|
1kits （10Ibikoresho）
| Umubare: | |
|---|---|
▎ Imiterere ya Sel
Inkomoko: PubChem |
Urukurikirane: TKPRPGP Inzira ya molekulari: C 33H 57N 11O.9 Uburemere bwa molekuline: 751.9 g / mol Numero ya CAS: 129954-34-3 PubChem CID: 11765600 Synonyme: Sel |
Sel Research Ubushakashatsi
Ni ubuhe bushakashatsi bwakozwe na Sel?
Neuroadaptation hamwe na Endogenous Opioid Sisitemu:
Sisitemu ya endogenous opioid igira uruhare mubikorwa bya neuroadaptation biterwa na opioide exogenous. Sel, synthèse ya anxiolytike ishingiye ku kugenzura peptide tuftsin igenga, irashobora guhagarika ibikorwa byimisemburo ya enkephalin yangiza, bityo ikongera urwego rwa leucine enkephalin muri plasma (Nadorova AV, 2022). Ibi byerekana ko Sel ishobora gukoresha ingaruka zayo muguhindura sisitemu ya endogenous opioid.
Guhangayika no guhungabana ni bimwe mubibazo byubuzima bwo mumutwe bikunze kugaragara kwisi yose. Imiti ikoreshwa cyane mubuvuzi bwa anxiolytike yibanda cyane cyane kumiti ya farumasi yibikorwa byubwonko bwa GABA. Nyamara, ibiyobyabwenge nkibi bikunze kugira ibibazo byubuvuzi nko kwishingikiriza no kutagira kwibuka (Vyunova TV, 2018). Hariho kumenyekanisha uruhare rwa neuropeptide na bioactive lipide muri pathophysiologie yimyumvire no guhangayika. Sel ya heptapeptide Sel igaragaza ingaruka ndende za anxiolytike na nootropique (TV ya Vyunova, 2018).
Ni ubuhe buryo bwo gukora bwa Sel?
Ni ubuhe buryo bwo gukora bwa Sel ku guhangayika no guhungabana?
Kugenga Sisitemu yo Kwakira GABA:
Guhangayika no guhungabana ni ibibazo bikunze kugaragara ku buzima bwo mu mutwe ku isi. Imiti ikoreshwa cyane mubuvuzi bwa anxiolytique ivura cyane cyane ingaruka zayo muguhuza ibikorwa bya sisitemu ya reseptor ya GABA mubwonko, ariko akenshi usanga bafite ibibazo nko kwishingikiriza no kutagira ubwenge. Ubushakashatsi bwerekanye ko Sel ya heptapeptide (Thr-Lys-Pro-Arg-Pro-Gly-Pro) igira ingaruka zo kuvura amaganya no guhungabana. Uburyo bwo gusesengura Radioligand-reseptor bwerekanye ko Sel igira ingaruka kuri [3H] GABA ihuza nka moderi nziza ya allosteric. Igikorwa cya Sel hamwe na benzodiazepine zimwe na zimwe zigenga ibikorwa bya GABA [3H] guhuza ibikorwa muburyo bwihariye. Ingaruka ntabwo yongeyeho kandi itandukanye no gukoresha ibintu byonyine. Sel irashobora guhagarika ibikorwa bigenga diazepam na olanzapine. Ikibanza cyacyo gihuza bigaragara ko gitandukanye n’ibiyobyabwenge, ariko birashobora guhuzagurika igice [1] . Biravugwa rero ko bumwe mu buryo bwa molekulike bwingaruka za Sel ya anxiolytike ya Sel bushobora kuba bufitanye isano na subtype-selitifike yibanze-biterwa na allosteric igenga reseptors ya GABA.
Ni ubuhe buryo bwa Sel mu kugabanya analgesia iterwa na morphine?
Kubuza Morphine Gukuramo Ibisubizo:
Ubushakashatsi bumwe bwerekanye ko ibintu bya peptide Sel bishobora kugabanya imbaraga zo gukuramo imbeba kuri morphine ku kigero runaka. Kurugero, muburyo bwo gukuramo morphine bwatewe na naloxone, inshinge imwe ya intraperitoneal yatewe na Sel (0.3mg / kg) irashobora kugabanya igipimo rusange cya syndrome de morphine yo kwikuramo 39,6%, bikagabanya cyane ibimenyetso nkibisubizo bihindagurika, ptose, hamwe nindwara ziterwa na posita, kandi bikongerera inshuro 9 ibyiyumvo byimbeba biterwa na morphine inshuro 9 [2] . Ibi byerekana ko Sel ishobora kugira ingaruka zitaziguye uburyo bwo gusesengura imiterere ya morphine muguhindura sisitemu yimitsi iterwa na morphine.
Ingaruka zo Kwisuzumisha hamwe na Morphine:
Mu bushakashatsi bw’inyamaswa, abashakashatsi basanze Sel yerekana ingaruka zo guhuza imbaraga iyo ikoreshejwe hamwe na morphine. Morphine irashobora gutera urugero runaka rwa analgesia ku kigero runaka, kandi nubwo Sel ubwayo idafite ingaruka zidasanzwe zo kuvura, iyo ikoreshejwe ifatanije na morphine ku gipimo runaka (0.9mg / kg), irashobora kongera ubukererwe bwimbeba zatewe nubushyuhe bwumuriro, bikazamura ingaruka zidasanzwe kuri 29.9% byingaruka zishoboka zose (MBE) [3] . Ibi byerekana ko Sel ishobora kongera ingaruka zidasanzwe za morphine binyuze munzira runaka.
Gukora kuri Sisitemu ya Enkephalin:
Hashingiwe ku bushakashatsi ku ngaruka zifatika za Sel n'ibice byayo, havugwa ko Sel ikora ku muyoboro wa casade ya peptide n'abunzi binyuze muri enkephalin. Enkephalin ni ubwoko bwa endogenous opioid peptide kandi igira uruhare runini mugutunganya ububabare. Sel irashobora kugira ingaruka mbi kuri morphine muguhindura imikorere yimisemburo ya enkephalin yangiza no kongera urwego rwa leucine enkephalin muri plasma [4].
Ingaruka za Sel (0.3 mg / kg) ku kumenyekanisha ikintu gishya mu mbeba zatewe n'ubusinzi ku gahato.
Inkomoko: Byatangajwe [7]
Ni irihe hame rishobora kuba Sel mu kuvura indwara zintege nke muri syndrome ya COVID?
Bishingiye ku ngaruka zo gukingira indwara:
Urebye uruhare runini rw’imiterere y’ubudahangarwa mu gutera indwara ya COVID-19, imiti ifite ingaruka z’ubudahangarwa isa n’ibyiringiro mu kuvura syndrome ya COVID nyuma ya COVID. Sel numuti wa peptide wakozwe ushingiye kuri tafcin ikingira indwara. Mu kuvura syndrome ya nyuma ya COVID, Sel irashobora kugabanya ibimenyetso byintege nke muguhindura sisitemu yumubiri no gukosora imikorere mibi yumubiri. Kurugero, Sel irashobora kugira ibikorwa bitaziguye kumikoranire yubudahangarwa cyangwa igakora mu buryo butaziguye kugabanya igisubizo nyuma yo guhangayika, bityo bikagumana imiterere isanzwe yimikorere yumubiri [5].
Anxiolytike no Gutezimbere Imyitwarire:
Muri syndrome ya nyuma ya COVID, abarwayi bakunze guhura nihungabana nko guhangayika no kwiheba, biherekejwe nintege nke no kugabanuka kwimikorere. Ubushakashatsi bwerekanye ko Sel ishobora kugabanya ibimenyetso byo guhangayika no kwiheba mugihe cyo kuvura. Uburyo bwibikorwa bushobora kuba bufitanye isano na Sel igenga sisitemu ya neurotransmitter mubwonko. Kurugero, Sel irashobora gukora nka moderi nziza ya allosteric modulator kugirango ihindure [3H] guhuza GABA, bityo igenzure ibikorwa bya sisitemu ya reseptor ya GABA kandi ikore ingaruka ya anxiolytike [1].
Ingaruka ya Neuroprotective:
Mu bushakashatsi, abarwayi bagabanyijwemo amatsinda abiri. Itsinda rimwe ryakoresheje urwego rwa neuroprotective complex (cholitilin, mexidol, milgamma) na Sel, irindi tsinda ryakoresheje gusa neuroprotective complex. Ibisubizo byerekanye ko abarwayi bakoresha Sel bagize ingaruka nziza mubijyanye nintege nke no kugabanuka kwimikorere. Ibi byerekana ko Sel ishobora gukorana hamwe na neuroprotective complex kugirango ikore neuroprotective, bityo bizamura ibimenyetso byintege nke zabarwayi [5].
Ingaruka za virusi:
Ubushakashatsi bwerekanye ko Sel ifite virusi ya virusi mu kwandura ibicurane. Nubwo kuri ubu nta kimenyetso cyerekana ko Sel igira ingaruka zo kurwanya virusi ya COVID-19, bitewe n’imikorere yayo mu kwandura ibicurane, Sel irashobora kugira ingaruka runaka kuri virusi ya COVID-19 ikoresheje uburyo runaka, bityo igafasha kuvura indwara y’intege nke muri syndrome ya COVID. Kurugero, mubushakashatsi bwa vivo, Sel yateje gene imvugo ya interferon-α (IFN-α), ishobora gufasha kongera ubushobozi bwa virusi ya virusi [6].
Ni izihe ngaruka za Sel?
Anxiolytike no Gutezimbere Imyitwarire:
Muri syndrome ya nyuma ya COVID, abarwayi bakunze guhura nihungabana nko guhangayika no kwiheba, biherekejwe nintege nke no kugabanuka kwimikorere. Ubushakashatsi bwerekanye ko Sel ishobora kugabanya ibimenyetso byo guhangayika no kwiheba mugihe cyo kuvura. Uburyo bwibikorwa bushobora kuba bufitanye isano na Sel igenga sisitemu ya neurotransmitter mubwonko. Kurugero, Sel irashobora gukora nka moderi nziza ya allosteric modulator kugirango ihindure [3H] guhuza GABA, bityo igenzure ibikorwa bya sisitemu ya reseptor ya GABA kandi ikore ingaruka ya anxiolytike [1].
Ingaruka ya Neuroprotective:
Mu bushakashatsi, abarwayi bagabanyijwemo amatsinda abiri. Itsinda rimwe ryakoresheje urwego rwa neuroprotective complex (cholitilin, mexidol, milgamma) na Sel, irindi tsinda ryakoresheje gusa neuroprotective complex. Ibisubizo byerekanye ko abarwayi bakoresha Sel bagize ingaruka nziza mubijyanye nintege nke no kugabanuka kwimikorere. Ibi byerekana ko Sel ishobora gukorana hamwe na neuroprotective complex kugirango ikore neuroprotective, bityo bizamura ibimenyetso byintege nke zabarwayi [5].
Kuruhura Analgesia Yatewe na Morphine:
Ubushakashatsi bumwe bwerekanye ko Sel, anxiolytique ikomatanya ishingiye kuri peptide tuftsin igenga, igira ingaruka kuri analgesie iterwa na morphine mubyitegererezo by'inyamaswa. Kurugero, iyo dose ya morphine ari 3.0mg / kg (inshinge za intraperitoneal), irashobora gutera antinociception, hamwe ningaruka zishoboka (MBE) ya 9%. Mugihe urugero rwa Sel ya 0,9mg / kg nta ngaruka zirwanya ubwayo, iyo rwabanje kuvurwa na morphine, rushobora kongera igihe cyo kwitwara rwihishwa kandi rugatera antinociceptive ya 29.9% MBE [3].
Kugabanya Ibimenyetso Byanga Gukuramo Morphine:
Igikorwa cya peptide tuftsin analog Sel yizwe muburyo bwo gukuramo morphine yatewe na naloxone. Inshinge imwe ya intraperitoneal ya Sel ku gipimo cya anxiolytike ya 0.3mg / kg irashobora kugabanya igipimo rusange cya syndrome de morphine ikuramo 39.6%, ku buryo bugaragara (p ＜ 0.0001) igabanya ingaruka ziterwa no guhungabana, ptose, hamwe n’imivurungano y’imyanya, kandi bikongera inshuro 9 ugereranije n’itsinda rishinzwe kugenzura neza. Muri icyo gihe, Sel iri munsi gato ya diazepam ku kigero cya 2mg / kg mu bijyanye na farumasi (kugabanya igipimo rusange cya syndrome de morphine ikuramo 49.3% kandi ikongerera inshuro 13 ibyiyumvo). Kubwibyo, nka diazepam, Sel irashobora kugabanya ibimenyetso byanga byo kwikuramo morphine bitewe na opioid biterwa nimbeba [2].
Kurinda Ethanol iterwa no kutibagirwa:
Imbeba zabonye Ethanol 10% nkisoko yonyine y’amazi mu gihe cy’ibyumweru 30, hakozwe ubushakashatsi ku ngaruka za Sel, imiti ya peptide ishingiye kuri peptide ikomoka kuri peptide tuftsin ya endogenous peptide tuftsin, ku bijyanye no kutibuka neza ndetse n’ubwonko bukomoka ku bwonko (BDNF). Mu bizamini byo kumenyekanisha ibintu, Sel yerekanye ingaruka zongera ubwenge mu mbeba zamezi 9 zidahuye na Ethanol kandi ikabuza iterambere rya memoire iterwa na Ethanol no kutitaho mugihe cyo kunywa inzoga. Mu bushakashatsi bwa vitro bwerekanye ko Sel ishobora kubuza kwiyongera kwa Ethanol kwiyongera kurwego rwa BDNF muri hippocampus na cortex ibanza. Duhereye ku bimaze kuvugwa haruguru, dushobora kwanzura ko iyi mikorere ya synaptogenic igira ingaruka nziza kubumuga bwo kwibuka buterwa n'imyaka bifitanye isano no guterwa n'inzoga zidakira, kandi ikemeza ko uburyo bwa BDNF bujyanye na neurotrophique bufite uruhare mubikorwa bya Sel [7].
Kuvura Indwara ya COVID-19:
Indwara ya nyuma ya COVID-19 ibaho nyuma yo kwandura COVID-19 kandi irashobora no kugaragara mugihe cyindwara zoroheje cyangwa zidafite ibimenyetso. Ibimenyetso bikunze kugaragara kuri syndrome ya kiraro ni umunaniro no kugabanuka kwimikorere, bikurikirwa nubumuga bwo kutamenya. Bitewe n'uruhare nyamukuru rwo kugabanya ubudahangarwa bw'umubiri mu gutera indwara ya COVID-19, imiti ikingira indwara igira ingaruka ku buryo butaziguye cyangwa izigumana mu buryo butaziguye imikorere y’ubudahangarwa mu kugabanya ibisubizo nyuma yo guhangayika bitanga amasezerano yo kuvura.
Sel ni umuti wa peptide wakozwe ushingiye kuri immunomodulator tafcin, ufite akamaro mukuvura neurose zitandukanye nindwara zisa na neurose. Iyo ikoreshejwe kumupanga wibitonyanga 2-3 inshuro enye kumunsi muminsi 30 ikurikiranye, Sel igira ingaruka nziza zo kuvura abarwayi bafite umunaniro nubumuga bwo kutamenya. Kugabanya ibimenyetso byo guhangayika no kwiheba nabyo birashobora kugaragara [5].
Gukosora ibibazo by’ubwenge n’amarangamutima ku barwayi bafite dermatite ya Atopic: Ubushakashatsi bwasesenguye ibibazo by’ubwenge n’amarangamutima ku barwayi 65 barwaye dermatite ya Atopic (AD) maze bigabanya abarwayi mu matsinda abiri agereranywa n’imibare.
Itsinda rya mbere ry’abarwayi bahawe imiti isanzwe y’ubuvuzi bwa Atopic dermatitis (BT), mu gihe itsinda rya kabiri ryakiriye imiti ya serank na BT binyuze mu buyobozi bw’imbere (S + BT), butangwa inshuro eshatu buri munsi, hamwe n’ibitonyanga bibiri byinjijwe muri buri mazuru kuri dose, iminsi 14 yose. Itsinda rishinzwe kugenzura ryari rigizwe n'abantu 30 bafite ubuzima bwiza. Guhangayikishwa n'umuntu ku giti cye (LT), guhangayika (RT), urugero rwa yohimbine, amaraso β-endorphine, hamwe n'ubuzima bwiza (QOL) byasuzumwe mbere yo kuvurwa n'iminsi 30 nyuma yo gutangira kwivuza.
Ibyavuye mu bushakashatsi byagaragaje ko urwego rwa RT mu barwayi ba AD rwikubye inshuro 4.2 ugereranije n’abari mu itsinda rishinzwe kugenzura, urwego rwa LT rwikubye inshuro 3,2, naho urwego rwa yekhtumia rwikubye inshuro 18. Mu itsinda rya BT, RT yagabanutseho 1,4 naho LT igabanuka inshuro 1.3 nyuma yiminsi 30 nyuma yo gutangira kwivuza. Mu itsinda rya C + BT, kugabanuka muri LT na RT byari bifite akamaro nkako, byombi inshuro 2.4.
Nta mpinduka nini zigeze zigaragara mu bimenyetso bya yekutumia cyangwa β-endorphine mu maraso y'abarwayi bo mu itsinda rya BT. Mu itsinda rya S + BT, ibibazo by'amarangamutima ya Alexis byagabanutseho 1,2, naho β-endorphine mu maraso yiyongereyeho 1,9. Ireme ry'ubuzima bw'abarwayi bo mu itsinda rya BT ryaragabanutseho inshuro 1,2 nyuma y'iminsi 30 nyuma yo gutangira kuvurwa, mu gihe iry'abarwayi bo mu itsinda rya S + BT ryagabanutseho 1,7. Umwanzuro nuko urwego rwo hejuru rwimyitwarire yumuntu ku giti cye, guhangayika bikabije, na yekhtumia kubarwayi ba AD bigabanya imibereho yabo. Ikoreshwa rya peptide Sel igenga ubuvuzi bwuzuye bw’abarwayi ba AD igira ingaruka zikosora ku ihungabana ry’amarangamutima n’ubwenge, kugabanya urwego rwo guhangayika, guhangayika bikabije, na yekhtumia, kongera urugero rwa end-endorphine mu maraso, no kuzamura imibereho y’abarwayi [8].
Mu gusoza, nk'imiti ya peptide ya peptide yatejwe imbere ishingiye kuri cluster ya peptide isanzwe, Sel yerekanye ubushobozi bwinshi bwo gukoresha mubikorwa byubuvuzi nubushakashatsi. Agaciro kayo kingenzi ni ugutanga ibisubizo bishya byindwara nkindwara ziterwa no guhangayika, indwara ziterwa no guhangayika, kutagira kwibuka, hamwe n’indwara ziterwa n’umubiri mu kugenzura sisitemu ya neurotransmitter, kongera imikorere y’umubiri, no kunoza imikorere y’ubwenge. Ubushakashatsi ku mavuriro bwemeje ko Sel ishobora kugabanya neza ibimenyetso byo guhangayika no kwiheba, kunoza intege nke n’indwara zo mu bwenge muri syndrome ya COVID, kandi bigahuriza hamwe imbaraga zo kurwanya inflammatory mu kuvura dermatite ya Atopic. Ugereranije nibiyobyabwenge gakondo, bifite ingaruka nkeya, igihe kirekire cyibikorwa, kandi byerekana ibyiza byihariye mubice bya analgesia, kurwanya ibiyobyabwenge, na neuroprotection.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
TV ya Vyunova ni umuhanga mu bumenyi bw’ibinyabuzima w’Uburusiya, umuhanga mu bya shimi, umuhanga mu binyabuzima, n’umushakashatsi. Yatanze umusanzu ukomeye mubijyanye na biochemie & biologiya biologiya, chimie, biofiziki, farumasi & farumasi, na physiologiya. Vyunova yifatanije n’ibigo bizwi nkikigo cy’igihugu cy’ubushakashatsi 'Ikigo cya Kurchatov ' hamwe n’ishuri ry’ubumenyi ry’Uburusiya. Ubushakashatsi bwa Vyunova nabwo bwatumye habaho patenti nyinshi, bugaragaza uburyo bushya bwo gukemura ibibazo bya siyansi. Ubwitange bwe mu guteza imbere ubumenyi mubyiciro bye byatumye aba umuntu wubahwa mubumenyi bwa siyanse. TV ya Vyunova iri kurutonde rwerekanwe [1].
