生物活性Eflornithine(Difluoromethylornithine,DFMO,MDL-71782,RMI-71782,α-difluoromethylornithine)hydrochloridehydrate通過(guò)對(duì)鳥(niǎo)氨酸脫羧酶的不可逆抑制作用,抑制多胺生物合成。它是一種化療保護(hù)劑,可阻止血管生成。其生物半衰期為8小時(shí)。靶點(diǎn)TargetValueOrndecarboxylase體外研究用α-difluoromethyl-Orn處理BY2細(xì)胞,抑制其過(guò)氧化氫的產(chǎn)生,但并沒(méi)有發(fā)生程序性細(xì)胞死亡。體內(nèi)研究EflornithineistheonlynewmoleculeregisteredforthetreatmentofhumanAfricantrypanosomiasisoverthelast50years.Itisthedrugusedmainlyasaback-upformelarsoprolrefractoryTrypanosomabruceigambiensecases.Insubjectswithexcessive,unwantedfacialhair,eflornithine15%creamissuperiortoplaceboinreducinghairgrowth.After24weeks'treatment,58%ofeflornithineand34%ofplacebosubjectshaveatleastsomeimprovementinfacialhirsutism.Thehairgrowthinhibitoryactivityofeflornithineissignificantlyenhancedwhentheeflornithinecreamisappliedontoamouseskinareapretreatedwithmicroneedles.TreatmentofcoarctationhypertensiveratswitheflornithineresultsinanormalizationofthecontractileintensitytoKCIandnorepinephrineandrelaxationstoacetylcholineby14daysofhypertension.
湖北省揚(yáng)一鑫盛生物醫(yī)藥有限公司
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