1 ngwa (10 Vials)
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▎ Gịnị bụ KPV?
KPV bụ akụkụ peptide eke nwere ọtụtụ ihe omume ndụ. Ọ na-arụ ọrụ nke ọma na ngalaba mgbochi mbufụt. Site n'ịchịkwa nzaghachi mgbochi ahụ, ọ na-ebelata mbufụt, nke dị oke mkpa maka ọgwụgwọ ọrịa ndị dị ka ọrịa na-egbuke egbuke. Ka ọ dị ugbu a, KPV nwere mmetụta antibacterial megide nje ndị dị ka Staphylococcus aureus na Candida albicans, na-enyere aka belata ọrịa. Na mgbakwunye, ọ nwere ike mee ka ọgwụgwọ ọnya dị ngwa ngwa, kwalite nrụzi anụ ahụ, ma melite ahụike akpụkpọ ahụ na ngalaba cosmetology. KPV nwere ezigbo mmiri solubility na biocompatibility. Ọ gaghị akpalite nzaghachi mgbochi ọrịa, yana enwere ike imebi ya site n'omume nke enzymes n'ime ahụ, na-eme ka nchekwa dị elu. Multifunctionality ya na-enye ya atụmanya ngwa ngwa n'ọtụtụ mpaghara, gụnyere ọgwụ, cosmetology na biomaterials.
▎ Ọdịdị TKPV
Isi mmalite: PubChem |
IUPAC gbakọrọ: H-Lys-Pro-Val-OH Ụdị mkpụrụ ndụ: C 16H 30N 4O4 Arọ molekụla: 342.43g/mol Nọmba CAS: 67727-97-3 PubChem CID: 125672 Ụdị okwu: Msh (11-13) ;alpha-Msh (11-13) ;ACTH-(11-13) |
▎ Nyocha KPV
Kedu ihe ndabere nyocha nke KPV?
KPV bụ tripeptide sitere na α-melanocyte-stimulating hormone (α-MSH). α-MSH bụ homonụ polypeptide nwere ọtụtụ ọrụ dị ndụ, na-arụ ọrụ dị mkpa n'ịchịkwa ụcha akpụkpọ ahụ, njikwa mgbochi na akụkụ ndị ọzọ. Dịka akụkụ nke α-MSH, KPV kewapụrụ ma mụọ miri emi. Ọ bụ ezie na e nwewo ọganihu ụfọdụ na ngalaba ahụike n'afọ ndị na-adịbeghị anya, nhọrọ ọgwụgwọ maka ọrịa obi na-egbuke egbuke (IBD) ka na-adịghị mma, ọnụ ọgụgụ ịwa ahụ ka dị elu. Ya mere, ịchọta ụzọ ọgwụgwọ ọhụrụ ma dị irè aghọwo ọrụ dị ngwa ngwa. IBD gụnyere ulcerative colitis, ọrịa Crohn, wdg, bụ nke e ji na-egbuke egbuke eriri afọ na-adịghị ala ala ma na-emetụta ụdị ndụ nke ndị ọrịa. Usoro ọgwụgwọ ugbu a gụnyere ọgwụgwọ ọgwụ na ọgwụgwọ ịwa ahụ, mana ha abụọ nwere oke ụfọdụ. N'ime afọ ndị na-adịbeghị anya, a kọwawo mmetụta mgbochi mkpali nke melanocortin peptides dị ka α-MSH na dextran sulfate sodium (DSS) colitis na ụmụ oke. Nke a na-enye ihe ngosi maka ịmụ ikike mgbochi mkpali nke KPV. α-MSH nwere ọrụ dị ka usoro mgbochi ọrịa na mbelata mbufụt, na tripeptide KPV ewepụtara na ya na-ewerekwa na ọ ga-enwe ihe mgbochi mkpali yiri ya.
Kedu usoro ọrụ nke KPV?
Usoro nke ime ihe na ulcerative colitis
Na-eme ka nkwụsi ike yana mma nchịkwa nchịkwa:
KPV (Lys-Pro-Val) bụ tripeptide sitere na α-MSH (α-melanocyte-stimulating hormone) ma nwee mmetụta mgbochi mkpali megide colitis. Otú ọ dị, ngwọta KPV adịghị eguzosi ike n'ihe n'oge nchịkwa rectal, na-emetụta mmetụta ọgwụgwọ ya. N'ime ọmụmụ ihe ahụ, a na-emepụta cysteamine-grafted γ-polyglutamic acid (SH-PGA) site na ijikọta cysteamine na otu carboxyl nke γ-PGA. Na-ejighi onye na-emekọrịta ihe, 4% polymer ọdịnaya SH-PGA hydrogel malitere site na njikọ nke onwe nke otu sulfhydryl. KPV/SH-PGA hydrogel gosipụtara modulus na-agbanwe agbanwe (G') dị elu karịa nke kwekọrọ na viscous modulus (G'') na 0.01-10 Hz, na-egosipụta ezigbo nkwụsi ike n'ọrụ yana omume ịhịa aka n'ahụ, nke bara uru maka nchịkwa akụkụ. N'otu oge ahụ, nkwụsi ike nke KPV na SH-PGA hydrogel abawanyela nke ukwuu. Naanị 30% nke KPV ka a tọhapụrụ na KPV/SH-PGA hydrogel n'ime nkeji 20, na-esote omume ntọhapụ na-aga n'ihu [1].
Na-ebelata ihe mgbaàmà nke colitis:
Site na nnwale na oke nwere ulcerative colitis nke 2,4,6-trinitrobenzene sulfonic acid (TNBS) kpatara, enwetara mmetụta ọgwụgwọ ahụike nke KPV/SH-PGA hydrogel na colitis. Mgbe nchịkwa rectal nke KPV/SH-PGA hydrogel, mgbaàmà colitis gụnyere mbelata ibu na ọnụọgụ ọrụ ọrịa belatara nke ukwuu. Na mgbakwunye, ọgwụgwọ na KPV/SH-PGA hydrogel gbochiri mkpirisi eriri afọ n'ime oke ndị a gbanyere TNBS wee belata ọkwa myeloperoxidase colonic. Mgbe a gwọchara ya na KPV/SH-PGA hydrogel, morphology nke colon, gụnyere mgbochi epithelial, crypts, na sel goblet na-emebibeghị, eweghachiri. N'otu oge ahụ, KPV/SH-PGA hydrogel belatara okwu nke cytokines pro-inflammatory dị ka tumor necrosis factor α na interleukin 6 [1].
Usoro nke ime ihe na ụdị òké nke ọrịa afọ ọzịza
Ụdị DSS colitis: N'ụdị DSS colitis, ọgwụgwọ na KPV mere ka mgbake mbụ ma kwalite mgbake dị arọ. N'ihe gbasara akụkọ ihe mere eme, ntinye nke mkpasu iwe na ụmụ oke ndị a na-emeso KPV belatara nke ukwuu, bụ nke akwadoro site na mbelata dị ukwuu nke ọrụ myeloperoxidase (MPO) na anụ ahụ colonic mgbe ọgwụgwọ KPV gasịrị [2]..
CD45RB (hi) nnyefe colitis nlereanya:
N'ịkwado nchoputa ndị a dị n'elu, ọgwụgwọ KPV nke a na-ebufe colitis na-eduga na mgbake ọrịa, mgbake dị arọ, na mbelata mgbanwe mgbanwe ọkụ site na ọdịdị akụkọ ihe mere eme [2].
Ụdị òké MC1Re/e:
N'ime ụmụ oke na-ekwupụta melanocortin-1 onye na-anabata ihe na-adịghị arụ ọrụ (MC1Re/e), ọgwụgwọ KPV zọpụtara anụmanụ niile nọ na otu ọgwụgwọ site na ọnwụ n'oge DSS colitis. Nke a na-egosi na mmetụta mgbochi mkpali nke KPV yiri ka ọ dịkarịa ala na-adabereghị na akara ngosi MC1R [2].
Usoro nke ime ihe na bronchial epithelial cell mbufụt
Ana m egbochi nrịbama NF-κB:
N'ime mkpụrụ ndụ epithelial bronchial na-adịghị anwụ anwụ, ndị melanocortin metụtara peptide KPV na agonist α-MSH nke epithelium ikuku (MC3R) gbochiri akara NF-κB site na igbochi mbubata nuklia nke p65RelA na ime ka epithelial MC3R rụọ ọrụ, n'otu n'otu. Kpọmkwem, mmetụta nke KPV metụtara mbubata nuklia ya, nke nwere ike igbochi ntụgharị nuklia nke p65RelA nke ejiri YFP. N'otu oge ahụ, saịtị njikọ nke KPV na Imp-α / β dị na p65RelA, ikekwe gụnyere igbochi mbubata-α armadillo ngalaba 7 na 8 [3].
Usoro nke ime ihe na chemotherapy na-ebute ọnụ mucositis
Antibacterial, mgbochi mkpali, na nrụzi mmetụta:
N'iji PLGA-PEG-PLGA (PPP) na-enwe mmetụta okpomọkụ dị ka matrix na epigallocatechin-3-gallate (EGCG) nwere ọrụ nje bacteria dị n'ime ya dị ka onye na-eme ka adhesion na-eme ka ọ dịkwuo mma, a kwadoro hydrogel mucosal mucosal (PPP_E) nke ọma. A gbajiri KPV tripeptide na oyi na-atụ PPP_2% E precursor solution dị ka ọgwụ nlereanya iji kwado KPV@PPP_2% E hydrogel. A na-echekwa ọrụ mgbochi mkpali na ikike ịkwalite mbugharị cell nke KPV na PPP-2% E hydrogel. Na mgbakwunye, KPV@PPP_2% E nwere mmetụta antibacterial siri ike megide Staphylococcus aureus. Mgbe etinyere KPV@PPP_2% E hydrogel na gingival mucosa nke oke nwere chemotherapy na-ebute ọnụ mucositis, ọ nwere ike gbanwee ngwa ngwa ka ọ bụrụ hydrogel ma rapara n'elu ọnya ahụ maka awa 7, na-eme ka nri oriri na mgbake oke nke oke. N'otu oge ahụ, site n'ịkwalite nkwupụta nke CK10 na PCNA, KPV@PPP_E hydrogel mekwara nke ọma n'ụdị anụ ahụ nke gingiva ọnya. Na mgbakwunye, KPV@PPP_2% E hydrogel gbochiri cytokines mkpali nke gụnyere IL-1β na TNF-α, ma n'otu oge ahụ kwalitere IL-10 [4].

Isi mmalite: PubMed [5]
Kedu ihe bụ ngwa ngwa ụlọ ọgwụ nke ọgwụ KPV?
Ọgwụgwọ nke ulcerative colitis
Nlekọta site na hydrogel na-agafe onwe ya:
N'ime ọmụmụ ihe, a na-emepụta cysteamine-grafted γ-polyglutamic acid (SH-PGA) ma mee ka ọ bụrụ hydrogel iji mee ka tripeptide KPV guzosie ike . KPV/SH-PGA hydrogel gosipụtara mmetụta ọgwụgwọ dị mma na ụdị oke nke ulcerative colitis nke 2,4,6-trinitrobenzene sulfonic acid (TNBS) kpatara. Kpọmkwem, mgbe nchịkwa rectal gasịrị, mgbaàmà colitis dị ka mbelata ibu na ọnụọgụ ọrụ ọrịa belatara nke ukwuu, ọ nwekwara ike igbochi mbelata eriri afọ n'ime oke ndị a gbanyere TNBS wee belata ọkwa myeloperoxidase colonic. N'otu oge ahụ, morphology nke colon, gụnyere ihe mgbochi epithelial, crypts, na sel goblet na-emebibeghị, ka eweghachiri ya na KPV/SH-PGA hydrogel, hydrogel na-ebelatakwa okwu nke cytokines pro-inflammatory dị ka tumor necrosis factor α na interleukin 6.
Nlekọta site na hydrogel netwọk abụọ:
Ọmụmụ ihe ọzọ wuru hydrogel-netwọk abụọ (PMSP) nke kpụrụ γ-polyglutamic acid na thiolated γ-polyglutamic acid site na thiol-maleimide cross-linking na onwe-oxidation nke thiols [5] . Nke a hydrogel nwere ike ịrapara n'ahụ mucosa na-ere ọkụ karịa mucosa dị mma, ma nwee ike ọrụ dị mma na nchikota ndu. KPV, dị ka ọgwụ nlereanya, PMSP na-ejide ngwa ngwa site na mmekọrịta electrostatic, si otú a na-ejigide ọrụ ndụ ya ogologo oge n'okpuru ọnọdụ okpomọkụ dị elu. N'ime oke nwere colitis nke TNBS kpatara, mgbe nchịkwa nchịkwa nke PMSP-KPV gasịrị, mmetụta na-ebelata nke KPV na colitis na-eme ka ọ dịkwuo mma, ma weghachite ihe mgbochi epithelial nke colon ahụ nke ọma. Na mgbakwunye, PMSP-KPV na-ahazikwa ahịhịa intestinal ma mụbaa ụbara microorganisms bara uru na eriri afọ.
Maka ọgwụgwọ nke chemotherapy kpatara ọnụ mucositis
A na-edozi hydrogel mucosal mucosal (PPP_E) site na iji PLGA-PEG-PLGA (PPP) nke nwere mmetụta okpomọkụ dị ka matrix na epigallocatechin-3-gallate (EGCG) dị ka onye na-eme ka adhesion [4] . A gbajiri KPV tripeptide na oyi na-atụ PPP_2% E precursor solution dị ka ọgwụ nlereanya iji kwado KPV@PPP_2% E hydrogel. Nke a hydrogel nwere mgbochi mkpali, antibacterial, na nrụzi mmetụta na chemotherapy-ebutere onu mucositis. Kpọmkwem, ọ nwere ike ịnọgide na-arụ ọrụ mgbochi mkpali nke KPV na ikike ịkwalite mbugharị cell, ma nwee mmetụta antibacterial siri ike megide Staphylococcus aureus. Mgbe nchịkwa na mucosa gingival nke oke nwere chemotherapy-induced oral mucositis, PPP_2% E precursor ngwọta ngwa ngwa ghọọ hydrogel ma na-arapara n'elu ọnya ahụ maka awa 7. Ọgwụgwọ na KPV@PPP_2% E hydrogel kwalitere nri oriri na mgbake dị arọ nke oke, kwalite okwu nke CK10 na PCNA, rụziri nke ọma morphology anụ ahụ nke gingiva ọnya ahụ, ma n'otu oge ahụ gbochiri cytokines mkpali dị ka IL-1β na TNF-α, ma kwalite okwu 10. Nke a hydrogel nwekwara mmetụta antibacterial na ọnya gingival ọrịa Staphylococcus aureus na-eguzogide methicillin (MRSA), ma na-egbochi ntinye nke mkpụrụ ndụ mkpali n'ime anụ ahụ submucosal.
Ọgwụgwọ ọrịa afọ ọzịza
Ụfọdụ ọmụmụ egosila na KPV nwere ike ịbụ ọgwụ ọgwụgwọ ọhụrụ maka ọrịa obi na-egbuke egbuke (IBD) [6] . N'ime mkpụrụ ndụ epithelial intestinal mmadụ (Caco2-BBE na HT29-Cl.19A) na mkpụrụ ndụ T mmadụ (Jurkat), mgbe mkpali na cytokines pro-inflammatory, mgbakwunye nke KPV nwere ike igbochi mmalite nke NF-κB na MAP kinase na-egosi ụzọ mgbaàmà ma belata nzuzo nke pro-inflammatory cytokin. Nnyocha ahụ chọpụtara na KPV na-arụ ọrụ site na hPepT1 gosipụtara na sel epithelial na-alụso ọrịa ọgụ na eriri afọ. Tụkwasị na nke ahụ, na ụdị òké nke colitis nke dextran sulfate sodium (DSS) na TNBS kpatara, nchịkwa ọnụ nke KPV nwere ike ibelata okwu nke cytokines pro-inflammatory na mkpali nke colitis.
N'ikpeazụ, dị ka ihe bioactive nwere ike dị ukwuu, KPV na-egosi uru pụrụ iche na ọgwụgwọ ọrịa dị iche iche. N'ihe gbasara ọrịa obi na-egbuke egbuke, ma ọ bụ na nyocha ụdị òké ma ọ bụ na nyocha nke ụzọ nchịkwa dị iche iche maka ọnyá afọ, KPV nwere ike ibelata nsị nsị nke ọma, meziwanye morphology anụ ahụ, na-edozi okwu cytokine, na-egosipụta mmetụta mgbochi mkpali dị ukwuu site na usoro ndị dị ka PepT1 njem. Na ọgwụgwọ nke chemotherapy na-ebute ọnụ mucositis, hydrogel nke nwere KPV nke a kwadebere na matrix a kapịrị ọnụ na ihe mgbakwunye adhesion nwere ike ọ bụghị naanị ijigide ihe mgbochi mkpali na mgbasa ozi cell na-akwalite ọrụ kamakwa ọ nwere ikike antibacterial dị ike, na-eme ka mgbaàmà ndị yiri nke oke oke dịkwuo elu ma na-akwalite mmezi anụ ahụ. Ọ bụ ezie na ngwa ngwa ụlọ ọgwụ ugbu a nke KPV ka nwere oke, nsonaazụ nyocha dị adị na-egosipụta n'ụzọ zuru oke uru ọgwụgwọ ya. N'ọdịnihu, ọ bụrụ na enwere ike nweta ọganihu na nyocha miri emi maka imeziwanye nkwụsi ike ọgwụ na nnyefe nnyefe, ịgbasa ihe ngosi ụlọ ọgwụ, na-ewusi nlekọta ahụike na nlekọta ahụike ike, a na-atụ anya na KPV ga-eweta nhọrọ ọgwụgwọ dị elu na nke ọma maka ọtụtụ ndị ọrịa ma rụọ ọrụ dị mkpa na ọgwụgwọ ụlọ ọgwụ.
Banyere Onye dere ya
Ihe niile a kpọtụrụ aha n'elu bụ Cocer Peptides na-enyocha, dezie ma chịkọta ya.
Onye ode akwụkwọ akụkọ sayensị
Dalmasso G bụ onye nyocha na ngalaba ọgwụ, yana ntụzịaka nyocha na-ekpuchi ọgwụ, biochemistry na mkpụrụ ndụ ihe nketa, n'etiti mpaghara ndị ọzọ. Ọ rụrụ ọrụ n'ọtụtụ ụlọ ọrụ ndị a ma ama, gụnyere 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, na Universidad Nacional Rio Cuarto. Ụlọ ọrụ ndị a bụ ndị a na-akwanyere ùgwù nke ukwuu n'ubi ha dị iche iche, na nkwado Dalmasso G na ha enyela aka na ọganihu nke ọzụzụ metụtara ya. Nchọpụta nyocha ya nwere ike ịbara nnukwu uru maka mmepe sayensị ahụike, ọkachasị n'ịkwalite nsonaazụ ọgwụgwọ ọrịa yana ụdị ndụ ndị ọrịa. Dalmasso G ka edepụtara na ntụnye aka nke ntụaka [6].
▎ Okwu ndị dị mkpa
[1] Sun J, Xue P, Liu J, et al. Hydrogel nke jikọrọ onwe ya nke Cysteamine-Grafted γ-Polyglutamic Acid Stabilized Tripeptide KPV maka ibelata TNBS-Induced Ulcerative Colitis na Rats[J]. Acs Biomaterials Science & Engineering, 2021,7 (10):4859-4869.DOI:10.1021/acsbiomaterials.1c00792.
[2] Konnegiesser K, Maaser C, Heidemann J, et al. KPV tripeptide enwetara Melanocortin nwere ikike mgbochi mkpali na ụdị murine nke ọrịa afọ ọzịza [J]. Ọrịa afọ na-egbuke egbuke, 2008,14 (3): 324-331.DOI: 10.1002 / ibd.20334.
[3] Ala S C. Mgbochi nke cellular na systemic mbufụt ihe na-egosi na mmadụ bronchial epithelial cell site melanocortin metụtara peptides: usoro nke KPV omume na ọrụ maka MC3R agonists.[J]. Akwụkwọ akụkọ International nke Physiology, Pathophysiology na Pharmacology, 2012,4 (2): 59-73. https://pubmed.ncbi.nlm.nih.gov/22837805/
[4] Shao W, Chen R, Lin G, et al. Na situ mucoadhesive hydrogel na-ejide tripeptide KPV: mgbochi mkpali, antibacterial na nrụzi mmetụta na chemotherapy na-ebute ọnụ mucositis[J]. Nkà mmụta sayensị biomaterials, 2021,10 (1): 227-242.DOI: 10.1039 / d1bm01466h.
[5] Zhao Y, Xue P, Lin G, et al. Hydrogel na-ejikọta KPV na-ejikọta ọnụ abụọ na-eweghachi ihe mgbochi mucosal gut na eriri afọ na-ere ọkụ [J]. Acta Biomaterialia, 2022,143:233-252.DOI:10.1016/j.actbio.2022.02.039.
[6] Dalmasso G, Charrier-Hisamuddin L, Nguyen HTT, et al. PepT1-mediated tripeptide KPV na-ebelata mbufụt nke eriri afọ [J]. Gastroenterology, 2008,134 (1): 166-178.DOI:10.1053/j.gastro.2007.10.026.
Edemede na ozi ngwaahịa niile enyere na webụsaịtị a bụ naanị maka mgbasa ozi na ebumnuche mmụta.
Ngwaahịa ndị enyere na webụsaịtị a bụ naanị maka nyocha in vitro. A na-eme nyocha in vitro (Latin: * na iko *, nke pụtara na ihe eji enyo) na mpụga ahụ mmadụ. Ngwaahịa ndị a abụghị ọgwụ, ndị US Food and Drug Administration (FDA) akwadoghị ya, ha agaghịkwa eji ya gbochie, gwọọ, ma ọ bụ gwọọ ọnọdụ ahụike ọ bụla, ọrịa, ma ọ bụ ọrịa. Iwu amachibidoro nke ọma iwebata ngwaahịa ndị a n'ime ahụ mmadụ ma ọ bụ anụmanụ n'ụdị ọ bụla.