Faculty of Chemistry Repository - Cherry
University of Belgrade - Faculty of Chemistry
    • English
    • Српски
    • Српски (Serbia)
  • English 
    • English
    • Serbian (Cyrillic)
    • Serbian (Latin)
  • Login
View Item 
  •   Cherry
  • Hemijski fakultet
  • Doktorati
  • View Item
  •   Cherry
  • Hemijski fakultet
  • Doktorati
  • View Item
JavaScript is disabled for your browser. Some features of this site may not work without it.

Dobijanje alkilamino i aralkilamino derivata marinskog hinona avarona i model-jedinjenja i ispitivanje njihove citotoksične i antibakterijske aktivnosti

Preparation of alkylamino and aralkylamino derivatives of marine quinone avarone and its model compound and investigation of their cytotoxic and antibacterial activity

Thumbnail
2018
3219-teza.pdf (5.602Mb)
3219.pdf (457.4Kb)
Authors
Jeremić, Marko
Contributors
Sladić, Dušan
Novaković, Irena T.
Pešić, Milica
Zlatović, Mario
Doctoral thesis (Published version)
Metadata
Show full item record
Abstract
U okviru ove doktorske disertacije sintetisana je serija alkilamino i aralkilamino derivata marinskog seskviterpenskog hinona avarona, izolovanog iz morskog sunĊera Dysidea avara, i njegovog model-jedinjenja terc-butilhinona.Za sintezu su odabrani derivati za koje se smatralo da će imati negativniji redoks potencijal od polaznih hinona, i samim tim pokazivati veću biološku aktivnost.OdreĊena je in vitro citotoksiĉna aktivnost derivata prema ćelijskoj liniji nesitnoćelijskog karcinoma pluća − NCI-H460, višestruko rezistentnoj ćelijskoj liniji nesitnoćelijskog karcinoma pluća – NCI-H460/R, kao i normalnim ćelijama humanih keratinocita – HaCaT.Pored inhibicije rasta ćelija, ispitivana je i sposobnost derivata za indukciju ćelijske smrti, u pomenutim ćelijskim linijama.Nekoliko derivata koji su pokazali visok stepen efikasnosti i selektivnosti ka tumorskim ćelijama, ušli su u dalja ispitivanja mehanizma dejstva i to prema sposobnosti generisanja superoksidnog anjona, kao i prema sposobnost...i za narušavanje membranskog potencijala mitohondrija.UtvrĊena je i antibakterijska aktivnost novih derivata prema seriji Gram-pozitivnih, kao i Gram-negativnih bakterija. Pored toga, ispitana je i inhibitorna aktivnost prema odabranim sojevima gljivica.

In this doctoral dissertation, a series of alkylamino and aralkylamino derivatives of marine sesquiterpene quinone avarone, isolated from marine sponge Dysidea avara, and its model compound tert-butylquinone was synthesized.Derivatives, for which it was anticipated to possess more negative redox potentials than the parent quinones, and therefore stronger activity were chosen for synthesis.In vitro cytotoxic activity of derivatives toward three cell lines, non-small cell lung carcinoma – NCI-H460, its resistant counterpart – NCI-H460/R, as well as normal human keratinocytes – HaCaT, was determined.Besides cell growth inhibition, ability of derivatives to induce cell death, was also investigated.Several derivatives with high efficacy and selectivity toward cancer cells have entered into further investigation of their mechanism according to the potential to generate superoxide radical anion, as well as the ability to change mitochondrial membrane potential.Antibacterial activity of novel ...derivatives towards Gram-positive and Gram-negative strains of bacteria, as well as antimicotic activity against few fungal strains, were determined.

Keywords:
avaron, terc-butilhinon, citotoksiĉnost, mitohondrije, apoptoza, nekroza, reaktivne kiseoniĉne vrste, antimikrobna aktivnost / avarone, tert-butylquinone, citotoxicity, mitochondria, apoptosis, necrosis, reactive oxygen species, antimicrobial activity
Source:
Универзитет у Београду, 2018
Publisher:
  • Универзитет у Београду, Хемијски факултет
[ Google Scholar ]
Handle
https://hdl.handle.net/21.15107/rcub_nardus_10633
URI
http://eteze.bg.ac.rs/application/showtheses?thesesId=6489
https://fedorabg.bg.ac.rs/fedora/get/o:19228/bdef:Content/download
http://vbs.rs/scripts/cobiss?command=DISPLAY&base=70036&RID=50770703
http://nardus.mpn.gov.rs/123456789/10633
https://cherry.chem.bg.ac.rs/handle/123456789/3168
Collections
  • Doktorati
Institution/Community
Hemijski fakultet
TY  - THES
AU  - Jeremić, Marko
PY  - 2018
UR  - http://eteze.bg.ac.rs/application/showtheses?thesesId=6489
UR  - https://fedorabg.bg.ac.rs/fedora/get/o:19228/bdef:Content/download
UR  - http://vbs.rs/scripts/cobiss?command=DISPLAY&base=70036&RID=50770703
UR  - http://nardus.mpn.gov.rs/123456789/10633
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/3168
AB  - U okviru ove doktorske disertacije sintetisana je serija alkilamino i aralkilamino derivata marinskog seskviterpenskog hinona avarona, izolovanog iz morskog sunĊera Dysidea avara, i njegovog model-jedinjenja terc-butilhinona.Za sintezu su odabrani derivati za koje se smatralo da će imati negativniji redoks potencijal od polaznih hinona, i samim tim pokazivati veću biološku aktivnost.OdreĊena je in vitro citotoksiĉna aktivnost derivata prema ćelijskoj liniji nesitnoćelijskog karcinoma pluća − NCI-H460, višestruko rezistentnoj ćelijskoj liniji nesitnoćelijskog karcinoma pluća – NCI-H460/R, kao i normalnim ćelijama humanih keratinocita – HaCaT.Pored inhibicije rasta ćelija, ispitivana je i sposobnost derivata za indukciju ćelijske smrti, u pomenutim ćelijskim linijama.Nekoliko derivata koji su pokazali visok stepen efikasnosti i selektivnosti ka tumorskim ćelijama, ušli su u dalja ispitivanja mehanizma dejstva i to prema sposobnosti generisanja superoksidnog anjona, kao i prema sposobnosti za narušavanje membranskog potencijala mitohondrija.UtvrĊena je i antibakterijska aktivnost novih derivata prema seriji Gram-pozitivnih, kao i Gram-negativnih bakterija. Pored toga, ispitana je i inhibitorna aktivnost prema odabranim sojevima gljivica.
AB  - In this doctoral dissertation, a series of alkylamino and aralkylamino derivatives of marine sesquiterpene quinone avarone, isolated from marine sponge Dysidea avara, and its model compound tert-butylquinone was synthesized.Derivatives, for which it was anticipated to possess more negative redox potentials than the parent quinones, and therefore stronger activity were chosen for synthesis.In vitro cytotoxic activity of derivatives toward three cell lines, non-small cell lung carcinoma – NCI-H460, its resistant counterpart – NCI-H460/R, as well as normal human keratinocytes – HaCaT, was determined.Besides cell growth inhibition, ability of derivatives to induce cell death, was also investigated.Several derivatives with high efficacy and selectivity toward cancer cells have entered into further investigation of their mechanism according to the potential to generate superoxide radical anion, as well as the ability to change mitochondrial membrane potential.Antibacterial activity of novel derivatives towards Gram-positive and Gram-negative strains of bacteria, as well as antimicotic activity against few fungal strains, were determined.
PB  - Универзитет у Београду, Хемијски факултет
T2  - Универзитет у Београду
T1  - Dobijanje alkilamino i aralkilamino derivata marinskog hinona avarona i model-jedinjenja i ispitivanje njihove citotoksične i antibakterijske aktivnosti
UR  - https://hdl.handle.net/21.15107/rcub_nardus_10633
ER  - 
@phdthesis{
author = "Jeremić, Marko",
year = "2018",
abstract = "U okviru ove doktorske disertacije sintetisana je serija alkilamino i aralkilamino derivata marinskog seskviterpenskog hinona avarona, izolovanog iz morskog sunĊera Dysidea avara, i njegovog model-jedinjenja terc-butilhinona.Za sintezu su odabrani derivati za koje se smatralo da će imati negativniji redoks potencijal od polaznih hinona, i samim tim pokazivati veću biološku aktivnost.OdreĊena je in vitro citotoksiĉna aktivnost derivata prema ćelijskoj liniji nesitnoćelijskog karcinoma pluća − NCI-H460, višestruko rezistentnoj ćelijskoj liniji nesitnoćelijskog karcinoma pluća – NCI-H460/R, kao i normalnim ćelijama humanih keratinocita – HaCaT.Pored inhibicije rasta ćelija, ispitivana je i sposobnost derivata za indukciju ćelijske smrti, u pomenutim ćelijskim linijama.Nekoliko derivata koji su pokazali visok stepen efikasnosti i selektivnosti ka tumorskim ćelijama, ušli su u dalja ispitivanja mehanizma dejstva i to prema sposobnosti generisanja superoksidnog anjona, kao i prema sposobnosti za narušavanje membranskog potencijala mitohondrija.UtvrĊena je i antibakterijska aktivnost novih derivata prema seriji Gram-pozitivnih, kao i Gram-negativnih bakterija. Pored toga, ispitana je i inhibitorna aktivnost prema odabranim sojevima gljivica., In this doctoral dissertation, a series of alkylamino and aralkylamino derivatives of marine sesquiterpene quinone avarone, isolated from marine sponge Dysidea avara, and its model compound tert-butylquinone was synthesized.Derivatives, for which it was anticipated to possess more negative redox potentials than the parent quinones, and therefore stronger activity were chosen for synthesis.In vitro cytotoxic activity of derivatives toward three cell lines, non-small cell lung carcinoma – NCI-H460, its resistant counterpart – NCI-H460/R, as well as normal human keratinocytes – HaCaT, was determined.Besides cell growth inhibition, ability of derivatives to induce cell death, was also investigated.Several derivatives with high efficacy and selectivity toward cancer cells have entered into further investigation of their mechanism according to the potential to generate superoxide radical anion, as well as the ability to change mitochondrial membrane potential.Antibacterial activity of novel derivatives towards Gram-positive and Gram-negative strains of bacteria, as well as antimicotic activity against few fungal strains, were determined.",
publisher = "Универзитет у Београду, Хемијски факултет",
journal = "Универзитет у Београду",
title = "Dobijanje alkilamino i aralkilamino derivata marinskog hinona avarona i model-jedinjenja i ispitivanje njihove citotoksične i antibakterijske aktivnosti",
url = "https://hdl.handle.net/21.15107/rcub_nardus_10633"
}
Jeremić, M.. (2018). Dobijanje alkilamino i aralkilamino derivata marinskog hinona avarona i model-jedinjenja i ispitivanje njihove citotoksične i antibakterijske aktivnosti. in Универзитет у Београду
Универзитет у Београду, Хемијски факултет..
https://hdl.handle.net/21.15107/rcub_nardus_10633
Jeremić M. Dobijanje alkilamino i aralkilamino derivata marinskog hinona avarona i model-jedinjenja i ispitivanje njihove citotoksične i antibakterijske aktivnosti. in Универзитет у Београду. 2018;.
https://hdl.handle.net/21.15107/rcub_nardus_10633 .
Jeremić, Marko, "Dobijanje alkilamino i aralkilamino derivata marinskog hinona avarona i model-jedinjenja i ispitivanje njihove citotoksične i antibakterijske aktivnosti" in Универзитет у Београду (2018),
https://hdl.handle.net/21.15107/rcub_nardus_10633 .

DSpace software copyright © 2002-2015  DuraSpace
About CHERRY - CHEmistry RepositoRY | Send Feedback

re3dataOpenAIRERCUB
 

 

All of DSpaceInstitutions/communitiesAuthorsTitlesSubjectsThis institutionAuthorsTitlesSubjects

Statistics

View Usage Statistics

DSpace software copyright © 2002-2015  DuraSpace
About CHERRY - CHEmistry RepositoRY | Send Feedback

re3dataOpenAIRERCUB