7,8-Dihydroxyflavone (7,8-DHF) ni flavonoide isanzwe iboneka yerekana amasezerano mubice bitandukanye byubuzima. Niba ushishikajwe ninyongeramusaruro cyangwa ibiribwa bishobora gufasha ubuzima bwubwonko, kumererwa neza, no kumererwa neza muri rusange, 7,8-DHF irashobora kuba nziza kubushakashatsi. Ifu ya 7,8-Dihydroxyflavone itangwa na Suzhou Myland ifite CAS numero 38183-03-8 nubuziranenge bugera kuri 98%. Ibicuruzwa byagenzuwe neza kandi byujuje ubuziranenge mpuzamahanga, byemeza neza umutekano n’ibicuruzwa. , bikwiranye nubushakashatsi bwa siyanse, guteza imbere ibiyobyabwenge, umusaruro wibikorwa byubuzima nizindi nzego, biguha amahitamo yizewe.
7,8-Dihydroxyflavone (7,8-DHF)ni gake ugereranije flavonoid compound isanzwe iboneka muri kamere. Yagaragaye muri Astragalus pumila, Primula grandifolia na Hubei crabapple. yagaragaye nkikintu cyiza cya nootropic. Yerekanye ingaruka zitandukanye za neuropharmacologique mubushakashatsi bwibanze,
Flavonoide ni urwego rwibintu byinshi bya polifenolike biboneka mu mbuto zitandukanye, imboga, n’andi masoko y’ibimera. Mu myaka yashize, bagiye bitabwaho cyane kubera antioxydants, anti-inflammatory, na neuroprotective.
Ibi bikoresho byagaragaye ko bifite ingaruka nziza mubwonko, harimo kongera imikorere yubwenge no kwirinda indwara zifata ubwonko. 7,8-DHF nimwe mubintu bizwi cyane bya polifenolike byitabirwa cyane nka nootropic. Yakozweho ingaruka zishobora kuba kumyumvire, kwibuka, kwiga, guhangayika, nibindi bikorwa byubwenge.
Ingaruka zifata ubwonko bwa 7,8-DHF zitekereza ko zahujwe n’imikoranire yazo na reseptor zihariye. Byagaragaye ko ari TrkA, reseptor igira uruhare mu mikurire yikura ryerekana ibimenyetso kandi bifite akamaro mubuzima bwa neuronal na plastike.
7,8-DHF ikora muguhuza imvugo ya reseptors zitandukanye, harimo glutamate reseptor subunits na BDNF. Iragira kandi ingaruka kumikorere ya synaps, metabolism yingufu, no kurekura acetyloline mubice bimwe byubwonko.
Byongeye kandi, osteoporose izwi nka "umwicanyi ucecetse" w'umubiri w'umuntu, ibangamira cyane ubuzima bw'abantu bageze mu za bukuru ndetse n'abageze mu za bukuru, cyane cyane abagore batangiye gucura. Mubihe bisanzwe byimiterere yumubiri, kuvugurura amagufwa biri muburyo bwiza; ariko iyo habaye ubusumbane hagati yamagufwa ya osteoblast-yunganirwa na osteoclast-medrated bone resorption, kandi ubwinshi bwamagufwa yakozwe ntibihagije kugirango hongerwe amagufwa yakiriwe, ubwinshi bwamagufwa buzagabanuka. , microstructure ya tissue yamagufa irasenyutse, itera osteoporose.
7,8-Dihydroxyflavone (7,8-DHF) ni flavonoide ikomoka ku bimera ishobora kwigana imikorere y’ibintu bikomoka mu bwonko biva mu bwonko (BDNF), bigatera igihe cyo kwangirika kwakirwa na TrkB no gukora molekile zayo zerekana ibimenyetso bya molekile. Ubushakashatsi bwerekanye ko BDNF ishobora guteza imbere itandukaniro rya osteoblast no kwimuka kandi byihutisha gukira kuvunika.
7,8-DHF irashobora guteza imbere ikwirakwizwa no gutandukanya osteoblasts muguhuza na TrkB no gukora inzira yerekana ibimenyetso bya Wnt / β-catenin, kandi irashobora kubuza kubyara osteoclasts muguhindura ibintu byandikirwa c-fos; hiyongereyeho, 7, 8-DHF irashobora kunoza imitekerereze ya osteoporose muri imbeba ya ovariectomized.
Imiterere yimiti nimiterere ya 7,8-dihydroxyflavone
Irimo amatsinda abiri ya hydroxyl kumpeta ya benzene nitsinda rimwe rya hydroxyl kumpeta ya pyrrolone. Reka dusuzume neza imiterere yimiti ya 7,8-dihydroxyflavone:
Inzira ya molekile ya 7,8-DHF ni C15H10O5, byerekana ko igizwe na atome 15 za karubone, atome 10 ya hydrogène, na atome 5 za ogisijeni.
7,8-Dihydroxyflavone ni kristaline yumuhondo ikomeye ifite uburemere bwa 286.24 g / mol. Irashobora gushonga gato mumazi kubera amatsinda menshi ya hydroxyl ashobora guhuza hydrogen na molekile zamazi.
7,8-DHF uburyo bwibikorwa: amabwiriza ya BDNF no gukora reseptor ya Trkb
Kubijyanye nuburyo bwibikorwa, 7,8-DHF izwiho guteza imbere umusaruro wa BDNF (ubwonko bukomoka mu bwonko bukomoka ku bwonko) mu guhuza no gukora reseptor yayo TrkB. Utabonye tekiniki cyane, ibi nabyo biganisha kuri casade yibikorwa bya selile bifite akamaro mukubungabunga imikorere myiza ya neuronal no guteza imbere neurogenezi.
Reka dusuzume neza uburyo bukuru bwibikorwa 7,8-DHF hepfo.
Ubwonko bukomoka mu bwonko (BDNF) n'uruhare rwayo muri neuroplastique
Hamwe no kuvumbura ko imvugo ikomoka mu bwonko ikomoka mu bwonko (BDNF) igabanuka mu ndwara zifata ubwonko, cyane cyane indwara ya Alzheimer (AD), akamaro kayo mu kubungabunga no kuzamura ubuzima bw’ubwonko buragenda bugaragara. .
BDNF ni ingenzi kumikorere itandukanye ya neuronal kuko iteza imbere kwanduza synaptic, synaptogenez, hamwe na plastike ya synaptic binyuze mukumenyesha hamwe na reseptor ya TrkB. Ibi bituma inzira ya BDNF-TrkB yerekana inzira itanga intego yo guteza imbere ibikorwa byo kuvura bigamije kurwanya indwara zifata ubwonko.
Ubushakashatsi buherutse gucukumbura inyungu zishobora guterwa na molekile nto ya TrkB agonist 7,8-dihydroxyflavone (7,8-DHF) mu kugabanya ingaruka zambere z’indwara ya AD. Mu bushakashatsi bwakozwe kuri moderi yimbeba 5xFAD ya AD, imbeba zavuwe na 7.8-DHF mumezi abiri guhera mukwezi kumwe.
Ibyavuye muri iri perereza byerekana ubushobozi bwo kuvura 7,8-DHF mugukemura ibibazo bya AD bijyanye na neurochemiki ihindagurika hamwe nibimenyetso byindwara. Ikigaragara ni uko 7,8-DHF ivura byatumye kugabanuka kwa cortical Aβ plaque, ikimenyetso cyingenzi cya AD.
Byongeye kandi, irinda cortical neuron cortical kugabanuka kwa dendritic arbor igoye, ifasha kugumana imiterere rusange ya neuronal. Ariko, ntabwo byagize ingaruka cyane mubucucike bwa dendritic.
Nk’uko Aytan, Nurgul n'abandi babitangaza ngo ubwo buvuzi bwerekanye kandi ingaruka zo mu bwoko bwa neuroprotective muri hippocampus, birinda urugero rwinshi rw’ibintu birimo choline ndetse no gutakaza glutamate.
Tropomyosin reseptor kinase B (Trkb) reseptor yerekana inzira
Mu mwaka wa 2010, itsinda rya Porofeseri Ye Keqiang wo muri kaminuza ya Emory ryatangaje ku nshuro ya mbere muri Proceedings of the National Academy of Science (PNAS) ko 7.8-DHF ishobora gukoreshwa nka molekile ntoya yihariye ya tropomyosine reseptor kinase B ( TrkB), ishobora kwigana Imikorere yibintu bikomoka mu bwonko bikomoka mu bwonko (BDNF) irusheho gukora inzira yerekana ibimenyetso kumanuka ya TrkB, nka MAPK / ERK, PI3K / Akt na PKC. Byongeye kandi, ubushakashatsi bwakurikiyeho bwerekanye ko 7,8-DHF ishobora kugabanya umubyibuho ukabije w’imirire iterwa n’imbeba z’abagore ukoresheje imitsi ya skeletale TrkB, ikerekana itandukaniro rishingiye ku gitsina.
Ubwonko bukomoka mu bwonko (BDNF) bushobora guteza imbere itandukaniro rya osteoblast, kwimuka no gukira kuvunika. BDNF ni umwe mu bagize umuryango wa neurotrophique factor kandi ikagenga inzira zitandukanye z’ibinyabuzima cyane cyane mu guhuza reseptor ya tromosine kinase B (TrkB). Nubwo bimeze bityo, ikimenyetso cya BDNF cyatewe na TrkB cyabaye gito muminota 10 kandi kigeze kuri min 60. Ariko, BDNF ifite ubuzima bucye kandi ntishobora kurenga inzitizi yubwonko bwamaraso.
7,8-dihydroxyflavone (7,8-DHF) ni flavonoide ikomoka ku bimera ibasha gutsinda imbogamizi zavuzwe haruguru za BDNF kandi byagaragaye ko yigana BDNF ikora kandi ubu ikoreshwa muri sisitemu zitandukanye za biohimiki na selile Byaragenzuwe ko irashobora gutera TrkB dimerisation no gukora ibikorwa byayo byerekana ibimenyetso bya molekile.
Reseptor ya tropomyosine kinase B (TrkB) igira uruhare runini muguhuza ingaruka za BDNF kuri neuron. Nka reseptor ya tyrosine kinase reseptor, TrkB niyakirwa ryambere rya BDNF kandi itangiza caskade yibintu byerekana ibimenyetso byerekana ibimenyetso bya neurotrophique.
BDNF ikora TrkB kugirango itere inzira nyinshi zingenzi zingirangingo, harimo fosifatiidilinositol 3-kinase (PI3K) -Ibikorwa, mitogen-ikora protein kinase (MAPK) -ibimenyetso bidasanzwe bigengwa na kinase (ERK), na fosifolipase Cγ (PLCγ) -protein kinase C ( PKC) inzira. Buri nzira muriyi nzira igira uruhare muburyo butandukanye bwimikorere ya neuronal n'imibereho myiza.
Inzira ya PI3K-Akt ningirakamaro mugutezimbere ubuzima bwa neuronal no kubuza apoptose. Ibimenyetso bya BDNF-TrkB bifasha iyi nzira kugirango ubuzima bwiyongere bwimikorere muguhagarika ibintu biterwa na apoptotique no gukangurira ibintu birwanya apoptotique, bityo bikarinda neurone nzima.
Kurundi ruhande, inzira MAPK-ERK igira uruhare runini mugutandukanya imitsi no gukwirakwira. Ibimenyetso bya BDNF-TrkB biteza imbere gukora inzira ya MAPK-ERK, nayo igashyigikira gukura kwa neuronal no gutandukana no kwinjiza mumiyoboro isanzwe ya neuronal.
Inzira ya PLCγ-PKC ningirakamaro mugutunganya plastike ya synaptique, inzira yibanze yo kwiga no kwibuka. Ibimenyetso bya BDNF-TrkB bihindura ibikorwa byiyi nzira, amaherezo biganisha kumahinduka mumbaraga za synaptic no guhuza.
Iri hindurwa riteza imbere guhuza no kuvugurura imiyoboro y’imitsi isubiza ibyabaye bishya hamwe n’ibidukikije.
Imiterere ya Neuroprotective
Ubushakashatsi bwerekana ko iyi flavonoide irinda neuron guhagarika umutima na apoptose (progaramu ya progaramu ya selile). Guhangayikishwa na Oxidative ni ikintu gikomeye mu ndwara zifata ubwonko nka Alzheimer's na Parkinson. Mugukata radicals yubusa no kugabanya kwangiza okiside, 7,8-DHF irashobora gufasha kurinda ubusugire bwimikorere nimikorere.
Mu bushakashatsi bw’inyamaswa, 7,8-DHF yerekanwe kunoza imikorere yubwenge no kwibuka. Kurugero, mubyitegererezo byindwara ya Alzheimer, 7,8-DHF yerekanwe kuzamura plastike ya synaptic, ifite akamaro kanini mukwiga no kwibuka. Uburyo bwibikorwa
Ingaruka zo kurwanya inflammatory
Usibye imiterere ya neuroprotective, 7,8-dihydroxyflavone nayo igira ingaruka zo kurwanya inflammatory. Indwara idakira ni ikintu gikunze kugaragara mu ndwara nyinshi, harimo n'indwara zifata ubwonko. Muguhindura inzira yumuriro, 7,8-DHF irashobora gufasha kugabanya neuroinflammation, akenshi iba ifitanye isano no kugabanuka kwubwenge.
Indwara ya Antioxydeant: ROS scavenging na lipid peroxidation
7,8-DHF ifite antioxydeant nkuko bigaragazwa nubushobozi bwayo bwo gusiba ubwoko bwa ogisijeni ikora (ROS) no kugabanya lipide peroxidation. Izi ngaruka zigira uruhare mu ngaruka za neuroprotective mukugabanya imbaraga za okiside iterwa na neuronal kwangirika no kudakora neza.
Ubushakashatsi bwerekanye ko 7,8-DHF ibuza gukora cytokine itera umuriro kandi ikagabanya imikorere ya microglia, selile immunite muri sisitemu yo hagati. Izi ngaruka zo kurwanya inflammatory ntizirinda gusa neuron ahubwo inarema ibidukikije byiza kumikorere yubwenge.
Urebye ingaruka zacyo ku buzima bwubwonko, 7,8-dihydroxyflavone ifite uburyo bushobora gukoreshwa mubice bitandukanye byubuzima nubuvuzi. Bimwe mubimenyerewe bizwi harimo:
Guhuza kwibuka no kugarura
7,8-DHF yabonetse kugirango yongere imbaraga zo kwibuka no kugarura mubikorwa bitandukanye bya hippocampal biterwa no kwiga hamwe nibikorwa byo kwibuka muburyo bwimbeba. Ubu bushakashatsi bwerekana ko 7,8-DHF ishobora kuba nootropic itanga icyizere cyo kunoza imikorere yibuka kubantu bafite ubuzima bwiza nabafite ubumuga bwo kwibuka.
Plastike ya synaptique: imbaraga zigihe kirekire no kwiheba
Nkuko byavuzwe haruguru, 7,8-DHF yerekanwe guhindura plastike ya synaptique iteza imbere LTP no kugabanya LTD muri hippocampus. Izi ngaruka zitekerezwa kuba zahujwe nubushobozi bwayo bwo gukora reseptor ya TrkB hanyuma bikazamura inzira ya BDNF yerekana inzira.
Ihindurwa rya plastike ya synaptique igira uruhare mugutezimbere mumikorere yubwenge yagaragaye nyuma yubuyobozi 7,8-DHF.
Kongera ubumenyi
Nkuko byavuzwe mbere, 7,8-DHF yerekana ubushobozi bwo kuzamura imikorere yubwenge no kwibuka. Ibi bituma iba umukandida winyongera zigamije kuzamura imikorere yibitekerezo, cyane cyane mubantu bageze mu za bukuru cyangwa abantu bafite ubwenge buke.
Absorption, Ikwirakwizwa, Metabolism, na Excretion (ADME): 7,8-DHF yerekana imiti myiza ya farumasi, harimo kwinjiza vuba, gukwirakwizwa kwinshi, no kwinjira neza mubwonko. Ihindurwa cyane cyane numwijima, hamwe ninshi mubisohokera bisohoka mumyanda hamwe na bike bisohoka muminkari.
Amaraso-ubwonko bwa barrière yinjira hamwe nubwonko bwubwonko. Kimwe mu bintu by'ingenzi biranga 7,8-DHFni ubushobozi bwayo bwo kurenga inzitizi yubwonko bwamaraso (BBB) no kwinjira mubice byubwonko, bifite akamaro kanini mubikorwa bya nootropique.
Umwirondoro w’umutekano wa Preclinical - Ubushakashatsi bukabije kandi budakira: Ubushakashatsi bw’umutekano bwerekanye ko 7,8-DHF ifite umutekano mwiza, nta ngaruka mbi zigaragara zagaragaye mu bushakashatsi bw’uburozi bukabije kandi budakira mu nzoka. Nyamara, irindi suzuma ryumutekano, harimo ubushakashatsi ku nyamaswa zo hejuru n’amasomo y’abantu, birasabwa kumenya umutekano waryo wo gukoresha amavuriro.
Nubwo ubushakashatsi bwibanze bwerekanye ko 7,8-DHF ifite umutekano mwiza, ingaruka zishobora guterwa mubantu ntizwi. Kimwe nikindi kintu icyo ari cyo cyose gishya, hagomba kwitonderwa n'ingaruka mbi zishobora gukurikiranwa mugihe cyo gusuzuma imikoreshereze yabantu.
Ukurikije uburyo bwa 7.8-DHF bwibikorwa n'ingaruka ku bakira TrkB, ingaruka zimwe zishobora kuba zifitanye isano na 7,8-DHF zishobora kubamo:
Kubabara umutwe: Gukora kwa BDNF na TrkB bigenga ibikorwa bya neuronal hamwe nibyishimo; ubuyobozi bwa 7,8-DHF bushobora gutera umutwe kubantu bamwe.
Kudasinzira: Kongera ibikorwa bya neuronal hamwe na plastike ya synaptique bishobora kugira ingaruka kubitotsi, bishobora gutera kudasinzira cyangwa guhagarika ibitotsi.
Ibibazo bya Gastrointestinal: Kimwe na bioactive compound, 7,8-DHF irashobora gutera ingaruka mbi zo munda, nko kugira isesemi, kuruka, cyangwa impiswi mubantu bamwe.
Ni ngombwa kumenya ko izo ngaruka zishobora kuba zigomba kwigwa mubigeragezo byamavuriro. Bitewe nubushobozi bwayo bwo guhindura ibimenyetso bya BDNF hamwe no gukora reseptor ya TrkB, hagomba kandi kwitonderwa mugihe uhuza 7,8-DHF nibindi biyobyabwenge byibasira iyi nzira cyangwa bifite uburyo busa bwibikorwa.
Nkurwego rukomeye, 7,8-Dihydroxyflavone yakuruye abantu benshi kubera ibikorwa byihariye byibinyabuzima. Ku bashakashatsi mu bya siyansi n’inganda, ni ngombwa kubona ifu nziza-7,8-Dihydroxyflavone. Ifu ya 7,8-Dihydroxyflavone itangwa na Suzhou Myland ifite CAS numero 38183-03-8 nubuziranenge bugera kuri 98%. Ibicuruzwa byagenzuwe neza kandi byujuje ubuziranenge mpuzamahanga, byemeza neza umutekano n’ibicuruzwa. , bikwiranye nubushakashatsi bwa siyanse, guteza imbere ibiyobyabwenge, umusaruro wibikorwa byubuzima nizindi nzego, biguha amahitamo yizewe.
Ubwishingizi bufite ireme
Turabizi ko ubwiza bwibicuruzwa byacu bigira ingaruka ku buryo butaziguye ubushakashatsi bwabakiriya bacu nibisubizo byabyo. Kubwibyo, Suzhou Myland ikurikiza byimazeyo GMP (Imyitozo ngororamubiri myiza) hamwe na ISO yo gutanga ibyemezo mugihe cyo gukora kugirango habeho ituze kandi rihamye kuri buri cyiciro cyibicuruzwa. Byongeye kandi, itsinda ryacu R&D rikomeje gukora udushya mu ikoranabuhanga kandi riharanira gukomeza kunoza ubuziranenge n’imikorere.
Serivise y'abakiriya
Suzhou Myland ntabwo itanga ibicuruzwa byujuje ubuziranenge gusa, ahubwo inita kubyo abakiriya bakeneye. Dufite itsinda ryabahanga ryubuhanga rishobora guha abakiriya ibyifuzo byo gukoresha ibicuruzwa nubuyobozi bwa tekiniki kugirango dufashe abakiriya kugera kubisubizo byiza mubushakashatsi no kubishyira mubikorwa. Yaba igeragezwa rito cyangwa umusaruro munini, turashobora gutanga ibisubizo byoroshye kugirango duhuze ibyo abakiriya batandukanye bakeneye.
Nigute Wabona 7,8-Ifu ya Dihydroxyflavone
Niba ushaka ubuziranenge bwo hejuru 7,8-Dihydroxyflavone Powder, Suzhou Myland nibyo wahisemo. Urashobora kutwandikira kuri:
Urubuga rwemewe: Sura urubuga rwemewe rwa Suzhou Myland kugirango umenye byinshi kubyerekeye amakuru y'ibicuruzwa n'inkunga ya tekiniki.
Kugisha inama kumurongo: Vugana neza nitsinda ryabakiriya bacu binyuze mumikorere yo kugisha inama kumurongo itangwa nurubuga kugirango ubone amakuru yibicuruzwa hamwe na cote ukeneye.
Twandikire kuri terefone: Hamagara numero yacu kugirango tuvugane nabakozi bashinzwe kugurisha babigize umwuga kandi ubone amakuru arambuye yibicuruzwa nibitekerezo byo kugura.
Kubaza imeri: Urashobora kandi kutubaza amakuru yibicuruzwa ukoresheje imeri, kandi tuzagusubiza vuba bishoboka.
Mu gusoza
Nkurwego rwingenzi hamwe nibikorwa byinshi byibinyabuzima, 7,8-Dihydroxyflavone igenda ihinduka ikintu cyingenzi mubushakashatsi bwa siyanse no mubikorwa byinganda. Ifu yuzuye-7,8-Dihydroxyflavone Ifu yatanzwe na Suzhou Myland izatanga inkunga ikomeye mubushakashatsi bwawe no guteza imbere ibicuruzwa hamwe na serivise nziza kandi yizewe. Dutegereje kuzakorana nawe kugirango dushakishe byinshi mubishobora gukoreshwa 7,8-Dihydroxyflavone.
Ikibazo: 7,8-dihydroxyflavone ni iki?
Igisubizo: 7,8-Dihydroxyflavone ni flavonoide isanzwe ibaho izwiho kuba ishobora kuba neuroprotective kandi ikaba irimo kwigwa ku ngaruka zayo ku mikorere yubwenge no kuzamura imyumvire.
Ikibazo: Ni izihe nyungu zishobora kubaho 7,8-dihydroxyflavone?
Igisubizo: Ubushakashatsi bwerekana ko 7,8-dihydroxyflavone ishobora gufasha kunoza kwibuka, kugabanya amaganya, no kwirinda indwara zifata ubwonko. Imiterere ya antioxydeant irashobora kandi guteza imbere ubuzima muri rusange mukurwanya okiside.
Ikibazo: Niki bioavailable ya 7,8-DHF?
Igisubizo: Bioavailable ya 7,8-dihydroxyflavone (7,8-DHF) mubushakashatsi bwinyamanswa igera kuri 5% (mu mbeba) bitewe nubushake buke bwayo no guhindagurika vuba. Nubwo bioavailable nkeya, 7,8-DHF irashobora kurenga inzitizi yubwonko bwamaraso kandi ikagira ingaruka mubwonko. Ubundi bushakashatsi burakenewe kugirango umenye bioavailable yabantu no gushakisha uburyo bwo kuyitezimbere.
Ikibazo: Nigute 7,8-DHF igutera kumva?
Igisubizo: Nka nootropique, 7,8-dihydroxyflavone (7,8-DHF) igira ingaruka nziza kumikorere yubwenge no mumutima. Umuntu ku giti cye yibuka neza, kwibanda cyane, hamwe nubushobozi bwo kwiga.
Inshingano: Iyi ngingo ni iyamakuru rusange gusa kandi ntigomba gusobanurwa nkinama zose zubuvuzi. Amwe muma poste yamakuru aturuka kuri enterineti kandi ntabwo ari umwuga. Uru rubuga rufite inshingano zo gutondeka, gutunganya no guhindura ingingo. Intego yo gutanga amakuru menshi ntabwo bivuze ko wemera ibitekerezo byayo cyangwa kwemeza ukuri kwibirimo. Buri gihe ujye ubaza inzobere mu buzima mbere yo gukoresha inyongeramusaruro cyangwa guhindura ibintu byubuzima bwawe.
Igihe cyo kohereza: Ukwakira-14-2024
