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1 khoom (10Vials)
| Ntim: | |
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▎ TKPV Structure
Source: PubChem |
IUPAC Condensed: H-Lys-Pro-Val-OH Molecular Formula: C 16H 30N 4O4 Molecular Luj: 342.43g / mol CAS Nr .: 67727-97-3 PubChem CID: 125672 Synonyms: Msh (11-13) ; alpha-Msh (11-13) ; ACTH-(11-13) |
▎ KPV Research
Kev tshawb fawb keeb kwm ntawm KPV yog dab tsi?
KPV yog tripeptide muab los ntawm α-melanocyte-stimulating hormone (α-MSH). α-MSH yog polypeptide cov tshuaj hormones nrog ntau yam kev ua haujlwm lom neeg, ua lub luag haujlwm tseem ceeb hauv kev tswj cov tawv nqaij pigmentation, kev tiv thaiv kab mob, thiab lwm yam. Raws li ib feem ntawm α-MSH, KPV tau raug cais tawm thiab kawm tob heev. Txawm hais tias qee qhov kev nce qib tau ua tiav hauv kev kho mob hauv xyoo tas los no, cov kev xaiv kho mob rau cov kab mob plab hnyuv (IBD) tseem tsis txaus siab, thiab kev phais tus nqi tseem siab. Yog li ntawd, nrhiav txoj kev kho tshiab thiab ua tau zoo tau dhau los ua txoj haujlwm ceev. IBD suav nrog ulcerative colitis, Crohn's disease, thiab lwm yam, uas yog tus cwj pwm los ntawm kev mob plab hnyuv thiab cuam tshuam rau lub neej zoo ntawm cov neeg mob. Txoj kev kho tam sim no suav nrog kev kho tshuaj thiab kev phais mob, tab sis ob qho tib si muaj qee yam kev txwv. Hauv xyoo tas los no, cov tshuaj tiv thaiv kab mob ntawm melanocortin peptides xws li α-MSH tau piav qhia hauv dextran sulfate sodium (DSS) colitis hauv cov nas. Qhov no muab cov lus qhia rau kev kawm txog kev tiv thaiv kab mob ntawm KPV. α-MSH muaj lub luag haujlwm xws li kev tiv thaiv kev tiv thaiv kab mob thiab kev mob o, thiab tripeptide KPV tau los ntawm nws kuj tau txiav txim siab tias muaj peev xwm muaj cov tshuaj tiv thaiv zoo sib xws.
Lub mechanism ntawm kev txiav txim ntawm KPV yog dab tsi?
Mechanism ntawm kev ua nyob rau hauv ulcerative colitis
Txhim kho stability thiab kev tswj lub qhov quav kom yooj yim:
KPV (Lys-Pro-Val) yog ib qho tripeptide muab tau los ntawm α-MSH (α-melanocyte-stimulating hormone) thiab muaj cov tshuaj tiv thaiv kab mob colitis. Txawm li cas los xij, cov tshuaj KPV tsis ruaj khov heev thaum lub sij hawm tswj qhov quav, cuam tshuam rau nws txoj kev kho mob. Hauv txoj kev tshawb no, cysteamine-grafted γ-polyglutamic acid (SH-PGA) tau tsim los ntawm kev sib txuas cysteamine nrog pawg carboxyl ntawm γ-PGA. Yog tsis siv tus neeg sawv cev sib txuas, 4% cov ntsiab lus polymer SH-PGA hydrogel tau tsim los ntawm kev sib txuas tus kheej ntawm sulfhydryl pawg. Lub KPV / SH-PGA hydrogel tau pom qhov elastic modulus (G') siab dua qhov sib thooj viscous modulus (G') ntawm 0.01-10 Hz, qhia txog kev ruaj ntseg zoo thiab shear thinning tus cwj pwm, uas muaj txiaj ntsig zoo rau kev tswj xyuas qhov quav. Nyob rau tib lub sijhawm, kev ruaj ntseg ntawm KPV hauv SH-PGA hydrogel tau txhim kho zoo. Tsuas yog 30% ntawm KPV raug tso tawm los ntawm KPV / SH-PGA hydrogel nyob rau hauv 20 feeb, ua raws li tus cwj pwm tso tawm tas mus li [1].
Alleviating colitis cov tsos mob:
Los ntawm kev sim ntawm cov nas uas muaj kab mob ulcerative tshwm sim los ntawm 2,4,6-trinitrobenzene sulfonic acid (TNBS), qhov kev kho kom zoo ntawm KPV / SH-PGA hydrogel ntawm colitis tau lees paub. Tom qab kev tswj hwm qhov quav ntawm KPV / SH-PGA hydrogel, cov tsos mob ntawm tus kab mob colitis nrog rau kev poob phaus thiab cov kab mob kev ua ub no tau txo qis. Tsis tas li ntawd, kev kho mob nrog KPV / SH-PGA hydrogel tiv thaiv qhov ua kom luv ntawm txoj hnyuv hauv cov nas txhaj tshuaj TNBS thiab txo cov qib ntawm colonic myeloperoxidase. Tom qab kev kho mob nrog KPV / SH-PGA hydrogel, morphology ntawm txoj hnyuv, nrog rau cov epithelial barrier, crypts, thiab cov kab mob goblet tsis zoo, tau rov qab los. Nyob rau tib lub sijhawm, KPV / SH-PGA hydrogel txo qhov kev qhia ntawm pro-inflammatory cytokines xws li qog necrosis factor α thiab interleukin 6 [1].
Mechanism ntawm kev ua nyob rau hauv nas qauv ntawm inflammatory plob tsis so tswj kab mob
DSS colitis qauv: Hauv DSS colitis qauv, kev kho mob nrog KPV coj mus rau kev rov qab ua ntej thiab txhim kho qhov hnyav. Histologically, inflammatory infiltration hauv KPV-kho nas tau txo qis, uas tau lees paub los ntawm qhov txo qis hauv kev ua haujlwm ntawm myeloperoxidase (MPO) hauv cov nqaij mos tom qab kho KPV [2].
CD45RB (hi) hloov colitis qauv:
Txhawb nqa qhov kev tshawb pom saum toj no, KPV kev kho mob ntawm cov kab mob kis tau coj mus rau cov kab mob rov qab, qhov hnyav rov qab, thiab txo qis kev hloov pauv ntawm qhov kev xav ntawm histological [2].
MC1Re/e nas qauv:
Hauv cov nas uas qhia txog qhov tsis ua haujlwm ntawm melanocortin-1 receptor (MC1Re/e), KPV kev kho mob cawm txhua tus tsiaj hauv pab pawg kho mob los ntawm kev tuag thaum DSS colitis. Qhov no qhia tau hais tias cov tshuaj tiv thaiv kab mob ntawm KPV zoo li yog qhov tsawg kawg ntawm kev ywj pheej ntawm MC1R signaling [2].
Mechanism ntawm kev ua nyob rau hauv bronchial epithelial cell o
Kuv nhibiting NF-κB signaling:
Hauv immortalized human bronchial epithelial cells, melanocortin-related peptide KPV thiab agonist α-MSH ntawm pa pa epithelium (MC3R) inhibited NF-κB signaling los ntawm inhibiting nuclear ntshuam ntawm p65RelA thiab activating epithelial MC3R, feem. Tshwj xeeb, cov txiaj ntsig ntawm KPV muaj feem cuam tshuam rau nws cov khoom siv hluav taws xob, uas tuaj yeem cuam tshuam kev hloov pauv ntawm lub zog ntawm p65RelA sau nrog YFP. Nyob rau tib lub sijhawm, cov chaw sib txuas ntawm KPV thiab Imp-α / β nyob ntawm p65RelA, tejzaum nws cuam tshuam nrog kev thaiv cov importin-α armadillo domains 7 thiab 8 [3].
Mechanism of action in chemotherapy-induced oral mucositis
Antibacterial, anti-inflammatory, thiab kho cov teebmeem:
Siv cov kub-rhiab heev PLGA-PEG-PLGA (PPP) raws li cov matrix thiab epigallocatechin-3-gallate (EGCG) nrog rau cov kab mob hauv nruab nrog cev raws li cov adhesion enhancer, ib qho in-situ mucosal nplaum hydrogel (PPP_E) tau ua tiav tiav. Lub tripeptide KPV tau yaj nyob rau hauv txias PPP_2% E precursor tov raws li ib tug qauv tshuaj los npaj cov KPV@PPP_2% E hydrogel. Kev ua haujlwm tiv thaiv kab mob thiab lub peev xwm los txhawb kev hloov pauv ntawm tes ntawm KPV hauv PPP-2% E hydrogel tau khaws cia zoo. Tsis tas li ntawd, KPV@PPP_2% E muaj cov kab mob muaj zog tiv thaiv Staphylococcus aureus. Thaum KPV@PPP_2% E hydrogel tau siv rau gingival mucosa ntawm nas nrog tshuaj tua kab mob hauv qhov ncauj mucositis, nws tuaj yeem hloov pauv sai sai rau hauv hydrogel thiab ua raws li lub qhov txhab rau 7 teev, txhim kho kev noj zaub mov zoo thiab hnyav rov qab ntawm cov nas. Nyob rau tib lub sijhawm, los ntawm kev txhawb nqa kev qhia ntawm CK10 thiab PCNA, KPV@PPP_E hydrogel kuj tau kho cov ntaub so ntswg morphology ntawm ulcerated gingiva. Tsis tas li ntawd, KPV@PPP_2% E hydrogel cuam tshuam inflammatory cytokines nrog rau IL-1β thiab TNF-α, thiab tib lub sij hawm upregulated IL-10 [4].
Source: PubMed [5]
Dab tsi yog cov ntaub ntawv thov kev kho mob ntawm cov tshuaj KPV?
Kev kho mob ntawm ulcerative colitis
Kev tswj hwm los ntawm tus kheej-crosslinking hydrogel:
Hauv kev tshawb nrhiav, cysteamine-grafted γ-polyglutamic acid (SH-PGA) tau tsim thiab ua rau hauv hydrogel kom stabilize tripeptide KPV [1] . KPV / SH-PGA hydrogel tau pom zoo kho cov teebmeem hauv cov qauv nas ntawm cov kab mob ulcerative tshwm sim los ntawm 2,4,6-trinitrobenzene sulfonic acid (TNBS). Tshwj xeeb, tom qab kev tswj hwm ntawm qhov quav, cov tsos mob ntawm tus kab mob xws li poob phaus thiab cov qhab nia ntawm cov kab mob ua haujlwm tau txo qis, thiab nws tseem tuaj yeem tiv thaiv qhov ua kom luv ntawm txoj hnyuv hauv cov nas txhaj nrog TNBS thiab txo cov qib ntawm colonic myeloperoxidase. Nyob rau tib lub sijhawm, morphology ntawm txoj hnyuv, nrog rau cov kab mob epithelial, crypts, thiab cov kab mob goblet tsis zoo, tau rov qab los tom qab kev kho mob nrog KPV / SH-PGA hydrogel, thiab cov hydrogel kuj txo cov kev qhia ntawm pro-inflammatory cytokines xws li qog necrosis factor α thiab interleukin 6.
Kev tswj hwm los ntawm dual-network hydrogel:
Lwm txoj kev tshawb fawb tau tsim dual-network hydrogel (PMSP) tsim los ntawm maleated γ-polyglutamic acid thiab thiolated γ-polyglutamic acid los ntawm thiol-maleimide cross-linking thiab nws tus kheej-oxidation ntawm thiols [5] . Qhov hydrogel no tuaj yeem ua raws li cov kab mob uas ua rau mob ntau dua li cov mucosa noj qab haus huv, thiab muaj zog txhua yam zoo thiab lom neeg adhesion. KPV, raws li cov qauv tshuaj, tau yooj yim ntes los ntawm PMSP los ntawm kev sib cuam tshuam electrostatic, yog li tswj nws cov kev ua ub no rau lub sijhawm ntev dua nyob rau hauv qhov kub thiab txias. Hauv cov nas uas muaj cov kab mob colitis tshwm sim los ntawm TNBS, tom qab kev tswj hwm ntawm qhov quav ntawm PMSP-KPV, qhov txo qis ntawm KPV ntawm cov kab mob colitis tau zoo dua, thiab cov kab mob epithelial ntawm txoj hnyuv tau rov qab zoo. Tsis tas li ntawd, PMSP-KPV kuj tswj cov hnyuv thiab ua kom muaj txiaj ntsig zoo ntawm cov kab mob hauv cov hnyuv.
Rau chemotherapy-induced qhov ncauj mucositis
Ib qho hauv-situ mucosal nplaum hydrogel (PPP_E) tau npaj siv qhov kub thiab txias PLGA-PEG-PLGA (PPP) ua cov matrix thiab epigallocatechin-3-gallate (EGCG) ua cov nplaum nplaum [4] . Lub tripeptide KPV tau yaj nyob rau hauv txias PPP_2% E precursor tov raws li ib tug qauv tshuaj los npaj cov KPV@PPP_2% E hydrogel. Cov hydrogel no muaj cov tshuaj tiv thaiv kab mob, tshuaj tua kab mob, thiab kho cov teebmeem ntawm cov tshuaj tua kab mob hauv qhov ncauj mucositis. Tshwj xeeb, nws muaj peev xwm tswj tau cov kev tiv thaiv kab mob ntawm KPV thiab lub peev xwm los txhawb kev tsiv teb tsaws ntawm tes, thiab muaj cov kab mob muaj zog tiv thaiv Staphylococcus aureus. Tom qab kev tswj hwm rau gingival mucosa ntawm nas nrog tshuaj tua kab mob hauv qhov ncauj mucositis, PPP_2% E precursor tov tau hloov pauv sai sai rau hauv hydrogel thiab ua raws li lub qhov txhab rau 7 teev. Kev kho mob nrog KPV@PPP_2% E hydrogel zoo heev txhim kho cov khoom noj thiab qhov hnyav rov qab ntawm cov nas, txhawb kev qhia ntawm CK10 thiab PCNA, zoo kho cov ntaub so ntswg morphology ntawm gingiva ulcerated, thiab tib lub sij hawm tseem ceeb heev inhibited inflammatory cytokines xws li IL-1β thiab TNF-a, kev qhia txog TNF-10, Cov hydrogel no kuj muaj cov kab mob tua kab mob ntawm cov kab mob gingival qhov txhab kis nrog methicillin-resistant Staphylococcus aureus (MRSA), thiab inhibits infiltration ntawm inflammatory cells rau hauv cov ntaub so ntswg submucosal.
Kev kho mob inflammatory plob tsis so tswj kab mob
Qee qhov kev tshawb fawb tau pom tias KPV tuaj yeem yog cov tshuaj kho mob tshiab rau kab mob plab hnyuv (IBD) [6] . Hauv tib neeg txoj hnyuv epithelial hlwb (Caco2-BBE thiab HT29-Cl.19A) thiab tib neeg T hlwb (Jurkat), tom qab stimulation nrog pro-inflammatory cytokines, qhov sib ntxiv ntawm KPV tuaj yeem inhibit qhov ua kom NF-κB thiab MAP kinase inflammatory signaling pathways thiab txo cov secretion ntawm pro-inflammatory cytokines. Txoj kev tshawb nrhiav pom tias KPV ua los ntawm hPepT1 qhia hauv lub cev tiv thaiv kab mob thiab plab hnyuv epithelial hlwb. Tsis tas li ntawd, nyob rau hauv nas qauv ntawm colitis induced los ntawm dextran sulfate sodium (DSS) thiab TNBS, qhov ncauj kev tswj ntawm KPV yuav txo tau cov kev qhia ntawm pro-inflammatory cytokines thiab qhov tshwm sim ntawm colitis.
Hauv kev xaus, raws li cov khoom siv bioactive nrog lub peev xwm zoo, KPV qhia tau hais tias muaj txiaj ntsig zoo hauv kev kho mob ntawm ntau yam kab mob. Hauv kev ua haujlwm ntawm cov kab mob hauv plab, txawm tias nyob rau hauv cov qauv kev sim nas lossis hauv kev tshawb nrhiav cov kev tswj hwm sib txawv rau cov kab mob ulcerative colitis, KPV tuaj yeem txo cov kab mob inflammatory infiltration, txhim kho cov ntaub so ntswg morphology, tswj cytokine qhia, thiab siv cov tshuaj tiv thaiv kab mob los ntawm cov txheej txheem xws li PepT1 thauj. Nyob rau hauv kev kho mob ntawm chemotherapy-induced lub qhov ncauj mucositis, cov hydrogel uas muaj KPV npaj nrog ib tug tshwj xeeb matrix thiab adhesion enhancer tsis tau tsuas yog tswj nws cov anti-inflammatory thiab cell migration-txhawb kev ua ub no tab sis kuj muaj ib tug haib antibacterial muaj peev xwm, ho txhim kho cov tsos mob ntawm nas thiab txhawb cov ntaub so ntswg kho. Txawm hais tias tam sim no daim ntawv thov kev kho mob ntawm KPV tseem txwv, cov kev tshawb fawb uas twb muaj lawm qhia tau hais tias nws cov nqi kho mob. Nyob rau hauv lub neej yav tom ntej, yog tias kev ua tiav tuaj yeem ua tiav hauv kev tshawb fawb tob txog kev txhim kho tshuaj ruaj khov thiab kev xa khoom zoo, nthuav tawm cov ntaub ntawv kho mob, thiab ntxiv dag zog rau kev soj ntsuam thiab kev tswj hwm, KPV yuav tsum coj cov kev kho mob zoo thiab muaj txiaj ntsig zoo rau ntau tus neeg mob thiab ua lub luag haujlwm tseem ceeb hauv kev kho mob.
Hais Txog Tus Sau
Cov ntaub ntawv hais saum toj no yog txhua yam tshawb fawb, kho thiab sau los ntawm Cocer Peptides.
Scientific Journal Author
Dalmasso G yog tus kws tshawb fawb hauv kev kho mob, nrog rau kev tshawb fawb qhia txog tshuaj, biochemistry, thiab noob caj noob ces, ntawm lwm qhov chaw. Nws tau ua haujlwm ntawm ntau lub tsev kawm muaj koob npe, suav nrog Universite Clermont Auvergne (UCA), CHU Clermont Ferrand, INRAE, Institut National de la Sante et de la Recherche Medicale (Inserm), Clermont Univ, Georgia State University, Emory University, Universite Cote d'Azur, thiab Universidad Nacional. Cov tsev kawm ntawv no muaj npe nrov hauv lawv txoj haujlwm, thiab Dalmasso G kev koom tes nrog lawv tau pab txhawb rau kev nce qib ntawm cov kev qhuab qhia ntsig txog. Nws cov kev tshawb fawb tshawb pom tej zaum yuav muaj txiaj ntsig zoo rau kev tsim kho kev tshawb fawb, tshwj xeeb hauv kev txhim kho cov txiaj ntsig kev kho mob thiab cov neeg mob lub neej zoo. Dalmasso G tau teev nyob rau hauv kev siv ntawm cov ntaub ntawv pov thawj [6].
