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▎ CJC1295 Nta DAC Incamake
C. Izi ngaruka zituma zigira uruhare runini mu kwiga uburyo bwo gusohora imisemburo ikura y’imisemburo, kuvura indwara ziterwa n’imisemburo ikura (urugero, kubura imisemburo ikura, dwarfisme, nibindi), ndetse no gushakisha intego nshya z’ibiyobyabwenge n’uburyo bwo kuvura. Byongeye kandi, uko tugenda dusaza, urwego rwimisemburo ikura mumibiri yacu rugenda rugabanuka buhoro buhoro, biganisha ku gusaza nko gutakaza imitsi, kubyibuha amavuta, no kutagira uruhu, nibindi. Mu rwego rwa siporo, CJC1295 nta DAC ishobora guteza imbere imikurire no gusana, kuzamura imikorere ya siporo, no kuzamura imikorere y'abakinnyi no guhatana, bityo ikaba yarakwegereye abakinnyi.
▎ CJC1295 Nta DAC Imiterere
Inkomoko: PubChem |
Urukurikirane: YADAXFXQSYRKVLAQLSARKLLQDXLSR Inzira ya molekulari: C 152H 252N 44O.42 Uburemere bwa molekuline: 3367.9g / mol Numero ya CAS: 446262-90-4 PubChem CID: 91976842 |
▎ CJC1295 Nta bushakashatsi bwa DAC
Ni ubuhe bushakashatsi bwakozwe na CJC1295 nta DAC?
Gukura imisemburo irekura imisemburo (GHRH) ikoreshwa mu kuvura kugira ngo imisemburo ikura ikure (GH), ariko ifite imbogamizi ikomeye, ni ukuvuga igihe gito cyo gukora [1] . Ibi bigabanya ikoreshwa rya clinique ya GHRH kandi bigasaba abashakashatsi gushakisha ubundi buryo bukora igihe kirekire. CJC1295 oya DAC numuti wa peptide ushingiye kuri acide 30 amine. Irashobora gukangura glande ya pitoito kurekura imisemburo ikura (GH). Uyu muti wa peptide uratandukanye nibiyobyabwenge bya peptide. Umwihariko wacyo uri imbere yitsinda ryitwa acide malimide propionic acide, rishobora guhuza hamwe na thiol yubusa hejuru ya proteine za plasma. Iyo umaze guhambira poroteyine za plasma, igihe gikora cya CJC1295 nta DAC mumaraso kiba kirekire. Ugereranije n’imiti ya peptide idafunze, iyo miti ya peptide idahambiriye izasohoka vuba mumubiri, mugihe CJC1295 ihambiriye nta DAC ishobora gukomeza gukora mumaraso igihe kirekire. Ubu buryo bwo guhuza butuma CJC1295 nta DAC ibiyobyabwenge bifite ingaruka zidasanzwe.
Nubuhe buryo bwo gukora bwa CJC1295 nta DAC?
Gukangura glande ya pitoito kugirango irekure imisemburo ikura: Uyu muti urashobora gukangura glande ya pitoito kurekura imisemburo ikura (GH). Iyo CJC1295 nta DAC yinjiye mumubiri, ikora kuri glande ya pitoito ikoresheje uburyo bwihariye, bigatuma selile pitoito yongera ururenda rwa GH. By'umwihariko, irashobora guhuza reseptor zihariye hejuru ya selile pitoito, igatangiza urukurikirane rw'inzira zohereza ibimenyetso, amaherezo bigatuma habaho kwiyongera kwa synthesis no kurekura GH [1, 2].
Guhambira poroteyine za plasma: CJC1295 nta DAC ifite ikintu cyihariye, ni ukuvuga ko hari itsinda ryitwara neza muburyo bwaryo, rishobora guhuza hamwe na thiol yubusa hejuru ya poroteyine za plasma. Uku guhambira kwongerera cyane igihe imiti ikomeza gukora mumaraso. Ugereranije n'imiti ya peptide idafunze, CJC1295 ihambiriwe nta DAC ifite ubuzima burebure [2] . Ubushakashatsi bumwe bwerekanye ko CJC-1295 ikubiyemo itsinda rya malimide ikora kuri C-terminus, ikayemerera guhuza hamwe na poroteyine za plasma nka serumu albumin. Bimaze guhambirwa, irashobora kuzamura umusaruro wa GH muminsi irenga itandatu nyuma yubuyobozi bumwe (Timms M, 2019, a).
Kongera imisemburo ya hormone yo gukura: Nyuma yo guterwa inshuro imwe ya CJC1295 nta DAC, bizatuma kwiyongera kwinshi guterwa no kwiyongera kwa plasma GH yibanze. Uku kwiyongera kurashobora kumara iminsi 6 cyangwa irenga, e. Uku kwiyongera kurashobora kumara iminsi 6 cyangwa irenga, hamwe no kwiyongera inshuro 2 kugeza 10 [2-4] . Mu bushakashatsi bwakozwe, nyuma yuko abantu bakuze bazima batewe inshinge zo mu bwoko bwa CJC-1295, habayeho kwiyongera gukabije, guterwa na dose mu rwego rwa GH. Ikigereranyo cya kabiri cyubuzima bwa CJC-1295 cyari iminsi 5.8 - 8.1 (Teichman SL, 2006). Imbeba za GHRH knockout (GHRHKO), imitungo isa nayo yerekanwe. Imiyoborere ya buri munsi ya CJC1295 irashobora kugumana imiterere isanzwe yumubiri no gukura [5].
Ingaruka zo gusohora kwa insuline zimeze nkikura I: CJC1295 nta DAC nayo izagira ingaruka kumasohoro yibintu bikura nka insuline I (IGF-I). Impuzandengo ya plasma IGF-I iziyongera muburyo buterwa na dose, hamwe no kwiyongera inshuro 1.5 kugeza kuri 3, kandi igihe kimara ni iminsi 9 - 11 [2-4] . Nyuma yubuyobozi bwinshi bwa CJC1295 nta dose ya DAC, impuzandengo ya IGF-I ikomeza kuba hejuru kurwego rwibanze muminsi 28 (Teichman SL, 2006). Imbeba za GHRHKO, CJC1295 nazo zatumye ubwiyongere bwa pitoito RNA na GH mRNA bwiyongera, byerekana ubwiyongere bw'uturemangingo dusohora imisemburo ikura imisemburo [5].

Plasma yo kubura umurongo wa CJC-1295 nyuma yo guterwa inshuro imwe. Herekanwa uburyo bwa SD igice cyubuzima.
Inkomoko: Byatangajwe [1]
Ni irihe tandukaniro riri mu buryo bwo kuvura CJC1295 nta DAC ku barwayi bafite imisemburo ikura yo mu byiciro bitandukanye?
Abarwayi b'abana: Abana bari mubihe bikomeye byo gukura no gukura, kandi imisemburo yo gukura igira uruhare runini mu mikurire no gukura kw'amagufwa yabo, imitsi, n'ingingo. Gukura imisemburo ya hormone birashobora gutera ibibazo nko gukura gahoro, uburebure buke, no gutinda kumagufwa kubana.
CJC1295 nta DAC iteza imbere imikurire niterambere ryabana mugukangurira glande ya pitoito gusohora imisemburo ikura. Irashobora kongera imisemburo nigihe kirekire cyimisemburo ikura, kandi ikazamura urwego rwimisemburo ikura hamwe niterambere rya insuline - I (IGF-I) muri serumu [3] . IGF-I ni umuhuza nyamukuru wibikorwa bya hormone yo gukura. Irashobora guteza imbere ikwirakwizwa ry'uturemangingo, gutandukanya, hamwe na sintezamubiri ya poroteyine, kandi ifite uruhare runini mu mikurire no gukura kw'amagufwa, imitsi, n'ingingo. CJC1295 nta DAC irashobora kandi guteza imbere ubwiyongere bwibipimo byerekana amagufwa nka osteocalcine na fosifata ya alkaline, ifasha gukura no kwangiza amagufwa. Mubyongeyeho, CJC1295 nta DAC nta ngaruka zigaragara kumikorere ya tiroyide kandi ifite urwego rwo hejuru rwumutekano.
Abarwayi bakuze:
Abarwayi bakuze bafite ikibazo cyo kubura imisemburo ya hormone barashobora guhura nibibazo nko kugabanuka kwimitsi, kongera amavuta, kugabanuka kwumubiri, kongera ibyago byindwara zifata umutima, na osteoporose. Ugereranije n’abarwayi b’abana, imikurire n’iterambere by’abarwayi bakuze byarangiye ahanini, kandi intego yo kuvura ni ukuzamura imikorere ya metabolike n’ubuzima bwiza. Uburyo bwo kuvura CJC1295 nta DAC ku barwayi bakuze ahanini ni ukongera imbaraga z'imitsi, kugabanya ibinure, kunoza imikorere y'umutima, gutinda gusaza, no kwirinda osteoporose wongera imisemburo ikura na IGF-I. Ubushakashatsi bwerekanye ko CJC1295 nta DAC ishobora kongera umubyibuho ukabije w’abarwayi bakuze, kugabanya ibinure by’ibinure, kunoza insuline, no kugabanya ibyago by’indwara zifata umutima. Byongeye kandi, CJC1295 nta DAC ishobora kandi guteza imbere gukura no kugabanuka kwamagufwa, kongera ubwinshi bwamagufwa, no kwirinda osteoporose [3, 5].
Abarwayi bageze mu zabukuru:
Hamwe no kwiyongera kwimyaka, gusohora imisemburo ikura mumubiri wumuntu bigenda bigabanuka buhoro buhoro, biganisha kubibazo nko kugabanuka kwimitsi, kubyibuha amavuta, osteoporose, no kugabanya ubudahangarwa bw'umubiri. Abageze mu zabukuru bafite ikibazo cyo kubura imisemburo ikura bafite ibyago byinshi byindwara, kandi kuvura biragoye. Uburyo bwo kuvura CJC1295 nta DAC ku barwayi bageze mu zabukuru busa n’ubwa barwayi bakuze, ariko dosiye igomba guhinduka neza kandi hagakurikiranwa ingaruka mbi. Bitewe no kugabanuka kwimikorere yumubiri yabarwayi bageze mu zabukuru hamwe nubushobozi buke bwo guhinduranya no gusohora imiti, urugero rwibiyobyabwenge rugomba kugabanuka kugirango wirinde gukwirakwiza ibiyobyabwenge no kubaho nabi.
Ubushakashatsi bujyanye
Ni izihe ngaruka za CJC1295 nta DAC?
Guteza imbere imisemburo ikura:
Nukugereranya imisemburo ikura ya hormone irekura (GHRH), CJC1295 nta DAC irashobora guhuza na reseptor ya GHRH mumyanya ndangagitsina ya pitoito kandi igatera imbaraga zo gusohora no gusohora imisemburo ikura ikoresheje selile ya hormone ikura. Imisemburo ikura ningirakamaro mu mikurire yumubiri no gukura, metabolism, hamwe nuburyo bwo gusana ingirangingo. Mu bushakashatsi bumwe na bumwe, nyuma yo gukoresha CJC1295 nta DAC, kwiyongera k'urwego rwa hormone yo gukura mu maraso birashobora kugaragara, bifasha guteza imbere gukura no gusana ingirangingo nk'amagufwa n'imitsi.
Kugenga metabolism:
Imisemburo ikura igira uruhare runini mugutunganya metabolism. CJC1295 nta DAC igira uruhare rutaziguye inzira ya metabolike iteza imbere imisemburo ikura. Irashobora guteza imbere ibinure, bigatuma ibinure bikoreshwa nkisoko yingufu, bifasha kugabanya ububiko bwamavuta mumubiri no kunoza ikwirakwizwa ryamavuta mumubiri. Muri icyo gihe, irashobora kandi guteza imbere intungamubiri za poroteyine, kongera ubwinshi bwa poroteyine mu ngingo z’imitsi, ifasha kuzamura ubwiza bw’imitsi n'imbaraga, no kongera ubushobozi bw'imyitozo ngororangingo no kwihangana. Byongeye kandi, CJC1295 nta DAC nayo igira ingaruka runaka kuri metabolisme glucose, kandi irashobora kongera insulitifike ya insuline, ifasha kugumana urugero rwamaraso glucose.
Guteza imbere gusana no kuvugurura:
Imisemburo ikura igira uruhare runini mugusana no kuvugurura ingirangingo zangiritse. CJC1295 nta DAC iteza imbere gusohora imisemburo ikura, ari nako itera ikwirakwizwa ry'uturemangingo no gutandukana, kwihutisha gukira ibikomere, kandi bigateza imbere gusana imyenda yangiritse. Mu bushakashatsi bumwe na bumwe bw’inyamaswa n’ubushakashatsi bw’ubuvuzi, byagaragaye ko bifasha mu gukiza kuvunika, gukomeretsa imitsi, no gukira ibikomere by’uruhu, n’ibindi, kandi bifite akamaro kanini mu kuzamura ubushobozi bw’umubiri no kugarura imikorere yimitsi yangiritse.
Nibihe bisabwa bya CJC1295 nta DAC?
Umuti wo kubura imisemburo ikura:
Ku barwayi bafite imisemburo ikura, CJC-1295 Hatabayeho DAC irashobora gutuma imisemburo ikura, bityo igatera imbere no gukura kwumubiri. Irashobora gutanga uburyo bushya bwo kuvura abo barwayi batitabira neza imiti gakondo ikura [3].
Kugena ibibazo byo guhindagurika:
Imisemburo ikura igira uruhare runini muguhindura imikorere yumubiri. C..
Kuvugurura uruhu:
Imisemburo ikura irashobora guteza imbere synthesis ya kolagen, kongera uruhu rworoshye, no kugabanya iminkanyari. CJC-1295 Hatabayeho DAC irashobora kugera ku kuvugurura uruhu mu gusohora imisemburo ikura [6].
Kunoza imikorere yumubiri:
Kwiyongera kwimyaka, imikorere itandukanye yumubiri izagenda igabanuka buhoro buhoro. Imisemburo ikura irashobora kongera imbaraga zimitsi, kongera ubwinshi bwamagufwa, no kongera ubudahangarwa, nibindi. CJC-1295 Hatabayeho DAC irashobora gufasha gutinza gusaza no kuzamura imibereho yabasaza [3].
Kongera imbaraga z'imitsi:
Gukura imisemburo irashobora guteza intungamubiri za poroteyine no kongera imitsi. Ku bakinnyi n’abakunzi ba fitness, CJC-1295 Hatari DAC irashobora gufasha kunoza imbaraga zimitsi no kwihangana [6].
Guteza imbere imyitozo ngororamubiri:
Nyuma y'imyitozo ngororamubiri ikabije, umubiri ukenera igihe cyo gukira. Imisemburo ikura irashobora kwihutisha gusana ingirangingo zangiritse no kugabanya igisubizo. CJC-1295 Hatari DAC irashobora gufasha kugabanya igihe cyo gukira nyuma yimyitozo ngororamubiri no kunoza imikorere y'imyitozo [3].
Kurwanya gusaza:
Hamwe no kurushaho kwita ku kurwanya gusaza, CJC1295 nta DAC nayo ifatwa nabantu bamwe bafite ubushobozi bwo kurwanya gusaza. Gukura imisemburo na IGF-I bigira uruhare runini mukubungabunga imikorere isanzwe yumubiri yumubiri no gusana ingirangingo. Kubwibyo, iyi ngingo irashobora kugira ingaruka mubikorwa byo gusaza muguhuza ibi bintu [3].
Nka analogue ya hormone ikura-imisemburo irekura, CJC1295 nta DAC igira ingaruka zikomeye. Irashobora gukangura glande ya pitoito kugirango irekure imisemburo ikura, igenga ururenda rwibintu bikura nka insuline, bityo bikagira ingaruka kumikurire no guhinduranya umubiri. Mubushakashatsi bwa siyanse, butanga ubufasha bwingenzi mugushakisha uburyo bwimikorere ya hormone ikura kandi bigateza imbere amahame yibyingenzi. Mubikorwa byubuvuzi, kubarwayi bafite imisemburo ikura ya hormone, byitezwe gutera imbaraga zo gusohora imisemburo ikura ya endogenous no kuzamura imikurire niterambere ndetse no guhindagurika kwa metabolike. Irerekana kandi ubushobozi bwo kugabanya imisemburo ya hormone no kurwanya impinduka zishaje mubushakashatsi bwo kurwanya gusaza. Muri rusange, bifite akamaro kanini mubushakashatsi bwa siyanse ndetse no mubuvuzi, bizana amahirwe mashya kubushakashatsi bujyanye no kuvura indwara.
Ibyerekeye Umwanditsi
Ibikoresho byavuzwe haruguru byose byakorewe ubushakashatsi, byahinduwe kandi byakozwe na Cocer Peptides.
Umwanditsi w'ikinyamakuru
Teichman SL ni umuhanga ufite uburambe bukomeye ningaruka mubijyanye n'ubuvuzi no guteza imbere ibiyobyabwenge. Afite ubufatanye bwa hafi n’ibigo byinshi n’inganda bizwi cyane, harimo Amashyirahamwe Concentr Analges Inc, Teichman Drug Dev Consulting, Kaminuza y’ubuvuzi ya Wroclaw, BEAT Biotherapeut Corp, Corthera Inc hamwe n’isosiyete ikorana na yo yitwa Corthera, Chiasma, ARYx Therapeut Inc Inc, n'ibindi. Ibikorwa bye byumwuga bikubiyemo ibintu byinshi nka sisitemu yumutima nimiyoboro yumutima hamwe nubuvuzi bwumutima, ubuvuzi rusange bwimbere nubuvuzi rusange, ubwubatsi, endocrinology na metabolism, na farumasi na farumasi, cyane cyane ibyagezweho nintererano mugutezimbere ibiyobyabwenge na biotherapi. Teichman SL yanditse mubisobanuro byatanzwe [1].
Imirongo ijyanye
[1] Teichman SL, Neale A, Lawrence B, n'abandi. Kumara igihe kirekire imisemburo ikura (GH) hamwe na insuline imeze nkikura rya I isohoka na CJC-1295, igereranya rimaze igihe kinini ryerekana imisemburo ya GH irekura, kubantu bakuze bafite ubuzima bwiza [J]. Ikinyamakuru cya Clinical Endocrinology & Metabolism, 2006,91 (3): 799-805.DOI: 10.1210 / jc.2005-1536.
[2] Timms M, Ganio K, Steel R. Uburyo bwo kwemeza ihohoterwa rya CJC-1295 mu ngero zingana na plasma ya LC-MS / MS [J]. Kwipimisha no gusesengura ibiyobyabwenge, 2019,11 (8): 1248-1257.DOI: 10.1002 / dta.2599.
[3] Teichman SL, Neale A, Lawrence B, n'abandi. Kumara igihe kirekire imisemburo ikura (GH) hamwe na insuline imeze nkikura rya I isohoka na CJC-1295, igereranya rimaze igihe kinini ryerekana imisemburo ya GH irekura, kubantu bakuze bafite ubuzima bwiza [J]. Ikinyamakuru cya Clinical Endocrinology & Metabolism, 2006,91 (3): 799-805.DOI: 10.1210 / jc.2005-1536.
[4] Timms M, Ganio K, Forbes G, n'abandi. Ikirangantego cya immuno polymerase cyerekana uburyo bwo kumenya CJC-1295 hamwe nindi mikorere ikura-imisemburo ikura imisemburo igereranya plasma imwe [J]. Kwipimisha no gusesengura ibiyobyabwenge, 2019,11 (6): 804-812.DOI: 10.1002 / dta.2554.
[5] Alba M, Fintini D, Sagazio A, n'abandi. Imiyoborere ya buri munsi ya CJC-1295, igereranya imisemburo ikura-imisemburo ikura (GHRH) igereranya imikurire yimbeba ya GHRH knockout [J]. Ikinyamakuru cyo muri Amerika cya Physiology-Endocrinology na Metabolism, 2006,291 (6): E1290-E1294.DOI: 10.1152 / ajpendo.00201.2006.
6 Gukoresha Ibiyobyabwenge & Gukoresha nabi, 2016,51 (1): 73-84.DOI: 10.3109 / 10826084.2015.1082595.
INGINGO ZOSE N'AMAKURU Y’IBICURUZWA BITANZWE KURI URU RUBUGA BISANZWE KUBONA AMAKURU N'INTEGO Z'UBUREZI.
Ibicuruzwa byatanzwe kururu rubuga bigenewe gusa mubushakashatsi bwa vitro. Mu bushakashatsi bwa vitro (Ikilatini: * mu kirahure *, bisobanura mu bikoresho by'ibirahure) bikorwa hanze y'umubiri w'umuntu. Ibicuruzwa ntabwo ari imiti, ntabwo byemejwe n’ikigo cy’Amerika gishinzwe ibiryo n’ibiyobyabwenge (FDA), kandi ntigomba gukoreshwa mu gukumira, kuvura, cyangwa gukiza indwara iyo ari yo yose y’ubuvuzi, indwara, cyangwa indwara. Birabujijwe rwose n'amategeko kwinjiza ibyo bicuruzwa mumubiri wabantu cyangwa inyamaswa muburyo ubwo aribwo bwose.