Raws li bioactive peptide muab rho tawm los ntawm qhov chaw ntuj,qaub creamexerts cov teebmeem lom lom uas feem ntau poob rau hauv peb pawg loj: kev hloov kho ntawm cov lus teb inflammatory, kev kho mob cuam tshuam rau cov teeb meem, thiab toxicological profiles. Peb yam no cuam tshuam zoo thaum khaws lawv cov yam ntxwv. Lawv tsis tsuas yog hais txog qhov kev cia siab ntawm qhov kev tsim no rau kev tswj cov kab mob inflammatory, tab sis kuj txhais cov kev txwv kev nyab xeeb uas yuav tsum tau ua thaum siv cov tswv yim. Piv nrog rau lwm yam ntuj active peptides uas xa broad -spectrum teebmeem yam tsis muaj kev taw qhia tshwj xeeb, malittin nthuav tawm lub hom phiaj zoo kawg nkaus thiab sawv tawm nrog lub zog tshwj xeeb hauv kev tshawb fawb txog kev tshawb fawb thiab tiag - ntiaj teb daim ntawv thov scenarios. Daim ntawv no yuav ua ib qho kev sib tham hauv - qhov tob tob ntawm peb qhov tseem ceeb saum toj no, suav nrog cov txheej txheem ua haujlwm, cov xwm txheej siv tau zoo thiab cov yam ntxwv ntawm toxicological. Nws yog lub hom phiaj los txhais cov kev sib raug zoo ntawm cov khoom no thiab qhia txog cov txiaj ntsig ntawm meliittin rau kev tshawb fawb thiab kev siv ntxiv.



Melittin COA


Broad spectrum antibacterial clearance efficiency thiab tshuaj tiv thaiv zoo ntawm melitin
Melittin qab zibmuaj cov kab mob ua kom zoo thiab tshem tawm cov haujlwm, uas tuaj yeem tsom Gram zoo, Gram tsis zoo cov kab mob thiab cov kab mob fungi. Nws kuj tseem muaj qhov cuam tshuam loj heev rau kev kho mob ntau yam tshuaj ntau yam -cov kab mob resistant. Nws hom kev ua tshwj xeeb tsis yooj yim rau induce microbial tsis kam, muab lub tswv yim tshiab rau kev tiv thaiv thiab tswj cov tshuaj - tiv thaiv kab mob thiab tuav txoj haujlwm tseem ceeb hauv cov tshuaj tua kab mob ntuj.
Inhibition thiab Barrier Breakthrough ntawm Gram Negative Bacteria
Lub lipopolysaccharide barrier ntawm Gram tsis zoo cov kab mob ua rau lawv resistant rau feem ntau cov tshuaj tua kab mob, thiab meliittin tuaj yeem tawg los ntawm qhov teeb meem no los ntawm kev kho nws cov molecular conformation, inhibiting pathogenic kab mob xws li Escherichia coli thiab Pseudomonas aeruginosa, thiab tshuaj - resistant hom.
Nws cov txiaj ntsig zoo helical C-terminus anchors lub taub hau hydrophilic ntawm lipopolysaccharides, thiab nws hloov tau N-terminus binds phosphate pawg, cuam tshuam plasmalemmas diffusibility thiab inducing kab mob apoptosis tom qab permeation; Nws cov kev hloov kho derivative tuaj yeem txhim kho kev tiv thaiv kab mob ntxiv, tshwj xeeb tshaj yog txhawm rau txhim kho cov nyhuv tshem tawm ntawm cov tshuaj - cov kab mob resistant xws li Pseudomonas aeruginosa.
Kev loj hlob inhibition ntawm cov kab mob fungal
Melitin tuaj yeem cuam tshuam cov kab mob fungal xws li Candida albicans thiab Aspergillus, thaiv lawv cov kab mob germination, hyphal colonization, thiab kev loj hlob.
Los ntawm kev cuam tshuam nrog fungal plasmalemmas synthesis thiab homeostasis, nws cuam tshuam cov membrane kev ncaj ncees thiab ua rau cov tshuaj metabolic to, yog li inhibiting kev loj hlob los yog inducing lysis. Tsis tas li ntawd, nws muaj peev xwm inhibit fungal biofilm tsim thiab thim rov qab fungal tsis kam rau azole tshuaj.
Kev npaj tshuaj uas muajqaub creamHauv cov qauv nas tuaj yeem ua tiav cov kev kho mob mycological, ua kom pom qhov muaj peev xwm kho mob zoo.


Lub hom phiaj tshem tawm cov kab mob Gram zoo
Melitin tuaj yeem ua haujlwm ruaj khov kom tshem tawm cov kab mob Gram zoo xws li Staphylococcus epidermidis thiab Staphylococcus aureus, nrog rau cov kab mob resistant xws li MRSA thiab vancomycin resistant enterococci. Nws cuam tshuam cov homeostasis ntawm cov kab mob plasmalemmas, cuam tshuam nrog kev thauj khoom thiab lub zog metabolism, ua rau cov metabolism tsis zoo, lysis, thiab tuag ntawm cov kab mob. Kev sib koom ua ke ntawm ntau lub hom phiaj tuaj yeem zam cov tshuaj tiv thaiv los ntawm ib lub hom phiaj hloov pauv. Kev sim hauv vitro tau pom tias nws qhov tsawg kawg nkaus inhibitory concentration tiv thaiv kab mob Gram zoo yog tsawg li 12.5 μ g / mL, nrog rau qhov pib sai thiab tshem tawm zoo dua li qee cov tshuaj tua kab mob.
Cov yam ntxwv tseem ceeb ntawm cov tshuaj tiv thaiv qis
Meliittin tsis yooj yim rau induce microbial tsis kam, uas txawv ntawm ib lub hom phiaj ntawm cov tshuaj tua kab mob. Nws ua rau cov kab mob sib kis los ntawm ntau lub hom phiaj thiab txoj hauv kev, ua rau nws nyuaj rau cov kab mob kom yoog los ntawm cov noob hloov pauv. Cov kev sim tau pom tias tom qab 21 hnub ntawm cov tshuaj tiv thaiv induction, qhov tsawg kawg nkaus inhibitory concentration tsuas yog nce me ntsis, thiab lub peev xwm ntawm cov tshuaj tiv thaiv induction yog qis dua li cov tshuaj tiv thaiv kab mob. Kev siv lub sij hawm ntev tseem tuaj yeem tswj cov kab mob tiv thaiv kab mob ruaj khov.
Qhov no lub hom phiajmob phemplasmalemmas tsis muaj kev sib kho receptor
Kev txheeb xyuas cia siab rau lub cev thiab tshuaj lom neeg ntau dua li cov protein receptors
Lub hom phiaj khi ntawmqaub creamtsis vam khom rau kev lees paub thiab ua kom cov protein receptors tshwj xeeb rau ntawm qhov chaw ntawm malignancy cytocyte. Nws cov txheej txheem anchoring cia siab rau ob qho tib si physicochemical rog: electrostatic adsorption thiab hydrophobic kev sib cuam tshuam, tsis tas yuav tsum muaj plasmalemmas receptors los koom rau hauv kev paub txog teeb liab, kev sib txuam, thiab kev sib khi ua ke, yog li tsim kev ywj pheej ntawm receptor mediated dependency tej yam kev mob.
Lub hom phiaj yog cov qauv lipid thiab tsis koom nrog cov receptor protein
Cov hom phiaj tseem ceeb xav tau kev khi rau daim nyias nyias cov protein receptors kom siv tau, thaum mellittin lub hom phiaj kev lees paub yog cov kua qaub lipids (phosphatidylserine) uas txawv txav hauv cov kab mob plasmalemmas, uas yog cov txheej txheem ntawm cov lipid membrane thiab tsis ua haujlwm receptor proteins. Cov lipid no tau nthuav dav rau sab nraud ntawm cov kab mob malignancy cytocyte thiab tuaj yeem khi ncaj qha yam tsis muaj kev pab ntawm receptors.


Hom kev ua yog tsis yog - tshwj xeeb adsorption ntawm lub cev, tsis muaj teeb liab dependence
Receptor mediated binding yuav tsum muaj qhov sib txuam ligand receptor txuam, downstream teeb liab ua kom muaj zog, thiab qhov tshwj xeeb siab; Thiab mellittin yog ib qho dav -spectrum lub cev chimeric hom, tso siab rau nws cov amphiphilic physicochemical zog rau ncaj qha thauj tog rau nkoj rau txawv txav thiab lipid qauv ntawm cov qog nqaij hlav plasmalemmas, tsis tas yuav tsum tau rau cytocyte los muab cov kev lees paub ntawm receptor systems, yog li tsis muaj receptor kev koom tes thoob plaws hauv cov txheej txheem.
Zam kev txwv qhov sib txawv ntawm cov receptors thiab hloov mus rau dav -spectrum tiv thaiv- cov khoom mob qog noj ntshav
Muaj cov subtypes thiab sib txawv qhia qib ntawm cov protein receptors hauv qog noj ntshav cytocyte, thiab cov kab mob lipid txawv txav yog ib qho ntawm feem ntau cov qog nqaij hlav cancer.Melittin qab zibtsis vam khom rau receptor mediation thiab tsis cuam tshuam los ntawm kev hloov pauv hauv receptor qhia. Nws ruaj khov khi rau ntau yam malignancy plasmalemmas, uas yog nyob rau hauv txoj kab nrog nws dav -spectrum muaj peev xwm mus lyse cancer cytocyte.
Kev tshuaj xyuas qhov tsis txaus ntawm ib qho kev tiv thaiv -malignancy hom ntawm kev ua thiab qhov zoo sib xws ntawm nws
(I) Ua tsis tiav ntawm kev cia siab ib leeg ntawm lub cev daim nyias nyias tawg
Ib hom kev tua kabmob kheesxaws tsuas yog los ntawm kev rhuav tshem cov qauv plasmalemmas belongs rau kev tua lub cev tsis muaj zog, nrog qhov pom tseeb:
- 1. Muaj qhov kev txwv rau kev tua: hom no tsuas yog ua haujlwm ntawm qhov chaw thiab cov kab mob malignancy cytocyte nyob rau hauv siab concentration tshuaj ua. Rau malignancy cytocyte raug tsis tshua muaj concentration, nyob rau hauv ib tug dormant lub xeev, thiab muaj zog daim nyias nyias qauv stability, nws yog ib qho nyuaj rau tag nrho rhuav tshem thiab tshem tawm lawv, thiab nws muaj feem yuav tawm hauv cov qog nqaij hlav ciaj sia.
- 2. Tsis muaj peev xwm tshem tawm qhov muaj peev xwm rau kev loj hlob ntawm malignancy: Lub cev lysis tsuas tuaj yeem rhuav tshem cov qauv cytocyte, ua rau mob cytocyte necrosis, thiab tsis tuaj yeem cuam tshuam rau hauv cov noob caj noob ces thiab apoptosis tswj txoj hauv kev hauv cov hlwb malignancy. Ib qho me me ntawm cov kab mob qog noj ntshav cytocyte tuaj yeem kho cov kab mob sai sai, rov ua kom muaj peev xwm, thiab ua rau cov qog rov ua dua.
- 3. Homogenization thiab tsis tsom mus rau qhov tob ntawm cov nyhuv: ntshiab daim nyias nyias uas tsis muaj phiaj xwm tua ntawm qib molecular tswj tsuas tuaj yeem ua tiav cov kab mob tua kab mob thiab ua kom tsis muaj menyuam, tab sis tsis tuaj yeem thaiv cov txheej txheem tseem ceeb ntawm cov qog nqaij hlav cancer cytocyte proliferation thiab ntxeem tau ntawm qib molecular, thiab cov tshuaj tiv thaiv - cov nyhuv qog yog superficial thiab tsis kav ntev.


(II) Shortboard ntawm kev cia siab ib leeg rau ib qho txiaj ntsig ntawm inducing cell apoptosis
Ib hom tshuaj pharmacological ntawm kev ua rau mob qog nqaij hlav ntawm tes apoptosis nkaus xwb los ntawm txoj hauv kev molecular yog hom tseem ceeb ntawm kev txiav txim ntawm cov tshuaj tiv thaiv kab mob loj, tab sis nws muaj cov kev txwv hauv keeb kwm:
- 1. Muaj kev vam meej ntawm lub hom phiaj qhia: Apoptosis induction cia siab rau kev tswj hwm molecular xws li txoj hauv kev mitochondrial thiab txoj kev tuag receptor. Yog hais tias malignancy cytocyte undergo lub hom phiaj kev hloov pauv lossis txoj hauv kev ntsiag to, lawv yuav ncaj qha txhim kho cov tshuaj tiv thaiv, ua rau ua tiav cov tshuaj tsis ua tiav.
- 2. Kev pib qeeb qeeb thiab tsis muaj tshuaj tua kab mob thiab ua kom tsis muaj menyuam: Apoptosis yog txheej txheem kev tuag qeeb, uas yuav tsum muaj kev cuam tshuam los ntawm kev ua haujlwm xws li teeb liab ua kom muaj zog, kev tswj hwm cov protein, kev qhia cov noob thiab lwm yam. Nws tsis tuaj yeem tswj tau sai sai ntawm kev loj hlob ntawm malignancy cytocyte, thiab nws yog ib qho nyuaj rau tiv nrog cov yam ntxwv pathological ntawm kev loj hlob sai thiab nthuav dav ntawm cov qog nqaij hlav cancer.
- 3. Kev cuam tshuam loj heev los ntawm cellular microenvironment: Lub hypoxia, o, thiab metabolic ntshawv siab nyob rau hauv cov qog microenvironment tuaj yeem inhibit apoptosis signaling, ua rau tsis muaj zog tiv thaiv -malignancy effect induced by single apoptosis, and lead to cancer cytocyte escaping and surviving.
Cov ntaub ntawv
Yang H, Ma R, Chen JR, et al. Discovery of melttin as Triple-Action Agent: Broad-Spectrum Antibacterial, Anti-Biofilm, thiab Potential Anti-Quorum Sensing Activities. Molecules, 2024, 29(3): 558.
Zhang Yan, Li Min, Wang Hao Txoj kev tshem tawm thiab kev sim kev tshawb fawb ntawm melttin tiv thaiv Gram zoo tshuaj -cov kab mob resistant Journal of Microbiology, 2024, 64 (2): 789-798
Synergistic Anti-Cancer Activity ntawm Melttin thiab Erlotinib hauv Tsis yog-Me me cytocyte Lung malignancy (https://pmc.ncbi.nlm.nih.gov/articles/PMC11989111/)
Melttin Inhibits Colorectal Cancer Loj hlob thiab Metastasis los ntawm Ac-Tivating lub Mitochondrial Apoptotic Pathway thiab Suppressing Epithelial-Mesenchymal Transition thiab Angiogenesis (https://pmc.ncbi.nlm.nih.gov/articles/PMC11546240/)
FAQ
Melittiin tuaj yeem ua rau mob tonic thiab mob peripheral. Kev txhaj tshuaj hauv zos nrog mellittin tuaj yeem ua rau hyperalgesia, allodynia thiab inflammatory teb nyob rau hauv qhov chaw txhaj tshuaj (161). Mellittin txhim kho qhov excitability ntawm spinal nociceptive neurons.
Txawm li cas los xij, mellittin muaj ntau qhov zoo ntawm cov amino acid residues hauv nws cov qauv molecular. Cov pab pawg them nyiaj no tso cai rau peptide tuaj yeem cuam tshuam ncaj qha nrog lipid bilayers thiab tsim cov txheej txheem transmembrane nyob rau saum npoo ntawm plasmalemmas. Qhov kev puas tsuaj no inevitably ua rau pom tseeb hemolysis ntawm cov ntshav liab cytocyte. Meanwhile, mellittin kuj exerts tsis yog - tshwj xeeb cytotoxicity tawm tsam ib txwm somatic hlwb. Cov kev tsis zoo tshuaj lom neeg zoo li no tau dhau los ua qhov tseem ceeb, txwv tsis pub nws txoj kev loj hlob ntxiv thiab dav - ntau yam kev siv tshuaj kho mob.
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