By Cocer Peptides 
Watanni 1 da suka gabata
DUKKANIN LABARI DA BAYANIN KYAUTATAWA DA AKE BAYAR A WANNAN SHAFIN KAWAI DOMIN WATSA BAYANI NE DA MANUFOFIN ILIMI.
Kayayyakin da aka bayar akan wannan gidan yanar gizon an yi niyya ne kawai don binciken in vitro. Binciken in vitro (Latin: *a cikin gilashi*, ma'ana a cikin gilashin gilashi) ana gudanar da shi a wajen jikin mutum. Waɗannan samfuran ba magunguna ba ne, Hukumar Abinci da Magunguna ta Amurka (FDA) ba ta amince da su ba, kuma dole ne a yi amfani da su don hanawa, magani, ko warkar da duk wani yanayi na likita, cuta, ko cuta. Doka ta haramta shigar da waɗannan samfuran cikin jikin mutum ko dabba ta kowace hanya.
Bayani na PE22-28
PE22-28 shine peptide 7-amino acid wanda aka tsara bisa bincike a cikin Spadin (PE 12-28). Bacin rai, rashin lafiyar hankali da ke shafar kusan kashi 20% na al'ummar duniya, a halin yanzu ana kula da su tare da magungunan rage damuwa waɗanda ke fama da al'amura irin su jinkirin fara aiki da sakamako mai tsanani. Spadin an kwatanta shi a matsayin peptide endogenous tare da aikin antidepressant wanda ke toshe tashar TREK-1 musamman, amma aikinsa ya ɓace cikin sa'o'i 7 bayan gudanarwa. Don haɓaka kwanciyar hankali na Spadin da bioavailability a cikin vivo, masu bincike sun bincika analogs da abubuwan da suka samo asali, suna nazarin samfuran lalata jini na Spadin, kuma a ƙarshe sun tsara PE22-28.
Hoto 1 Spadin-analog takamaiman. (A-D) PE 22-28 an yi amfani dashi azaman wakilin peptide don gwada ƙayyadaddun spadin-analogs vs. sauran tashoshin K2P, TREK-2 (A), TRAAK (B), TRESK (C), da TASK-1 (D).
Saukewa: PE22-28
Tasiri akan Tashoshi TREK-1
Nazarin in vitro ta amfani da fasahar faci-clamp akan ƙwayoyin hTREK-1 / HEK sun nuna cewa PE22-28 yana nuna ƙayyadaddun ƙayyadaddun ƙayyadaddun ƙayyadaddun ƙayyadaddun ƙayyadaddun ƙayyadaddun ƙayyadaddun tashoshi na TREK-1 idan aka kwatanta da Spadin. Takamaiman bayanai sun nuna cewa IC₅₀ na PE22-28 shine 0.12 nM, yayin da na Spadin shine 40-60 nM. Wannan yana nufin cewa a ƙarƙashin yanayi guda, PE22-28 na iya yin aiki akan tashar TREK-1 mafi inganci a ƙananan ƙima, ta haka yana aiwatar da tasirin ilimin halittarsa daidai. Har ila yau, binciken ya lura cewa a karkashin yanayi guda, gyare-gyare daban-daban a N- ko C-terminus na PE22-28 na iya kiyayewa ko kawar da ayyukan tashar TREK-1 ba tare da tasiri ga dangantaka da tashar TREK-1 ba. Wannan ƙayyadaddun tsarin tsari na ayyukan tashoshi da alaƙa yana ba da mahimman bayanai don ƙarin bincike game da tsarin aikin sa da haɓakar ƙwayoyi.
Abubuwan antidepressant a cikin vivo
Ingantacciyar ƙirar ƙirar ɗabi'a: A cikin nau'ikan halayen baƙin ciki kamar gwajin ninkaya tilas, an tabbatar da kaddarorin antidepressant na PE22-28 da abubuwan da suka samo asali. Mice da aka yi amfani da su tare da analogues na Spadin (ciki har da PE22-28) sun nuna raguwa mai yawa a lokacin rashin motsi. Lokacin rashin motsa jiki shine muhimmiyar alamar nuna rashin tausayi-kamar hali a cikin mice a lokacin gwajin motsa jiki na tilastawa, kuma raguwa a lokacin rashin motsi yana nuna raguwa a cikin halin rashin tausayi, yana nuna cewa PE22-28 yana da tasirin antidepressant. A cikin sabon gwajin ciyarwar da aka hana bayan kwanaki 4 na jiyya na subchronic, PE22-28 ya rage lokacin jinkirin beraye don cinye pellet ɗin abinci. Gwajin ciyarwar da aka hana sabon abu hanya ce ta gwaji don tantance yardan beraye na cin abinci a cikin sabon yanayi. Wani ɗan gajeren lokacin latency yana nuna rage damuwa da halayen da ke da alaƙa a cikin mice, yana ƙara tabbatar da tasirin antidepressant na PE22-28.
Tasiri kan neurogenesis da synaptogenesis: Bayan kwanaki 4 kawai na jiyya, PE22-28 da analogues ɗin sa sun haifar da neurogenesis, tare da G / A-PE22-28 yana nuna tasirin musamman. Neurogenesis yana taka muhimmiyar rawa a cikin pathogenesis na ciki da kuma amsa magani, da kuma samar da sababbin ƙwayoyin cuta na taimakawa wajen inganta aikin jijiyoyi da yanayin yanayi. A cikin ƙananan ƙwayoyin cuta na linzamin kwamfuta, PE22-28 da abubuwan da suka samo asali kuma sun inganta synaptogenesis, kamar yadda aka auna ta yawan matakan magana na PSD-95. PSD-95 furotin ne wanda ke da alaƙa da yanki mai yawa na postsynaptic, kuma ƙara yawan matakan magana yana nuna haɓakar haɓakar haɓakar synapse da aiki, sauƙaƙe watsa bayanai tsakanin ƙwayoyin cuta da gyare-gyaren kewayen jijiyoyi, wanda ke da mahimmancin mahimmanci don haɓaka alamun damuwa.
Abũbuwan amfãni a cikin tsawon lokacin aiki: Idan aka kwatanta da Spadin, tsawon lokacin aikin PE22-28 da analogues yana inganta sosai. Spadin ya rasa aikinsa 7 hours bayan gudanarwa, yayin da tsawon lokacin aikin PE22-28 zai iya kaiwa zuwa 23 hours. Tsawon lokacin aiki yana nufin cewa tasirin ilimin halittar sa na iya dawwama na dogon lokaci a cikin vivo, rage yawan gudanarwa da haɓaka yarda da haƙuri, wanda ke da mahimmancin abubuwan amfani ga jiyya na asibiti.
Bayanan Bayani na PE22-28
Abubuwan da za a iya amfani da su a cikin jiyya na ciki: An ba da kyakkyawan aikin PE22-28 a cikin halayen halayen antidepressant, tsarin aikinta na musamman akan tashar TREK-1, da kuma tasirinsa mai kyau akan neurogenesis da synaptogenesis, yana wakiltar kwayar halitta mai ban sha'awa tare da yiwuwar maye gurbin Spadin a cikin maganin ciki. Fitowar PE22-28 tana ba da sabbin zaɓuɓɓukan jiyya don baƙin ciki. Ya zama jagora mai mahimmanci don ci gaban ƙarni na gaba na magungunan antidepressant. Ta hanyar ci gaba da bincike da ci gaba, inganta tsarin samar da miyagun ƙwayoyi da hanyoyin gudanarwa, ana sa ran samar da mafi kyawun zaɓuɓɓukan magani ga marasa lafiya da ciki.
Source
[1] Djillani A, Pietri M, Moreno S, et al. Shortened Spadin Analogs Nuna Mafi Kyau TREK-1 Inhibition, In Vivo Stability and Antidepressant Activity [J]. Iyaka a cikin Ilimin Magunguna, 2017,8:643.DOI:10.3389/fphar.2017.00643.
Samfura akwai don amfani da bincike kawai:
