Impembelelo ye-anti-malaria ye-artemisinin

[Amagqabantshintshi]
Artemisinin (QHS) yi noveli sesquiterpene lactone equlathe peroxy ibhulorho esecaleni iyeza Chinese herbal iArtemisia annua L. Artemisinin inesakhiwo ezizodwa, ukusebenza kakuhle kunye netyhefu ephantsi.Ine-anti-tumor, anti-tumor, anti-bacterial, anti-malarial, kunye ne-immune-enhancing pharmacological effects.Ineziphumo ezikhethekileyo ekuxhatshazweni kohlobo lwengqondo kunye nokuxhatshazwa okunonya.Lichiza elichasene nemalariya elivunyiweyo kwihlabathi eTshayina.Iye yaba lelona chiza lifanelekileyo lokunyanga isifo seengcongconi elicetyiswa nguMbutho wezeMpilo weHlabathi.
[Iimpawu zomzimba nezekhemikhali]
I-Artemisinin yikristale yenaliti engenambala enendawo yokunyibilika ye-156 ~ 157 ° C. Inyibilika ngokulula kwi-chloroform, i-acetone, i-ethyl acetate kunye ne-benzene.Iyanyibilika kwi-ethanol, i-ether, ukunyibilika kancinane kwi-ether yepetroleum ebandayo, kwaye iphantse yanganyibiliki emanzini.Ngenxa yeqela elikhethekileyo le-peroxy, alizinzile ukutshisa kwaye lichithwa ngokulula ngenxa yempembelelo yezinto ezimanzi, ezishushu kunye nokunciphisa.
[Isenzo sonyango]
1. I-Anti-malarial effect I-Artemisinin ineepropati ezikhethekileyo ze-pharmacological kwaye inesiphumo esihle kakhulu sonyango kwi-malaria.Kwisenzo sokulwa nesifo seengcongconi se-artemisinin, i-artemisinin ibangela ukuqhekeka okupheleleyo kwesakhiwo sombungu ngokuphazamisana nomsebenzi we-membrane-mitochondrial we-malaria parasite.Uhlalutyo oluphambili lwale nkqubo lulandelayo: iqela le-peroxy kwisakhiwo semolekyuli ye-artemisinin ivelisa i-radicals yamahhala nge-oxidation, kwaye i-radicals yamahhala ibophelela kwiprotheni yemalariya, ngaloo ndlela isebenze kwi-membrane ye-protozoa ye-parasitic, itshabalalisa inwebu; I-membrane yenyukliya kunye ne-plasma membrane.I-mitochondria idumbile kwaye i-membrane yangaphakathi nangaphandle iyahlukana, ekugqibeleni itshabalalisa isakhiwo seselula kunye nomsebenzi we-malaria parasite.Kule nkqubo, iichromosomes kwinucleus ye-malaria parasite nazo ziyachaphazeleka.Uqwalaselo lwe-Optical kunye ne-electron microscopy lubonisa ukuba i-artemisinin ingangena ngokuthe ngqo kwi-membrane isakhiwo se-Plasmodium, enokuthi ithintele ngokufanelekileyo unikezelo lwezondlo ze-Plasmodium ezixhomekeke kwi-host blood cell pulp, ngaloo ndlela iphazamise umsebenzi we-membrane-mitochondrial ye-Plasmodium ( Kunokuba iphazamise i-folate metabolism, ekugqibeleni ikhokelela ekuweni ngokupheleleyo kwe-malaria parasite Ukusetyenziswa kwe-artemisinin kwakhona kunciphisa kakhulu umthamo we-isoleucine efakwe yi-Plasmodium, ngaloo ndlela inqanda ukuhlanganiswa kweeprotheni kwi-Plasmodium.
Ukongeza, impembelelo ye-antimalarial ye-artemisinin ikwanxulumene noxinzelelo lwe-oksijini, kwaye uxinzelelo lwe-oksijini ephezulu luya kunciphisa ugxininiso olusebenzayo lwe-artemisinin kwi-P. falciparum ekhuliswe kwi-vitro.Ukutshatyalaliswa kwe-malaria parasite yi-artemisinin yahlulwe ibe ziindidi ezimbini, enye kukutshabalalisa ngokuthe ngqo i-malaria parasite;enye kukonakalisa iiseli ezibomvu zegazi lemalariya, nto leyo ekhokelela ekufeni kwesifo seengcongconi.Impembelelo ye-antimalarial ye-artemisinin inesiphumo sokubulala ngokuthe ngqo kwisigaba se-erythrocyte sePlasmodium.Akukho mpembelelo ibalulekileyo kwizigaba zangaphambili kunye ne-extra-erythrocytic.Ngokungafaniyo nezinye ii-antimalarials, indlela yokulwa nesifo seengcongconi ye-artemisinin ixhomekeke ikakhulu kwi-peroxyl kwisakhiwo semolekyuli ye-artemisinin.Ubukho bamaqela e-peroxyl budlala indima eqinisekileyo kumsebenzi wokulwa nesifo seengcongconi we-artemisinin.Ukuba akukho qela leperoxide, i-artemisinin iyakuphulukana nomsebenzi wayo wokulwa nemalariya.Ngoko ke, kunokutshiwo ukuba indlela yokulwa nemalariya ye-artemisinin inxulumene ngokusondeleyo nokusabela kokubola kwamaqela e-peroxyl.Ukongeza kwisiphumo sayo esilungileyo sokubulala kwizifunxi-gazi zemalariya, i-artemisinin ikwanefuthe elithile lokuthintela kwezinye izifunxi-gazi.
2. I-Anti-tumor effect i-Artemisinin ineempembelelo ezicacileyo zokuthintela ukukhula kweeseli ezahlukeneyo zethumba ezifana neeseli zomhlaza wesibindi, iiseli zomhlaza wamabele kunye neeseli zomhlaza womlomo wesibeleko.Inani lophononongo lubonise ukuba i-artemisinin inendlela efanayo yokulwa nesifo seengcongconi kunye ne-anticancer, eyile, i-anti-malaria kunye ne-anti-cancer ngama-radicals asimahla eveliswa yi-peroxy bridge breaks in the molecular structure of artemisinin.Kwaye i-artemisinin derivative efanayo iyakhetha ukuthintela iintlobo ezahlukeneyo zeeseli zethumba.Isenzo se-artemisinin kwiiseli zethumba sixhomekeke ekwenziweni kwe-apoptosis yeseli ukugqiba ukubulawa kweeseli zethumba.Kwisiphumo esifanayo se-antimalarial, i-dihydroartemisinin inqanda ukusebenza kwezinto ezibangela i-hypoxia ngokunyusa iqela le-oksijini elisebenzayo.Ngokomzekelo, emva kokusebenza kwi-membrane yeseli yeeseli ze-leukemia, i-artemisinin inokunyusa i-intracellular concentration ye-calcium ngokutshintsha ukufikeleleka kwe-membrane yeseli yayo, engasebenzi nje i-calpain kwiiseli ze-leukemia, kodwa ikhuthaza nokukhululwa kwezinto ze-apoptotic.Ukukhawulezisa inkqubo apoptosis.
3. Iziphumo ze-Immunomodulatory I-Artemisinin inempembelelo yokulawula kwi-immune system.Phantsi kokuba idosi ye-artemisinin kunye nezinto eziphuma kuyo ayibangeli i-cytotoxicity, i-artemisinin inokuthintela i-T lymphocyte mitogen kakuhle, kwaye ngaloo ndlela inokubangela ukwanda kwe-spleen lymphocytes kwiimpuku.I-Artesunate inokunyusa umsebenzi opheleleyo wokuzalisekisa i-serum ye-mouse ngokuphucula umphumo wokugonyeka okungaqhelekanga.I-Dihydroartemisinin inokunqanda ngokuthe ngqo ukwanda kwee-lymphocytes ze-B kunye nokunciphisa ukukhutshwa kwe-autoantibodies yi-B lymphocytes, ngaloo ndlela inqanda impendulo ye-immune immune.
4. Isenzo se-Antifungal Isenzo se-antifungal se-artemisinin sibonakaliswa ekuthinteleni kwayo i-fungi.I-Artemisinin i-slag powder kunye ne-decoction ineempembelelo ezinamandla zokuthintela kwi-Staphylococcus epidermidis, i-Bacillus anthracis, i-diphtheria kunye ne-catarrhalis, kwaye ibe nemiphumo ethile kwi-Pseudomonas aeruginosa, i-Shigella, i-Mycobacterium tuberculosis kunye ne-Staphylococcus aureus.Isithintelo.
5. Anti-Pneumocystis carinii inyumoniya isiphumo Artemisinin ikakhulu utshabalalisa isakhiwo Pneumocystis carinii inwebu inkqubo, ebangela vacuoles kwi cytoplasm kunye nepakethe sporozoite trophozoites, ukudumba mitochondria, ukugqabhuka inwebu yenyukliya, ukudumba kwe endoplasmic reticulum iingxaki kunye ne-Intracapsulalural iingxaki ezifana ne-discapsula. utshintsho lwezakhiwo.
6. Anti-pregnancy effect Amachiza e-Artemisinin anetyhefu ephezulu ekhethiweyo kwiimbumba.Iidosi ezisezantsi zinokubangela ukuba iimbumba zife kwaye zikhuphe isisu.Inokuphuhliswa njengamachiza okuqhomfa.
7. I-Anti-Schistosomiasis Iqela elisebenzayo le-anti-schistosomiasis yibhulorho ye-peroxy, kwaye indlela yayo yokwelapha kukuchaphazela i-metabolism yeswekile yombungu.
8. Imiphumo ye-cardiovascular effects I-Artemisinin inokuthintela ngokuphawulekayo i-arrhythmia ebangelwa yi-ligation ye-coronary artery, enokuthi ilibazise kakhulu ukuqala kwe-arrhythmia ebangelwa yi-calcium chloride kunye ne-chloroform, kunye nokunciphisa kakhulu i-fibrillation ye-ventricular.
9. I-Anti-fibrosis Inxulumene nokuvimbela ukwanda kwe-fibroblast, ukunciphisa i-collagen synthesis, kunye ne-anti-histamine-induced collagen decomposition.
10. Ezinye iziphumo I-Dihydroartemisinin inempembelelo ebalulekileyo yokuthintela kwi-Leishmania donovani kwaye inxulumene nedosi.Isicatshulwa seArtemisia annua ikwabulala iTrichomonas vaginalis kunye nelysate amoeba trophozoites.


Ixesha lokuposa: Jul-19-2019