1 kits (10 Vials)
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▎ Menene KPV?
KPV wani yanki ne na peptide na halitta tare da ayyukan halitta masu yawa. Yana aiki sosai da kyau a fagen rigakafin kumburi. Ta hanyar daidaita tsarin rigakafi, yana rage kumburi, wanda ke da mahimmanci ga maganin cututtuka irin su ciwon ƙwayar cuta. A halin yanzu, KPV yana da tasirin antibacterial akan ƙwayoyin cuta irin su Staphylococcus aureus da Candida albicans, suna taimakawa wajen rage cututtuka. Bugu da ƙari, zai iya hanzarta warkar da raunuka, inganta gyaran nama, da inganta lafiyar fata a fagen kwaskwarima. KPV yana da kyakkyawan solubility na ruwa da biocompatibility. Ba zai haifar da amsawar rigakafi ba, kuma ana iya lalata shi ta dabi'a ta hanyar aikin enzymes a cikin jiki, yana tabbatar da babban matakin aminci. Multifunctionality ɗin sa yana ba shi damar aikace-aikacen fa'ida a fagage da yawa, gami da magani, kayan kwalliya, da kayan halitta.
▎ Tsarin TKPV
Source: PubChem |
IUPAC Narke: H-Lys-Pro-Val-OH Tsarin kwayoyin halitta: C 16H 30N 4O4 Nauyin Kwayoyin Halitta: 342.43g/mol Lambar CAS: 67727-97-3 Saukewa: 125672 Synonyms: Msh (11-13) ;alpha-Msh (11-13) ;ACTH-(11-13) |
▎ Binciken KPV
Menene asalin bincike na KPV?
KPV wani tripeptide ne wanda aka samo daga α-melanocyte-stimulating hormone (α-MSH). α-MSH shine hormone na polypeptide tare da ayyuka masu yawa na halitta, yana taka muhimmiyar rawa wajen daidaita launin fata, tsarin rigakafi, da sauran bangarori. A matsayin wani ɓangare na α-MSH, KPV an ware kuma an yi nazari sosai. Ko da yake an sami wasu ci gaba a fannin likitanci a cikin 'yan shekarun nan, zaɓuɓɓukan jiyya na cututtukan hanji (IBD) har yanzu ba su da daɗi, kuma yawan aikin tiyata ya kasance mai girma. Saboda haka, gano sababbin hanyoyin magani masu inganci ya zama aiki na gaggawa. IBD ya haɗa da ulcerative colitis, cutar Crohn, da dai sauransu, waɗanda ke da alamun kumburi na hanji na yau da kullum kuma suna tasiri sosai ga rayuwar marasa lafiya. Hanyoyin jiyya na yanzu sun haɗa da maganin miyagun ƙwayoyi da magani na tiyata, amma duka biyu suna da wasu iyakoki. A cikin 'yan shekarun nan, an bayyana tasirin anti-mai kumburi na melanocortin peptides kamar α-MSH a cikin dextran sulfate sodium (DSS) colitis a cikin mice. Wannan yana ba da ma'ana don nazarin yuwuwar rigakafin kumburin KPV. α-MSH yana da ayyuka kamar tsarin rigakafi da rage kumburi, kuma KPV tripeptide da aka samu daga gare ta ana kuma la'akari da yiwuwar samun irin wannan kaddarorin anti-mai kumburi.
Menene tsarin aikin KPV?
Hanyar aiki a cikin ulcerative colitis
Inganta kwanciyar hankali da dacewa da gudanarwar dubura:
KPV (Lys-Pro-Val) wani tripeptide ne wanda aka samo daga α-MSH (α-melanocyte-stimulating hormone) kuma yana da tasirin anti-mai kumburi akan colitis. Duk da haka, maganin KPV yana da matukar rashin kwanciyar hankali a lokacin gudanar da rectal, yana rinjayar tasirin warkewa. A cikin binciken, an haɗa cysteamine-grafted γ-polyglutamic acid (SH-PGA) ta hanyar haɗa cysteamine tare da ƙungiyar carboxyl na γ-PGA. Ba tare da yin amfani da wakili mai haɗin kai ba, an kafa 4% polymer abun ciki SH-PGA hydrogel ta hanyar haɗin kai na ƙungiyoyin sulfhydryl. KPV/SH-PGA hydrogel ya nuna modulus na roba (G') mafi girma fiye da madaidaicin modulus na viscous (G'') a 0.01-10 Hz, yana nuna kyakkyawan kwanciyar hankali na inji da halayen ɓacin rai, wanda ke da fa'ida ga gudanarwar dubura. A lokaci guda, an inganta kwanciyar hankali na KPV a cikin SH-PGA hydrogel. Kashi 30% na KPV kawai an sake shi daga KPV/SH-PGA hydrogel a cikin mintuna 20, sannan ci gaba da halayyar sakin [1].
Rage bayyanar cututtuka na colitis:
Ta hanyar gwaje-gwaje akan berayen tare da ulcerative colitis wanda 2,4,6-trinitrobenzene sulfonic acid (TNBS) ya haifar, an tabbatar da ingantaccen tasirin warkewa na KPV/SH-PGA hydrogel akan colitis. Bayan gudanar da gyaran fuska na KPV/SH-PGA hydrogel, alamun colitis gami da asarar nauyi da ƙididdigar ayyukan cututtuka sun ragu sosai. Bugu da kari, jiyya tare da KPV/SH-PGA hydrogel ya hana raguwar hanji a cikin berayen da aka yi musu allura tare da TNBS kuma sun rage matakin myeloperoxidase na colonic. Bayan jiyya tare da KPV/SH-PGA hydrogel, an dawo da yanayin halittar hanji, gami da shingen epithelial, crypts, da ƙwayoyin goblet mara kyau. A lokaci guda, KPV/SH-PGA hydrogel ya rage maganganun cytokines masu kumburi irin su ƙwayar necrosis factor α da interleukin 6 [1].
Hanyar aiki a cikin nau'ikan linzamin kwamfuta na cututtukan hanji mai kumburi
Samfurin DSS colitis: A cikin samfurin DSS colitis, jiyya tare da KPV ya haifar da farfadowa a baya da kuma inganta farfadowa mai mahimmanci. A tarihi, an rage kutsewar kumburi a cikin berayen da aka yi wa maganin KPV, wanda aka tabbatar da raguwar yawan ayyukan myeloperoxidase (MPO) a cikin nama na hanji bayan maganin KPV [2].
CD45RB (hi) canja wurin colitis model:
Taimakawa binciken da ke sama, maganin KPV na colitis da aka canjawa wuri ya haifar da farfadowa da cututtuka, farfadowa mai nauyi, da raguwa a cikin canje-canje na kumburi daga hangen nesa na tarihi [2].
MC1Re/e samfurin linzamin kwamfuta:
A cikin berayen da ke bayyana mai karɓar melanocortin-1 mara aiki (MC1Re / e), jiyya na KPV ya ceci duk dabbobi a cikin rukunin jiyya daga mutuwa a lokacin DSS colitis. Wannan yana nuna cewa tasirin anti-kumburi na KPV yana da alama ya kasance aƙalla wani ɓangare mai zaman kansa daga siginar MC1R [2].
Hanyar aiki a cikin kumburi epithelial cell kumburi
Ina hana siginar NF-κB:
A cikin ƙwayoyin cuta na ƙwayar cuta na ɗan adam mara mutuwa, peptide KPV da ke da alaƙa da melanocortin da agonist α-MSH na epithelium na iska (MC3R) sun hana siginar NF-κB ta hanyar hana shigo da makaman nukiliya na p65RelA da kunna epithelial MC3R, bi da bi. Musamman, tasirin KPV yana da alaƙa da shigo da makaman nukiliyarta, wanda zai iya hana jujjuyawar makaman nukiliya na p65RelA da aka yiwa lakabi da YFP. A lokaci guda, wuraren dauri na KPV da Imp-α/β suna kan p65RelA, mai yiwuwa sun haɗa da toshe wuraren shigo da-α armadillo 7 da 8 [3].
Hanyar aiki a cikin ƙwayar cuta ta hanyar ƙwayar cuta ta ƙwayar cuta
Antibacterial, anti-mai kumburi, da kuma tasirin gyarawa:
Yin amfani da PLGA-PEG-PLGA mai zafin jiki (PPP) a matsayin matrix da epigallocatechin-3-gallate (EGCG) tare da aikin ƙwayoyin cuta na ainihi a matsayin mai haɓakaccen mannewa, an yi nasarar shirya wani adhesive mucosal mucosal hydrogel (PPP_E). An narkar da KPV tripeptide a cikin sanyi PPP_2% E precursor bayani azaman samfurin samfurin don shirya KPV@PPP_2% E hydrogel. Ayyukan anti-mai kumburi da yuwuwar haɓaka ƙaura na KPV a cikin PPP-2% E hydrogel an kiyaye su da kyau. Bugu da kari, KPV@PPP_2% E yana da tasirin kashe kwayoyin cuta mai karfi akan Staphylococcus aureus. Lokacin da aka yi amfani da KPV@PPP_2% E hydrogel zuwa ga gingival mucosa na berayen tare da chemotherapy-induced na baka mucositis, zai iya sauri canza zuwa wani hydrogel da kuma manne da rauni surface na 7 hours, ƙwarai inganta ci abinci da kuma nauyi dawo da berayen. A lokaci guda kuma, ta hanyar haɓaka maganganun CK10 da PCNA, KPV@PPP_E hydrogel shima ya gyara yanayin ƙwayoyin nama na gingiva ulcerated. Bugu da ƙari, KPV @ PPP_2% E hydrogel ya hana cytokines masu kumburi ciki har da IL-1β da TNF-α, kuma a lokaci guda ya inganta IL-10 [4].

Source:PubMed [5]
Menene lokuta aikace-aikacen asibiti na magungunan KPV?
Maganin ulcerative colitis
Gudanarwa ta hanyar haɗin gwiwar hydrogel:
A cikin binciken, an haɗa cysteamine-grafted γ-polyglutamic acid (SH-PGA) kuma an sanya shi cikin hydrogel don daidaita KPV tripeptide [1] . KPV/SH-PGA hydrogel ya nuna sakamako mai kyau na warkewa a cikin ƙirar bera na ulcerative colitis wanda 2,4,6-trinitrobenzene sulfonic acid (TNBS) ya haifar. Musamman, bayan gudanarwar dubura, alamun colitis irin su asarar nauyi da ƙididdigar ayyukan cututtuka sun ragu sosai, kuma yana iya hana rage ƙwayar hanji a cikin berayen da aka yi wa allurar TNBS da rage matakin myeloperoxidase na colonic. A lokaci guda kuma, an sake dawo da ilimin halittar hanji, gami da shingen epithelial, crypts, da ƙwayoyin goblet mara kyau, bayan jiyya tare da KPV/SH-PGA hydrogel, kuma hydrogel kuma ya rage bayyanar cututtukan cytokines masu kumburi irin su tumor necrosis factor α da interleukin 6.
Gudanarwa ta hanyar hanyar sadarwa biyu ta hydrogel:
Wani binciken ya gina hydrogel mai dual-network (PMSP) wanda aka kafa ta maleated γ-polyglutamic acid da thiolated γ-polyglutamic acid ta hanyar haɗin gwiwar thiol-maleimide da haɗin kai na thiols [5] . Wannan hydrogel na iya mannewa musamman ga mucosa mai kumburi maimakon lafiyayyen mucosa, kuma yana da ƙarfin injina da mannewa na halitta. KPV, a matsayin samfurin samfurin, PMSP yana iya kama shi cikin sauƙi ta hanyar hulɗar lantarki, don haka yana ci gaba da aikin nazarin halittu na tsawon lokaci a ƙarƙashin yanayin zafi mai zafi. A cikin berayen tare da colitis da TNBS ta jawo, bayan gudanarwar PMSP-KPV, rage tasirin KPV akan colitis ya inganta sosai, kuma an dawo da shingen epithelial na hanji sosai. Bugu da kari, PMSP-KPV kuma ya tsara flora na hanji kuma yana haɓaka yawan ƙwayoyin cuta masu amfani a cikin hanji.
Don cutar mucositis ta baka ta haifar da chemotherapy
An shirya wani in-situ mucosal adhesive hydrogel (PPP_E) ta amfani da zafin jiki-PLGA-PEG-PLGA (PPP) a matsayin matrix da epigallocatechin-3-gallate (EGCG) a matsayin mai haɓaka adhesion [4] . An narkar da KPV tripeptide a cikin sanyi PPP_2% E precursor bayani azaman samfurin samfurin don shirya KPV@PPP_2% E hydrogel. Wannan hydrogel yana da anti-mai kumburi, antibacterial, da kuma gyara sakamako a kan chemotherapy-jawo baki mucositis. Musamman, yana iya kula da aikin KPV mai kumburi da kuma yuwuwar haɓaka ƙaura ta tantanin halitta, kuma yana da tasirin ƙwayar cuta mai ƙarfi akan Staphylococcus aureus. Bayan gudanarwa zuwa ga gingival mucosa na berayen tare da chemotherapy-induced na baka mucositis, da PPP_2% E precursor bayani da sauri rikide zuwa wani hydrogel kuma manne da rauni surface na 7 hours. Jiyya tare da KPV@PPP_2% E hydrogel ya inganta ci abinci da kuma dawo da nauyi na berayen, inganta bayyanar CK10 da PCNA, da kyau gyara yanayin halittar nama na ulcerated gingiva, kuma a lokaci guda ya hana cytokines masu kumburi kamar IL-1β da TNF-α, da kuma daidaita maganganun 1.0. Wannan hydrogel kuma yana da tasirin kashe kwayoyin cuta akan raunukan gingival ulcer da suka kamu da methicillin-resistant Staphylococcus aureus (MRSA), kuma yana hana shigar da ƙwayoyin kumburi a cikin nama na submucosal.
Maganin ciwon kumburin hanji
Wasu nazarin sun nuna cewa KPV na iya zama sabon maganin warkewa don cututtukan cututtuka (IBD) [6] . A cikin kwayoyin epithelial na hanji na mutum (Caco2-BBE da HT29-Cl.19A) da kuma kwayoyin T na mutum (Jurkat), bayan ƙarfafawa tare da cytokines pro-inflammatory, ƙari na KPV zai iya hana kunna NF-κB da MAP kinase hanyoyin siginar kumburi da kuma rage ɓoyewar cytokin mai kumburi. Binciken ya gano cewa KPV yana aiki ta hanyar hPepT1 da aka bayyana a cikin kwayoyin epithelial na rigakafi da na hanji. Bugu da ƙari, a cikin nau'in linzamin kwamfuta na colitis da dextran sulfate sodium (DSS) da TNBS suka haifar, gudanarwa na KPV na baka zai iya rage maganganun cytokines masu kumburi da kuma abin da ya faru na colitis.
A ƙarshe, a matsayin abu mai mahimmanci tare da babban yuwuwar, KPV yana nuna fa'idodi na musamman a cikin maganin cututtuka daban-daban. In the field of inflammatory bowel disease, whether in mouse model experiments or in the exploration of different administration methods for ulcerative colitis, KPV can effectively reduce inflammatory infiltration, improve tissue morphology, regulate cytokine expression, and exert significant anti-inflammatory effects through mechanisms such as PepT1 transport. A cikin maganin cutar mucositis na baka, hydrogel wanda ke dauke da KPV wanda aka shirya tare da takamaiman matrix da mai haɓaka adhesion ba zai iya kawai kula da ayyukanta na rigakafin kumburi da ƙaura ba amma kuma yana da ƙarfin ƙwayar cuta mai ƙarfi, yana inganta haɓakar alamun da ke da alaƙa da berayen da haɓaka gyaran nama. Kodayake shari'o'in aikace-aikacen asibiti na yanzu na KPV har yanzu suna da iyaka, sakamakon binciken da ake ciki yana nuna cikakkiyar ƙimar warkewa. A nan gaba, idan za a iya samun ci gaba a cikin bincike mai zurfi game da inganta kwanciyar hankali na miyagun ƙwayoyi da isar da isarwa, faɗaɗa alamun asibiti, da ƙarfafa kulawa da kulawa na asibiti, ana sa ran KPV zai kawo mafi inganci da ingantattun zaɓuɓɓukan magani don ƙarin marasa lafiya da kuma taka muhimmiyar rawa a cikin jiyya na asibiti.
Game da Marubuci
Abubuwan da aka ambata a sama duk bincike ne, gyara su kuma Cocer Peptides ne suka haɗa su.
Mawallafin Jaridar Kimiyya
Dalmasso G mai bincike ne a fannin likitanci, tare da kwatancen bincike da suka shafi magunguna, nazarin halittu, da kwayoyin halitta, da dai sauransu. Ya yi aiki a manyan manyan cibiyoyi, ciki har da Jami'ar Clermont Auvergne (UCA), CHU Clermont Ferrand, INRAE, Institut National de la Sante et de la Recherche Medicale (Inserm), Clermont Univ, Jami'ar Jihar Georgia, Jami'ar Emory, Jami'ar Cote d'Azur, da Universidad Nacional Rio Cuarto. Wadannan cibiyoyi sun yi suna sosai a fannonin su, kuma hadin gwiwar Dalmasso G da su ya taimaka wajen ci gaban darussa masu alaka. Sakamakon bincikensa na iya zama babban mahimmanci ga ci gaban kimiyyar likitanci, musamman wajen inganta sakamakon maganin cututtuka da ingancin rayuwar marasa lafiya. Dalmasso G an jera shi a cikin ambaton ambato [6].
▎ Abubuwan da suka dace
[1] Sun J, Xue P, Liu J, et al. Hydrogel-Cross-Cross-Linked Hydrogel na Cysteamine-Grafted γ-Polyglutamic Acid Stabilized Tripeptide KPV don Rage TNBS-Induced Ulcerative Colitis a cikin berayen[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 wanda aka samu Melanocortin yana da yuwuwar rigakafin kumburi a cikin samfuran murine na cututtukan hanji mai kumburi [J]. Cututtukan Ciwon Hanji, 2008,14 (3):324-331.DOI:10.1002/ibd.20334.
[3] Land S C. Hanawa na salon salula da tsarin kumburi a cikin ƙwayoyin epithelial na ɗan adam ta hanyar peptides masu alaka da melanocortin: tsarin aikin KPV da kuma rawar da ake yi na agonists na MC3R.[J]. Jarida ta Duniya na Ilimin Halittar Halitta, Pathophysiology da Pharmacology, 2012,4 (2): 59-73. https://pubmed.ncbi.nlm.nih.gov/22837805/
[4] Shao W, Chen R, Lin G, et al. A cikin yanayin mucoadhesive hydrogel yana ɗaukar KPV tripeptide: anti-mai kumburi, antibacterial da gyara tasirin cutar mucositis ta baka [J]. Kimiyyar Halitta, 2021,10 (1): 227-242.DOI: 10.1039/d1bm01466h.
[5] Zhao Y, Xue P, Lin G, et al. KPV mai ɗaurin hanyar sadarwa biyu na hydrogel yana dawo da shingen mucosal na hanji a cikin hanji mai kumburi [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-matsakaici tripeptide KPV yana rage kumburin hanji [J]. Gastroenterology, 2008,134 (1): 166-178.DOI:10.1053/j.gastro.2007.10.026.
DUKKANIN LABARI DA BAYANIN KYAUTATAWA DA AKE BAYAR A WANNAN SHAFIN KAWAI DOMIN WATSA BAYANI NE DA MANUFOFIN ILIMI.
Kayayyakin da aka bayar akan wannan gidan yanar gizon an yi niyya ne kawai don binciken in vitro. Binciken in vitro (Latin: *a cikin gilashi*, ma'ana a cikin gilashin gilashi) ana gudanar da shi a wajen jikin mutum. Waɗannan samfuran ba magunguna ba ne, Hukumar Abinci da Magunguna ta Amurka (FDA) ba ta amince da su ba, kuma dole ne a yi amfani da su don hanawa, magani, ko warkar da duk wani yanayi na likita, cuta, ko cuta. Doka ta haramta shigar da waɗannan samfuran cikin jikin mutum ko dabba ta kowace hanya.