Alzheimer ta miyagun ƙwayoyi (AD magani) 'yan takara: J147, CMS121, CAD31
1. Menene Alzheimer da Geroprotectors (GNPs)
Alzheimer ta ne Mafi na kowa hanyar gigin-tsufa, shi ne wani irin gigin-tsufa da cewa yana sa matsaloli tare da memory, tunani da halayya. Alamun yakan ci gaba sannu a hankali da kuma samun mafi muni a kan lokaci, zama m isa ya tsoma baki da kullum ayyuka.Alzheimer ta cutar asusun 60 ya kai kashi 80 bisa dari na shari'ar cutar. Kuma tsofaffi shine mafi girman haɗari ga cututtuka masu yawa, ciki har da cutar Alzheimer (AD) da ciwon daji.
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2.Saboda cutar Alzheimer
Masu binciken sun yi imanin cewa babu wani dalili guda daya da ke haifar da cutar mantuwa. Ta yaya za ka samu Alzheimer ta cutar? Cutar m tasowa daga mahara dalilai, kamar halittar jini, salon da kuma yanayi. Masana kimiyya sun gano abubuwan da kara hadarin Alzheimer ta. Duk da yake wasu matsalolin na daban - shekaru, iyali tarihi da kuma gadar hali - ba za a iya canza, kunno shaida da shawara a can iya zama wasu dalilai ba za mu iya tasiri.
-Age
A mafi girma a san hadarin factor ga Alzheimer ta ne kara shekaru, amma Alzheimer ta ba da wata al'ada kashi na tsufa. Duk da yake shekaru qara hadarin shi ne, ba a kai tsaye hanyar Alzheimer ta.
Mafi mutane da cutar ne 65 kuma mazan. Bayan shekaru 65, da hadarin da Alzheimer ta maimaita kowace shekara biyar. Bayan shekaru 85, haɗarin ya kai kusan kashi ɗaya bisa uku.
- Tarihin iyali
Wani muhimmin haɗarin haɗari shine tarihin iyali. Wadanda suke da iyaye, ɗan'uwa ko 'yar'uwa tare da Alzheimer zasu iya haifar da cutar. Rashin haɗari yana ƙarawa idan fiye da ɗaya daga cikin mahaifa yana da rashin lafiya.
-Genetics (heredity)
Masana kimiyya sun san kwayoyin suna cikin Alzheimer's. Kashi biyu na kwayoyin halitta suna tasiri ko mutum ya tasowa cutar: kwayoyin cutar da kwayoyin halitta.
-Head rauni
Akwai wata mahada tsakanin shugaban rauni da kuma nan gaba hadarin gigin-tsufa. Kare kwakwalwa ta buckling your wurin zama bel, saka your kwalkwali a lokacin da halartar wasanni, da kuma "fada-proofing" your gida.
- Haɗin kawance
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3. Masu neman maganin cutar Alzheimer (AD magani): J147, CMS121, CAD31
Yau, Alzheimer ta ne a gaba wajen ilimin halittu da aikin likita da bincike. Masu bincike suna aiki zuwa uncover kamar yadda da yawa al'amurran da Alzheimer ta cutar da kuma sauran dementias kamar yadda zai yiwu. Wasu daga cikin mafi ƙwarai ci gaban ya zubar da haske a kan yadda za Alzheimer ta rinjayar da kwakwalwa. Begen shine wannan fahimtar za ta kai ga sabon jiyya. Yawancin hanyoyin da ake amfani da su a halin yanzu ana binciken su a duk duniya.
Magunguna na asibiti na 2,4-Dinitrophenol (DNP) yana da amfani wajen gina jiki
Cibiyar Nazarin Neurobiology Salk ta fara ne tare da sunadarai guda biyu da aka samo a cikin tsire-tsire waɗanda suka nuna alamun magani: fisetin, samfurin halitta wanda aka samo daga 'ya'yan itatuwa da kayan marmari, da kuma curcumin, daga curry spice turmeric. Daga waɗannan, kungiyar ta haɗa uku AD magani 'yan takara dangane da ikon su don kare ƙananan ƙwayoyin cuta daga abubuwa masu yawa da ke hade da kwakwalwa tsufa. Labarin ya nuna cewa waɗannan 'yan takara guda uku (wanda aka sani da CMS121, CAD31 da kuma J147), kazalika da fisetin da curcumin, rage alamomin kwayoyin na tsufa, da kuma lalata, da kuma kara yawan ƙwayar mice ko kwari.
Abin mahimmanci, ƙungiyar ta nuna cewa hanyoyin da kwayoyin kwayoyi masu gudana daga wadannan 'yan takarar miyagun ƙwayoyi na AD sun kasance kamar guda biyu masu magungunan roba masu bincike waɗanda aka sani don kara yawan dabbobi. Saboda wannan dalili, kuma bisa ga sakamakon binciken da suka gabata, kungiyar ta ce fisetin, curcumin da 'yan takarar miyagun ƙwayoyi guda uku da ke AD sun hada da ma'anar kasancewa geroneuroprotectors.
Sauran nazarin a cikin labarun suna tabbatar da cewa waɗannan mahadi suna da tasiri a kan gabobin a waje da kwakwalwa. "Idan waɗannan kwayoyi suna da amfani ga sauran tsarin jiki, irin su ci gaba da aikin koda da kuma cikakken lafiyar tsoka, za a iya amfani da su wajen ƙarin hanyoyin magance ko hana cututtuka na tsufa," in ji Schubert.
- Alzheimer ta miyagun ƙwayoyi (AD miyagun ƙwayoyi) da 'yan takara: J147
Curcumin, babban sashi na turryic curry na Indiya, shi ne rukuni na multitarget wanda ya rage kumburi, samar da ROS, maye gurbin amyloid, da excitotoxicity, kuma yana da matukar tasiri a cikin nau'in AD. Duk da haka, curcumin yana da ƙananan aikin neurotrophic, rashin lafiya mai kyau, da rashin kwakwalwar kwakwalwa. Don inganta aikin neurotrophic da kwanciyar hankali na yanayi na curcumin, munyi amfani da ilimin kimiyya na SAR don inganta tsarin kantin kayan pharmacological kuma a lokaci guda yana kara karfinta da kuma abubuwan da ke tattare da ayyukan halittu. Da farko dai tsarin gyaran tsarin labile na labile ya canza zuwa pyrazole don yin CNB-001, tare da inganta zaman lafiyar da aikin neuroprotective akan curcumin. Bincike na kamfanonin kungiyoyi uku na CNB-001 sun nuna cewa kungiyoyin hydroxyl ba dole ba ne don aiki a cikin gwaji bakwai. Bugu da ƙari na ƙungiyoyi biyu na methyl zuwa pyrazole a haɗe phenyl lamarin ya jagoranci CNB-023 tare da karfin aiki akan CNB-001. Duk da haka, CNB-023 ne sosai lipophilic (cLogP = 7.66), kuma masu haɗuwa da high lipophilicity suna da ƙididdiga masu yawa. Don rage lipophilicity da kuma gano ƙayyadaddun tsari na aiki, an cire ɗaya daga cikin ƙungiyar cinnamyl guda biyu kuma ƙara ingantawa ya haifar da wani ƙananan kwayoyin halitta J147. J147 shine 5-10 sau sau da yawa a cikin dukkanin gwajin gwagwarmaya kamar CNB-001, yayin da curcumin yana da kadan ko babu aiki a kowace gwaji. J147 ba kawai mai yiwuwa ba ne amma har yana da kyawawan kayan aikin physicochemical (MW = 350, cLogP = 4.5, tPSA = 42). J147 (1146963-51-0) An yi nazarin yawancin al'amuran al'ada da kuma AD inda yake da inganci na asibiti.
Wani ya damu da cewa yayi J147 na iya kaskantar da shi zuwa amines / hydrazines masu yuwuwar cutar kansa. Don bincika wannan yiwuwar, da na rayuwa da kwanciyar hankali na J147 aka yi karatu a microsomes, a linzamin kwamfuta jini, kuma a vivo. An nuna cewa J147 (1146963-51-0) ba kaskanta zuwa aromatic amines ko hydrazines, cewa scaffold ne exceptionally barga, da kuma cewa shi ne modified zuwa biyu ko uku oxidative metabolites a mutum, linzamin kwamfuta, bera, biri, da kuma kare hanta microsomes. Don nazarin lafiyar wadannan ƙwayar mota, mun hada dukkanin hanta na mutum guda uku na microabal metabolites kuma sun gwada su don aikin nazarin halittu a cikin gwajin neuroprotection. Babu wani daga cikin wadannan matakan da suke da maɗaurai, kuma yawancinsu na rayuwa suna da ayyukan nazarin halittu kamar su na J147.
- 'Yan takarar Alzheimer (AD drug)' yan takara: CMS121
CMS121 shi ne ƙari na fisetin. A cikin fewan shekarun da suka gabata, mun nuna cewa flavonoid fisetin yana aiki ne da baki, kwayar halitta, da haɓaka haɓakar sani a cikin dabbobin dabbobi da yawa na rikicewar CNS. Fisetin yana kai tsaye aiki antioxidant da kuma iya kula da kwayuka matakan GSH karkashin danniya. Bugu da kari, fisetin yana da aikin neurotrophic da anti-inflammatory. Wannan fadi da kewayon ayyuka da shawara cewa fisetin yana da ikon don rage asarar neurological aiki hade tare da mahara cuta. Duk da haka, da in mun gwada high EC50 a cell tushen kima (2-5 μM), low lipophilicity (cLogP 1.24), high tPSA (107), da kuma talakawa bioavailability sun iyakance fisetin domin kara ci gaba da matsayin magani dan takarar.
Thealubalen shine inganta ƙarfin fisetin a cikin hanyoyi masu yawa na neuroprotective yayin kuma a lokaci guda canza kimiyyar kimiyyar ta jiki don daidaitawa da waɗanda magungunan CNS masu nasara (nauyin kwayar ≤ 400, cLogP ≤ 5, tPSA-90, HBD ≤ 3, HBA ≤ 7) .Anyi amfani da hanyoyi daban-daban guda biyu don inganta fisetin. A farkon, an canza ƙungiyoyin hydroxyl daban-daban a cikin tsari don kawar da yiwuwar metabolites na sulfate / glucuronidate. A hanya ta biyu, an canza sifar flavone zuwa quinoline, yayin kuma a lokaci guda kiyaye muhimman abubuwa na fisetin.Yin amfani da dabarun gano magungunan mu na zamani da yawa, mun samar da wasu abubuwa da yawa tare da ingantattun ayyuka a cikin oxytosis neuroprotective and in gwajin bitro ischemia. Arin ayyuka uku na fisetin an riƙe su a cikin maɓuɓɓuka, gami da kiyaye GSH, hana kwayar cutar lipopolysaccharide (LPS) ta haifar da kunna microglial, da kuma bambancin kwayar PC12, ma'aunin aikin neurotrophic. Flavone wanda ya samo asali CMS-140 da kuma Cino-121 wanda yake da quinolone shine 600 da kuma 400 sau da yawa, bi da bi, fiye da fisetin a cikin gwajin ischemia (Hoto
- Alzheimer ta miyagun ƙwayoyi (AD miyagun ƙwayoyi) da 'yan takara: CAD31
Dukkanin abubuwa masu ilimin lissafi na CAD31 sun kasance masu dacewa a cikin mahallin hana wasu abubuwa masu guba a cikin cututtukan da ke tattare da tsohuwar haihuwa.
CAD31 ne Alzheimer ta cutar (AD) miyagun ƙwayoyi dan takarar da aka zaba a kan tushen da ikon ta da kwafi na mutum tayi kara cell-samu na tsarin jijiya precursor Kwayoyin kazalika a APPswe / PS1ΔE9 AD beraye. Don matsar da CAD-31 wajen asibitin, gwaje-gwajen da aka Kanmu sanin da neuroprotective kuma pharmacological Properties, kazalika da kima da warkewa inganci a tsaurara linzamin kwamfuta model na AD.
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4.Conciko
Kungiyar bincike yanzu tana mayar da hankalin samun samun GNP biyu cikin gwaji na asibiti. Aiki na fisetin, CMS121, a halin yanzu a cikin nazarin ilimin toxicology na dabba da ake bukata don yarda da FDA don fara gwaji. A curcumin m, J147, yana ƙarƙashin tsarin FDA na bada izini don fara gwaje-gwaje na asibiti don AD a farkon shekara mai zuwa. Ƙungiyar ta yi niyya don kunshe da alamomi na biochemical don tsufa a cikin gwaje-gwaje na asibitoci don gwadawa ga tasiri mai tasiri mai tasiri. Masu bincike sun ce ganowar wadannan 'yan takarar miyagun ƙwayoyi na AD sun tabbatar da samfurin bincike na likitanci wanda suka bunkasa a matsayin hanya mai kyau don gano ƙarin GNP mahadi wannan zai taimaka wajen bunkasa tsufa. Wannan zai iya inganta hanzarin gaggawa don maganin cututtuka don magance cututtuka na tsufa wanda babu halin magani.
AASraw shine ƙwararren ƙwararren J147, CMS121, CAD31 foda wanda ke da dakin gwaje-gwaje mai zaman kansa da babban masana'anta a matsayin tallafi, duk samarwa za a gudanar da su a ƙarƙashin tsarin CGMP da tsarin kula da ingancin kulawa. Tsarin samar da kayayyaki yana da karko, duka dillalai da umarni na siyarwa suna karba. Barka da zuwa don ƙarin koyo game da AASraw!
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