Poyang'anizana ndi matenda omwe akuchulukirachulukira owopsa a mabakiteriya osamva mankhwala ambiri, kupita patsogolo kwa mankhwala omwe akuwunikiridwa kumakopa chidwi cha asayansi. Zoyang'ana masiku ano, Murepavadin (CAS: 944252-63-5), ndiye buku la antimicrobial lopangidwira kuthana ndi matenda a Pseudomonas aeruginosa. Kachitidwe kake kapadera kachitidwe komanso kulunjika kwapadera kwateteza malo ake apamwamba pa kafukufuku wokhudzana ndi machiritso olimbana ndi mabakiteriya.
Monga cyclic peptide antibiotic yopangidwa ndi 14 amino acid, mwayi wofunikira kwambiri wa murepavadin umakhala pakukhazikika kwake. Imalunjika ndendende LptD, lipopolysaccharide yonyamula puloteni D mu nembanemba yakunja ya Pseudomonas aeruginosa. Poletsa kuyika kwa lipopolysaccharides ku nembanemba yakunja, kumasokoneza kukhulupirika kwa envelopu ya bakiteriya, ndipo pamapeto pake kumabweretsa kufa kwa bakiteriya. Njira yomwe imayang'aniridwa iyi sikuti imangopewa njira zachikhalidwe zolimbana ndi maantibayotiki komanso zimachepetsa kusokonezeka kwa ma microbiota amunthu, ndikuthana bwino ndi vuto lakusalinganika kwa m'mimba komwe kumakhudzana ndi maantibayotiki ambiri.
Deta ya sayansi yatsimikizira kwa nthawi yayitali zochita zake zolimbana ndi mabakiteriya: M'kafukufuku wambiri mu vitro murepavadin inasonyeza MIC₅₀ ndi MIC₉₀ yotsika kwambiri mpaka 0.12 mg/L motsutsana ndi Pseudomonas aeruginosa. Idalepheretsa 99.1% yazachipatala zopitilira 1,200 zosonkhanitsidwa kuchokera ku US, Europe, ndi China, kuwonetsa zochitika 4 mpaka 8 kuposa zomwe polymyxin B ndi colistin. Mu zitsanzo za matenda a murine, mlingo wochokera ku 2 mpaka 10 mg / kg umakhala ndi moyo wapamwamba mpaka 100% pambuyo pa matenda pamene amachepetsa kwambiri mabakiteriya m'magazi ndi peritoneal fluid. Makamaka, imakhalabe yogwira ntchito motsutsana ndi carbapenem-, colistin-, ndi mitundu ina yosamva mankhwala, yopereka njira yatsopano yothanirana ndi matenda a XDR (osamva mankhwala kwambiri).
Kafukufuku waposachedwa wawonetsanso kuthekera kwake kochizira: Kuchulukira kwa murepavadin kumatha kupititsa patsogolo mphamvu ya bakiteriya yakunja kwa membrane, kuwongolera mphamvu ya bakiteriya ya maantibayotiki a β-lactam. Kuphatikizikako sikunangowonetsa zotsatira zochiritsira zachibayo mumitundu yayikulu yachibayo komanso kuchedwetsa kukula kwa maantibayotiki kukana. Kuphatikiza apo, monga chitetezo cha peptide mimetic, imayambitsa ntchito za immunomodulatory za mast cell, kuthandizira wolandirayo kuchotsedwa kwa mabakiteriya ndi kukonza minofu - kukwaniritsa zotsatira ziwiri za "antibacterial action + immune modulation".
Pakalipano, Murepavadin ali m'mayesero achipatala a Phase III, makamaka akuyang'ana chibayo chopezeka m'chipatala ndi chibayo chokhudzana ndi mpweya wabwino chomwe chimayambitsidwa ndi Pseudomonas aeruginosa. Panthawi yomwe matenda a bakiteriya osamva mankhwala akuwopseza thanzi la anthu padziko lonse lapansi, mankhwala atsopanowa, omwe amadziwika ndi kutsimikizika kwake, mphamvu zake, komanso kawopsedwe kakang'ono, mosakayikira amabweretsa chiyembekezo chatsopano chachipatala. Kafukufuku wokhudzana ndi izi akupita patsogolo mosalekeza, ndipo tikuyembekeza kuti posachedwa adzasintha kukhala chithandizo chamankhwala chomwe chilipo, ndikuwonjezera chida chachikulu cholimbana ndi matenda osamva mankhwala.
Nthawi yotumiza: 2026-02-09