18 research outputs found
Promena ugljenohidradnog sastava zrna kukuruza Å”eÄerca (Zea mays L. Saccharata) tokom razvoja endosperma
Sweet corn is consumed as human food in the milk stage of grain development when grain is tender, soft and sweet. Sucrose, a dominant sugar at this stage of the endosperm development, causes sweetness of grain. The changes of grain carbohydrate composition of two genotypes (ZPSC 311 su and ZPSC 450 su) were monitored over stages of maturity (10, 15, 20, 23 and 28 days after pollination). This composition was determined by high pressure chromatography on the column with chemically bound stationary phase, type NH2 and polar mobile phase of acetonitrile-water. Carbohydrate composition of grain changed during the endosperm development in a way that the percentage share of fructose and glucose decreased, while the share of sucrose increased. The maximum value of a sucrose content on the 25th day after pollination amounted to 77.00% and 89.81% in ZPSC 450 su and 78.38% and 77.92% in ZPSC 311 su, in 1999 and 2000, respectively. Thereafter opposite changes occurred. Significant differences (of glucose, fructose) in the share of certain sugars over developmental stages in, were determined. A strong rank correlation between contents of glucose and fructose was detected indicating that the increased glucose content resulted in the increased fructose content and vice versa. Negative values for rank correlation was determined between contents of sucrose and glucose and contents of sucrose and fructose indicating that the increase of the sucrose content leads to the decrease of glucose and fructose contents and vice versa.Kukuruz Å”eÄerac se upotrebljava za ishranu ljudi u mleÄnoj fazi razvoja zrna kada je ono nežno, soÄno i slatko. U toj fazi dominantan Å”eÄer u endospermu je saharoza koja daje slatkoÄu zrnu. U ovom radu praÄene su promene ugljenohidratnog sastava zrna dva genotipa kukuruza Å”eÄerca (ZPSC 311 su i ZPSC 450 su) po fazama zrenja (10, 15, 20, 23 i 28 dana posle oplodnje). Ugljenohidratni sastav zrna odreÄivan je metodom visokopritisne hromatografije na koloni sa hemijski vezanom stacioniranom fazom tipa NH2 i polarnom mobilnom fazom acetonitril-voda. Dobijeni rezultati pokazuju da se ugljenohidratni sastav zrna menjao tokom procesa razvoja endosperma, tako Å”to se smanjivao udeo fruktoze i glukoze, a istovremeno poveÄavao udeo saharoze. Maksimalna vrednost sadržaja saharoze utvrÄena je u fazi 25 dana posle oplodnje, 77,00% i 89,81% za ZPSC 450 su i 78,38% i 77,92% za ZPSC 311 su, tokom 1999. i 2000. godine. Nakon toga odvijale su se suprotne promene. UtvrÄene su statistiÄki znaÄajne razlike u udelu pojedinih Å”eÄera po fazama zrenja, odnosno u zavisnosti od broja dana od oplodnje. UtvrÄena je jaka korelativna veza izmeÄu sadržaja glukoze i fruktoze, Å”to ukazuje na to da se poveÄanjem sadržaja glukoze poveÄava i sadržaj fruktoze i obrnuto. Negativne vrednosti korelacije ranga naÄene su izmeÄu sadržaja saharoze i glukoze i sadržaja saharoze i fruktoze, Å”to znaÄi da se poveÄanjem sadržaja saharoze smanjuje sadržaj glukoze i fruktoze, i obrnuto
Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners
Malaria is a severe and life-threatening disease caused by Plasmodium parasites that are spread to humans through bites of infected Anopheles mosquitoes. Here, we report on the efficacy of aminoquinolines coupled to benzothiophene and thiophene rings in inhibiting Plasmodium falciparum parasite growth. Synthesized compounds were evaluated for their antimalarial activity and toxicity, in vitro and in mice. Benzothiophenes presented in this paper showed improved activities against a chloroquine susceptible (CQS) strain, with potencies of IC50 = 6 nM, and cured 5/5 Plasmodium berghei infected mice when dosed orally at 160 mg/kg/day x 3 days. In the benzothiophene series, the examined antiplasmodials were more active against the CQS strain D6, than against strains chloroquine resistant (CQR) W2 and multidrug-resistant (MDR) TM91C235. For the thiophene series, a very interesting feature was revealed: hypersensitivity to the CQR strains, resistance index (RI) of lt 1. This is in sharp contrast to chloroquine, indicating that further development of the series would provide us with more potent antimalarials against CQR strains
Investigation of antiproliferative activity of new benzothiazolamine derivatives against MCF-7 human breast cancer cell line
Poznato je da se mnogi lekovi, derivati benzotiazola, vrlo uspeŔno koriste u tretmanu
razliÄitih kliniÄkih stanja.1
TakoÄe, znaÄajno mesto zauzimaju u istraživanjima
antitumorskih agenasa i veliki broj strukturnih modifikacija jezgra benzotiazola naÄinjen je
s ciljem poboljŔanja njihove antitumorske aktivnosti. U okviru naŔih istraživanja u ovoj
oblasti sintetisana je serija novih karbamata i amida 6-alkiltio-supstituisanih
benzotiazolamina i ispitana je njihova antiproliferativna aktivnost prema MCF-7 Äelijskoj
liniji humanog karcinoma dojke. Pokazano je da derivati benzotiazolamina izazivaju visoko
specifiÄnu programiranu Äelijsku smrt apoptozu u znaÄajnom procentu tretiranih MCF-7
Äelija. Ispitan je i uticaj novih jedinjenja na Äelijski ciklus, mitohondrijski membranski
potencijal i nivo unutarÄelijskih reaktivnih kiseoniÄnih vrstaNumerous benzothiazole-based clinical drugs have been extensively used in practice to
treat various type of diseases with high therapeutic efficacy.1
In addition, benzothiazole derivatives are compounds of an undoubted interest in anticancer research and a lot of structural modifications on their core nuclei have been made to improve their antitumor activety. Therefore, we have synthesized a series of novel 6-alkylthio-substituted benzothiazolamine carbamates and amides. To investigate their anticancer potency, we have used MCF7 human breast cancer cell line. Benzothiazolamine derivatives show great potency for
promoting highly specific programmed cell death apoptosis in MCF-7 cancer cell line. Our
research continued towards examination of our compounds influence on cell cycle phase
distribution, reactive oxygen species level and mitochondrial membrane potential
New benzothiazolamine derivatives as inducers of an early apoptosis in MCF-7 human breast cancer cell line
Background
Cancer is the second leading cause of morbidity and mortality worldwide, with approximately 14 million
new cases and 8.2 million cancer-related deaths in 2012.1
Current chemotherapy targets the proliferative
advantage of tumor cells over healthy cells, but the lack of selectivity of chemotherapeutic agents usually
leads to serious side effects. A major challenge in the development of effective and safe cancer treatment
is to identify the agents that could affect cellular processes essential for, or greatly enhanced in, malignant
cells only.
Aims
Benzothiazole derivatives represent a series of compounds of an undoubted interest because of the broad
spectrum of biological effects associated with this scaffold.2
In addition, benzothiazoles have attracted
considerable attention in anticancer research and a lot of structural modifications on their core nuclei have
been made to improve the antitumor activity. Therefore, we have synthesized novel benzothiazolamine
derivatives and investigated their anticancer potential against MCF-7 human breast cancer cell line.
Methods
We have synthesized a series of novel benzothiazolamine carbamates and amides starting from 1-chloro4-nitrobenzene and an appropriate alkylthiol, 3 followed by cyclization to benzothiazolamine and further
derivatization of amino-group. The selected compounds were subjected to a panel of NCI-60 cell line for
in vitro determination of antitumor activity. For better insight into possible mechanism of antiproliferative
activity, we have examined the cell cycle phase distribution and apoptosis in MCF-7 human breast cancer
cell line using flow cytometry methods, after treatment with synthesized compounds. Our research
continued towards examination of our compoundsā influence on the reactive oxygen species level,
mitochondrial membrane potential, as well as cell cycle regulators.
Results
The cell cycle phase distribution and apoptosis in MCF-7 human breast cancer cell line were investigated
after exposure to IC50 concentrations, obtained in vitro, of four selected compounds (Figure 1.b) for 24
and 48 hours, respectively. Using flow cytometry after PI staining we showed that our compounds affect cell cycle distribution in a
time dependent manner. After 24 h treatment, the portion of cells in G2/M phase increased, suggesting
cell cycle arrest in mitosis. After 48 hours, the number of sub G1 phase cells increased, which indicates
apoptosis.
Following incubation with selected compounds for 48 hours, the proapoptotic effect was reflected by the
increase of portion of early apoptotic cells up to 63 % measured by bivariate Annexin V/PI flow
cytometry (Figure 1.a). Moreover, we observed the loss of mitochondrial membrane potential, which
could indicate that our compounds promote apoptosis via the mitochondrial pathway in MCF-7 cells. In
addition, reactive oxygen species level in MCF-7 cells significantly decreased after treatment with
benzothiazolamine derivatives.
Conclusion
Benzothiazolamine carbamates and amides showed great potency for promoting highly specific
programmed cell death apoptosis in MCF-7 cancer cell line. Further examination will eventually provide
identification of molecular targets of benzothiazolamines. Our data offer a significant contribution to the
search for medicinally active compounds and may lead to discovery of a new potent antitumor agent
Dominantna svojstva efikasnog fotosintetiÄno-fluorescentnog modela u oplemenjivanju i savremenoj proizvodnji kvalitetnog merkatilnog kukuruza
The following three prestigious maize inbred lines with erect top leaves: ZPPL 16, ZPPL 218 and ZPPL 62 were observed in this study. Each of these inbreds, either as a female or a male component, was included into the development of over 45 maize hybrids. However, maize hybrids ZP 431, ZP 434, ZP 578 and ZP 684 are widely commercially used in this medium-term period. This study conforms the hypothesis that there are elite maize inbred lines with erect top leaves and hybrids derived from them that have a dominant property of an efficient photosynthetic-fluorescence model that is successfully used in breeding and production technologies of hybrid seed and commercial maize. The presented results on the position of top leaves, increased density, dynamics of grain dry down, quality of hybrid and commercial maize and on photosynthetic and fluorescence parameters: temperature dependence on the chlorophyll delayed fluorescence intensity, Arrhenius plot for the determination of critical temperatures (phase transition temperatures) and activation energies, show that the properties of observed inbred lines and their maize hybrids are based on positive effects and the nature of structural and functional changes that occur in their thylakoid membranes and other chemical structures of grain and leaf tissues. Furthermore, other relevant breeding and seed production properties of observed prestigious maize inbred lines and hybrids derived from them were analyzed (dependence of yields on densities and quality of commercial maize on the structure of grain and physical and chemical properties).U ovom radu potvrÄuje se naÅ”a hipoteza da postoje elitne samooplodne linije i sa njima stvoreni hibridi kukuruza, sa uspravnim položajem vrÅ”nih listova, koje poseduju dominantno svojstvo efikasnog fotosintetiÄno-fluorescentnog modela Å”to se uspeÅ”no koristi u oplemenjivanju, savremenim tehnologijama proizvodnje hibridnog semena i merkatilnog kukuruza. Izloženi rezultati o uspravnom položaju vrÅ”nih listova, poveÄanoj gustini, dinamici otpuÅ”tanja vode iz zrna u periodu sazrevanja, kvalitetu semena hibridnog i merkantilnog kukuruza i o fotosintetiÄno-fluorescentnim pokazateljima: temperaturnoj zavisnosti intenziteta zakasnele fluorescencije hlorofila, Arenijusovom kriterijumu za odreÄivanje kritiÄnih temperatura (temperature faznih prelaza) i energija aktivacije, pokazuju da su svojstva prouÄavanih linija i njihovih hibrida kukuruza zasnovana na pozitivnim efektima i prirodi strukturnih i funkcionalnih promena, koje se odigravaju u njihovim tilakoidnim membranama i drugim hemijskim strukturama tkiva zrna i lista. U radu se analiziraju i druge relevantne selekcione i semenarske karakteristike prouÄavanih prestižnih samooplodnih linija kukuruza i sa njima stvorenih hibrida kukuruza (zavisnost prinosa od gustine i kvalitet merkantilnog kukuruza preko strukture zrna i fiziÄkih i hemijskih parametara)
TELEX HEBDOMADAIRE NR 186 DU 12 OCTOBRE 1984 ADRESSE A L'ENSEMBLE DES DELEGATIONS EXTERIEURES ET BUREAUX DE PRESS ET D'INFORMATION INDEPENDANTS DANS LES PAYS TIERS = WEEKLY MEMO NO. 186 ON OCTOBER 12, 1984 TO FOREIGN DELEGATIONS AND PRESS BUREAUS OF THIRD COUNTRIES
Inhibitory activities against BoNT/A LC and holotoxin in proteolytic and cell-based assay for all tested compounds; fluorescence and UVāvis spectra for determination of 16 binding to HSA and AGP; ligand interaction diagrams, docking scores, and dockingāin vitro inhibitory activity correlations; spectral and analytical data for all synthesized compounds; detailed procedures for the determination of the HPLC purity.Supporting information I for: KonstantinoviÄ, J. M., Kiris, E., Kota, K. P., Kugelman-Tonos, J., VidenoviÄ, M., Cazares, L. H., TerziÄ-JovanoviÄ, N., VerbiÄ, T., AnÄelkoviÄ, B. D., Duplantier, A. J., Bavari, S.,& Å olaja, B. (2018). New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry, American Chemical Society (ACS)., 61(4), 1595-1608. [https://doi.org/10.1021/acs.jmedchem.7b01710]The published version of the article: [https://cer.ihtm.bg.ac.rs/handle/123456789/2325]The peer-reviewed version of the article: [http://cer.ihtm.bg.ac.rs/handle/123456789/2935]Additional supporting information (NMR spectra and HPLC purity spectra of all tested compounds): [https://cer.ihtm.bg.ac.rs/handle/123456789/4516]Molecular formula strings and additional data: [https://cer.ihtm.bg.ac.rs/handle/123456789/4517
Supporting Information II for: "New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model"
NMR spectra and HPLC purity spectra of all tested compoundsSupporting information II for: KonstantinoviÄ, J. M., Kiris, E., Kota, K. P., Kugelman-Tonos, J., VidenoviÄ, M., Cazares, L. H., TerziÄ-JovanoviÄ, N., VerbiÄ, T., AnÄelkoviÄ, B. D., Duplantier, A. J., Bavari, S.,& Å olaja, B. (2018). New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry, American Chemical Society (ACS)., 61(4), 1595-1608. [https://doi.org/10.1021/acs.jmedchem.7b01710]The published version of the article: [https://cer.ihtm.bg.ac.rs/handle/123456789/2325]The peer-reviewed version of the article: [http://cer.ihtm.bg.ac.rs/handle/123456789/2935]Additional supporting information: [https://cer.ihtm.bg.ac.rs/handle/123456789/4515]Molecular formula strings and additional data: [https://cer.ihtm.bg.ac.rs/handle/123456789/4517
Nonsuicidal Self-Injury (NSSI) in Serbia: Nationally representative sample study
Although NSSI has been drawing the attention of researchers intensely for the last 30 years, to date there is no published study about rates of NSSI behaviors in countries of south-eastern Europe. The study aimed to explore NSSI in the Republic of Serbia. Data were collected using multistage random sampling. The final sample consisted of 2792 participants (57.4% female) while the NSSI subsample consisted of 405 participants (54.3% males). Results showed the NSSI rate in Serbia is 4.3% based on a percentage of people who answered affirmatively to lifetime NSSI engagement. However, when the percentage of people who reported at least one positive answer through the NSSI behaviors checklist, the rate rises to 14.5%. The most frequent NSSI behavior is wound picking. NSSI rate drops to 8.8% when wound picking is excluded. Those engaged in NSSI were more likely to report suicide attempts and seek professional help than those who did not report NSSI. Gender differences in NSSI frequency are found only in cases of headbanging and burning oneself. This study showed the scope of NSSI-related problems is similar in Serbia compared to other countries. It also raised questions about the lack of preventive programs and treatment strategies for dealing with NSSI in Serbia.[https://www.sciencedirect.com/science/article/pii/S2772598722000320]Corresponding author. Institute for Educational Research, Dobrinjska 11/3, 11 000, Belgrade, Serbia. E-mail addresses: [email protected], [email protected] (A. RadanoviÄ)