter the structure' renderin% a %reater fluidity in the mem$rane (9ur. J. Pharm. )iopharm. 2002;5! 32,31#.
3n the same issue of the 9uropean Journal of Pharmaceutics and )iopharmaceutics in .hich these findin%s .ere pu$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 0ran/ diffusion cells throu%h porcine s5in' and found that phloretin enhanced lidocaine permeation 1.3,-fold in the hydrophilic formulation and 1.25- to 1.!1-fold in the lipophilic formulations (9ur. J. Pharm. )iopharm. 2002;5! 30!-12#.
;ore recently' -uner et al. shed li%ht on the mechanisms of action of phloretin and 1-5etocholestanol. -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 (3nt. J. Pharm. 2005;2,2 12,-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-1-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. 0ood +hem. 2003;51 1511-20#.
Phloretin has also recently $een studied in a com$ination solution. 3n a paper no. under revie. for pu$lication' >resa%o et al. evaluated the effects of a topical antio&idant formulation containin% phloretin' vitamin +' and ferulic acid in miti%atin% ultraviolet (?:#-induced harm. )iomar5ers of cutaneous dama%e' includin% the formation of sun$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 s5in (>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 s5in. 8u$mitted for pu$lication' 2010#.
Skin Care Potential 3n 200!' @in et al. isolated and identified 13 compounds from the 0ormosan 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.
3n 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 5inetic analysis of mushroom tyrosinase. (he investi%ators concluded that $oth compounds have potential as cosmetic a%ents (Phytochemistry 200!;1" 11",-,,#. (he tyrosinase-reducin% activities of phloretin also su%%est intri%uin% potential as a s5in-li%htenin% a%ent.
8everal of the same investi%ators previously reported on seven phenolic compounds isolated from the 0ormosan apple that .ere assessed for their potential application in s5in care. (he researchers found that the compounds 3-hydro&yphlorid/in' 3-hydro&yphloretin' and 4uercetin sho.ed the most potent free radical-scaven%in% properties a%ainst 1'1-diphenyl-2-picrylhydra/yl (6PP7# and supero&ide radicals. (he phloretin compounds (phlorid/in is the %lucosidic form# also e&hi$ited inhi$itory activity a%ainst &anthine o&idase and elastase.
3n addition' these compounds inhi$ited matri& metalloproteinase-1 synthesis in human fi$ro$last cells. (he results are si%nificant $ecause these en/ymes $rea5 do.n 5ey dermal constituents' contri$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. 2001;2, !20-5#.
;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. 0ood *es. 200";52(81# 82"-822#. (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 )11 melanoma' 7@10 human leu5emia cells' and 7(-2, human colon cancer cells. 3n an investi%ation of the effects of the flavonoid on human colon cancer cells' Par5 et al. speculated that the inhi$itory effects may $e mediated via mitochondrial mem$rane permea$ility alterations and activation of caspase path.ays (J. ;ed. 0ood 200!;10 5"1-1#.
Conclusions (he 4uantity of research thus far conducted on phloretin' a phenolic compound found most a$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 s5in' 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 $enefits to the s5in. 3t is found in Phloretin +0 (85in+euticals 3nc.#.
Dr. Baumann writes the "Cosmeceutical Critique" column, which appears regularly in Skin & Allergy News, an Else ier pu!lication. Dr. Baumann is in pri ate practice in "iami Beach. #o respon$ to this column, or to suggest topics %or %uture columns, write to her at sknews&else ier.com.
Derived from apples and the root bark of fruit trees including apple, pear, and grapefruit, phloretin is a broad- spectrum molecule newly identified for its antioxidant properties and recently studied for use as a pigment- regulating and penetrationenhancing agent in the medical community. Classified as a special family of flavonoids called dihydrochalcones, phloretin’s unique carbonyl structure is responsible for particularly potent antioxidant activity in peroxynitrite scavenging and in the inhibition of lipid peroxidation. dditionally, it displays a wide range of bioactivities such as anticancer, antifungal, antibacterial, antiviral, and anti-inflammatory. !hloretin C" represents a new class of preventive and corrective topical antioxidant treatment. #his patent- pending breakthrough technology combines the broad-range power of phloretin with vitamin C and ferulic acid in a synergistic biodiverse formulation to divide and conquer sources of damage at every level of the skin. !hloretin C" is a broad-spectrum treatment that protects against not only free radicals, but the range of other reactive molecules known to cause damage and D$ mutations among the integral cell types. %n addition to preventing photodamage, it corrects existing damage by stimulating the synthesis of essential proteins and fibers and accelerating cell turnover. #he result & a strengthened support structure on the inside and a more youthful, firm, radiant appearance on the outside. 'enefits( )ynergistic ntioxidant Combination * 'road-)pectrum "ormulation prevents premature signs of aging and corrects existing photodamage, especially age spots and laxity divides and conquers the range of reactive oxygen species +,-). throughout the skin facilitates cellular repair and maintains cell diversity reconstructs the skin’s support structure boosts skin’s natural immunity against D$ impairment to preserve cellular integrity and help prevent serious skin
conditions like skin cancer provides significantly better results than any one antioxidant alone properly formulated with optimal concentrations at the precise p/ to ensure maximum bioavailiability 01 !hloretin 2 neutrali3es free radicals and suppresses radiation-induced oxidative reactions 2 accelerates cell turnover 2 inhibits 45-induced melanogenesis 671 8- scorbic cid 2 neutrali3es free radicals and suppresses radiation-induced oxidative reactions 2 prevents 45 immunosuppression 2 promotes collagen synthesis 7.91 "erulic cid 2 neutrali3es free radicals and suppresses radiation-induced oxidative reactions 2 inhibits 45-induced melanogenesis 4sage ,ecommendations 2 hyperpigmentation 2 erythema 2 uneven skin tone 2 loss of elasticity 2 mottled appearance 2 photodamaged skin -nce daily using fingertips, apply :-9 drops of !hloretin C"#; to face, neck, and chest.
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Phloretin is a dihydrochalcone, a type of natural phenols. It can be found in apple tree
leaves. Phloretin inhibits the active transport of glucose into cells by SGLT1 and SGLT2, though the inhibition is wea er than by its glycoside phlori!in."2# $rally consu%ed phlori!in is nearly entirely converted into phloretin by hydrolytic en!y%es in the s%all intestine."&#"'# (n i%portant effect of this is the inhibition of glucose absorption by the s%all 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 GL+T2.
Phloretin hydrolase uses phloretin and water to produce phloretate and phloroglucinol
, , Phlori!in is the 2-.glucoside of phloretin. /aringin dihydrochalcone is a diglycoside of phloretin
Jump up ^ Picinelli (.0 1apena 2.0 3angas 4. 4. 5166)7. 8Polyphenolic pattern in apple tree leaves in relation to scab resistance. ( preli%inary study8. Journal of Agricultural and Food Chemistry 43 597: 22;&<22;9. doi:1=.1=21>?f===)*a=);. Jump up ^ @han, Stephen S.0 Aillia% 1. Lotspeich 516*2.12.=17. 8@o%parative effects of phlori!in and phloretin on glucose transport in the cat idney8. American Journal of Physiology -- Legacy Content 203 5*7: 6;)<6;6. ISS/ ===2.6)1&. Betrieved 2=12.1=.21.
C 4u%p up to: a b Idris, I.0 1onnelly, B. 52==67. 8Sodiu%.glucose co.transporter.2 inhibitors: (n e%erging new class of oral antidiabetic drug8. Diabetes, Obesity and Metabolism 11 527: ;6. doi:1=.1111>?.1'*&.1&2*.2==9.==692.D. edit C 4u%p up to: a b @respy, E.0 (pri ian, $.0 3orand, @.0 Fesson, @.0 3anach, @.0 1e%ignG, @.0 BG%Gsy, @. 52==17. 8Fioavailability of phloretin and phlorid!in in rats8. The Journal of nutrition 131 5127: &22;<&2&=. P3I1 11;&69;1. edit Jump up ^ Henton, Bobert (.0 @hung.Lin @hou, Gavin S. Stewart, @raig P. S%ith, 3ar (. Inepper 52=='.=).117. 8+rinary concentrating defect in %ice with selective deletion of phloretin.sensitive urea transporters in the renal collecting duct8. Proceedings of the ational Academy of !ciences of the "nited !tates of America 101 5167: ;'*6<;';'. doi:1=.1=;&>pnas.='=1;='1=1. ISS/ ==2;.9'2'. Betrieved 2=12.1=.21.
Jump up ^ Shaya ul, @hairat0 Jiroyasu Tsu aguchi, +rs E. Ferger, 3atthias (. Jediger 52==1.=&.=17. 83olecular characteri!ation of a novel urea transporter fro% idney inner %edullary collecting ducts8. American Journal of Physiology - #enal Physiology 280 5&7: <'9;<H'6'. ISS/ 16&1.9);K. Betrieved 2=12.1=.21. /wiki/Help:CS1_errors
Glycosylcera%idase Hro% Ai ipedia, the free encyclopedia 5Bedirected fro% Phloretin.glucosidase7 In en!y%ology, a lycosylceramidase 52@ &.2.1.*27 is an en!y%e that cataly!es the che%ical reaction glycosyl./.acylsphingosine L J2$ /.acylsphingosine L a sugar Thus, the two substrates of this en!y%e are glycosyl./.acylsphingosine and J2$, whereas its two products are /.acylsphingosine and sugar. This en!y%e belongs to the fa%ily of hydrolases, specifically those glycosidases that hydrolyse $. and S.glycosyl co%pounds. The syste%atic na%e of this en!y%e class is lycosyl!"! acylsphin osine lycohydrolase. $ther na%es in co%%on use include phlori#in hydrolase, phloretin! lucosidase, lycosyl ceramide lycosylhydrolase, cerebrosidase, phlorid#in beta! lucosidase, lactase!phlori#in hydrolase, and phlorid#in lucosidase. References$edit% , Leese J4, Se%en!a G 516;&7. 8$n the identity between the s%all intestinal en!y%es phlori!in hydrolase and glycosylcera%idase8. J$ %iol$ Chem$ 248 52&7: 91;=<&. P3I1 ';)26'6. Loren!.3eyer J, Flu% (L, Jae%%erli JP, Se%en!a G 516;27. 8( second en!y%e defect in acMuired lactase deficiency: lac of s%all.intestinal phlori!in.hydrolase8. &ur$ J$ Clin$ 'n(est$ 2 5)7: &2*<&1. doi:1=.1111>?.1&*).2&*2.16;2.tb==*)9.D. P3I1 )=92=*9. 3alathi P, @rane BI 516*67. 8Phlori!in hydrolase: a beta.glucosidase of ha%ster intestinal brush border %e%brane8. %iochim$ %io)hys$ Acta$ 1&3 527: 2')<)*. P3I1 );;';;).
3!'4!(ydro)y!phenyl*!1!'2+4+ ,!trihydro)y!phenyl*!propan!1!one ! -btained from the decomposition of phlorid#in and used in the treatment of malaria as a .uinine replacer/ 0tudies ha1e sho2n it inhibits protein 3inase 4 and effects the sodium5potassium transfer across membranes/ 6t is found in the root bar3 of apple trees as a lucoside called phlorid#in/ -ne study concerned its effect and treatment of the disease cystic fibrosis7 others pointed to its uses as an anta onist of prosto landins in the reduction of inflammation and eneral s3in disorders/ Phloretin is a dihydrochalcone+ a type of natural phenols/ 6t can be found in apple tree lea1es/$
Phloretin inhibits the active transport of glucose into cells by SGLT1 and SGLT2, though the inhibition is wea er than by its glycoside phlori!in."2# $rally consu%ed phlori!in is nearly entirely converted into phloretin by hydrolytic en!y%es in the s%all intestine."&#"'# (n i%portant effect of this is the inhibition of glucose absorption by the s%all intestine"'# and the inhibition of
renal glucose reabsorption."&# Phloretin also inhibits a variety of urea transporters.")#"*# It induces urea loss and diuresis when coupled with high protein diets.
'road-range antioxidant treatment combining 01 phloretin, 671 8-ascorbic acid, and 7.91 ferulic acid This broad-spectrum treatment provides advanced environmental protection to defend skin against the reactive molecules +including free radicals. that are known to cause cellular damage. %n addition to its superior antioxidant capabilities, it has been proven to correct existing damage from the inside out.
!rovides advanced environmental protection against 45 and 45' radiation )timulates collagen synthesis to improve signs of aging Diminishes hyperpigmentation and accelerates cellular renewal to retexture skin -nce absorbed, this serum can’t be washed or rubbed off. %t remains effective for a minimum of =0 hours, making it an excellent addition to sunscreen.
clinical st !" In#$i$o% Phloretin CF si&ni'icantl" re! ces (ean s n) rn cell co nt $s* place)o when e+pose! to solar#si( late! li&ht* In#$i$o% Phloretin CF pro$i!es a hi&h le$el o' protection a&ainst ,-# in! ce! re!ness when e+pose! to solar#si( late! li&ht* Science .eri$e! 'ro( the )ark o' apple trees% phloretin is a )roa!#spectr ( (olec le newl" i!enti'ie! 'or its antio+i!ant properties an! st !ie! 'or se as a pi&(ent#re& latin& an! penetration#enhancin& a&ent* It also !ispla"s a wi!e ran&e o' )ioacti$it" s ch as anti#cancer% anti#' n&al% anti)acterial% anti#in'la((ator" properties* Inno$ation 1 !hloretin C" protects integral cells responsible for facilitating the skin’s natural repair process and Inno$ation / !hloretin C" stimulates collagen and elastin synthesis to help maintain the integrity of the extra-cellular
matrix. accelerates cell renewal.
In the (ornin& a'ter cleansin&% appl" 0#1 !rops to a !r" 'ace% neck an! chest*
%t is normal for vitamin C products to darken after opening due to air and light exposure. ny change in color does not affect the product>s efficacy.
2e" In&re!ient 1 01 phloretin( $eutrali3es free radicals, accelerates cell turnover and reduces the production of unwanted 2e" In&re!ient / 671 8-ascorbic acid( $eutrali3es free radicals and promotes collagen synthesis. 2e" In&re!ient 3 7.91 ferulic acid( #his plant-based antioxidant neutrali3es free radicals, inhibits 45-induced melanogenesis,
and has anti-inflammatory properties. pigment.
Phloretin, a dihydrochalcone flavonoid
Author(s) ABther, Carola !lace of birth( )premberg 1. Referee !rof. Dr. med. 5. )tangl Further !riv.-Do3. Dr. med. %. -tt Referee(s) !riv.-Do3. Dr. 5. 'Chm Classificatio D67 ;edical sciencesE ;edicine n (DDC) Summary !hloretin, a dihydrochalcone flavonoid, is a plant-derived phytochemical mainly present in apples, especially in the peel. %t has until now been found also in strawberries and tomatoes. !hloretin possess antioxidative properties and act as an antidiabetic agent via inhibition of glucose cotransporter 6. ,ecent epidemiological studies indicate beneficial effects of plant-derived compounds on cardiovascular health. #he generation of reactive oxygen species is closely associated with the development and progression of atherosclerosis. )ince phloretin is reported to promote antioxidative activities, we investigated the effects of phloretin on agonist-induced activation of human blood platelets from healthy volunteers. !hloretin was incubated with whole blood and the expression of A!%%b*%%%a and !-selectin was measured in the flow cytometry. #he results show a reduction on agonist-stimulated ! C-6 activation in a dose dependent manner. #his flavonoid shows no effect on !selectin expression. Demonstrating the functional relevance of this differential regulation in flow cytometry, phloretin reduced also the platelet aggregation via aggregometry. %n summary, our results demonstrate that phloretin diminished activation of human blood platelets by reducing A!%%b*%%%a expression and inhibit platelet aggregation. #hese biological actions may contribute to the observed
protective cardiovascular effect of diet rich in flavonoids.
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