[Saib xyuas]
Artemisinin (QHS) yog ib qho tshiab sesquiterpene lactone uas muaj tus choj peroxy cais los ntawm Suav tshuaj ntsuab Artemisia annua L. Artemisinin muaj cov qauv tshwj xeeb, kev ua haujlwm siab thiab tsis muaj tshuaj lom.Nws muaj cov tshuaj tiv thaiv qog, tiv thaiv qog, tiv thaiv kab mob, tiv thaiv kab mob npaws, thiab tiv thaiv kev tiv thaiv cov tshuaj siv tshuaj.Nws muaj kev cuam tshuam tshwj xeeb rau kev tsim txom lub hlwb thiab kev tsim txom phem.Nws yog tib lub thoob ntiaj teb lees paub tshuaj tiv thaiv kab mob malarial hauv Suav teb.Nws tau dhau los ua cov tshuaj zoo tshaj plaws rau kev kho mob malaria pom zoo los ntawm World Health Organization.
[Lub cev thiab tshuaj muaj zog]
Artemisinin yog ib tug tsis muaj kob koob siv lead ua nrog ib tug melting point ntawm 156 ~ 157 ° C. Nws yog yooj yim soluble nyob rau hauv chloroform, acetone, ethyl acetate thiab benzene.Nws yog soluble nyob rau hauv ethanol, ether, me ntsis soluble nyob rau hauv txias petroleum ether, thiab yuav luag insoluble nyob rau hauv dej.Vim tias nws cov pab pawg tshwj xeeb peroxy, nws tsis ruaj khov rau cov cua sov thiab yooj yim decomposed los ntawm kev cuam tshuam ntawm ntub dej, kub thiab txo cov tshuaj.
[Pharmacological kev txiav txim]
1. Anti-malarial effect Artemisinin muaj cov khoom siv tshuaj tshwj xeeb thiab muaj kev kho mob zoo heev ntawm malaria.Nyob rau hauv cov tshuaj tiv thaiv kab mob ntawm artemisinin, artemisinin ua kom tiav kev tawg ntawm cov qauv ntawm tus cab los ntawm kev cuam tshuam nrog kev ua haujlwm ntawm daim nyias nyias-mitochondrial ntawm tus kab mob malaria.Lub ntsiab kev tsom xam ntawm cov txheej txheem no yog raws li nram no: pawg peroxy nyob rau hauv cov qauv molecular ntawm artemisinin generates dawb radicals los ntawm oxidation, thiab cov dawb radicals khi rau cov malaria protein, yog li ua rau lub membrane qauv ntawm cov kab mob parasitic protozoa, rhuav tshem daim nyias nyias, nuclear membrane thiab plasma membrane.Lub mitochondria yog o thiab cov ntaub so ntswg sab hauv thiab sab nrauv raug tshem tawm, nws thiaj li rhuav tshem cov qauv ntawm tes thiab kev ua haujlwm ntawm tus kab mob malaria.Nyob rau hauv cov txheej txheem no, cov chromosomes nyob rau hauv lub nucleus ntawm tus kab mob malaria parasite kuj raug cuam tshuam.Optical thiab electron microscopy soj ntsuam pom tau hais tias artemisinin tuaj yeem nkag ncaj qha mus rau hauv daim nyias nyias ntawm Plasmodium, uas tuaj yeem cuam tshuam cov khoom noj ntawm Plasmodium-dependent tus tswv tsev cov qe ntshav liab, thiab yog li cuam tshuam nrog lub membrane-mitochondrial kev ua haujlwm ntawm Plasmodium (tsis yog cuam tshuam nws. Kev siv cov artemisinin kuj tseem txo tau cov isoleucine noj los ntawm Plasmodium, yog li inhibiting synthesis ntawm cov proteins hauv Plasmodium.
Tsis tas li ntawd, cov nyhuv antimalarial ntawm artemisinin kuj muaj feem xyuam rau cov pa oxygen, thiab cov pa oxygen siab yuav txo tau cov concentration ntawm artemisinin ntawm P. falciparum cultured hauv vitro.Kev puas tsuaj ntawm cov kab mob malaria los ntawm artemisinin tau muab faib ua ob hom, ib qho yog los rhuav tshem cov kab mob malaria ncaj qha;lwm qhov yog ua kom cov qe ntshav liab ua rau cov kab mob malaria parasite, uas ua rau cov kab mob malaria tuag.Cov nyhuv antimalarial ntawm artemisinin muaj cov nyhuv ncaj qha tua ntawm erythrocyte theem ntawm Plasmodium.Tsis muaj qhov cuam tshuam tseem ceeb ntawm cov theem ua ntej thiab ntxiv-erythrocytic.Tsis zoo li lwm cov tshuaj tiv thaiv kab mob, cov tshuaj tiv thaiv kab mob ntawm artemisinin tso siab rau peroxyl hauv cov qauv molecular ntawm artemisinin.Lub xub ntiag ntawm cov pab pawg peroxyl ua lub luag haujlwm txiav txim siab hauv kev ua haujlwm tiv thaiv kab mob ntawm artemisinin.Yog tias tsis muaj cov pab pawg peroxide, artemisinin yuav poob nws cov tshuaj tiv thaiv kab mob.Yog li, nws tuaj yeem hais tau tias cov tshuaj tiv thaiv kab mob ntawm artemisinin muaj feem cuam tshuam nrog cov tshuaj tiv thaiv decomposition ntawm peroxyl pawg.Ntxiv nrog rau nws cov nyhuv tua zoo ntawm cov kab mob malaria, artemisinin kuj muaj qee yam cuam tshuam rau lwm yam kab mob.
2. Cov nyhuv tiv thaiv qog nqaij hlav Artemisinin muaj qhov pom tseeb inhibitory cuam tshuam rau kev loj hlob ntawm ntau cov qog hlwb xws li qog nqaij hlav qog nqaij hlav, cov qog nqaij hlav cancer mis thiab cov qog nqaij hlav qog noj ntshav.Ntau cov kev tshawb fawb tau pom tias artemisinin muaj tib lub tswv yim ntawm kev tawm tsam malaria thiab anticancer, uas yog, anti-malarial thiab anti-cancer los ntawm dawb radicals generated los ntawm peroxy choj so nyob rau hauv lub molecular qauv ntawm artemisinin.Thiab tib yam artemisinin derivative yog xaiv rau inhibition ntawm ntau hom qog hlwb.Qhov kev txiav txim ntawm artemisinin ntawm cov qog hlwb tso siab rau qhov induction ntawm cell apoptosis kom ua tiav kev tua cov qog hlwb.Nyob rau hauv tib cov nyhuv antimalarial, dihydroartemisinin inhibits qhov ua rau ntawm hypoxia inducing yam los ntawm kev ua kom cov pa reactive pa.Piv txwv li, tom qab ua yeeb yam ntawm cov cell membrane ntawm leukemia hlwb, artemisinin tuaj yeem nce cov calcium hauv cov cell los ntawm kev hloov cov permeability ntawm nws cov cell membrane, uas tsis tsuas yog activates calpain nyob rau hauv leukemia hlwb, tab sis kuj txhawb kev tso tawm ntawm apoptotic tshuaj.Ceev cov txheej txheem ntawm apoptosis.
3. Cov teebmeem Immunomodulatory Artemisinin muaj kev tswj xyuas kev tiv thaiv kab mob.Nyob rau hauv cov xwm txheej uas ntau npaum li cas ntawm artemisinin thiab nws cov derivatives tsis ua rau cytotoxicity, artemisinin tuaj yeem inhibit T lymphocyte mitogen zoo, thiab yog li tuaj yeem ua rau muaj qhov nce ntawm spleen lymphocytes hauv cov nas.Artesunate tuaj yeem ua kom tag nrho cov haujlwm ntxiv ntawm nas cov ntshav los ntawm kev txhim kho cov txiaj ntsig ntawm kev tiv thaiv tsis tshwj xeeb.Dihydroartemisinin tuaj yeem cuam tshuam ncaj qha rau kev loj hlob ntawm B lymphocytes thiab txo qhov tso tawm ntawm autoantibodies los ntawm B lymphocytes, yog li inhibiting lub zog tiv thaiv kab mob.
4. Antifungal action Cov tshuaj tiv thaiv kab mob ntawm artemisinin yog tshwm sim hauv nws cov inhibition ntawm fungi.Artemisinin slag hmoov thiab decoction muaj zog inhibitory teebmeem ntawm Staphylococcus epidermidis, Bacillus anthracis, diphtheria thiab catarrhalis, thiab kuj muaj qee yam teebmeem ntawm Pseudomonas aeruginosa, Shigella, Mycobacterium tuberculosis thiab Staphylococcus aureus.Inhibition.
5. Anti-Pneumocystis carinii pneumonia nyhuv Artemisinin tsuas yog rhuav tshem cov qauv ntawm Pneumocystis carinii membrane system, ua rau vacuoles nyob rau hauv lub cytoplasm thiab pob ntawm sporozoite trophozoites, mitochondria o, nuclear membrane rupture, o ntawm endoplasm thiab restructuring teeb meem xws li o. kev hloov ntawm ultrastructural.
6. Cov tshuaj tiv thaiv cev xeeb tub cov tshuaj Artemisinin muaj kev xaiv toxicity rau embryos.Cov koob tshuaj qis dua tuaj yeem ua rau embryos tuag thiab ua rau nchuav menyuam.Nws tuaj yeem tsim los ua tshuaj rho menyuam.
7. Anti-Schistosomiasis Cov tshuaj tiv thaiv kab mob schistosomiasis active pab pawg yog ib tug peroxy choj, thiab nws cov tshuaj mechanism yog cuam tshuam rau cov piam thaj metabolism ntawm tus cab.
8. Cov teebmeem ntawm cov hlab plawv Artemisinin tuaj yeem tiv thaiv arrhythmia uas tshwm sim los ntawm ligation ntawm cov hlab ntsha, uas tuaj yeem cuam tshuam qhov pib ntawm arrhythmia tshwm sim los ntawm calcium chloride thiab chloroform, thiab txo qis ventricular fibrillation.
9. Anti-fibrosis Nws muaj feem xyuam rau inhibiting fibroblast proliferation, txo collagen synthesis, thiab anti-histamine-induced collagen decomposition.
10. Lwm yam teebmeem Dihydroartemisinin muaj cov nyhuv inhibitory tseem ceeb ntawm Leishmania donovani thiab muaj feem cuam tshuam txog koob tshuaj.Artemisia annua extract kuj tua Trichomonas vaginalis thiab lysate amoeba trophozoites.
Post lub sij hawm: Jul-19-2019