Iimveliso

Ukuvinjelwa kwe-β-carbonic anhydrases (CAs, EC 4.2.1.1) kwi-pathogenic fungi Cryptococcus neoformans (Can2) kunye ne-Candida albicans (Nce103) kunye nochungechunge lwe-25 ye-branched aliphatic kunye ne-carboxylates enuka kamnandi iphandwe.I-isoforms yabantu i-hCA I kunye ne-II nazo zibandakanyiwe kwisifundo ukuze kuthelekiswe.I-Aliphatic carboxylates ngokuqhelekileyo yayiyi-millimolar hCA I kunye ne-II inhibitors kunye ne-micromolar / submicromolar β-CA inhibitors ephantsi.I-carboxylates enuka kamnandi yayiziinhibitors ze-micromolar zee-enzymes ezine kodwa ezinye zazo zibonise umsebenzi ophantsi we-nanomolar ngokuchasene ne-fungal pathogenic enzymes.I-4-Hydroxy- kunye ne-4-methoxy-benzoate inhibited Can2 ene-K (I) ye-9.5-9.9 nM.I-methyl esters, i-hydroxamates, i-hydrazides kunye ne-carboxamides yezinye zezi zinto ziphuma nazo zaziyi-inhibitors ezisebenzayo ze-α- kunye ne-β-CAs zaphandwa apha.

I-Parabens ziphakathi kwezona zigcina zisetyenziswa rhoqo ukuthintela ukukhula kwe-microbial kunye nokwandisa ubomi beshelufu yoluhlu lweemveliso zabathengi.Injongo yolu phononongo lwangoku yayikukufumana ukuqonda kwimetabolism ye-parabens kwiiseli zomhlaza webele (MCF7) kuba baye babonisa umsebenzi we-estrogenic kwezi seli kwaye zifunyenwe kwizicubu zomhlaza webele.Ubuthi be-parabens kwiiseli ze-MCF7 zagqitywa ngokusebenzisa iimvavanyo ze-MTT.I-Hydrolysis ye-methyl-, i-butyl kunye ne-benzyl-paraben kwi-p-hydroxybenzoic acid yahlalutywa kwiiseli ze-MCF7 ezikhuliswe kunye nakwii-homogenates zeselula.I-Glucuronidation kunye ne-sulfoconjugation zafundwa kwi-MCF7 homogenates, kwaye i-parabens yahlaziywa yi-HPLC.I-Methyl-paraben iboniswe ukuba inetyhefu encinci kune-butyl kunye ne-benzyl-paraben.IiParabens zazizinzile ngokupheleleyo kwi-MCF7 homogenates ngelixa i-p-nitrophenyl acetate, uhlobo lwe-substrate, lwenziwa i-hydrolysis.I-MCF7 i-homogenates yeeseli ayizange ibonise imisebenzi ye-glucuronidation kunye ne-sulfoconjugation ngokubhekiselele kwi-parabens.Ukuzinza okuphezulu kweparabens kunokuchaza ukuqokelela kwabo kwizicubu zomhlaza webele.