3.2.2. Study of biological activity of biomolecules

Leading researcher: Prof. Jana Tchekalarova

Theme: Biological science, Medical science

The studies of biological activity and pharmacodynamics of newly synthesized compounds with biological activity, as well as extracts of natural products, is an important part of their future practical application. Within the framework of the new scientific group, emphasis will be placed on:

• Determination of cytotoxicity and antiproliferative effect of the newly synthesized peptide molecules, bioconjugates with a second pharmacophore and their metal complexes with bioactive metals;
• Determination of anti-pain and anti-inflammatory activity of the newly synthesized molecules and their bioconjugates with heterocyclic compounds;
• Neuropharmacological studies of the nosynthesized compounds regarding potential anticonvulsant, opioid, analgesic and behavioral activities in experimental models in mice;
• Investigation of the effects of the obtained new compounds on the processes of inflammation and pain sensitivity through models of subchronic visceral (writhing test) and acute phase and tonic inflammatory pain (formalin test) and in mice;
• Investigation of lipid peroxidation and activity of antioxidant enzymes by analysis of thiobarbituric acid breakdown products of fatty acids /TBARS/ and the ratio of reduced to oxidized glutathione (GSH:GSSG) in brain homogenates and in blood from experimental animals treated with the test substances with aim to determine the antioxidant action of the newly synthesized hemorphine analogues.

Публикации:

1. J. Tchekalarova, D. Krushovlieva, P. Ivanova, L. Kortenska, Spontaneously hypertensive rats vs. Wistar Kyoto and Wistar rats: An assessment of anxiety, motor activity, memory performance, and seizure susceptibility, Physiology & Behavior, 269, 2023, 114268, ISSN 0031-9384, https://doi.org/10.1016/j.physbeh.2023.114268 , (f. 3.742, Q2)
2. J. Tchekalarova, P. Todorov, Ts. Stoyanova, M. Atanasova, Comparative Analysis of Anticonvulsant Activity of Trans and Cis 5,5 -Diphenylhydantoin Schiff Bases, International Journal of Molecular Sciences, 2023, 24(22):16071, https://doi.org/10.3390/ijms242216071, (f. 5.6, Q1).
3. J. Tchekalarova, P. Todorov, M. Rangelov, Ts. Stoyanova, N. Todorova, Additive Anticonvulsant Profile and Molecular Docking Analysis of 5,5′-Diphenylhydantoin Schiff Bases and Phenytoin, Biomedicines, 2023; 11(11):2912. https://doi.org/10.3390/biomedicines11112912, (f. 4.9, Q1).
4. Karadashka, I.; Ivanova, V.; Jordanov, V.; Karadjova, V. Glass Formation and Properties of Multicomponent Glasses of the As2Se3-Ag2Te-GeTe System, Inorganics 2024, 12, 11. https://doi.org/10.3390/inorganics12010011  (f. 2.9, Q2)
5. V. Mantareva, D. Braikova, N. Vilhelmova-Ilieva, I. Angelov, I. Iliev, Accomplishment of α-Chymotrypsin on Photodynamic Effect of Octa-Substituted Zn(II)- and Ga(III)-Phthalocyanines against Melanoma Cells, Inorganics, 2024, 12, 204. https://doi.org/10.3390/inorganics12080204 (f. 2.9, Q2)
6. Tchekalarova J, Ivanova P, Krushovlieva D. Age-Related Effects of AT1 Receptor Antagonist Losartan on Cognitive Decline in Spontaneously Hypertensive Rats. Int J Mol Sci. 2024 Jul 4;25(13):7340. https://doi.org/10.3390/ijms25137340 IF = 5.6 Q1
7. Tchekalarova, J., Pechlivanova, D., Rangelov, M., Todorova, N., Stoyanova, T., Assenov, B., Todorov, P. A novel cinnamic and caffeic acid-conjugated peptide analogs with anticonvulsant and analgesic potency: Comparative analyses of trans/cis isomers. Drug Development Research, 85, e22236. https://doi.org/10.1002/ddr.22236 IF = 3.5
8. A. Gyurova, V. Milkova, I. Iliev, N. Lazarova-Zdravkova, V. Rashev, L. Simeonova, N. Vilhelmova-Ilieva, Anti-Coronavirus Activity of Chitosan-Stabilized Liposomal Nanocarriers Loaded with Natural Extracts from Bulgarian Flora, Life, 2024, 14, 1180. https://doi.org/10.3390/life14091180 (f. 3.2, Q1)
9. B. Borisova, Hr. Nocheva, I. Iliev, M. Laronze-Cochard, St. Gérard, St. Petrin, D. Danalev, Synthesis and analgesic activity of new analogs of FELL tetrapeptide containing D-Phe in the first position, Current Research in Biotechnology, 2024, 8, 100249, https://doi.org/10.1016/j.crbiot.2024.100249 (f. 4.0, Q2)
10. Hr. Zlatanova-Tenisheva, St. Vladimirova, Experimental screening for analgesic and anti-inflammatory effect of novel compounds with a pyrrole heterocycle, Pharmacia, 2024, 71: 1–10, https://doi.org/10.3897/pharmacia.71.e121943 (f. 1.0, Q4)
11. Mantareva V., Braikova D., Vilhelmova-Ilieva N., Angelov I., Iliev I. Accomplishment of α-Chymotrypsin on Photodynamic Effect of Octa-Substituted Zn(II)- and Ga(III)-Phthalocyanines against Melanoma Cells, Inorganics, 2024, 12(8): 204 https://doi.org/10.3390/inorganics12080204   (i.f.  3.1, Q2)
12. Ts. Foteva, Nanotechnology in the cosmetic industry (Review), J. Chem. Technol. Metall., 59, 1, 2024, 3-14 https://doi.org/10.59957/jctm.v59.i1.2024.1 (SJR 0.194, Q3, SCOPUS)
13. B. Yakimova, R. Alexova, L. Dobreva, Y. Rainova, St. Dobrev, Sv. Danova, S. Angelova, I. Stoineva, Isolation and characterization of peptides from milk as natural inhibitors of ace i and food additives, J. Chem. Technol. Metall., 2024, 59, 4, 789-796 https://doi.org/10.59957/jctm.v59.i4.2024.5 (SJR 0.194, Q3, SCOPUS)
14. S. Georgieva,  P. Todorov, J.  Tchekalarova, S. Subaer, P. Peneva, K. Chakarov, H. Hartati, and S. Faika,  Chemical Behavior and Bioactive Properties of Spinorphin Conjugated to 5,5′-Dimethyl- and 5,5′-Diphenylhydantoin Analogs” Pharmaceuticals 17, no. 6: 770. https://doi.org/10.3390/ph17060770, IF: 4.3, Q2;
15. Stefanov E., Georgieva S., Speciation Analysis of Arsenic in Soil Samples by Liquid-Liquid Extraction and Electrochemical Detection with Gold micro-wire electrode, Metall. Mater. Q4, 2024, accepted (preprint)
16. D. Pechlivanova, B. Assenov, P. Mateeva, E. Dzhambazova, P. Peneva, P. Todorov. Synthesis of peptide analogs of VV-Hemorphin-7 – antinociceptive and antihyperalgesic effect. Journal of Chemical Technology and Metallurgy, Vol. 58 No. 3 (2023): Volume 58, Issue 3, DOI: https://doi.org/10.59957/jctm.v58i3.89
17. Georgieva S, Todorov P, Staneva D, Grozdanov P, Nikolova I, Grabchev I. Metal–Peptide Complexes with Antimicrobial Potential for Cotton Fiber Protection. Journal of Functional Biomaterials. IF=4.8, Q2; 2023; 14(2):106. https://doi.org/10.3390/jfb14020106