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Sinteza novih steroidnih jedinjenja od potencijalnog biomedicinskog značaja / Synthesis of new steroidal compounds of potentialbiomedical importanceNikolić Andrea 25 April 2014 (has links)
<p>Cilj ove doktorske disertacije je bila sinteza novih steroidnih 16,17-seko-16,17a-dinitrila polazeći od dehidroepiandrosterona (1), odnosno estrona (14). U androstanskoj seriji su izvršene modifikacije 16,17-seko-16,17a-dinitrila 12 u A i/ili B prstenu steroidnog jezgra, pri čemu novosintetizovana jedinjenja sadrže 4-en-3-on, 1,4-dien-3-on ili 1,4,6-trien-3-on sistem, kao i supstituente u položajima C-4, odnosno C-6 (6-metilen, 6-keto i 6-oksimino). U radu je takođe proučavan uticaj odabranih novosintetizovanih jedinjenja na proliferaciju sedam ćelijskih linija humanih tumora, dok je kao kontrola služila jedna zdrava humana ćelijska linija.</p> / <p>Starting from dehydroepiandrosterone (1) or estrone (14) new steroidal 16,17-seco-16,17a-dinitriles were synthesized. Modification of 16,17-seco-16,17a-dinitrile 12 afforded androstane derivatives containing 4-en-3-on, 1,4-dien-3-on or 1,4,6-trien-3-on system, with different substituents on position C-4 or C-6 (6-methylene, 6-keto i 6-oximino). Antiproliferative activity of some newly synthesized compounds were examined against seven human tumor cell lines, while healthy cells served as control.</p>
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Uticaj modifikovanih steroidnih jedinjenja na ćelijski ciklus, indukciju apoptoze i nastanak genetskih oštećenja u humanim tumorskim ćelijama / Effect of modified steroid compounds on cell cycle, apoptosis induction and occurrence of genetic defects in human tumor cellsJakimov Dimitar 28 October 2016 (has links)
<p>U radu je ispitan uticaj odabranih modifikovanih steroida na proliferaciju ćelija humanih malignih tumora i zdravih ćelija, a zatim njihov uticaj na modifikaciju ćelijskog ciklusa, indukovanje apoptoze i genetskih oštećenja u tumorskim ćelijama najsenzitivnijim na ova jedinjenja (MDA-MB-231 ćelijska linija humanog adenokarcinoma dojke, ER-). Ispitana je<em> in vitro </em>citotoksičnost odabranih steroidnih derivata prema ćelijskim linijama MCF-7, MDA-MB-231, PC3, HeLa, HT-29, MRC-5, K562 i A549, i proučavan ćelijski mehanizam koji je u osnovi uočenog antiproliferativnog efekta svakog od ispitivanih derivata. Sva ispitivana jedinjenja indukuju apoptozu MDA-MB-231 ćelija, na različite načine i sa različitim potencijalom. Genotoksikološka studija upotpunjuje rezultate proučavanja efekta ispitivanih steroidnih jedinjenja na biološke sisteme, ukazujući na izostanak genotoksičnosti ovih jedinjenja i njihov biomedicinski potencijal.</p> / <p>In this work the effect of selected modified steroids on proliferation of human malignant tumor and healthy cells, as well as their impact on the modification of cell cycle arrest, induction of apoptosis and genetic defects in tumor cells most sensitive to these compounds (MDA-MB-231 cell line of human breast adenocarcinoma, ER-) were examined. We examined the<em> in vitro </em>cytotoxicity of selected steroidal derivatives towards MCF-7, MDA-MB-231, PC-3, HeLa, HT-29, MRC-5, K562 and A549 cell lines, and studied the cellular mechanism that is underlying the antiproliferative activity expressed by these steroidal derivatives. All tested compounds induced apoptosis of MDA-MB-231 cells, in different ways and with different potential. Genotoxicological study complements the results of the study of the effect of tested steroidal compounds on biological systems, pointing out the lack of genotoxicity of these compounds and therefore their biomedical potential.</p>
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Definisanje lipofilnosti, farmakokinetičkih parametara i antikancerogenog potencijala novosintetisane serije stiril laktona / Defining of lipophilicity, pharmacokinetic parameters and anticancer potential of newly synthesized series of styryl lactonesLončar Davor 15 October 2018 (has links)
<p style="text-align: justify;">Reverzno-faznom tečnom hromatografijom pod visokim pritiskom primenom dva sistema<br />rastvarača ispitano je ponašanje i hromatografska lipofilnost prirodnih stiril laktona 7-(+)-<br />goniofufurona, 7-epi-(+)-goniofufurona, krasalaktona B i C i dvadeset njihovih<br />novosintetizovanih derivata i analoga. U ranijim ispitivanjima pokazalo se da ova jedinjenja<br />imaju veliki biološki potencijal jer pokazuju zapaženu citotoksičnost prema više humanih<br />tumorskih ćelijskih linija. Hromatografsko ponašanje jedinjenja uglavnom je u skladu sa<br />njihovom strukturom. Ustanovljene su linearne veze između hromatografskih retencionih<br />konstanti i većine in silico parametara lipofilnosti. Primenom hemometrijske QSRR analize<br />utvrđeni su veoma dobri multi linearni regresioni prediktivni modeli kvantitativne zavisnosti<br />između eksperimentalno dobijene hromatografske retencione konstante, koja definiše<br />retenciju jedinjenja u čistoj vodi i in silico molekulskih deskriptora odnosno strukture<br />jedinjenja. Lipofilnost jedinjenja ima najveći uticaj na njihove farmakokinetičke, tj. ADME<br />(apsorpcija, distribucija, metabolizam, eliminacija) osobine. Definisani su i statistički<br />potvrđeni najbolji multi linearni regresioni modeli zavisnosti farmakokinetičkih parametara<br />stiril laktona i od drugih molekulskih deskriptora. In vitro citotoksična aktivnost jedinjenja<br />evaluirana je prema četiri nove humane maligne ćelijske linije: kancer prostate (PC3), kancer debelog creva (HT-29), melanom (Hs294T), adenokancer pluća (A549). Najaktivnije<br />novosintetizovano jedinjenje je triciklični 4-fluorocinamatni analog, koji ispoljava<br />nanomolarnu aktivnost (IC<sub>50</sub> 2,1 nM) prema ćelijama melanoma i aktivniji je preko 2250 puta od komercijalnog antitumorskog agensa doksorubicina (DOX). SAR analizom utvrđena je zavisnost između strukture i biološke aktivnosti jedinjenja. Molekulskim dokingom ispitana je veza stiril laktona i ciljanog proteina značajnog za kancer prostate. Jedinjenja sa visokom inhibitornom aktivnošću prema ćelijama kancera prostate imaju visok doking skor i mogu graditi koordinativno-kovalentnu vezu sa Fe<sup>2</sup>+jonom prisutnim u aktivnom centru enzima. 3D-QSAR analizom, koja je izvedena metodama komparativnih polja CoMFA i CoMSIA, formiran je značajan prediktivni model između hemijske strukture i biološke aktivnosti stiril laktona.</p> / <p>The behavior and the chromatographic lipophilicity natural styryl lactone 7-(+)-<br />goniofufurone, 7-epi-(+)-goniofufurone, crassalactones B and C and twenty of their newly<br />synthesized derivatives and analogs were examined using reverse-phase high performance liquid chromatography in the two solvent systems. In previous studies it has been shown that these compounds have great biological potential toward several human tumor cell lines. Chromatographic behavior of the compounds is generally in accordance with their structure. The relationships between the chromatographic retention constants and the majority of their in silico lipophilicity parameters are linear. The application of chemometric QSRR analysis determined very good multiple linear regression predictive models of quantitative correlation between experimentally obtained chromatographic retention constant, which determines the retention of the compound in pure water and in silico molecular descriptors, i.e. the structure of the compound. The lipophilicity of the compounds has a major influence on their pharmacokinetics, i.e. ADME (absorption, distribution, metabolism, elimination) properties. The best multi-linear regression models depending on the pharmacokinetic parameters of styryl lactone and other molecular descriptors have been defined and statistically validated. In vitro cytotoxic activity of the compounds was evaluated according to four novel human malignant cell lines: prostate cancer (PC3), colon cancer (HT-29), melanoma (Hs294T), lung adenocarcinom (A549). The most active compound was tricyclic 4-fluorocinnamic analog, which exhibits a nanomolar activity (IC50 2,1 nM) toward melanoma cells. This compound is over 2250 times more active than commercial antitumor agent doxorubicin (DOX). SAR analysis has revealed a correlation between the structure and the biological activity of the compounds. Using the molecular docking the relationship of the styryl lactone and the target protein important for prostate cancer was examined. The compounds with high inhibitory activity against prostate cancer cells have a high docking score and are capable to form a coordinative-covalent bond with a Fe2+ ion present in the active centre of the enzyme. 3DQSAR analysis, which was performed by methods of comparative CoMFA and CoMSIA fields, has formed a good predictive model between chemical structure and biological activity of the styryl lactone.</p>
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Vrste tribusa Scandicae (Apiaceae Lindley 1836, subfam. Apioideae) potencijalni izvor biološki i farmakološki aktivnih sekundarnih biomolekula / Scandiceae tribe (Apiaceae Lindley 1836, subfam. Apioideae) species – potential resources of biologically and pharmacologically active secondary biomoleculesOrčić Dejan 02 July 2010 (has links)
<p>Ispitani su hemijski sastav i biološka aktivnost šest samoniklih vrsta iz tribusa Scandiceae<br />(familija Apiaceae): Anthriscus sylvestris, Anthriscus cerefolium, Chaerophyllum bulbosum,<br />Chaerophyllum hirsutum, Chaerophyllum temulentum i Scandix pecten-veneris. LC-MS-MS<br />analizom ekstrakata identifikovano je više desetina sekundarnih biomolekula iz klasa flavonoida,<br />fenilpropenskih kiselina, lignana i kumarina. GC-MS analiza pružila je uvid u sastav volatilnih<br />komponenti i njihov hemosistematski značaj. Potvrđeno je da sve ispitivane vrste imaju umereno<br />antioksidantno, antiinflamatorno i antiproliferativno dejstvo.</p> / <p> Chemical composition and biological activity of six wild-growing species from<br /> Scandiceae tribe (Apiaceae family) – Anthriscus sylvestris, Anthriscus cerefolium, Chaerophyllum<br /> bulbosum, Chaerophyllum hirsutum, Chaerophyllum temulentum and Scandix pecten-veneris – was<br /> examined. By LC-MS-MS analysis, a large number of secondary biomolecules was identified in<br /> extracts, including flavonoids, phenylpropenic acids, lignans and coumarins. GC-MS analysis<br /> provided insight into volatile components composition and chemosystematic significance. All<br /> investigated species exhibited moderate antioxidant, anti-inflammatory and antiproliferative<br /> activity.</p>
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Sinteza i fizičko-hemijska karakterizacija N-aromatičnih monosupstituisanih derivata karbohidrazona i tiokarbohidrazona / Synthesis and physicochemical haracterization of N-aromatic monosubstituted carbohydrazones аnd thiocarbohydrazonesMrđan Gorana 25 September 2020 (has links)
<p>U ovoj doktorskoj disertaciji je radi fizičko-hemijske karakterizacije i ispitivanja potencijalne<br />biološke aktivnosti sintetisano 40 derivata mono(tio)karbohidrazona. Strukture dobijenih jedinjenja su potvrđene NMR i FT–IR spektroskopijom, elementalnom i rendgenskom strukturnom analizom. Uticaj rastvarača i prisutnog supstituenta na položaje apsorpcionih maksimuma ispitani su po principima LSER i LFER metoda. Teorijski proračuni za sintetisana jedinjenja izvedeni su primenom TD–DFT metode. Jonizacione konstante derivata mono(tio)karbohidrazona su određene potenciometrijskim titracijama. Antioksidativna aktivnost je određena primenom tri testa: DPPH, ABTS i FRAP testa. Antimikrobna aktivnost je ispitana mikrodilucionom metodom na dva soja bakterija: Staphylococcus aureus i Escherichia coli. Za jedinjenja koja su pokazali antimikrobnu aktivnost je ispitan procenat citotoksičnosti. Sveukupan zaključak o sličnosti i razlikama sintetisanih derivata izveden je na osnovu multivarijatnih metoda klaster analize i analize glavnih komponenti.</p> / <p>In this doctoral dissertation, 40 mono(thio)carbohydrazone derivatives were synthesized for the purpose of physico-chemical characterization and examination of potential biological activity. The structures of the obtained compounds were confirmed by NMR and FT –IR spectroscopy, elemental analysis and X-ray structural analysis. The influence of solvent and substituent present on the positions of absorption maxima was examined according to the principles of LSER and LFER methods. Theoretical calculations for the synthesized compounds were performed by the TD–DFT method. The acid constants of mono(thio)carbohydrazone derivatives were determined by potentiometric titrations. Antioxidant activity was determined using three tests: DPPH, ABTS and FRAP test. Antimicrobial activity was examined by microdilution method on two strains of bacteria: Staphylococcus aureus and Escherichia coli. The percentage of cytotoxicity was examined for compounds that showed antimicrobial activity. Overall conclusion about the similarities and differences of the synthesized derivatives was studied by multivariate methods of cluster analysis and analysis of principal components.</p>
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Sekundarni biomolekuli u vrstama Allium sect. Codonoprasum Rchb. – biološke aktivnosti, fitohemijski i hemotaksonomski aspekti / Secondary metabolites from selected species of genus Allium sect. Codonoprasum Rchb. – biological activities, phytochemical and chemotaxonomic aspectsSimin Nataša 30 January 2015 (has links)
<p>U ovoj doktorskoj disertaciji ispitan je hemijski sastav i biološke aktivnosti<br />ekstrakata deset samoniklih taksona roda <em>Allium</em> sect. <em> Codonoprasum: A. carinatum</em> subsp. <em>pulchellum, A. carinatum </em> subsp. <em>carinatum, A. fuscum </em> var. <em>gracile, A. fuscum </em> var. <em>fuscum, A. flavum</em> subsp. <em>flavum, A. melanantherum, A. paniculatum </em> subsp. <em> marginatum, A. pallens</em> subsp. <em>tenuiflorum, A. oleraceum </em>i <em> A. rhodopeum</em>, sakupljenih na 27 lokaliteta u Srbiji. Cilj rada bio je da se dobiju podaci o sadržaju biološki aktivnih jedinjenja u ovim, do sada veoma malo ispitanim vrstama roda <em>Allium</em>, i utvrdi njihova potencijalna lekovita vrednost.</p><p>Analiza hemijskog sastava obuhvatila je: analizu volatilnih komponenti svežih <br />lukovica primenom headspace GC-MS tehnike, kvalitativnu analizu metanolnih <br />ekstrakata primenom tečnohromatografskih metoda (LC-DAD-MS i LC-MS-MS), <br />kvantitativnu analizu odabranih fenolnih jedinjenja LC-MS-MS tehnikom, određivanje sadržaja ukupnih monomernih antocijana i određivanje aktivnosti aliinaze. Ispitivanja bioloških aktivnosti ekstrakata obuhvatila su: određivanje antioksidantne, antiinflamatorne, antimikrobne, antimutagene i genotoksične aktivnosti, kao i ispitivanje uticaja na rast zdravih i tumorskih ćelija i sposobnosti indukcije ćelijske smrti. </p><p>Sumiranjem dobijenih rezultata može se zaključiti da ispitivani predstavnici roda <br /><em>Allium </em> sect. <em>Codonoprasum </em> predstavljaju bogate izvore biološki aktivnih jedinjenja sa širokim spektrom bioloških aktivnosti. Sa hemotaksonomskog aspekta značajno je da se dimetil-disulfid izdvaja kao najdominantnija i često jedina isparljiva komponenta, da ekstrakti većine vrsta sadrže veliku količinu flavonoida (prvenstveno derivata kvercetina), da se vrste <em> A. pallens </em> i <em>A. oleraceum</em> izdvajaju od ostalih po tome što ne sadrže rutin a sadrže hiperozid, da je vrsta <em> A. rhodopeum</em> siromašna fenolnim jedinjenjima i da su sve vrste, osim vrste <em>A. flavum</em>, bogate antocijanima. Aktivnost aliinaze je visoka u svim ispitivanim vrstama. Većina ispitivanih ekstrakata, izuzev ekstrakata vrsta <em>A. carinatum </em>i <em>A. melanantherum</em>, pokazala je izraženu antioksidantnu aktivnost, dok su ekstrakti vrsta <em>A. flavum</em>, <em>A. rhodopeum</em>, <em>A. oleraceum </em>i <em>A. paniculatum </em>snažni antiinflamatorni agensi. Ekstrakti ispitivanih predstavnika sect. <em> Codonoprasum </em>nisu pokazali antimikrobnu i antimutagenu aktivnost. Takođe, ovi ekstrakti nisu ispoljili genotoksični efekat na ćelije zdravog tkiva (izuzev slabog genotoksičnog efekta ekstrakta nadzemnih delova <em> A. flavum</em>), što ukazuje na bezbednost upotrebe vrsta sect. <em>Codonoprasum </em> kao hrane ili u obliku lekova. Ekstrakti celih biljaka <em>A. paniculatum</em> i <em>A. rhodopeum</em>, kao i ekstrakt nadzemnih delova <em>A. melanantherum</em> pokazali su snažnu antiproliferativnu aktivnost sa povoljnim ne-tumor/tumor koeficijentima i indukovali apoptozu u tumorskim ćelijama, iz čega se može zaključiti da imaju visok potencijal primene u antitumorskoj terapiji. </p> / <p>In the present doctoral thesis the chemical composition and biological activities of <br />10 wild growing taxa of genus <em>Allium</em> sect. <em>Codonoprasum</em> (<em>A. carinatum </em> subsp. <br /><em>pulchellum, A. carinatum </em> subsp. <em>carinatum, A. fuscum </em> var. <em>gracile, A. fuscum</em> var. <br /><em>fuscum, A. flavum </em> subsp. <em>flavum, A. melanantherum, A. oleraceum, A. paniculatum</em><br />subsp. <em>marginatum, A. pallens</em> subsp. <em>tenuiflorum</em> and <em>A. rhodopeum</em>) were investigated. The samples were collected from 27 locations in Serbia. The aim of the study was to obtain data on the content of biologically active compounds in extracts of these unexplored species of the genus Allium and to determine their potential medicinal value.</p><p>Phytochemical caracterisation included: headspace GC-MS analysis of fresh bulb <br />volatiles, LC-DAD-MS and LC-MS-MS qualitative analysis of methanol extracts, LC-MS-MS quantitative analysis of 44 selected phenolic compounds in methanol extracts, determination of total monomeric anthocyanins content and alliinase activity. In order to assess the biological potential of methanol extracts, the antioxidant, anti-inflammatory, antimicrobial, antimutagenic, genotoxic and antiproliferative activities of the extracts were studied.</p><p>Summing up all the results obtained, it can be concluded that species of genus <em>Allium </em> sect. <em>Codonoprasum </em> are rich sources of biologically active compounds with a broad spectrum of biological activities. Dimethyl disulfide is the most dominant and often the only volatile component of most species, which is significant from chemotaxonomic point of view. The methanol extracts of investigated species contain high levels of flavonoids (primarily quercetin derivatives). Specificity of <em>A. pallens</em> and <em>A. oleraceum</em> extracts is that they do not contain rutin, but contain hyperoside, while small quantity of phenolic compounds is characteristic for <em>A. rhodopeum</em> extract. All investigated species, except of <em>A. flavum</em>, are rich in anthocyanins. Alliinase activity was high in all examined species. Most of the extracts, except <em>A. carinatum</em> and <em>A. melanantherum</em> extracts, express considerable antioxidant activity, while extracts of <em> A. flavum</em>, <em>A. rhodopeum</em>, <em>A. paniculatum</em> and <em>A. oleraceum </em> are potent anti-inflammatory agents. The investigated <em>Allium</em> extracts did not show antimicrobial and antimutagenic activity. Also, the extracts did not express genotoxic effect on healthy tissue cells (except the weak genotoxic effects of aerial parts extract of <em>A. flavum</em>), indicating that the use of these species as a food or as a drug is safe. Whole plant extracts of <em>A. paniculatum</em> and <em> A. rhodopeum</em>, as well as aerial parts extract of <em> A. melanantherum</em> showed strong antiproliferative activity (with a favorable non-tumor/tumor ratios) and induced apoptosis in tumor cells, suggesting that these plants have a high potential for application in antitumor therapy.</p>
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Fitohemijski sastav, lekoviti potencijal i senzorne karakteristike sorti vrsta Brassica oleracea L. i Brassica rapa L. (Brassicaceae) iz organskog i konvencionalnog sistema proizvodnje / The phytochemical composition, healing potential and sensory characteristics of cultivars of Brassica oleracea L. i Brassica rapa L. species (Brassicaceae) from organic and conventional cropping systemsBošković Svetlana 29 September 2016 (has links)
<p>U ovom radu su ispitani hemijski sastav i biološka aktivnost vrsta <em> Brassica oleracea </em>i<em> Brassica rapa</em> poreklom iz organskog i konvencionalnog sistema proizvodnje. Ispitivanja hemijskog sastava su obuhvatila određivanje volatilnih komponenata primenom headspace GC-MS tehnike, kvalitativnu analizu sokova ispitivanih vrsta pomoću LC-DAD-MS/MS tehnike, kvantifikaciju odabranih fenolnih jedinjenja pomoću LC-MS/MS tehnike i spektrofotometrijsko određivanje sadržaja ukupnih glukozinolata, fenola i flavonoida i sadržaja ukupnih monomernih antocijana. Biološka aktivnost povrća je ispitana određivanjem antioksidantnog potencijal, antimikrobne i antitumorske aktivnosti sokova. Dobijeni rezultati pokazuju da su glavne volatilne komponente ispitivanih vrsta degradacioni proizvodi masnih kiselina i organosumpornih jedinjenja od kojih neke od identifikovanih komponenata predstavljaju ključne mirisne komponente. Na osnovu njihove distribucije nije bilo moguće utvrditi uticaj sistema proizvodnje na miris i ukus ispitivanih vrsta. Pomoću LC-DAD-MS/MS i LC-MS/MS tehnike je utvrđeno prisustvo primarnih metabolita, slobodnih hidroksibenzoevih i hidroksicimetnih kiselina, derivate hinske kiseline sa hidroksicimetnim kiselinama, glikozida flavonola, biflavonoida, i kumarina u sokovima spitivanih vrsta. Pored toga u svim sokovima subili prisutni kondenzacioni proizvodi degradacionih proizvoda indolnih glukozinolata sa askorbinskom kiselinom- askorbigen i metoksiaskorbigen. U sokovima crvenog kupusa su bili prisutni antocijani. Najveći sadržaj ukupnih glukozinolata je određen u brokoliju, dok je crveni kupus sadržao najveći sadržaj ukupnih fenola ukupnih flavonoida kao i hinske kiseline. Crveni kupus je bio varijetet koji je ispoljio najviši antioksidantni kapacitet u svim primenjenim testovima, brokoli i karfiol su ispoljili najjaču antimikrobnu aktivnost, dok je kelj bio varijetet sa najjačim antitumorskim delovanjem. Na osnovu analize hemijskog sastava i biološke aktivnosti vrsta <em>B</em>. <span id="cke_bm_177S" style="display: none;"> </span><em>oleracea</em><span id="cke_bm_177E" style="display: none;"> </span> i <em> B. rapa</em> može se <span id="cke_bm_178E" style="display: none;"> </span>zaključiti da u zavisnosti od primenjenog tipa proizvodnje mogu biti poboljšane neke od karakteristika ispitivanih vrsta i da je uticaj sistema proizvodnje značajan za pojedine varijetete, a nikako za celu vrstu. U konačnom obliku može se zaključiti da bi potencijalna kombinacija sokova crvenog kupusa, brokolija, karfiola i kelja mogla ostvariti značajno hemopreventivno i hemoterapeutsko delovanje, ispoljavajući istovremeno antioksidantnu, antimikrobnu i antitumorsku aktivnost.</p> / <p>Chemical composition and biological activity of<em> Brassica oleracea</em> and <em>B. rapa </em> species were investigated in the present work. Investigation of chemical composition encompassed determination of volatile compounds by headspace GC-MS technique, qualitative analysis of juices of investigated vegetables by LC-DAD-MS/MS technique, quantification of selected phenolic compounds by LC-MS/MS technique and spectrophotometric determination of total content of glucosinolates, phenolic compounds and flavonoids and total content of monomeric anthocyanes. Biological activity of vegetables was investigated by determination of antioxidant capacity, antimicrobial and antitumorigenic effect of juices. Obtained results showed that main volatile compounds were degradation products of fatty acids and organo-sulphur compounds among which some of the identified components were the key aroma compounds. Based on their distribution it was not possible to evaluate influence of cropping system on aroma and taste of investigated species. By LC-DAD-MS/MS and LC-MS/MS techniques, it was determined the presence of primary metabolites, freehydroxybenzoic and hydroxycinnamic acids, derivatives of quinic acid and hidroxicinnamic acids, flavonol glucosides, biflavnoids and a cumarin in juices of the investigated species. Furthermore, condensation products of degradation products of indole glucosinolates with ascorbic acid- ascorbigen and metoxiascorbigen were present in all juices. Anthocyanes were present in juices of red cabbage. The highest total content of glucosinolates was determined in broccoli, while red cabbage had the highest total phenolic content, total flavonoid content, as well as content of qunic acid. Red cabbage was a variety that showed the highest antioxidant capacity measured by different assays. Broccoli and cauliflower expressed the highest antimicrobial potential, while Savoy cabbage was a variety with the highest antitumor effect. Investigation of chemical composition and biological activity showed that applied cropping conditions may be useful for improving some of the characteristics of investigated species and significance of cropping system only for particular varieties, but not for the whole species in general. As the conclusion, potential combination of juices of red cabbage, broccoli, cauliflower and Savoy cabbage could be potent chemopreventive and chemotherapeutic agent, expressing simultaneously antioxidant, antimicrobial and antitumor activity.</p>
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Sinteza i biološka aktivnost novih steroidnih heterocikličnih jedinjenja / Synthesis and biological activity of new steroidal heterocyclic compoundsOklješa Aleksandar 24 July 2015 (has links)
<p>U ovoj doktorskoj disertaciji ispitane su 1,3-dipolarne<br />cikloadicione reakcije steroidnih azido-nitrila, nitrona i<br />nitril-oksida, pri čemu su sintetizovana različita<br />heterociklična steroidna jedinjenja androstanske i estranske<br />serije. Utvrdjene su strukture novosintetizovanih<br />jedinjenja. Ispitana je biološka aktivnost odabranih<br />jedinjenja.</p> / <p>In this PhD thesis 1,3-dipolar cycloadditions of<br />steroidal azido-nitriles, nitrones and nitrile-oxide were<br />examined. Various steroidal heterocyclic compounds in<br />the androstane and estrane series were synthesised. The<br />structural characterisation of newly synthesised<br />compounds was done. Biological activity of selected<br />compounds was examined.</p>
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