In an earlier study we demonstrated that hydroxyapatite nanoparticles coated with chitosan-poly(d... more In an earlier study we demonstrated that hydroxyapatite nanoparticles coated with chitosan-poly(d,l)-lactide-co-glycolide (HAp/Ch-PLGA) target lungs following their intravenous injection into mice. In this study we utilize an emulsification process and freeze drying to load the composite HAp/Ch-PLGA particles with 17-hydroxy-17-picolyl-androst-5-en-3-yl-acetate (A), a chemotherapeutic derivative of androstane and a novel compound with a selective anticancer activity against lung cancer cells. 1 H NMR and 13 C NMR techniques confirmed the intact structure of the derivative A following its entrapment within HAp/Ch-PLGA particles. The thermogravimetric and differential thermal analyses coupled with mass spectrometry were used to assess the thermal degradation products and properties of A-loaded HAp/Ch-PLGA. The loading efficiency, as indicated by the comparison of enthalpies of phase transitions in pure A and A-loaded HAp/Ch-PLGA, equaled 7.47 wt.%. The release of A from HAp/Ch-PLGA was sustained , neither exhibiting a burst release nor plateauing after three weeks. Atomic force microscopy and particle size distribution analyses were used to confirm that the particles were spherical with a uniform size distribution of d 50 = 168 nm. In vitro cytotoxicity testing of A-loaded HAp/Ch-PLGA using MTT and trypan blue dye exclusion assays demonstrated that the particles were cytotoxic to the A549 human lung carcinoma cell line (46 ± 2%), while simultaneously preserving high viability (83 ± 3%) of regular MRC5 human lung fibroblasts and causing no harm to primary mouse lung fibroblasts. In conclusion, composite A-loaded HAp/Ch-PLGA particles could be seen as promising drug delivery platforms for selective cancer therapies, targeting malignant cells for destruction, while having a significantly lesser cytotoxic effect on the healthy cells.
Institut za hemiju, Prirodno-matematiEki fakultet, ffooi Sod *lnstitut za tehnologiiu' rrlesa, m'... more Institut za hemiju, Prirodno-matematiEki fakultet, ffooi Sod *lnstitut za tehnologiiu' rrlesa, m'leka, ulia i masti, tto6o i poor6o, Tehnoloil+i fakultet, Nooi Sod (Primljeno 30. januara 1984) Izvod. U ovom radu razraden je pos'tupak za preparativno izolovanje solanina iz klica krompira koji predstavlja znaiaino pobolijanje u odnosu na ranije opisane postupfe. Eksfrakcija ukupnih glikoalkaloida. izvedena je 80/o sirdetnom kiselinom, pri demu je dobijena smeia glikoalkaloida u prinosu-od .0,99p/o Sto iznosi 96,if/o od teorijskog prinosa, a-zatim je iz smele glikoalka-l6ida izdvojen solairidin kristaliiacijom iz etanola u prinosu od 0,40{/o r-adu' nata na suvu materiju klica. U radu je razradlen i postupak za direktno dobi-janje solanidina iz klica krompira koji se zasniva na istovremenoj ekstrak-llji-gtit<oatkaloida i niihovoi hidrolizi pomoeu. 1,8 mol dmr hlorovodoniEne kiieline u metanolu, p-r.i eerriu je dobijen solanidin u p.rinosu od 0,4?o/o radu-nato na suvu mateiiiu klica, Sto iznosi 87,7plo od teorijskog prinosa' IstraZivanje prirodnilr izvora polaznilh materijala za industrijsku sin-tezu steroidnth ho,rmo,na ima veliki zmadaj. Postoji nekoliko biljnlh wsta i ku,ltura koje potencija'Lno mogu posluZiti kao izvor steroida. Tako' kli'ce krornpi'ra piedJtavljaju izvanrednu potencljaLnu sirovinu za ,pomenutu sv,rhu, s obairom da sadrte znatne kolidine giikoalka'loida steroidne strukture, sola-ntn i |akonisr. trstradivanja koja se ,odno'se na izolovanje, preii56avanje i hemijslke transformacije glikoall<aloida krornpira i aglikona solanidina (She-ma i.; u korisne intermetlijere u sintezi steroidnih hormona, imaju pored teorijskog i praktiEni znaEaj. U literaturi je poznat relativno mali bt'oj postupalka za preparati"rno izolovarnje glikoalka'loida krompira. Postqpak Soltysa i Walenfelsar zasniva se na ekstrakeiji si,rovih kli,ca lcornplra po,mo6u 3o/o s{.r6etne hiseline u tra-janju od dva dana. Prinos solanina u odnosu na sirove klice je 0,0250/s. Asla-nov i saradniciz su izolovali ukupne gtrikoalka'Iolde ia semena kromp[ra po-mo6u 30/o si,rr6etne kiseline tr pfiuroBu od 0,?0,10. Kotiste6i Pfanku,ch-ovru rne-todu,$ Gurpta i Garga su iaolovali solanin lz plo'dova bi,ljke Solanum leror Linn. u prinosr.l od 0,30/0. Actrterberg i saradnicio su izolovali glikoalka'loide
Odredivanje, izolor,'anje i prediSdavanje tomatina iz biljnog materijala KATARINA GASI, D. MILJKO... more Odredivanje, izolor,'anje i prediSdavanje tomatina iz biljnog materijala KATARINA GASI, D. MILJKOVIC, BRAbIKA LAZIC ,i Z. SAKAC IZVOD: U ovom radu detaljno su ispitivane sorte paradaiza MY-10, MY-13 i ,,Kambe,, u pogledu sadriaja tomatina u razliiitim delovi-ma b{ljke. (J tu svrhu koristili smo spektrofotometrijski i gravi-metriiski metod. Nadeno je da je sadriaj tomatina nainiii i sta-blu (oko 0,200t01, a naivi|i u cvetovima (oko 2,30/o). Liske su (Iistovi bez lisnih driki) sadrlavale do 1,50/o tomatina. Razradeni su razli-i.iti preparativni postupci za izolovanje i preiiSiavanje tomatina, kombircujudi metode iz literature i naie iopstvene eksperimente. Preii\iavanje tomatina postignuto je preko njegovog holesterolnog kom pI eks a'i t' inalnom r ekr isl alizaii i om iz et an"ota. F o stupak izoli-cije je jednostavniji u slutaju ekstrakcije tomatina iz stabla, a zna-tno sloleniji u sluiaju liski, kada je neophodna primena florisila.
Tall oil, a mixture of fatty and resin acids obtained as a byproduct of wood alkaline delignifica... more Tall oil, a mixture of fatty and resin acids obtained as a byproduct of wood alkaline delignification, was subjected to purification in the form ofa sulphate soap. A procedure has been developed, involving extraction oftall oil from an aqueous solution of sulphate soap with etbylacetate. The optimized rpeftil* conditions (volumes of water and ethylacetate, number of extractions, temperature and duration of the process) resulted in a separation efficiency of unsaponifiable matter up to 807o. The procedure yielded large amounts of unsaponifiable matter, mainly composed of phyto-sterols. Methods ofphytosterols isolation and identification have also been proposed. Talldl, eine Mischung von Fett-rurd Harzsiiure& daqs 1ar66trod der alkalis-chen Entfemung von Lignin aus Holz entsteht, war in der Form seiner Sulfatseife der Raffrnierung unterzogen. Ein Verfahren, das Extraktierung vom Talldl mit Essig-siiureethylester aus einet wiissriger Ldsung einschliesst, wurde ausgearbeitet. Opti-misierte Arbeitsbedinguogen (Verhiiltris der Wasser-und Essigsiiureethylester-vol-umen, Anzahl der Extraktierungen, Temperatur, Dauer der Prozedur) erm6glichten Ausscheidung bis zu 80% von unverseilbaren stoffen. Es wurde ebenso eine Me-thode fiir Identifizierung und Isolation der Phytosterine vorgeschlagen.
In an earlier study we demonstrated that hydroxyapatite nanoparticles coated with chitosan-poly(d... more In an earlier study we demonstrated that hydroxyapatite nanoparticles coated with chitosan-poly(d,l)-lactide-co-glycolide (HAp/Ch-PLGA) target lungs following their intravenous injection into mice. In this study we utilize an emulsification process and freeze drying to load the composite HAp/Ch-PLGA particles with 17-hydroxy-17-picolyl-androst-5-en-3-yl-acetate (A), a chemotherapeutic derivative of androstane and a novel compound with a selective anticancer activity against lung cancer cells. 1 H NMR and 13 C NMR techniques confirmed the intact structure of the derivative A following its entrapment within HAp/Ch-PLGA particles. The thermogravimetric and differential thermal analyses coupled with mass spectrometry were used to assess the thermal degradation products and properties of A-loaded HAp/Ch-PLGA. The loading efficiency, as indicated by the comparison of enthalpies of phase transitions in pure A and A-loaded HAp/Ch-PLGA, equaled 7.47 wt.%. The release of A from HAp/Ch-PLGA was sustained , neither exhibiting a burst release nor plateauing after three weeks. Atomic force microscopy and particle size distribution analyses were used to confirm that the particles were spherical with a uniform size distribution of d 50 = 168 nm. In vitro cytotoxicity testing of A-loaded HAp/Ch-PLGA using MTT and trypan blue dye exclusion assays demonstrated that the particles were cytotoxic to the A549 human lung carcinoma cell line (46 ± 2%), while simultaneously preserving high viability (83 ± 3%) of regular MRC5 human lung fibroblasts and causing no harm to primary mouse lung fibroblasts. In conclusion, composite A-loaded HAp/Ch-PLGA particles could be seen as promising drug delivery platforms for selective cancer therapies, targeting malignant cells for destruction, while having a significantly lesser cytotoxic effect on the healthy cells.
Institut za hemiju, Prirodno-matematiEki fakultet, ffooi Sod *lnstitut za tehnologiiu' rrlesa, m'... more Institut za hemiju, Prirodno-matematiEki fakultet, ffooi Sod *lnstitut za tehnologiiu' rrlesa, m'leka, ulia i masti, tto6o i poor6o, Tehnoloil+i fakultet, Nooi Sod (Primljeno 30. januara 1984) Izvod. U ovom radu razraden je pos'tupak za preparativno izolovanje solanina iz klica krompira koji predstavlja znaiaino pobolijanje u odnosu na ranije opisane postupfe. Eksfrakcija ukupnih glikoalkaloida. izvedena je 80/o sirdetnom kiselinom, pri demu je dobijena smeia glikoalkaloida u prinosu-od .0,99p/o Sto iznosi 96,if/o od teorijskog prinosa, a-zatim je iz smele glikoalka-l6ida izdvojen solairidin kristaliiacijom iz etanola u prinosu od 0,40{/o r-adu' nata na suvu materiju klica. U radu je razradlen i postupak za direktno dobi-janje solanidina iz klica krompira koji se zasniva na istovremenoj ekstrak-llji-gtit<oatkaloida i niihovoi hidrolizi pomoeu. 1,8 mol dmr hlorovodoniEne kiieline u metanolu, p-r.i eerriu je dobijen solanidin u p.rinosu od 0,4?o/o radu-nato na suvu mateiiiu klica, Sto iznosi 87,7plo od teorijskog prinosa' IstraZivanje prirodnilr izvora polaznilh materijala za industrijsku sin-tezu steroidnth ho,rmo,na ima veliki zmadaj. Postoji nekoliko biljnlh wsta i ku,ltura koje potencija'Lno mogu posluZiti kao izvor steroida. Tako' kli'ce krornpi'ra piedJtavljaju izvanrednu potencljaLnu sirovinu za ,pomenutu sv,rhu, s obairom da sadrte znatne kolidine giikoalka'loida steroidne strukture, sola-ntn i |akonisr. trstradivanja koja se ,odno'se na izolovanje, preii56avanje i hemijslke transformacije glikoall<aloida krornpira i aglikona solanidina (She-ma i.; u korisne intermetlijere u sintezi steroidnih hormona, imaju pored teorijskog i praktiEni znaEaj. U literaturi je poznat relativno mali bt'oj postupalka za preparati"rno izolovarnje glikoalka'loida krompira. Postqpak Soltysa i Walenfelsar zasniva se na ekstrakeiji si,rovih kli,ca lcornplra po,mo6u 3o/o s{.r6etne hiseline u tra-janju od dva dana. Prinos solanina u odnosu na sirove klice je 0,0250/s. Asla-nov i saradniciz su izolovali ukupne gtrikoalka'Iolde ia semena kromp[ra po-mo6u 30/o si,rr6etne kiseline tr pfiuroBu od 0,?0,10. Kotiste6i Pfanku,ch-ovru rne-todu,$ Gurpta i Garga su iaolovali solanin lz plo'dova bi,ljke Solanum leror Linn. u prinosr.l od 0,30/0. Actrterberg i saradnicio su izolovali glikoalka'loide
Odredivanje, izolor,'anje i prediSdavanje tomatina iz biljnog materijala KATARINA GASI, D. MILJKO... more Odredivanje, izolor,'anje i prediSdavanje tomatina iz biljnog materijala KATARINA GASI, D. MILJKOVIC, BRAbIKA LAZIC ,i Z. SAKAC IZVOD: U ovom radu detaljno su ispitivane sorte paradaiza MY-10, MY-13 i ,,Kambe,, u pogledu sadriaja tomatina u razliiitim delovi-ma b{ljke. (J tu svrhu koristili smo spektrofotometrijski i gravi-metriiski metod. Nadeno je da je sadriaj tomatina nainiii i sta-blu (oko 0,200t01, a naivi|i u cvetovima (oko 2,30/o). Liske su (Iistovi bez lisnih driki) sadrlavale do 1,50/o tomatina. Razradeni su razli-i.iti preparativni postupci za izolovanje i preiiSiavanje tomatina, kombircujudi metode iz literature i naie iopstvene eksperimente. Preii\iavanje tomatina postignuto je preko njegovog holesterolnog kom pI eks a'i t' inalnom r ekr isl alizaii i om iz et an"ota. F o stupak izoli-cije je jednostavniji u slutaju ekstrakcije tomatina iz stabla, a zna-tno sloleniji u sluiaju liski, kada je neophodna primena florisila.
Tall oil, a mixture of fatty and resin acids obtained as a byproduct of wood alkaline delignifica... more Tall oil, a mixture of fatty and resin acids obtained as a byproduct of wood alkaline delignification, was subjected to purification in the form ofa sulphate soap. A procedure has been developed, involving extraction oftall oil from an aqueous solution of sulphate soap with etbylacetate. The optimized rpeftil* conditions (volumes of water and ethylacetate, number of extractions, temperature and duration of the process) resulted in a separation efficiency of unsaponifiable matter up to 807o. The procedure yielded large amounts of unsaponifiable matter, mainly composed of phyto-sterols. Methods ofphytosterols isolation and identification have also been proposed. Talldl, eine Mischung von Fett-rurd Harzsiiure& daqs 1ar66trod der alkalis-chen Entfemung von Lignin aus Holz entsteht, war in der Form seiner Sulfatseife der Raffrnierung unterzogen. Ein Verfahren, das Extraktierung vom Talldl mit Essig-siiureethylester aus einet wiissriger Ldsung einschliesst, wurde ausgearbeitet. Opti-misierte Arbeitsbedinguogen (Verhiiltris der Wasser-und Essigsiiureethylester-vol-umen, Anzahl der Extraktierungen, Temperatur, Dauer der Prozedur) erm6glichten Ausscheidung bis zu 80% von unverseilbaren stoffen. Es wurde ebenso eine Me-thode fiir Identifizierung und Isolation der Phytosterine vorgeschlagen.
New salicylic (2-hydroxybenzoic) acid derivatives 1–6 were prepared by conventional heating or mi... more New salicylic (2-hydroxybenzoic) acid derivatives 1–6 were prepared by conventional heating or microwave irradiation of a mixture consisting of methyl salicylate and the corresponding amino alcohol (2,2 0-dihydroxydieth-ylamine, 2,2 0 ,2 00-trihydroxytriethylamine or N-phenyl-2,2 0-dihydroxydiethylamine) and metallic sodium as catalyst. For compounds 1, 3, and 5 X-ray structure analysis was performed , as well as molecular mechanics calculations (MMC), to define their conformation in terms of their energy minima. Comparison of crystal and MMC structures for these three compounds (1, 3, and 5) revealed that the intra-molecular hydrogen bonds play an important role, stabilizing conformation of the most part of the molecule. The antiox-idant activity and cytotoxicity of the synthesized derivatives were evaluated in a series of in vitro tests. The newly synthesized compounds exhibited strong activity against hydroxyl radical, as well as promising lipid peroxidation inhibition. The study showed that the electronic effects of the groups at the N atom are responsible for neutralization of the
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