Hauv kev tshawb fawb txog bioactive tshuaj tau los ntawm apples,PhloretinthiabPhlorizin, raws li cov neeg sawv cev ntawm dihydrochalcone tebchaw, tau txais kev saib xyuas thoob plaws hauv zej zog kev tshawb fawb hauv xyoo tas los no. Txawm hais tias ob yam khoom no muaj tib lub hauv paus thiab cov qauv zoo sib xws, lawv muaj qhov sib txawv tseem ceeb hauv kev ua haujlwm lom neeg thiab cov nqi siv.
1. Cov txheej txheem tshuaj sib txawv thiab cov yam ntxwv
1.1 Molecular structural yam ntxwv
PhloretinthiabPhlorizinmuaj kev sib raug zoo hauv cov qauv tshuaj tab sis muaj qhov sib txawv tseem ceeb. Phloretin yog dihydrochalcone flavonoid compound nrog cov qauv molecular yooj yim. Phlorizin yog glucoside ntawm phloretin, uas yog txuas mus rau ib pawg piam thaj ntawm C2 'site ntawm phloretin molecule (cov qauv tseeb yog phloretin 6'-O-glucoside).[1]Qhov sib txawv ntawm cov qauv no txiav txim siab lawv qhov sib txawv ntawm lub cev thiab tshuaj lom neeg: phlorizin muaj cov dej solubility zoo dua vim muaj cov piam thaj hauv cov pab pawg, thaum resveratrol muaj zog lipid solubility.
Kev taw qhia ntawm cov piam thaj molecules tau hloov pauv lub zog physicochemical ntawm cov khoom sib xyaw: qhov hnyav molecular tau nce los ntawm 274.27 mus rau 436.41, lub log P tus nqi txo los ntawm 3.5 mus rau 0.45, thiab cov dej solubility nce los ntawm ze li peb qhov kev txiav txim ntawm qhov ntau.
1.2 Kev sib piv ntawm lub cev thiab tshuaj lom neeg
| Feature | Phloretin | Phlorizin |
| Molecular hnyav | 274.27 g / mol | 436,41 g / mol |
| Dej- soluble | Micro soluble (0.1 mg / ml) | Soluble (50 mg / ml) |
| Log P | 3.5 | 0.45 |
| Kev ruaj ntseg | Sensitivity rau lub teeb thiab kub | kuj ruaj khov |
Nyob rau hauv xyoo tas los no, muaj kev vam meej tseem ceeb hauv kev tshawb fawb biosynthesis. Pab neeg los ntawm Lub Tsev Kawm Ntawv Cotton Research Institute ntawm Suav Academy ntawm Kev Tshawb Fawb Txog Kev Ua Liaj Ua Teb tau txheeb xyuas cov noob tseem ceeb GhUGT88F3, uas tswj cov biosynthesis ntawmphlorizin uanyob rau hauv upland paj rwb, thiab elucidated nws molecular mechanism ntawm converting phlorizin los ntawm glycosylation tshuaj. Kev tshawb fawb tau txheeb xyuas phloretin-2'-O-glycosyltransferase (P2'GT) hauv txiv apples raws li tus nqi txwv enzyme rau phlorizin biosynthesis. Nyob rau hauv lub xub ntiag ntawm uridine diphosphate qabzib, nws muaj peev xwm tshwj xeeb catalyze cov tshuaj tiv thaiv glycosylation ntawm C2 'txoj hauj lwm ntawm phloretin los tsim phlorizin.[2]
2. Phloretin vs. Phlorizin: Yuav Ua Li Cas Lawv Cov Kev Ua Si lom neeg thiab cov txheej txheem sib txawv?
2.1 Absorption thiab Metabolic Dynamics
Phlorizin yog nqus los ntawm sodium -dependent glucose transporter protein (SGLT1) ntawm cov kab mob hauv plab hnyuv me, txheej txheem nyob ntawm nws cov piam thaj moieties. Cov yam ntxwv no tom qab ncaj qha mus rau kev txhim kho ntawm SGLT2 inhibitor chav kawm cov tshuaj hypoglycemic. Lub nqus mechanism ntawm phloretin yog txawv kiag li. Raws li hydrophobic glycoside, nws tuaj yeem cuam tshuam thoob plaws cell membranes, ua rau lub qhov ncauj bioavailability siab. Txawm li cas los xij, nws dhau mus rau theem II cov metabolism hauv lub cev, feem ntau tsim cov khoom glucuronidation thiab sulfation.
2.2 Pharmacological kev sib piv
(1) Antioxidant kev ua haujlwm
Ob leegphloretin thiab phlorizinqhia txog kev ua haujlwm antioxidant tseem ceeb, txawm tias lawv txawv ntawm lawv cov txheej txheem thiab lub zog. Ib txoj kev tshawb fawb sib piv cov tshuaj tiv thaiv antioxidant ntawm tsib lub ntuj polyphenols pom tias phloretin tau pom tias muaj kev ua tau zoo hauv DPPH radical scavenging, ABTS radical scavenging, thiab hlau ion txo kev soj ntsuam. Nyob rau hauv sib piv, qhov ncaj qha antioxidant peev xwm ntawm resveratrol kuj tsis muaj zog.[3]Txawm hais tias resveratrol nws tus kheej tau txwv cov kev ua haujlwm antioxidant ncaj qha, nws tuaj yeem ua rau hydrolyzed los ntawm plab microbiota rau hauv cov metabolites uas tsis ncaj qha rau cov tshuaj tiv thaiv antioxidant thiab tiv thaiv - cov teebmeem inflammatory.
Ob lub tebchaw qhib lub cellular Nrf2 / HO-1 antioxidant txoj hauv kev, txo qis hauv cov cellular reactive oxygen hom (ROS), tsub kom glutathione (GSH) qib, thiab pab txhawb kev ua haujlwm antioxidant.[4] Txawm li cas los xij, kev sim molecular docking tau qhia tias phloretin khi rau qhov kev hloov pauv Nrf2 nrog lub zog qis dua thiab muaj kev ruaj ntseg ntau dua li phlorizin, qhia tias muaj zog antioxidant zog.
(2) Kev ua haujlwm hypoglycemic
Ob leegphloretin thiab phlorizinpom muaj cov teebmeem hypoglycemic, txawm tias los ntawm cov txheej txheem sib txawv.Phlorizinua raws li lub zog uas tsis yog - xaiv kev sib tw SGLT inhibitor, nrog Ki qhov txiaj ntsig ntawm 300 nM rau hSGLT1 thiab 39 nM rau hSGLT2. Nws sib tw nrog D-glucose rau kev khi rau SGLT1 thiab SGLT2 thauj khoom, yog li txo qis lub raum qabzib reabsorption thiab txo qis cov ntshav qabzib. Txawm hais tias phloretin kuj qhia tau tias muaj cov nyhuv hypoglycemic nruab nrab, nws cov txheej txheem yog ntau ntau, suav nrog kev txhim kho insulin rhiab heev thiab kev tiv thaiv ntawm pancreatic beta hlwb.
(3) Kev ua kom tawv nqaij dawb
Phloretinyog dav lees paub tias yog ib qho zoo tyrosinase inhibitor, txhawb cov shedding ntawm melanocytes, fading me ntsis, thiab brightening ntawm daim tawv nqaij laus. Nws lub zog inhibitory ntawm tyrosinase yog ntau tshaj 50 npaug ntawm phlorizin. Cov txheej txheem ntawm kev ua muaj xws li: ncaj qha inhibition ntawm tyrosinase kev ua, inhibition ntawm tyrosinase noob qhia, thiab inhibition ntawm superoxide dawb radical ntau lawm.
Cov tsis muaj zog whitening nyhuv ntawmphlorizin uatej zaum yuav cuam tshuam rau nws qhov loj me me molecular thiab cov tawv nqaij tsis zoo permeability. Txawm li cas los xij, vim nws cov dej solubility zoo dua thiab ruaj khov, nws feem ntau yog siv los ua cov tshuaj pleev ib ce hauv cov tshuaj pleev ib ce, tso cov cag ntoo extract los ntawm daim tawv nqaij microbiota lossis enzymatic hydrolysis.
3. Phloretin vs. Phlorizin: Yuav Ua Li Cas LawvDaim ntawv thov tebTxawv?
3.1 Pharmaceutical teb
Phlorizin tau pib tshawb xyuas raws li kev kho mob ntshav qab zib hom 2; Txawm li cas los xij, tom qab ntawd nws tau hloov pauv los ntawm ntau cov khoom siv hluavtaws xws li canagliflozin thiab dapagliflozin, vim nws cov bioavailability tsawg thiab tsis yog - xaiv inhibition ntawm SGLT transporters. Txawm li cas los xij, nws tseem yog ib qho tseem ceeb hauv kev tsim cov tshuaj hypoglycemic tshiab. Phloretin, vim nws cov kev ua haujlwm lom neeg muaj zog thiab ntau yam kev ua haujlwm, tau qhia dav dav hauv kev tiv thaiv thiab kho cov kab mob metabolic.
3.2 Kev lag luam tshuaj pleev ib ce
Hauv kev lag luam tshuaj pleev ib ce, phloretin tau dhau los ua cov khoom siv hnub qub hauv siab -end whitening khoom. Nws cov nyiaj ntxiv ntawm 0.1-0.5% tuaj yeem cuam tshuam melanin ntau lawm thiab muaj kev sib koom ua ke nrog cov tshuaj ntxuav hniav dawb xws li vitamin C thiab arbutin. Phlorizin feem ntau yog siv los ua ib qho precursor rau phloretin hauv dej-raws li formulations vim nws zoo stability thiab dej solubility. Cov kev tshawb fawb tsis ntev los no qhia tau hais tias phlorizin nthuav tawm cov khoom tiv thaiv glycation los ntawm inhibiting kev tsim cov khoom kawg glycation kawg (AGEs).
3.3 Kev lag luam zaub mov
Ob qho tib si yog siv los ua cov khoom xyaw ua khoom noj. Phlorizin tau raug pom zoo ua FOSHU (Tshwj xeeb Kev Noj Qab Haus Huv Khoom Noj) muaj nyob hauv Nyij Pooj rau siv hauv cov khoom siv tswj ntshav qabzib. Phloretin yog ua hauj lwm raws li ib tug natural khoom noj preservative vim nws cov tshuaj tua kab mob, tshwj xeeb tshaj yog nws cov tseem ceeb inhibitory nyhuv tiv thaiv Gram - cov kab mob zoo. Txawm li cas los xij, kev saib xyuas yuav tsum tau them rau nws cov bioavailability. Phlorizin yuav tsum tau hydrolyzed los ntawm plab hnyuv enzymes rau hauv phloretin ua ntej nws yuav nqus tau thiab siv.
Raws li ib txwm muab los ntawm bioactive tebchaw, phlorizin thiab phloretin yog cov txheej txheem muaj feem xyuam tsis tau pom cov tshuaj lom neeg thiab cov yam ntxwv sib txawv. Phlorizin ua kom pom cov dej solubility ntau dua thiab ua haujlwm raws li lub zog SGLT inhibitor nrog qhov tshwj xeeb. Phloretin qhia txog kev muaj zog lipid solubility thiab ib qho kev nthuav dav ntawm kev ua haujlwm lom neeg lom zem -tshwj xeeb tshaj yog rau nws cov antioxidant, tawv nqaij - whitening, thiab tiv thaiv - inflammatory zog. Yog xav paub ntxiv txogPhloretinthiabPhlorizin, txuas nrog Serrisha los ntawm APPCHEM. (Email:cwj@appchem.cn; +86-138-0919-0407)
Siv:
[1] Bai Huirong. Flavonoids los ntawm Malus Rockii Rehder [D]. Dali University, 2023. DOI: 10.27811/d.cnki.gdixy.2023.000004.
[2] Zhang Tingjing. ENZYMATIC CHARACTERISTICS THIAB CATALYTIC MECHANISM ntawm APPLEPHLORETIN-2'-0-GLYCOSYLTRANSFERASE[D]. Northwest A & F University, 2017. DOI: 10.27409/d.cnki.gxbnu.2017.000235.
[3] Fan Jinbo, Cai Xitong, Feng Xuqiao, et al. Kev sib piv ntawm tsib lub ntuj phenolic tebchaw ntawm kev ua haujlwm antioxidant hauv vitro [J]. Food and Fermentation Industries, 2014, 40(07:77-83. DOI: 10.13995/j.cnki.11-1802/ts.2014.07.002.
[4] Yang Shengnan. Kev sib piv ntawm Oxidative Stress puas tsuaj ntawm HepG2 Cells ntawm Phlorizin thiab Phloretin [D]. Tianjin University of Science & Technology, 2019. DOI: 10.27359/d.cnki.gtqgu.2019.000199.