TY  - JOUR
AU  - Brborić, Jasmina
AU  - Klisić, Aleksandra
AU  - Kotur-Stevuljević, Jelena
AU  - Delogu, Giovanna
AU  - Gjorgieva Ackova, Darinka
AU  - Kostić, Kristina
AU  - Dettori, Maria Antonietta
AU  - Fabbri, Davide
AU  - Carta, Paola
AU  - Saso, Luciano
PY  - 2023
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4964
AB  - Introduction: Phenols are a large family of natural and synthetic compounds with known antioxidant activity. The aim of this study was to perform in vitro screening of natural and natural-like phenol monomers and their C2-symmetric dimers (hydroxylated biphenyls) in order to identify those representatives whose pharmacophores have the strongest antioxidant and the lowest prooxidant activity. Material and methods: Antioxidative properties of 36 compounds (monomers and their C2-symmetric dimers) were evaluated in vitro. Different (red/ ox) assays were used to measure their total oxidative potential (TOP), their total antioxidative capacity (TAC), the pro-oxidative-antioxidant balance (PAB) and total SH-group content (SHG) in a biologically relevant environment. The Pro-oxidative Score, Antioxidative Score and the Oxy Score were also calculated. Trolox, a water soluble analogue of α-tocopherol, was used as a positive control. Results: In an assay consisting of pooled human serum, 6 of the 36 compounds showed significant antioxidant activity (compounds 6, 7, 12, 13, 26, and 27), whereas 4 showed extremely weak antioxidant activity (compounds 2, 29, 30, and 31). Within the 36 compounds comprising zingerone, dehydrozingerone, aurone, chalcone, and magnolol derivatives, in both monomeric and dimeric forms, the 2 compounds that indicated the highest antioxidant activity were dehydrozingerone derivatives (compounds 6 and 12). Trolox’s activity was found between the strong and weak antioxidant compounds analysed in our study. Conclusions: In this study selected dehydrozingerones were identified as good candidates for in-depth testing of their biological behaviour and for possible precursors for synthesis of novel polyphenolic molecules with potential therapeutic applications.
PB  - Termedia Publishing House
T2  - Archives of Medical Science
T1  - Natural and natural-like polyphenol compounds: in vitro antioxidant activity and potential for therapeutic application
VL  - 19
IS  - 3
SP  - 651
EP  - 671
DO  - 10.5114/aoms/135379
ER  - 

@article{
author = "Brborić, Jasmina and Klisić, Aleksandra and Kotur-Stevuljević, Jelena and Delogu, Giovanna and Gjorgieva Ackova, Darinka and Kostić, Kristina and Dettori, Maria Antonietta and Fabbri, Davide and Carta, Paola and Saso, Luciano",
year = "2023",
abstract = "Introduction: Phenols are a large family of natural and synthetic compounds with known antioxidant activity. The aim of this study was to perform in vitro screening of natural and natural-like phenol monomers and their C2-symmetric dimers (hydroxylated biphenyls) in order to identify those representatives whose pharmacophores have the strongest antioxidant and the lowest prooxidant activity. Material and methods: Antioxidative properties of 36 compounds (monomers and their C2-symmetric dimers) were evaluated in vitro. Different (red/ ox) assays were used to measure their total oxidative potential (TOP), their total antioxidative capacity (TAC), the pro-oxidative-antioxidant balance (PAB) and total SH-group content (SHG) in a biologically relevant environment. The Pro-oxidative Score, Antioxidative Score and the Oxy Score were also calculated. Trolox, a water soluble analogue of α-tocopherol, was used as a positive control. Results: In an assay consisting of pooled human serum, 6 of the 36 compounds showed significant antioxidant activity (compounds 6, 7, 12, 13, 26, and 27), whereas 4 showed extremely weak antioxidant activity (compounds 2, 29, 30, and 31). Within the 36 compounds comprising zingerone, dehydrozingerone, aurone, chalcone, and magnolol derivatives, in both monomeric and dimeric forms, the 2 compounds that indicated the highest antioxidant activity were dehydrozingerone derivatives (compounds 6 and 12). Trolox’s activity was found between the strong and weak antioxidant compounds analysed in our study. Conclusions: In this study selected dehydrozingerones were identified as good candidates for in-depth testing of their biological behaviour and for possible precursors for synthesis of novel polyphenolic molecules with potential therapeutic applications.",
publisher = "Termedia Publishing House",
journal = "Archives of Medical Science",
title = "Natural and natural-like polyphenol compounds: in vitro antioxidant activity and potential for therapeutic application",
volume = "19",
number = "3",
pages = "651-671",
doi = "10.5114/aoms/135379"
}

Brborić, J., Klisić, A., Kotur-Stevuljević, J., Delogu, G., Gjorgieva Ackova, D., Kostić, K., Dettori, M. A., Fabbri, D., Carta, P.,& Saso, L.. (2023). Natural and natural-like polyphenol compounds: in vitro antioxidant activity and potential for therapeutic application. in Archives of Medical Science
Termedia Publishing House., 19(3), 651-671.
https://doi.org/10.5114/aoms/135379

Brborić J, Klisić A, Kotur-Stevuljević J, Delogu G, Gjorgieva Ackova D, Kostić K, Dettori MA, Fabbri D, Carta P, Saso L. Natural and natural-like polyphenol compounds: in vitro antioxidant activity and potential for therapeutic application. in Archives of Medical Science. 2023;19(3):651-671.
doi:10.5114/aoms/135379 .

Brborić, Jasmina, Klisić, Aleksandra, Kotur-Stevuljević, Jelena, Delogu, Giovanna, Gjorgieva Ackova, Darinka, Kostić, Kristina, Dettori, Maria Antonietta, Fabbri, Davide, Carta, Paola, Saso, Luciano, "Natural and natural-like polyphenol compounds: in vitro antioxidant activity and potential for therapeutic application" in Archives of Medical Science, 19, no. 3 (2023):651-671,
https://doi.org/10.5114/aoms/135379 . .

TY  - JOUR
AU  - Gjorgieva-Ackova, Darinka
AU  - Kotur-Stevuljević, Jelena
AU  - Mishra, Chandra Bhushan
AU  - Luthra, Pratibha Mehta
AU  - Saso, Luciano
PY  - 2019
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3327
AB  - Oxidant/antioxidant imbalance in the body has been implicated as one of the pathophysiological mechanisms leading to disease development. Therefore, we searched for a good antioxidant candidate that can be used as a therapeutic agent alone or in combination with other reported drugs. Earlier, we reported the A(2A) receptor antagonist properties of 7-Imino-3-substituted-2-thioxo-3,7-dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl)-urea derivatives (compounds 1-12) and the neuroprotective effect of compound 2. Therefore, in the present work, the antioxidant potential of compounds 1-12 was studied. Compounds 1-12 were screened using different (red/ox) tests, such as the Ferric Reducing Antioxidant Power (FRAP) assay, to determine total antioxidant activity, redox status tests (with and without prooxidants) such as Advanced Oxidation Protein Products (AOPP) and Total Oxidative Status (TOS) which measures H2O2 and lipid hydroperoxides, Paraoxonase-1 Enzyme Activity (PON1), Total SH-groups content, and Total Antioxidative Status (TAS) for antioxidant determination. The Prooxidative Score, Antioxidative Score, and Oxy Score were also calculated. From the obtained results, compounds 6 (8720 FRAP value and 39.31 Oxy Score) and 12 (7866 FRAP value and 36.41 Oxy Score) were found to possess significant antioxidant activity with reasonable potential for therapeutic activity.
PB  - MDPI, Basel
T2  - Applied Sciences, Basel
T1  - Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents
VL  - 9
IS  - 1
DO  - 10.3390/app9010113
ER  - 

@article{
author = "Gjorgieva-Ackova, Darinka and Kotur-Stevuljević, Jelena and Mishra, Chandra Bhushan and Luthra, Pratibha Mehta and Saso, Luciano",
year = "2019",
abstract = "Oxidant/antioxidant imbalance in the body has been implicated as one of the pathophysiological mechanisms leading to disease development. Therefore, we searched for a good antioxidant candidate that can be used as a therapeutic agent alone or in combination with other reported drugs. Earlier, we reported the A(2A) receptor antagonist properties of 7-Imino-3-substituted-2-thioxo-3,7-dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl)-urea derivatives (compounds 1-12) and the neuroprotective effect of compound 2. Therefore, in the present work, the antioxidant potential of compounds 1-12 was studied. Compounds 1-12 were screened using different (red/ox) tests, such as the Ferric Reducing Antioxidant Power (FRAP) assay, to determine total antioxidant activity, redox status tests (with and without prooxidants) such as Advanced Oxidation Protein Products (AOPP) and Total Oxidative Status (TOS) which measures H2O2 and lipid hydroperoxides, Paraoxonase-1 Enzyme Activity (PON1), Total SH-groups content, and Total Antioxidative Status (TAS) for antioxidant determination. The Prooxidative Score, Antioxidative Score, and Oxy Score were also calculated. From the obtained results, compounds 6 (8720 FRAP value and 39.31 Oxy Score) and 12 (7866 FRAP value and 36.41 Oxy Score) were found to possess significant antioxidant activity with reasonable potential for therapeutic activity.",
publisher = "MDPI, Basel",
journal = "Applied Sciences, Basel",
title = "Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents",
volume = "9",
number = "1",
doi = "10.3390/app9010113"
}

Gjorgieva-Ackova, D., Kotur-Stevuljević, J., Mishra, C. B., Luthra, P. M.,& Saso, L.. (2019). Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents. in Applied Sciences, Basel
MDPI, Basel., 9(1).
https://doi.org/10.3390/app9010113

Gjorgieva-Ackova D, Kotur-Stevuljević J, Mishra CB, Luthra PM, Saso L. Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents. in Applied Sciences, Basel. 2019;9(1).
doi:10.3390/app9010113 .

Gjorgieva-Ackova, Darinka, Kotur-Stevuljević, Jelena, Mishra, Chandra Bhushan, Luthra, Pratibha Mehta, Saso, Luciano, "Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents" in Applied Sciences, Basel, 9, no. 1 (2019),
https://doi.org/10.3390/app9010113 . .