Indolicidinyog luv peptide nrog cov tshuaj tua kab mob, koom nrog ib hom tshuaj tiv thaiv kab mob ntuj peptide. Tsim los ntawm 13 amino acid residues, cov amino acids no txuas ua ke los ntawm peptide daim ntawv cog lus los tsim cov saw hlau peptide. Hauv kev daws teeb meem, nws nthuav tawm helical conformation uas pab txhawb nws kev sib cuam tshuam nrog lwm cov molecules lossis cellular qauv. Vim nws qhov tshwj xeeb amino acid muaj pes tsawg leeg thiab ib ntus, nws tuaj yeem xaiv khi rau lub hom phiaj hauv cov kab mob, yog li siv nws cov tshuaj tua kab mob. Nyob rau hauv cov xwm txheej tsim nyog, nws tuaj yeem tswj tau qhov ruaj khov ntawm nws cov qauv thiab kev ua haujlwm. Txawm li cas los xij, ntawm qhov kub siab dua, nws cov ntawv cog lus peptide tuaj yeem cuam tshuam, ua rau kev hloov pauv ntawm cov qauv thiab tsis ua haujlwm. Yog li ntawd, hauv kev tshawb fawb thiab kev siv, nws yog ib qho tsim nyog los tswj qhov kev sim ntsuas kub kom ntseeg tau tias nws ruaj khov thiab ua haujlwm. Raws li ib tug natural antimicrobial peptide, nws muaj ntau yam haujlwm xws li tshuaj tua kab mob, tiv thaiv kab mob, tiv thaiv qog, thiab tshuaj tua kab mob.
Customized Bottle Caps & Corks
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Tshuaj Formula |
C100H132N26O13 |
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Exact Mass |
1905 |
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Molecular Luj |
1906 |
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m/z |
1906 (100.0%), 1905 (92.5%), 1907 (39.5%), 1907 (14.0%), 1908 (10.8%), 1907 (9.6%), 1906 (8.9%), 1908 (7.2%), 1909 (4.3%), 1908 (3.8%), 1908 (2.7%), 1907 (2.5%), 1907 (1.5%), 1909 (1.4%), 1906 (1.4%), 1908 (1.3%), 1909 (1.0%) |
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Elemental Analysis |
C, 63.01; H, 6.98; N, 19.10; O, 10.91 |
antibacterial kev ua haujlwm
Indolicidinnthuav tawm dav-spectrum antibacterial kev ua si tawm tsam ntau yam kab mob, nrog rau ntau yam kab mob aerobic Gram-negative, kab mob Gram-positive, thiab fungi. Qhov dav spectrum ntawm kev ua ub no ua rau nws yog ib tus neeg sib tw rau kev kho mob antimicrobial.
Membrane Permeabilization
Cov qauv tshuaj tshwj xeeb, nplua nuj nyob rau hauv tryptophan residues thiab nrog ib qho amidated carboxyl terminus, tso cai rau nws nkag mus rau cov kab mob cell membranes thiab cuam tshuam lawv kev ncaj ncees. Qhov no ua rau efflux ntawm cov kab mob, thaum kawg ua rau cov kab mob tuag.
DNA Binding thiab Inhibition ntawm Replication
Cov kev tshawb fawb tau pom tias nws tuaj yeem khi rau ob-helical DNA, muaj peev xwm inhibiting ntau cov enzymes ntsig txog DNA ua. Tshwj xeeb, PW-WP structural motif nyob rau hauv nruab nrab ntawm lub kaum peb-peptide yog ib tug tshwj xeeb structural yam uas yuav envelop B-daim DNA ob helix, txhim khu nws stability thiab inhibiting DNA replication thiab transcription.
Kev sim hauv vitro tau pom tias nws muaj peev xwm tua kab mob siab, nrog ze-ua tiav tua cov kab mob xws li Escherichia coli thiab Staphylococcus aureus. Qhov kev ua tau zoo no qhia txog nws lub peev xwm ua tus neeg sawv cev antimicrobial.
Kev txwv & Derivative Development
Txawm hais tias nws cov tshuaj tua kab mob tseem ceeb, daim ntawv thov kev kho mob tsuas yog txwv vim nws cytotoxicity rau cov qe ntshav liab, uas tuaj yeem ua rau hemolysis yooj yim. Tsis tas li ntawd, nws txoj kev sib raug zoo siab rau kev khi rau saum npoo lipopolysaccharides, thaum txhawb nqa nws cov nyhuv antibacterial, kuj tseem tuaj yeem ua rau kev txhim kho cov tshuaj tiv thaiv hauv qee yam kab mob.
Txhawm rau kov yeej cov kev txwv no, cov kws tshawb fawb tau tsim ntau yam khoom siv thiab analogs. Piv txwv li, Indolicidin acetate thiab Indolicidin TFA yog cov derivatives tau los ntawm kev hloov kho tshuaj uas tswj cov kab mob tua kab mob thaum txo cov tshuaj lom rau cov qe ntshav liab. Tsis tas li ntawd, qee qhov kev tshawb fawb tau sim txhim kho cov kab mob tua kab mob thiab txo cytotoxicity los ntawm kev hloov cov amino acid ib ntus, xws li X-indolicidin, uas yog tsim los ntawm oxidizing ob indole nplhaib sab chains thiab khaws tib cov amino acid ib ntus thiab cov kab mob tua kab mob thaum tiv taus. rau proteases.
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Antiviral teebmeem
Indolicidinkuj qhia tau hais tias cov tshuaj tiv thaiv kab mob, tshwj xeeb tshaj yog tawm tsam qee yam kab mob xws li HIV-1 thiab tus kab mob herpes simplex. Nws cov tshuaj tiv thaiv kab mob sib txawv me ntsis ntawm nws cov tshuaj tiv thaiv kab mob. Cov kev tshawb fawb tau pom tias nws tuaj yeem khi ncaj qha rau DNA, cuam tshuam nrog kev tsim cov kev sib xyaw ua ke-DNA complexes tsis yog khi rau kev sib koom ua ke nws tus kheej. Qhov kev khi no tuaj yeem cuam tshuam ntau yam enzymes cuam tshuam nrog DNA ua, yog li inhibiting viral replication.
HIV-1 Inhibition
Nws tau pom tias inhibit HIV-1 rov ua tau zoo. Cov tshuaj tiv thaiv kab mob xav tau ntau dua li qhov ua rau cov kab mob tua kab mob thiab tshuaj tua kab mob. Piv txwv li, qhov concentration ntawm 333 ug / ml tuaj yeem cuam tshuam HIV -1, nrog rau IC50 tus nqi xws li 67 mus rau 100 ug / ml ntawm 37 degree . Kev cuam tshuam rau nws rau 5 feeb ntawm 37 degree tuaj yeem cuam tshuam 50% ntawm tus kab mob HIV replication, thaum ua tiav cov tshuaj tiv thaiv kab mob yuav tsum tau kwv yees li 60 feeb.
Mechanism ntawm Action
Kev tshawb fawb qhia tias nws khi rau DNA, tshwj xeeb yog PW-WP tus qauv tsim nyob rau hauv indolicidin kaum peb-peptide, uas tuaj yeem qhwv ib ncig ntawm B-daim DNA ob lub helix, txhim kho nws txoj kev ruaj ntseg thiab inhibiting DNA replication thiab transcription. Qhov kev sib khi muaj peev xwm no yog qhov tseem ceeb rau nws txoj haujlwm tiv thaiv kab mob.
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Immunomodulatory teebmeem
Indolicidintau pom tias yuav txhawb lub cev tiv thaiv kab mob, pab lub cev zoo tiv thaiv kab mob thiab kab mob. Qhov no yog vim nws lub peev xwm los cuam tshuam nrog lub cev tiv thaiv kab mob thiab txhawb nqa lawv kom muaj zog tiv thaiv.
Cytokines yog qhov taw qhia cov molecules uas ua lub luag haujlwm tseem ceeb hauv kev tiv thaiv kab mob. Nws tuaj yeem cuam tshuam rau kev tsim cov cytokines, xws li interleukins thiab chemokines, uas koom nrog hauv orchestrating lub cev tiv thaiv kab mob. Los ntawm kev hloov kho cytokine milieu, nws tuaj yeem hloov lub cev tiv thaiv kab mob mus rau lub xeev zoo dua rau kev tawm tsam cov kab mob lossis qog.
Innate immune cells, xws li neutrophils, macrophages, thiab natural killer (NK) cells, yog thawj kab ntawm kev tiv thaiv kab mob. Nws tuaj yeem txhim kho cov haujlwm ntawm cov hlwb no, ua rau lawv muaj txiaj ntsig zoo ntawm kev tua cov kab mob lossis tsom mus rau cov hlwb txawv txav.
Txawm hais tias qhov cuam tshuam ncaj qha rau kev tiv thaiv kab mob (T thiab B cov lus teb ntawm tes) tsis tau kawm ntau, nws lub peev xwm los hloov kho cov tshuaj tiv thaiv kab mob hauv lub cev tuaj yeem cuam tshuam tsis ncaj qha rau kev tiv thaiv kab mob. Piv txwv li, los ntawm kev txhim kho kev ua kom thiab kev tsiv teb tsaws ntawm cov hlwb dendritic, nws tuaj yeem txhawb kev tsim cov tshuaj tiv thaiv kab mob tshwj xeeb T cell.
Ntxiv nrog rau nws cov kev ua haujlwm ncaj qha los tiv thaiv kab mob, nws kuj muaj cov tshuaj tiv thaiv kab mob. Qhov no yog qhov tseem ceeb hauv kev tiv thaiv kev mob ntau dhau, uas tuaj yeem ua rau cov ntaub so ntswg thiab lub cev puas tsuaj. Los ntawm kev tswj cov kab mob inflammatory, nws txhawb nqa kev tiv thaiv kab mob homeostasis.
Kev daws zaum kawg
Adjuvant Therapy hauv Cov Kab Mob Sib Kis
Los ntawm kev txhim kho lub cev tiv thaiv kab mob, nws tuaj yeem siv los ua kev kho mob ntxiv los txhim kho kev ua tau zoo ntawm cov tshuaj tua kab mob lossis tshuaj tiv thaiv.
Kev kho mob autoimmune
Los ntawm kev hloov kho lub cev tiv thaiv kab mob, nws yuav muaj txiaj ntsig zoo hauv kev kho mob ntawm cov kab mob autoimmune, xws li mob caj dab rheumatoid lossis kab mob lupus erythematosus, qhov twg lub cev tiv thaiv kab mob tawm tsam cov ntaub so ntswg noj qab haus huv.
Kev Kho Mob Cancer
Txawm hais tias cov tshuaj tiv thaiv kab mob ncaj qha tsis tau ua pov thawj pom tseeb, nws cov cuab yeej immunomodulatory tuaj yeem siv los txhim kho tus tswv tsev cov tshuaj tiv thaiv kab mob.
Indolicidinyog ib tug muaj zog antimicrobial peptide purified los ntawm cytoplasmic granules ntawm bovine neutrophils. Nws yog ib qho ntawm qhov tsawg tshaj plaws paub cov kab mob tua kab mob peptides, muaj tsuas yog 13 amino acids los ntawm 6 ntau hom. Qhov peptide no yog tus cwj pwm los ntawm nws cov ntsiab lus siab ntawm tryptophan residues (39%) thiab proline residues (23%), ua rau nws yog ib qho ntawm cov peptides nrog cov ntsiab lus tryptophan siab tshaj plaws hauv tsev neeg Catholicidins.
Nws nta cov qauv tshuaj tshwj xeeb nrog amidated carboxyl termini, uas ua rau nws muaj zog tiv thaiv kab mob. Nws qhia tau hais tias muaj peev xwm bactericidal siab hauv vitro, muaj peev xwm yuav luag tag nrho tua kab mob xws li Escherichia coli thiab Staphylococcus aureus. Tsis tas li ntawd, nws nthuav tawm dav dav ntawm cov tshuaj tiv thaiv kab mob, inhibiting parasites thiab kab mob, suav nrog Human Immunodeficiency Virus (HIV-1) thiab Herpes Simplex Virus. Nws cov tshuaj tiv thaiv kab mob cuam tshuam ncaj qha rau DNA, yog li inhibiting kev tsim ntawm intgrase-DNA complexes thiab impeding DNA replication thiab transcription.
Txawm hais tias nws cov txiaj ntsig zoo antimicrobial, daim ntawv thov kev kho mob tsuas yog txwv vim nws cov haujlwm hemolytic thiab muaj peev xwm ua rau muaj kev tiv thaiv kab mob. Cov kws tshawb fawb tau tsim cov derivatives thiab analogs los daws cov kev txwv no, xws li Indolicidin acetate thiab Indolicidin TFA, uas tswj cov tshuaj tua kab mob thaum txo cov tshuaj lom rau cov ntshav liab.
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