TY  - JOUR
AU  - Aksić, Jelena
AU  - Genčić, Marija
AU  - Stojanović, Nikola
AU  - Radulović, Niko
AU  - Zlatković, Dragan
AU  - Dimitrijević, Marina
AU  - Stojanović-Radić, Zorica
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Jovanović, Ljiljana
PY  - 2023
UR  - http://rimi.imi.bg.ac.rs/handle/123456789/1301
AB  - Herein, upgraded chloroquine (CQ) derivatives capable of overcoming Plasmodium resistance and, at the same time, suppressing excessive immune response and risk of concurrent bacteremia were developed. Twelve new ferrocene-CQ hybrids tethered with a small azathia heterocycle (1,3-thiazolidin-4-one, 1,3-thiazinan-4-one, or 5-methyl-1,3-thiazolidin-4-one) were synthesized and fully characterized. All hybrids were evaluated for their in vitro antiplasmodial, antimicrobial, and immunomodulatory activities. Additional assays were performed on selected hybrids to gain insights into their mode of action. Although only hybrid 4a was more potent than the parent drug toward CQ-resistant Dd2 Plasmodium falciparum strain, several other hybrids (such as 6b, 6c, and 6d) manifested substantially improved antimicrobial and immunomodulatory properties. Interesting structure-activity relationship data were obtained, hinting at future research for the development of new multitarget chemotherapies for malaria and other infectious diseases complicated by drug resistance, bacterial co-infection, and immune-driven pathology issues.
PB  - American Chemical Society
T2  - Journal of Medicinal Chemistry
T1  - New Iron Twist to Chloroquine─Upgrading Antimalarials with Immunomodulatory and Antimicrobial Features
EP  - 2101
IS  - 3
SP  - 2084
VL  - 66
DO  - 10.1021/acs.jmedchem.2c01851
ER  - 

@article{
author = "Aksić, Jelena and Genčić, Marija and Stojanović, Nikola and Radulović, Niko and Zlatković, Dragan and Dimitrijević, Marina and Stojanović-Radić, Zorica and Srbljanović, Jelena and Štajner, Tijana and Jovanović, Ljiljana",
year = "2023",
abstract = "Herein, upgraded chloroquine (CQ) derivatives capable of overcoming Plasmodium resistance and, at the same time, suppressing excessive immune response and risk of concurrent bacteremia were developed. Twelve new ferrocene-CQ hybrids tethered with a small azathia heterocycle (1,3-thiazolidin-4-one, 1,3-thiazinan-4-one, or 5-methyl-1,3-thiazolidin-4-one) were synthesized and fully characterized. All hybrids were evaluated for their in vitro antiplasmodial, antimicrobial, and immunomodulatory activities. Additional assays were performed on selected hybrids to gain insights into their mode of action. Although only hybrid 4a was more potent than the parent drug toward CQ-resistant Dd2 Plasmodium falciparum strain, several other hybrids (such as 6b, 6c, and 6d) manifested substantially improved antimicrobial and immunomodulatory properties. Interesting structure-activity relationship data were obtained, hinting at future research for the development of new multitarget chemotherapies for malaria and other infectious diseases complicated by drug resistance, bacterial co-infection, and immune-driven pathology issues.",
publisher = "American Chemical Society",
journal = "Journal of Medicinal Chemistry",
title = "New Iron Twist to Chloroquine─Upgrading Antimalarials with Immunomodulatory and Antimicrobial Features",
pages = "2101-2084",
number = "3",
volume = "66",
doi = "10.1021/acs.jmedchem.2c01851"
}

Aksić, J., Genčić, M., Stojanović, N., Radulović, N., Zlatković, D., Dimitrijević, M., Stojanović-Radić, Z., Srbljanović, J., Štajner, T.,& Jovanović, L.. (2023). New Iron Twist to Chloroquine─Upgrading Antimalarials with Immunomodulatory and Antimicrobial Features. in Journal of Medicinal Chemistry
American Chemical Society., 66(3), 2084-2101.
https://doi.org/10.1021/acs.jmedchem.2c01851

Aksić J, Genčić M, Stojanović N, Radulović N, Zlatković D, Dimitrijević M, Stojanović-Radić Z, Srbljanović J, Štajner T, Jovanović L. New Iron Twist to Chloroquine─Upgrading Antimalarials with Immunomodulatory and Antimicrobial Features. in Journal of Medicinal Chemistry. 2023;66(3):2084-2101.
doi:10.1021/acs.jmedchem.2c01851 .

Aksić, Jelena, Genčić, Marija, Stojanović, Nikola, Radulović, Niko, Zlatković, Dragan, Dimitrijević, Marina, Stojanović-Radić, Zorica, Srbljanović, Jelena, Štajner, Tijana, Jovanović, Ljiljana, "New Iron Twist to Chloroquine─Upgrading Antimalarials with Immunomodulatory and Antimicrobial Features" in Journal of Medicinal Chemistry, 66, no. 3 (2023):2084-2101,
https://doi.org/10.1021/acs.jmedchem.2c01851 . .

TY  - JOUR
AU  - Jovanović, Aleksandra A.
AU  - Vajić, Una Jovana
AU  - Mijin, Dušan Z.
AU  - Zdunić, Gordana M.
AU  - Šavikin, Katarina P.
AU  - Branković, Suzana
AU  - Kitić, Dušanka
AU  - Bugarski, Branko
PY  - 2022
UR  - http://rimi.imi.bg.ac.rs/handle/123456789/1332
AB  - In the present study, polyphenol extraction from Thymus serpyllum by-product (herbal dust) in microwave reactor was optimized through varying extraction time, ethanol concentration and solid-to-solvent ratiovia determination of total polyphenol and flavonoid contents, and antioxidant activity, using response surface methodology and a central composite design. Total polyphenol and flavonoids contents, as well as antioxidant activity of the extracts were statistically significantly affected by ethanol concentration and solid-to-solvent ratio. However, extraction time had statistically significant influence only on polyphenol yield. The extraction conditions that maximized polyphenol recovery were 48% ethanol and 0.0402 g/mL solid-to-solvent ratio during 86 s of microwave-assisted extraction, and under these conditions total polyphenol content was estimated to be 57.2 mg of gallic acid equivalents (GAE)/L, while measured value was 58.1 ± 3.2 mg GAE/L. Polyphenol content (HPLC analysis), antioxidant, antimicrobial and antispasmodic potential of the extract prepared under these optimal extraction conditions were evaluated. Rosmarinic acids, luteolin 7-O-glucuronide, caffeic acid, apigenin glucuronide, 6-hydroxyluteolin 7-O-glucoside, 6,8-di-C-glucosylapigenin, and traces of chlorogenic acid were quantified in the extract (descending order of content). The selected extract inhibited 95% ± 0.9 of lipid peroxidation in β-Carotene and linoleic acid emulsion. It was more effective against tested Gram-positive bacteria than against Gram-negative and showed dose-dependent antispasmodic activity on spontaneous contractions, acetylcholine- and potassium chloride-induced contractions. Microwave-assisted extraction could be selected as a successful technique for polyphenol extraction from wild thyme by-product. Biological activities shown in the study open the possibility of potential application of the extract in pharmaceutical, food, functional food and cosmetic products.
PB  - Elsevier
T2  - Journal of Applied Research on Medicinal and Aromatic Plants
T2  - Journal of Applied Research on Medicinal and Aromatic Plants
T1  - Polyphenol extraction in microwave reactor using by-product of Thymus serpyllum L. and biological potential of the extract
SP  - 100417
VL  - 31
DO  - 10.1016/j.jarmap.2022.100417
ER  - 

@article{
author = "Jovanović, Aleksandra A. and Vajić, Una Jovana and Mijin, Dušan Z. and Zdunić, Gordana M. and Šavikin, Katarina P. and Branković, Suzana and Kitić, Dušanka and Bugarski, Branko",
year = "2022",
abstract = "In the present study, polyphenol extraction from Thymus serpyllum by-product (herbal dust) in microwave reactor was optimized through varying extraction time, ethanol concentration and solid-to-solvent ratiovia determination of total polyphenol and flavonoid contents, and antioxidant activity, using response surface methodology and a central composite design. Total polyphenol and flavonoids contents, as well as antioxidant activity of the extracts were statistically significantly affected by ethanol concentration and solid-to-solvent ratio. However, extraction time had statistically significant influence only on polyphenol yield. The extraction conditions that maximized polyphenol recovery were 48% ethanol and 0.0402 g/mL solid-to-solvent ratio during 86 s of microwave-assisted extraction, and under these conditions total polyphenol content was estimated to be 57.2 mg of gallic acid equivalents (GAE)/L, while measured value was 58.1 ± 3.2 mg GAE/L. Polyphenol content (HPLC analysis), antioxidant, antimicrobial and antispasmodic potential of the extract prepared under these optimal extraction conditions were evaluated. Rosmarinic acids, luteolin 7-O-glucuronide, caffeic acid, apigenin glucuronide, 6-hydroxyluteolin 7-O-glucoside, 6,8-di-C-glucosylapigenin, and traces of chlorogenic acid were quantified in the extract (descending order of content). The selected extract inhibited 95% ± 0.9 of lipid peroxidation in β-Carotene and linoleic acid emulsion. It was more effective against tested Gram-positive bacteria than against Gram-negative and showed dose-dependent antispasmodic activity on spontaneous contractions, acetylcholine- and potassium chloride-induced contractions. Microwave-assisted extraction could be selected as a successful technique for polyphenol extraction from wild thyme by-product. Biological activities shown in the study open the possibility of potential application of the extract in pharmaceutical, food, functional food and cosmetic products.",
publisher = "Elsevier",
journal = "Journal of Applied Research on Medicinal and Aromatic Plants, Journal of Applied Research on Medicinal and Aromatic Plants",
title = "Polyphenol extraction in microwave reactor using by-product of Thymus serpyllum L. and biological potential of the extract",
pages = "100417",
volume = "31",
doi = "10.1016/j.jarmap.2022.100417"
}

Jovanović, A. A., Vajić, U. J., Mijin, D. Z., Zdunić, G. M., Šavikin, K. P., Branković, S., Kitić, D.,& Bugarski, B.. (2022). Polyphenol extraction in microwave reactor using by-product of Thymus serpyllum L. and biological potential of the extract. in Journal of Applied Research on Medicinal and Aromatic Plants
Elsevier., 31, 100417.
https://doi.org/10.1016/j.jarmap.2022.100417

Jovanović AA, Vajić UJ, Mijin DZ, Zdunić GM, Šavikin KP, Branković S, Kitić D, Bugarski B. Polyphenol extraction in microwave reactor using by-product of Thymus serpyllum L. and biological potential of the extract. in Journal of Applied Research on Medicinal and Aromatic Plants. 2022;31:100417.
doi:10.1016/j.jarmap.2022.100417 .

Jovanović, Aleksandra A., Vajić, Una Jovana, Mijin, Dušan Z., Zdunić, Gordana M., Šavikin, Katarina P., Branković, Suzana, Kitić, Dušanka, Bugarski, Branko, "Polyphenol extraction in microwave reactor using by-product of Thymus serpyllum L. and biological potential of the extract" in Journal of Applied Research on Medicinal and Aromatic Plants, 31 (2022):100417,
https://doi.org/10.1016/j.jarmap.2022.100417 . .