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Brigita Vigante   Dr.  Senior Scientist or Principal Investigator 
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Brigita Vigante published an article in June 2018.
Top co-authors See all
Marina Petrova

94 shared publications

Latvian Institute of Organic Synthesis

Gunars Duburs

52 shared publications

Latvian Institute of Organic Synthesis, Aizkraukles str. 21, Riga, LV-1006, Latvia

Aiva Plotniece

31 shared publications

Latvian Institute of Organic Synthesis, Aizkraukles Str. 21, Riga LV-1006, Latvia

Karlis Pajuste

16 shared publications

Latvian Institute of Organic Synthesis, Aizkraukles Str. 21, Riga LV-1006, Latvia

Egils Bisenieks

15 shared publications

Latvian Institute of Organic Synthesis, Aizkraukles str. 21, Riga, LV-1006, Latvia

19
Publications
22
Reads
4
Downloads
35
Citations
Publication Record
Distribution of Articles published per year 
(2001 - 2018)
Total number of journals
published in
 
14
 
Publications See all
Article 0 Reads 0 Citations Synthesis and Comparative Evaluation of Novel Cationic Amphiphile C12-Man-Q as an Efficient DNA Delivery Agent In Vitro Gunita Apsite, Irena Timofejeva, Aleksandra Vezane, Brigita ... Published: 26 June 2018
Molecules, doi: 10.3390/molecules23071540
DOI See at publisher website PubMed View at PubMed ABS Show/hide abstract
New amphiphilic 1,4-DHP derivative C12-Man-Q with remoted cationic moieties at positions 2 and 6 was synthesised to study DNA delivery activity. The results were compared with data obtained for cationic 1,4-DHP derivative D19, which is known to be the most efficient one among the previously tested 1,4-DHP amphiphiles. We analysed the effects of C12-Man-Q concentration, complexation media, and complex/cell contact time on the gene delivery effectiveness and cell viability. Transmission electron microscopy data confirms that lipoplexes formed by the compound C12-Man-Q were quite uniform, vesicular-like structures with sizes of about 50 nm, and lipoplexes produced by compound D19 were of irregular shapes, varied in size in the range of 25–80 nm. Additionally, confocal microscopy results revealed that both amphiphiles effectively delivered green fluorescent protein expression plasmid into BHK-21 cells and produced a fluorescent signal with satisfactory efficiency, although compound C12-Man-Q was more cytotoxic to the BHK-21 cells with an increase of concentration. It can be concluded that optimal conditions for C12-Man-Q lipoplexes delivery in BHK-21 cells were the serum free media without 0.15 M NaCl, at an N/P ratio of 0.9. Compound D19 showed higher transfection efficiency to transfect BHK-21 and Cos-7 cell lines, when transfecting active proliferating cells. Although D19 was not able to transfect all studied cell lines we propose that it could be cell type specific. The compound C12-Man-Q showed modest delivery activity in all used cell lines, and higher activity was obtained in the case of H2-35 and B16 cells. The transfection efficiency in cell lines MCF-7, HeLa, and Huh-7 appears to be comparable to the reference compound D19 and minimal in the HepG2 cell line.
Article 0 Reads 0 Citations Searching for inhibitors of human H 2 S-synthesizing enzymes by orthogonal methods Karim Zuhra, Pedro M.F. Sousa, Giulia Paulini, Ana Rita Lemo... Published: 01 May 2018
Free Radical Biology and Medicine, doi: 10.1016/j.freeradbiomed.2018.04.509
DOI See at publisher website
CONFERENCE-ARTICLE 16 Reads 0 Citations <strong>Design and Synthesis of Small-molecule Hepatitis B Virus Capsid Self-assembly Inhibitors</strong> Anda Sīpola, Unda Dubova, Brigita Vīgante, Karīna Spunde, Ta... Published: 01 November 2017
Proceedings of 3rd International Electronic Conference on Medicinal Chemistry, doi: 10.3390/ecmc-3-04679
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An estimated 240 million persons worldwide are chronically infected with hepatitis B virus (HBV). Chronic hepatitis B (CHB) in up to 40% of cases progresses to liver cirrhosis, hepatic decompensation, and hepatocellular carcinoma, a leading cause of cancer-related morbidity and mortality worldwide [1]. We are focused on original antiviral strategy intended to suppress the self-assembly process of HBV core (HBc) protein as one of the promising ways to cure CHB without induction of drug resistance. Targeting the capsid protein of HBV and thus interrupting normal capsid formation have been an attractive approach to block the replication of HBV.

Heteroaryldihydropyrimidines (HAPs) were shown to bind the HBV core proteins and misdirect the assembly of the capsid in vitro. We carried out structural optimizations based on HAPs analogue Bay 41-4109 and structure-activity relationship studies [2].

Newly synthesized HAPs 1 and 2 were evaluated for their ability to disrupt the capsid assembly in cell culture, and promising candidates were selected for further evaluation of antiviral activity and discovery of mechanisms of compound action.

 

Acknowledgments: The author gratefully acknowledges Gunārs and Renāte Duburi for provided scholarship.

References:

[1] World Health Organization (2016) WHO Hepatitis B Fact Sheet (World Health Organization, Geneva)

[2] Qiu, Z. et.al. (2016), Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors. J. Med. Chem. 59, 7651-7666

Article 0 Reads 2 Citations Modifications of expression of genes and proteins involved in DNA repair and nitric oxide metabolism by carbatonides [di... Kristīne Ošiņa, Elina Leonova, Sergejs Isajevs, Larisa Bauma... Published: 26 September 2017
Archives of Industrial Hygiene and Toxicology, doi: 10.1515/aiht-2017-68-2945
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Studies on the pathogenesis of diabetes mellitus complications indicate that the compounds reducing free radicals and enhancing DNA repair could be prospective as possible remedies. Carbatonides, the disodium-2,6-dimethyl-1,4- dihydropyridine-3,5-bis(carbonyloxyacetate) derivatives, were tested for these properties. EPR spectroscopy showed that metcarbatone was an effective scavenger of hydroxyl radicals produced in the Fenton reaction, etcarbatone, and propcarbatone were less effective, styrylcarbatone was ineffective. UV/VIS spectroscopy revealed that styrylcarbatone manifested a hyperchromic effect when interacting with DNA, while all other carbatonides showeda hypochromic effect. Rats with streptozotocin induced type 1 DM were treated with metcarbatone, etcarbatone or styrylcarbatone (all compounds at doses 0.05 mg kg-1 or 0.5 mg kg-1) nine days after the DM approval. Gene expression levels in kidneys and blood were evaluated by quantitative RT-PCR; protein expression - immunohistochemically in kidneys, heart, sciatic nerve, and eyes; DNA breakage - by comet assay in nucleated blood cells. Induction of DM induced DNA breaks; metcarbatone and styrylcarbatone (low dose) alleviated this effect. Metcarbatone and etcarbatone up-regulated mRNA and protein of eNOS in kidneys of diabetic animals; etcarbatone also in myocardium. Etcarbatone reduced the expression of increased iNOS protein in myocardium, nerve, and kidneys. iNos gene expression was up-regulated in kidneys by etcarbatone and metcarbatone in diabetic animals. In blood, development of DM increased iNos gene expression; etcarbatone and metcarbatone normalised it. Etcarbatone up-regulated the expression of H2AX in kidneys of diabetic animals but decreased the production of c-PARP1. Taken together, our data indicate that carbatonides might have a potential as drugs intended to treat DM complications.
Article 2 Reads 3 Citations Direct Aminolysis of Ethoxycarbonylmethyl 1,4-Dihydropyridine-3-carboxylates Brigita Vigante, Martins Rucins, Aiva Plotniece, Karlis Paju... Published: 12 November 2015
Molecules, doi: 10.3390/molecules201119697
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The ethoxycarbonylmethyl esters of 1,4-dihydropyridines were directly converted into carbamoylmethyl esters in the presence of 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) in good to excellent yields under mild conditions. The use of TBD is crucial for the successful aminolysis of ethoxycarbonylmethyl ester of 1,4-dihydropyridines with secondary amines as without it the reaction does not proceed at all. The aminolysis reaction proceeded regioselectively, as the alkyl ester conjugated with the 1,4-dihydropyridine cycle was not involved in the reaction. Screening of other N-containing bases, such as triethylamine (TEA), pyridine, 4-(N,N-dimethylamino)pyridine (DMAP), 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), 1,5-diazabicyclo[4.3.0]non-5-ene (DBN), imidazole, tetramethyl guanidine (TMG) and 7-methyl-1,5,7-triazabicyclo[4.4.0]dec-5-ene (MTBD) as catalysts revealed no activity in the studied reaction.
Article 0 Reads 4 Citations Design, synthesis and 3D-QSAR studies of novel 1,4-dihydropyridines as TGFβ/Smad inhibitors Daniel Längle, Viktoria Marquardt, Elena Heider, Brigita Vig... Published: 01 May 2015
European Journal of Medicinal Chemistry, doi: 10.1016/j.ejmech.2015.03.027
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