Bya Cocer Peptides 
omwezi gumu emabega
EBINTU BYONNNA N’AMAWULIRE GW’EBINTU EBIweereddwa KU MUTINDO GUNO BIKOZESEBWA KU KUSASANYA AMAWULIRE N’EBIKOLWA BY’OKUSOMESA.
Ebintu ebiweereddwa ku mukutu guno bigendereddwamu kunoonyereza mu kisenge (in vitro research) byokka. Okunoonyereza mu vitro (Olulattini: *mu ndabirwamu*, ekitegeeza mu bikozesebwa mu ndabirwamu) kukolebwa ebweru w’omubiri gw’omuntu. Ebintu bino si bya ddagala, tebikkiriziddwa kitongole kya Amerika ekivunaanyizibwa ku by’emmere n’eddagala (FDA), era tebirina kukozesebwa kuziyiza, kujjanjaba oba kuwonya mbeera yonna ya bujjanjabi, bulwadde oba bulwadde. Kikugirwa nnyo mu mateeka okuyingiza ebintu bino mu mubiri gw’omuntu oba ebisolo mu ngeri yonna.
Dermorphin ye opioid peptide ey’amaanyi eyawulwa okuva mu lususu lw’ebika by’ebikere ebimu.
Enkola y’ebikolwa bya Dermorphin mu kukendeeza obulumi
Enkolagana n’aba Opioid Receptors
Dermorphin okusinga ekola ebikolwa byayo eby’okukendeeza obulumi ng’ekwatagana n’ekirungo kya μ-opioid receptor (MOP). μ-opioid receptor ye mmemba omukulu mu famire ya opioid receptor era ekola kinene mu kukyusa obulumi. Dermorphin ne analogues zaayo zisobola okwesiba mu ngeri ey’enjawulo ku MOP receptor, okufaananako ekisumuluzo ekiyingira mu kkufulu, bwe kityo ne zikola amakubo g’obubonero wansi. [Cys (ATTO 488) 8] Dermorphin - NH2 (DermATTO488), analog ya Dermorphin eya fluorescent empya eyesigamiziddwa ku ATTO488, yeekwata ku butoffaali bwa HEK ne CHO obulaga ebikwata MOP by’omuntu era eraga engeri y’okusiba efaanagana ne Dermorphin. Kisitula okusiba kwa puloteyina ya G, kitumbula okusiba kwa GTPγ[35S], bwe kityo ne kikola okutambuza obubonero obukwatagana, era okukkakkana nga kiziyiza okutambuza obubonero bw’obulumi. Dermorphin era esitula ERK1/2 phosphorylation, okwongera okukwata ku nkola z’ebiramu mu butoffaali n’okwetaba mu kulungamya ebikolwa by’okukendeeza obulumi.
Okuziyiza okutambuza obubonero bw’obulumi ku ddaala ly’omugongo
Okunoonyereza okugezesa kulaga nti Dermorphin eziyiza nnyo okutambuza obubonero bw’obulumi ku ddaala ly’omugongo. Mu kugezesa, okufuyira 0.16 mg/kg Dermorphin mu misuwa kwaleeta okweyongera okw’amaanyi era okuwangaala mu nociceptive flexion reflex threshold mu bannakyewa abalamu, era ekikolwa kino kyali kyeyoleka kyenkanyi mu bantu abalina obuvune obujjuvu obw’omugongo obutawona, ekiraga nti Dermorphin okusinga eziyiza okutambuza nociceptive ku ddaala ly’omugongo. Enkola eno ey’okukola eyinza okuba nga yeekuusa ku Dermorphin okulungamya okufulumya obusimu obutambuza obusimu munda mu mugongo oba okukola kwayo obutereevu ku busimu bw’omugongo. Omugongo gukola ng’ekifo ekikulu eky’okutambuza obubonero bw’obulumi, era okukyusakyusa kwa Dermorphin ku nkola yaago kuziyiza bulungi okutambuza obubonero bw’obulumi okudda waggulu ku bwongo, bwe kityo ne kituuka ku bikolwa eby’okukendeeza obulumi.
Engeri ez’enjawulo ez’ekikolwa ky’ebikwata
Newankubadde naloxone esobola okuziyiza ddala ebikolwa bya morphine ne opioid analogs, esobola okuzzaawo ekitundu kyokka (nga 50%) okuzzaawo Dermorphin’s inhibitory effect ku nociceptive spinal reflexes. Kino kiraga nti Dermorphin ekwatagana n’ebibinja eby’enjawulo eby’ebikwata opioid mu mugongo nga ereeta eddagala eriweweeza ku bulumi, era enkola yaayo ey’okukola eyawukana ku y’eddagala ery’ekinnansi erya opioid. Engeri eno ey’okukola egaba ebirungi ebimu mu kukozesa eddagala eriweweeza ku bulumi, gamba ng’okukendeeza ku bikolwa eby’obubi ebya bulijjo ebikwatagana n’eddagala ery’ekinnansi erya opioid.
Enkola y’eddagala eriweweeza ku bulumi erya Dermorphin mu kugezesa ebisolo
Effective Analgesia mu bikolwa by’ebisolo ebingi
Mu bikolwa eby’enjawulo eby’obulumi bw’ebisolo, Dermorphin yalaga ebikolwa eby’amaanyi eby’okukendeeza obulumi. Mu kugezesa nga tail-flick, hot plate, tail pinch, formalin, ne acetic acid writhing tests, okuweebwa Dermorphin mu lubuto ne peptides ezikwatagana nayo kyakendeeza ku buwulize bw’ebisolo ku bulumi era ne kyongera ku miwendo gy’obulumi bwabyo. Okugezesa kuno kwakoppa obulumi obwa diguli n’ebika eby’enjawulo, nga bikakasa mu bujjuvu obusobozi bwa Dermorphin obw’okukendeeza obulumi. Mu kugezesebwa kwa hot plate, oluvannyuma lw’okuwa ebisolo Dermorphin, ekiseera eky’okusirika okukomba ebiwaawaatiro oba okubuuka kyali kiwanvu nnyo, ekiraga nti obulumi bwanafuye eri okusikirizibwa kw’ebbugumu, bwe kityo ne kiraga nti Dermorphin ekola bulungi nnyo mu kukendeeza obulumi.
Ebirungi Ebigeraageranyizibwa Ku ddagala eddala eriweweeza ku bulumi
Bw’ogeraageranya n’eddagala ery’ekinnansi eriweweeza ku bulumi nga morphine, Dermorphin eraga ebirungi bingi mu bintu ebimu. Mu bikolwa by’ebisolo, oluvannyuma lw’okuweebwa mu bwongo, Dermorphin yalaga ebikolwa eby’okulonda era eby’amaanyi eby’okukendeeza obulumi okusinga morphine, ng’ekola okumala ebbanga eddene. Ebimu ku bikozesebwa mu kukola Dermorphin tetrapepetides nabyo byalaga nti bikola nnyo okukendeeza obulumi, nga bikola amaanyi g’okukendeeza obulumi emirundi nga 1,500 n’emirundi 17 egya morphine oluvannyuma lw’okuweebwa mu bwongo oba wansi w’olususu mu mbeba, mu kulondako. Ebirungi bino biwa essuubi erisuubiza okukozesa Dermorphin mu bujjanjabi mu ddagala eriweweeza ku bulumi, ekiyinza okukola ku bbula ly’eddagala ery’ekinnansi eriweweeza ku bulumi, gamba ng’obutakola bulungi bwa ddagala eriweweeza ku bulumi oba ebbanga lye limala.
Okunoonyereza n’Okukozesa Okunoonyereza ku Dermorphin mu Bantu
Ebyava mu kugezesebwa mu bujjanjabi nga bukyali
Mu 1985, okugezesebwa okwakolebwa mu ngeri ey’ekifuulannenge, okwafugibwa placebo ku nkozesa ya Dermorphin ku bulumi oluvannyuma lw’okulongoosebwa kwalaga nti Dermorphin eyaweebwa ng’ayita mu mpiso mu nnyindo yasinga nnyo placebo ne morphine (ekozesebwa ng’ekirungo ekijuliziddwa) mu ngeri y’obulungi bw’eddagala eriweweeza ku bulumi. Okunoonyereza kuno okw’amaanyi kwawa obujulizi obukulu obuwagira okukozesa Dermorphin mu bujjanjabi mu ddagala eriweweeza ku bulumi, nga kulaga obusobozi bwayo obw’amaanyi mu kuddukanya obulumi oluvannyuma lw’okulongoosebwa.
Ensonga eziyinza okukolebwa
Enzirukanya y’obulumi oluvannyuma lw’okulongoosebwa: Obuvune obuva mu kulongoosa buyinza okuleeta obulumi obw’amaanyi oluvannyuma lw’okulongoosebwa, ekikosa nnyo abalwadde okuwona n’omutindo gw’obulamu. Obulung’amu bwa Dermorphin obwalaze mu kukendeeza obulumi oluvannyuma lw’okulongoosebwa mu kugezesebwa okw’obujjanjabi okusooka bugiteeka ng’enkola empya esuubiza ey’okukendeeza obulumi oluvannyuma lw’okulongoosebwa. Bw’ogeraageranya n’eddagala ery’ekinnansi eriweweeza ku bulumi oluvannyuma lw’okulongoosebwa, enkola yaayo ey’enjawulo ey’okukola n’ebirungi byayo —gamba ng’okukendeeza ku bulabe bw’okugumiikiriza eddagala n’okwesigamira —biwa abalwadde eddagala eriweweeza ku bulumi erisingako obukuumi era erikola obulungi.
Obujjanjabi bw’obulumi obutawona: Ku balwadde abalina obulumi obutawona naddala abo abataddamu bulungi ddagala eriweweeza ku bulumi ery’ekinnansi oba abafuna ebizibu ebinene, Dermorphin eyinza okukola ng’obujjanjabi obulala obw’omuwendo. Mu kuddukanya obulumi obutawona mu balwadde ba kookolo, enkola z’obujjanjabi eziriwo kati zikyalina obuzibu obumu. Okujja kwa Dermorphin kuleeta essuubi eppya eri omuwendo guno ogw’abalwadde. Ebikolwa byayo eby’okukendeeza obulumi ebiwangaala bisobola bulungi okufuga obulumi obutasalako mu balwadde ba kookolo n’okutumbula omutindo gw’obulamu bwabwe.
Obulabirizi obukkakkanya obulumi: Mu bifo eby‟obujjanjabi obukkakkanya obulumi, okukendeeza ku bulumi bw‟abalwadde kye kisinga okukulembezebwa. Dermorphin’s potent analgesic properties zigifuula esuubiza okukendeeza ku bulumi ku nkomerero y’obulamu mu bujjanjabi obukkakkanya obulumi. Okuyita mu nkola entuufu ey’okugaba n’okutereeza ddoozi, esobola okuyamba abalwadde okukendeeza ku kubonaabona n’okwongera okubudaabudibwa mu mitendera egy’enkomerero egy’obulamu.
Mu bufunzi
Ng’ekintu ekirina enkola ey’enjawulo ey’okukendeeza obulumi n’ebikolwa eby’amaanyi eby’okukendeeza obulumi, Dermorphin erina okukozesebwa okusuubiza mu kisaawe ky’okuddukanya obulumi.
Ensonda
[1] Giakomidi D, Ebinyonyi M. F., McDonald J., n’abalala. Okukebera [Cys(ATTO 488)8]Dermorphin-NH2 ng’ekintu ekipya eky’okunoonyereza ku μ-opioid peptide receptors[J]. Plos One, 2021,16 (4): e250011.DOI:10.1371/ekitabo ky’amawulire.pone.0250011.
[2] Hesselink J, Schatman M E. Okuddamu okuzuula eddagala erikadde: ensonga eyeerabirwa eya dermorphin olw’obulumi oluvannyuma lw’okulongoosebwa n’okukendeeza[J]. Journal of Okunoonyereza ku bulumi, 2018,11:2991-2995.DOI:10.2147/JPR.S186082.
[3] Guzevatykh L. S., Voronina T. A., Emel’Ianova T. G., n’abalala. Okwekenenya okugeraageranya emirimu gy’okukendeeza obulumi egya dermorphin, [DPro6]-dermorphin, ne C-terminal tripeptides zaabwe[J]. Izv Akad Nauk Ser Biol, 2007 (5): 577-582. http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Ggya&db=pubmed&dopt=Ebikwata ku biwandiiko&olukalala_uids=18038625&okubuuza_hl=1
[4] Sandrini G, Degli U. E., Salvadori S, n’abalala. Dermorphin eziyiza spinal nociceptive flexion reflex mu bantu[J]. Okunoonyereza ku bwongo, 1986, 371 (2): 364-367.DOI: 10.1016 / 0006-8993 (86) 90376-8.
[5] Salvadori S, Marastoni M, Balboni G, n’abalala. Okusengejja n’emirimu gya opioid egya dermorphin tetrapeptides ezirimu D-methionine S-oxide mu kifo 2[J]. Journal of Eddagala Kemiko, 1986, 29 (6): 889-894.DOI: 10.1021 / jm00156a003.
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