Depression is a multifactorial disorder that affects millions of people worldwide, and none of th... more Depression is a multifactorial disorder that affects millions of people worldwide, and none of the currently available therapeutics can completely cure it. Thus, there is a need for developing novel, potent, and safer agents. Recent medicinal chemistry findings on the structure and function of the serotonin 2A (5-HT2A) receptor facilitated design and discovery of novel compounds with antidepressant action. Eligible papers highlighting the importance of 5-HT2A receptors in the pathomechanism of the disorder were identified in the content-screening performed on the popular databases (PubMed, Google Scholar). Articles were critically assessed based on their titles and abstracts. The most accurate papers were chosen to be read and presented in the manuscript. The review summarizes current knowledge on the applicability of 5-HT2A receptor signaling modulators in the treatment of depression. It provides an insight into the structural and physiological features of this receptor. Moreover, ...
Receptors of glutamic acid are known for over 30 years for their action and for about 20 years fo... more Receptors of glutamic acid are known for over 30 years for their action and for about 20 years for their structure. Presence of at least three classes of ionotropic receptors was confirmed at the beginning of 80’. Recognition of the sequence and first cloning were done at the beginning of 90’. In 1994 ligand binding site was recognized at the junction of two subunits S1-S2 in the ligand-binding domain. Since then, many subtypes of ionotropic and metabotropic glutamate receptors were recognized, together with their localization and functions. In the meantime numerous orthosteric ligands, both agonists and antagonists were developed especially for NMDA ion channels. Their usefulness as drugs was rather low, due to the involvement in the excitatory tract. More interest was focused on metabotropic receptors, which are GPSR’s and can be modulated both by orthosteric and allosteric modulators. It seems like allosterism could be considered as promising future for glutamate receptors and io...
Isothiocyanates (R-NCS) are sulphur-containing phytochemicals. The main source are plants of the ... more Isothiocyanates (R-NCS) are sulphur-containing phytochemicals. The main source are plants of the Brassicaceae family. The best known plant-derived isothiocyanate is sulforaphane that has exhibited anticancer activity in both in vivo and in vitro studies. Recent attempts to expand their use in cancer therapy involve combining them with standard chemotherapeutics in order to increase their therapeutic efficacy. The aim of this paper is to determine the impact of sulforaphane and its natural analog alyssin on the anticancer activity of the well-known anticancer drug 5-fluorouracil. The type of drug-drug interactions was determined in prostate and colon cancer cell lines. Confocal microscopy, western blot and flow cytometry methods were employed to determine the mechanism of cytotoxic and cytostatic action of the combinations. The study revealed that additive or synergistic interactions were observed between 5-fluorouracil and both isothiocyanates, which enhanced the anticancer activity...
Breast cancer is one of the most common types of cancer in women. In 2012 alone, some 17000 women... more Breast cancer is one of the most common types of cancer in women. In 2012 alone, some 17000 women developed breast cancer and the condition accounted for 5574 deaths. Breast tumor poses a huge threat for women aged 46-65 (working age) and other age groups are at an only slightly lower risk. An early diagnosis of breast cancer would increase chances of survival, which means that it is essential to educate women about breast tumors, risk factors, symptoms and diagnosis.The authors of this work aimed at assessing the knowledge of women residents of Otwock County about breast tumors. The study included a questionnaire including 31 questions, containing queries looking at women’s knowledge of breast tumors and it was distributed to residents of Otwock County between September and October 2014.An analysis of the questionnaire responses suggests what follows: (i) women of all ages are not knowledgeable enough about cancer; (ii) medical professionals, like general practitioners, gynecologis...
Archives of biochemistry and biophysics, Jan 8, 2016
The effect of violaxanthin and zeaxanthin, two main carotenoids of the xanthophyll cycle, on mole... more The effect of violaxanthin and zeaxanthin, two main carotenoids of the xanthophyll cycle, on molecular organization of LHCII, the principal photosynthetic antenna complex of plants, was studied in a model system based on lipid-protein membranes, by means of analysis of 77 K chlorophyll a fluorescence and "native" electrophoresis. Violaxanthin was found to promote trimeric organization of LHCII, contrary to zeaxanthin which was found to destabilize trimeric structures. Moreover, violaxanthin was found to induce decomposition of oligomeric LHCII structures formed in the lipid phase and characterized by the fluorescence emission band at 715 nm. Both pigments promoted formation of two-component supramolecular structures of LHCII and xanthophylls. The violaxanthin-stabilized structures were composed mostly of LHCII trimers while, the zeaxanthin-stabilized supramolecular structures of LHCII showed more complex organization which depended periodically on the xanthophyll content. ...
The main electron ionisation induced fragmentation processes of fused norbornene analogues contai... more The main electron ionisation induced fragmentation processes of fused norbornene analogues containing SiMe2 or GeMe2 and oxygen bridges, as well as their dependence on substitution, were investigated using mass (MS) and tandem mass (MS/MS) spectrometric analysis. Formation of the rearrangement ions of m/z 176 in the mass spectra of fused norbornene analogues containing SiMe2 and m/z 222 in the mass spectrum of norbornene analogues containing GeMe2 provides firm evidence for the migration of a SiMe2 and GeMe2 bridge, respectively.
Novel 1,6-diaryl-5,7(1H)dioxo(dithio)-2,3-dihydroimidazo[1,2-a][1, 3, 5]triazines 8, and 9 were s... more Novel 1,6-diaryl-5,7(1H)dioxo(dithio)-2,3-dihydroimidazo[1,2-a][1, 3, 5]triazines 8, and 9 were synthesized by cyclization of the respective 1-(imidazolin-2-yl)ureas 4 or thioureas 6 with phosgene or thiophosgene in the presence of bases. 1-Aryl-2-aminoimidazolines 1 reacting with arylisocyanates 2 or arylisothiocyanates 3 form a mixture of isomeric imidazolin-2-yl 4 and 6 and imidazolin-3-yl 5 and 7 urea or thiourea derivatives. Isomers 4 and 6 can be easily separated and used for the cyclization reaction. The structures of the main intermediates and the final target compounds were confirmed by 1H-NMR spectral analysis. Discussion of the possible course of the reactions is also presented.
JPC - Journal of Planar Chromatography - Modern TLC, 2007
Five anti-diabetic thiazolidinediones have been chromatographed on C18 TLC plates with binary mob... more Five anti-diabetic thiazolidinediones have been chromatographed on C18 TLC plates with binary mobile phases containing water and the organic modifiers acetone, 1,4-dioxane, or methanol. Linear relationships were obtained between the RM values of the compounds and the concentration of organic modifier in the mobile phase. These RM values enabled calculation of RM0 values by extrapolation. Calibration equations were then obtained for nine standards of known lipophilicity in the range 0.83-6.04. From these equations the partition coefficients log PEXP were calculated for the drugs. Lipophilicity values were also calculated by use of computational methods. Finally, interesting relationships were obtained between experimental and theoretical log P values and pharmacological data from the literature.
JPC - Journal of Planar Chromatography - Modern TLC, 2002
Attempts have been made to find the optimum conditions for modification of silica gel and amino- ... more Attempts have been made to find the optimum conditions for modification of silica gel and amino- and cyanopropyl-bonded silica with Cu(II) and Ni(II) salts. The effect of conditions such as the type of salt and the solvent used were examined. The absolute concentration of metal on the layer was measured by use of atomic absorption spectrometry. The course of the reaction and the strength of metal bonding were evaluated by electron paramagnetic resonance spectrometry. The importance of the modification conditions, especially the role of the impregnation solvent used, were examined by analyzing retention data obtained for unsaturated fatty acid methyl esters in thin-layer chromatography.
Depression is a multifactorial disorder that affects millions of people worldwide, and none of th... more Depression is a multifactorial disorder that affects millions of people worldwide, and none of the currently available therapeutics can completely cure it. Thus, there is a need for developing novel, potent, and safer agents. Recent medicinal chemistry findings on the structure and function of the serotonin 2A (5-HT2A) receptor facilitated design and discovery of novel compounds with antidepressant action. Eligible papers highlighting the importance of 5-HT2A receptors in the pathomechanism of the disorder were identified in the content-screening performed on the popular databases (PubMed, Google Scholar). Articles were critically assessed based on their titles and abstracts. The most accurate papers were chosen to be read and presented in the manuscript. The review summarizes current knowledge on the applicability of 5-HT2A receptor signaling modulators in the treatment of depression. It provides an insight into the structural and physiological features of this receptor. Moreover, ...
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
Novel 1-(1,4-alkylaryldisubstituted-4,5-dihydro-1H-imidazo)-3-substituted urea derivatives have b... more Novel 1-(1,4-alkylaryldisubstituted-4,5-dihydro-1H-imidazo)-3-substituted urea derivatives have been synthesized and evaluated for their central nervous system activity. Compounds 3a–m were prepared in the reaction between the respective 1-alkyl-4-aryl-4,5-dihydro-1H-imidazol-2-amines 1a–c and appropriate isocyanates 2 in dichloromethane. The compounds were subjected to in silico ADMET studies in order to select best candidates for in vivo experiments. The effects of the compounds on the spontaneous locomotor activity and amphetamine-evoked hyperactivity were estimated. Analgesic activity, without or in the presence of naloxone, was assessed in the writhing test. The tendency to change the HTR, evoked by l-5-HTP and the involvement in alteration in body temperature in mice was studied. Additionally, to check possible occurrence of drug-induced changes in the muscle relaxant activity of mice, which may have contributed to their behaviour in other tests, the rota-rod and chimney tests...
There are several reports indicating that the roots of the Carlina acaulis L. used to be commonly... more There are several reports indicating that the roots of the Carlina acaulis L. used to be commonly applied as a treatment measure in skin diseases and as an antiparasitic agent, starting from antiquity to the 19th century; however, nowadays, it has lost its importance. Currently, numerous studies are being conducted assessing the possibility of reintroducing C. acaulis-derived extracts to phytotherapy. Determining the safety profile of the main constituents of the plant material is crucial for achieving this goal. Here, we aimed to determine the toxicity profile of carlina oxide, one of the most abundant components of the C. acaulis root extract. We obtained the carlina oxide by distillation of C. acaulis roots in the Deryng apparatus. The purity of the standard was evaluated using GC-MS, and the identity was confirmed by IR, Raman, and NMR spectroscopy. In vitro cytotoxicity was assessed using a panel of human cell lines of skin origin, including BJ normal fibroblasts and UACC-903, ...
Depression is a multifactorial disorder that affects millions of people worldwide, and none of th... more Depression is a multifactorial disorder that affects millions of people worldwide, and none of the currently available therapeutics can completely cure it. Thus, there is a need for developing novel, potent, and safer agents. Recent medicinal chemistry findings on the structure and function of the serotonin 2A (5-HT2A) receptor facilitated design and discovery of novel compounds with antidepressant action. Eligible papers highlighting the importance of 5-HT2A receptors in the pathomechanism of the disorder were identified in the content-screening performed on the popular databases (PubMed, Google Scholar). Articles were critically assessed based on their titles and abstracts. The most accurate papers were chosen to be read and presented in the manuscript. The review summarizes current knowledge on the applicability of 5-HT2A receptor signaling modulators in the treatment of depression. It provides an insight into the structural and physiological features of this receptor. Moreover, ...
Receptors of glutamic acid are known for over 30 years for their action and for about 20 years fo... more Receptors of glutamic acid are known for over 30 years for their action and for about 20 years for their structure. Presence of at least three classes of ionotropic receptors was confirmed at the beginning of 80’. Recognition of the sequence and first cloning were done at the beginning of 90’. In 1994 ligand binding site was recognized at the junction of two subunits S1-S2 in the ligand-binding domain. Since then, many subtypes of ionotropic and metabotropic glutamate receptors were recognized, together with their localization and functions. In the meantime numerous orthosteric ligands, both agonists and antagonists were developed especially for NMDA ion channels. Their usefulness as drugs was rather low, due to the involvement in the excitatory tract. More interest was focused on metabotropic receptors, which are GPSR’s and can be modulated both by orthosteric and allosteric modulators. It seems like allosterism could be considered as promising future for glutamate receptors and io...
Isothiocyanates (R-NCS) are sulphur-containing phytochemicals. The main source are plants of the ... more Isothiocyanates (R-NCS) are sulphur-containing phytochemicals. The main source are plants of the Brassicaceae family. The best known plant-derived isothiocyanate is sulforaphane that has exhibited anticancer activity in both in vivo and in vitro studies. Recent attempts to expand their use in cancer therapy involve combining them with standard chemotherapeutics in order to increase their therapeutic efficacy. The aim of this paper is to determine the impact of sulforaphane and its natural analog alyssin on the anticancer activity of the well-known anticancer drug 5-fluorouracil. The type of drug-drug interactions was determined in prostate and colon cancer cell lines. Confocal microscopy, western blot and flow cytometry methods were employed to determine the mechanism of cytotoxic and cytostatic action of the combinations. The study revealed that additive or synergistic interactions were observed between 5-fluorouracil and both isothiocyanates, which enhanced the anticancer activity...
Breast cancer is one of the most common types of cancer in women. In 2012 alone, some 17000 women... more Breast cancer is one of the most common types of cancer in women. In 2012 alone, some 17000 women developed breast cancer and the condition accounted for 5574 deaths. Breast tumor poses a huge threat for women aged 46-65 (working age) and other age groups are at an only slightly lower risk. An early diagnosis of breast cancer would increase chances of survival, which means that it is essential to educate women about breast tumors, risk factors, symptoms and diagnosis.The authors of this work aimed at assessing the knowledge of women residents of Otwock County about breast tumors. The study included a questionnaire including 31 questions, containing queries looking at women’s knowledge of breast tumors and it was distributed to residents of Otwock County between September and October 2014.An analysis of the questionnaire responses suggests what follows: (i) women of all ages are not knowledgeable enough about cancer; (ii) medical professionals, like general practitioners, gynecologis...
Archives of biochemistry and biophysics, Jan 8, 2016
The effect of violaxanthin and zeaxanthin, two main carotenoids of the xanthophyll cycle, on mole... more The effect of violaxanthin and zeaxanthin, two main carotenoids of the xanthophyll cycle, on molecular organization of LHCII, the principal photosynthetic antenna complex of plants, was studied in a model system based on lipid-protein membranes, by means of analysis of 77 K chlorophyll a fluorescence and "native" electrophoresis. Violaxanthin was found to promote trimeric organization of LHCII, contrary to zeaxanthin which was found to destabilize trimeric structures. Moreover, violaxanthin was found to induce decomposition of oligomeric LHCII structures formed in the lipid phase and characterized by the fluorescence emission band at 715 nm. Both pigments promoted formation of two-component supramolecular structures of LHCII and xanthophylls. The violaxanthin-stabilized structures were composed mostly of LHCII trimers while, the zeaxanthin-stabilized supramolecular structures of LHCII showed more complex organization which depended periodically on the xanthophyll content. ...
The main electron ionisation induced fragmentation processes of fused norbornene analogues contai... more The main electron ionisation induced fragmentation processes of fused norbornene analogues containing SiMe2 or GeMe2 and oxygen bridges, as well as their dependence on substitution, were investigated using mass (MS) and tandem mass (MS/MS) spectrometric analysis. Formation of the rearrangement ions of m/z 176 in the mass spectra of fused norbornene analogues containing SiMe2 and m/z 222 in the mass spectrum of norbornene analogues containing GeMe2 provides firm evidence for the migration of a SiMe2 and GeMe2 bridge, respectively.
Novel 1,6-diaryl-5,7(1H)dioxo(dithio)-2,3-dihydroimidazo[1,2-a][1, 3, 5]triazines 8, and 9 were s... more Novel 1,6-diaryl-5,7(1H)dioxo(dithio)-2,3-dihydroimidazo[1,2-a][1, 3, 5]triazines 8, and 9 were synthesized by cyclization of the respective 1-(imidazolin-2-yl)ureas 4 or thioureas 6 with phosgene or thiophosgene in the presence of bases. 1-Aryl-2-aminoimidazolines 1 reacting with arylisocyanates 2 or arylisothiocyanates 3 form a mixture of isomeric imidazolin-2-yl 4 and 6 and imidazolin-3-yl 5 and 7 urea or thiourea derivatives. Isomers 4 and 6 can be easily separated and used for the cyclization reaction. The structures of the main intermediates and the final target compounds were confirmed by 1H-NMR spectral analysis. Discussion of the possible course of the reactions is also presented.
JPC - Journal of Planar Chromatography - Modern TLC, 2007
Five anti-diabetic thiazolidinediones have been chromatographed on C18 TLC plates with binary mob... more Five anti-diabetic thiazolidinediones have been chromatographed on C18 TLC plates with binary mobile phases containing water and the organic modifiers acetone, 1,4-dioxane, or methanol. Linear relationships were obtained between the RM values of the compounds and the concentration of organic modifier in the mobile phase. These RM values enabled calculation of RM0 values by extrapolation. Calibration equations were then obtained for nine standards of known lipophilicity in the range 0.83-6.04. From these equations the partition coefficients log PEXP were calculated for the drugs. Lipophilicity values were also calculated by use of computational methods. Finally, interesting relationships were obtained between experimental and theoretical log P values and pharmacological data from the literature.
JPC - Journal of Planar Chromatography - Modern TLC, 2002
Attempts have been made to find the optimum conditions for modification of silica gel and amino- ... more Attempts have been made to find the optimum conditions for modification of silica gel and amino- and cyanopropyl-bonded silica with Cu(II) and Ni(II) salts. The effect of conditions such as the type of salt and the solvent used were examined. The absolute concentration of metal on the layer was measured by use of atomic absorption spectrometry. The course of the reaction and the strength of metal bonding were evaluated by electron paramagnetic resonance spectrometry. The importance of the modification conditions, especially the role of the impregnation solvent used, were examined by analyzing retention data obtained for unsaturated fatty acid methyl esters in thin-layer chromatography.
Depression is a multifactorial disorder that affects millions of people worldwide, and none of th... more Depression is a multifactorial disorder that affects millions of people worldwide, and none of the currently available therapeutics can completely cure it. Thus, there is a need for developing novel, potent, and safer agents. Recent medicinal chemistry findings on the structure and function of the serotonin 2A (5-HT2A) receptor facilitated design and discovery of novel compounds with antidepressant action. Eligible papers highlighting the importance of 5-HT2A receptors in the pathomechanism of the disorder were identified in the content-screening performed on the popular databases (PubMed, Google Scholar). Articles were critically assessed based on their titles and abstracts. The most accurate papers were chosen to be read and presented in the manuscript. The review summarizes current knowledge on the applicability of 5-HT2A receptor signaling modulators in the treatment of depression. It provides an insight into the structural and physiological features of this receptor. Moreover, ...
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
Novel 1-(1,4-alkylaryldisubstituted-4,5-dihydro-1H-imidazo)-3-substituted urea derivatives have b... more Novel 1-(1,4-alkylaryldisubstituted-4,5-dihydro-1H-imidazo)-3-substituted urea derivatives have been synthesized and evaluated for their central nervous system activity. Compounds 3a–m were prepared in the reaction between the respective 1-alkyl-4-aryl-4,5-dihydro-1H-imidazol-2-amines 1a–c and appropriate isocyanates 2 in dichloromethane. The compounds were subjected to in silico ADMET studies in order to select best candidates for in vivo experiments. The effects of the compounds on the spontaneous locomotor activity and amphetamine-evoked hyperactivity were estimated. Analgesic activity, without or in the presence of naloxone, was assessed in the writhing test. The tendency to change the HTR, evoked by l-5-HTP and the involvement in alteration in body temperature in mice was studied. Additionally, to check possible occurrence of drug-induced changes in the muscle relaxant activity of mice, which may have contributed to their behaviour in other tests, the rota-rod and chimney tests...
There are several reports indicating that the roots of the Carlina acaulis L. used to be commonly... more There are several reports indicating that the roots of the Carlina acaulis L. used to be commonly applied as a treatment measure in skin diseases and as an antiparasitic agent, starting from antiquity to the 19th century; however, nowadays, it has lost its importance. Currently, numerous studies are being conducted assessing the possibility of reintroducing C. acaulis-derived extracts to phytotherapy. Determining the safety profile of the main constituents of the plant material is crucial for achieving this goal. Here, we aimed to determine the toxicity profile of carlina oxide, one of the most abundant components of the C. acaulis root extract. We obtained the carlina oxide by distillation of C. acaulis roots in the Deryng apparatus. The purity of the standard was evaluated using GC-MS, and the identity was confirmed by IR, Raman, and NMR spectroscopy. In vitro cytotoxicity was assessed using a panel of human cell lines of skin origin, including BJ normal fibroblasts and UACC-903, ...
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