[Chidule]
Artemisinin (QHS) ndi buku sesquiterpene lactone munali peroxy mlatho olekanitsidwa ndi Chinese mankhwala azitsamba Artemisia annua L. Artemisinin ali dongosolo wapadera, dzuwa mkulu ndi otsika kawopsedwe.Lili ndi anti-chotupa, anti-tumor, anti-bacterial, anti-malarial, komanso chitetezo chamthupi chowonjezera mphamvu za pharmacological.Zimakhala ndi zotsatira zapadera pa nkhanza zamtundu waubongo komanso nkhanza zoyipa.Ndiwo mankhwala okhawo odziwika padziko lonse lapansi oletsa malungo ku China.Iwo wakhala mankhwala abwino kwambiri ochizira malungo omwe bungwe la World Health Organization limalimbikitsa.
[Zinthu zakuthupi ndi zamankhwala]
Artemisinin ndi kristalo wa singano wopanda mtundu wokhala ndi malo osungunuka a 156 ~ 157 ° C. Ndiwosavuta kusungunuka mu chloroform, acetone, ethyl acetate ndi benzene.Amasungunuka mu ethanol, ether, kusungunuka pang'ono mumafuta ozizira a petroleum ether, ndipo pafupifupi osasungunuka m'madzi.Chifukwa cha gulu lake lapadera la peroxy, silikhazikika kutentha ndipo limawonongeka mosavuta ndi mphamvu ya zinthu zonyowa, zotentha komanso zochepetsera.
[Pharmacological action]
1. Anti-malungo zotsatira Artemisinin ali wapadera pharmacological katundu ndipo ali wabwino kwambiri achire zotsatira pa malungo.Mu antimalarial zochita za artemisinin, artemisinin imayambitsa kuzimiririka kwathunthu kwa kapangidwe ka nyongolotsi mwa kusokoneza nembanemba-mitochondrial ntchito ya tizilombo ta malungo.Kusanthula kwakukulu kwa njirayi ndi motere: gulu la peroxy mu dongosolo la maselo a artemisinin limapanga ma radicals aulere ndi okosijeni, ndipo ma radicals aulere amamanga mapuloteni a malungo, potero akugwira ntchito pa nembanemba ya parasitic protozoa, kuwononga nembanemba. nyukiliya membrane ndi plasma membrane.Mitochondria imatupa ndipo nembanemba zamkati ndi zakunja zimabisika, ndipo pamapeto pake zimawononga ma cell ndi ntchito ya tizilombo ta malungo.Pochita zimenezi, ma chromosome omwe ali m’kati mwa tizilombo ta malungo amakhudzidwanso.Kuwona ndi electron microscopy kuona zikusonyeza kuti artemisinin akhoza mwachindunji kulowa nembanemba dongosolo Plasmodium, amene angathe kutsekereza michere kotunga Plasmodium amadalira khamu ofiira zamkati magazi, motero kusokoneza nembanemba-mitochondrial ntchito ya Plasmodium ( M'malo kusokoneza ake Kugwiritsidwa ntchito kwa artemisinin kumachepetsanso kwambiri kuchuluka kwa isoleucine yomwe imalowetsedwa ndi Plasmodium, motero imalepheretsa kaphatikizidwe ka mapuloteni mu Plasmodium.
Kuonjezera apo, mphamvu ya antimalarial ya artemisinin imagwirizananso ndi kuthamanga kwa okosijeni, ndipo kuthamanga kwa okosijeni kumachepetsa mphamvu ya artemisinin pa P. falciparum yolimidwa mu vitro.Kuwonongeka kwa tizilombo ta malungo ndi artemisinin kumagawidwa m'mitundu iwiri, imodzi ndiyo kuwononga mwachindunji tizilombo toyambitsa matenda;ina ndiyo kuwononga maselo ofiira a m’magazi a tizilombo toyambitsa malungo, zomwe zimachititsa kuti tizilombo toyambitsa malungo tizifa.The antimalarial zotsatira za artemisinin ali mwachindunji kupha kwenikweni pa erythrocyte gawo la Plasmodium.Palibe zotsatira zazikulu pazigawo zoyamba ndi zowonjezera-erythrocytic.Mosiyana ndi mankhwala ena oletsa malungo, njira yoletsa malungo ya artemisinin imadalira makamaka peroxyl mu kapangidwe ka molekyulu ya artemisinin.Kukhalapo kwa magulu a peroxyl kumagwira ntchito yolimbana ndi malungo ya artemisinin.Ngati palibe gulu la peroxide, artemisinin idzataya ntchito yake ya malungo.Choncho, tinganene kuti antimalarial mechanism ya artemisinin imagwirizana kwambiri ndi kuwonongeka kwa magulu a peroxyl.Kuphatikiza pa kupha kwabwino kwa majeremusi a malungo, artemisinin ilinso ndi zoletsa zina pa majeremusi ena.
2. Anti-chotupa zotsatira Artemisinin ali zoonekeratu chopinga zotsatira kukula kwa zosiyanasiyana chotupa maselo monga maselo a khansa ya chiwindi, maselo a khansa ya m'mawere ndi khomo lachiberekero maselo.Kafukufuku wambiri awonetsa kuti artemisinin ali ndi njira yofananira ndi malungo ndi anticancer, yomwe ndi anti-malarial ndi anti-cancer ndi ma free radicals opangidwa ndi peroxy mlatho wosweka mu kapangidwe ka maselo a artemisinin.Ndipo yemweyo wotumphukira artemisinin ndi kusankha kwa chopinga wa mitundu yosiyanasiyana ya chotupa maselo.Zochita za artemisinin pama cell chotupa zimadalira kulowetsa kwa cell apoptosis kuti amalize kupha maselo otupa.Momwemonso antimalarial tingati dihydroartemisinin linalake ndipo tikulephera kutsegula kwa hypoxia inducing zinthu ndi kuwonjezera zotakasika mpweya gulu.Mwachitsanzo, pambuyo pochita pa selo nembanemba wa khansa ya m'magazi, artemisinin akhoza kuonjezera okhudza maselo ambiri kashiamu ndende ndi kusintha permeability ake selo nembanemba, amene osati imayendetsa calpain mu khansa ya m'magazi, komanso amalimbikitsa amasulidwe apoptotic zinthu.Kufulumizitsa ndondomeko ya apoptosis.
3. Immunomodulatory zotsatira Artemisinin ali ndi ulamuliro zotsatira pa chitetezo cha m'thupi.Pansi pa chikhalidwe kuti mlingo wa artemisinin ndi zotumphukira zake sayambitsa cytotoxicity, artemisinin akhoza ziletsa T lymphocyte mitogen bwino, ndipo motero akhoza kulimbikitsa kuwonjezeka ndulu lymphocytes mu mbewa.Artesunate imatha kukulitsa ntchito yokwanira ya seramu ya mbewa powonjezera mphamvu ya chitetezo chamthupi chomwe sichinatchulidwe.Dihydroartemisinin akhoza mwachindunji ziletsa kuchulukana B lymphocytes ndi kuchepetsa katulutsidwe wa autoantibodies ndi B lymphocytes, potero inhibiting ndi humoral chitetezo poyankha.
4. Antifungal kanthu The antifungal zochita za artemisinin zimaonekera poletsa ake bowa.Artemisinin slag ufa ndi decoction ndi amphamvu inhibitory zotsatira pa Staphylococcus epidermidis, Bacillus anthracis, diphtheria ndi catarrhalis, komanso zotsatira zina pa Pseudomonas aeruginosa, Shigella, Mycobacterium chifuwa chachikulu ndi Staphylococcus aureus.Kuletsa.
5. Anti-Pneumocystis carinii chibayo zotsatira Artemisinin makamaka kuwononga dongosolo Pneumocystis carinii nembanemba, kuchititsa vacuoles mu cytoplasm ndi phukusi la sporozoite trophozoites, kutupa mitochondria, nyukiliya nembanemba kuphulika, kutupa kwa endoplasmic reticulum reticulum, Intracapsulal mavuto monga discapsular ndi discapsula. ultrastructural kusintha.
6. Anti-mimba zotsatira Artemisinin mankhwala ndi mkulu kusankha kawopsedwe kwa mazira.Mlingo wocheperako ungayambitse miluza kufa ndikupangitsa kupita padera.Itha kupangidwa ngati mankhwala ochotsa mimba.
7. Anti-Schistosomiasis Gulu logwira ntchito la anti-schistosomiasis ndi mlatho wa peroxy, ndipo njira yake yamankhwala imakhudza kagayidwe ka shuga wa nyongolotsi.
8. Zotsatira za mtima wa Artemisinin akhoza kwambiri kupewa arrhythmia chifukwa cha kulumikiza kwa mitsempha ya m'mitsempha, yomwe ingachedwetse kwambiri kuyambika kwa arrhythmia chifukwa cha calcium kolorayidi ndi chloroform, ndi kuchepetsa kwambiri fibrillation yamitsempha yamagazi.
9. Anti-fibrosis Zimakhudzana ndi kuletsa kufalikira kwa fibroblast, kuchepetsa kaphatikizidwe ka collagen, ndi kuwonongeka kwa antihistamine-induced collagen.
10. Zotsatira zina Dihydroartemisinin ili ndi mphamvu yoletsa kwambiri Leishmania donovani ndipo imagwirizana ndi mlingo.Kutulutsa kwa Artemisia annua kumaphanso Trichomonas vaginalis ndi lysate amoeba trophozoites.
Nthawi yotumiza: Jul-19-2019