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  1. 17 Acta Biochimica Polonica
  2. 8 Acta Poloniae Pharmaceutica - Drug Research
  3. 4 Progress on Chemistry and Application of Chitin and its Derivatives
  4. 3 Polish Journal of Chemistry
  5. 2 Szkło i Ceramika
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  1. 1 2021
  2. 5 2020
  3. 2 2019
  4. 4 2018
  5. 3 2017
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  1. 5 Čėnas N.
  2. 4 Nemeikaitė-Čėnienė A.
  3. 3 Marozienė A.
  4. 2 Ahmed M.
  5. 2 Ciołek L.
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1
Content available remote Cytotoxicity of anticancer aziridinyl-substituted benzoquinones in primary mice splenocytes
100%
Miliukienė V. , Nivinskas H. , Čėnas N.
Acta Biochimica Polonica
|
2014
|
tom 61
|
nr 4
833-836
EN
The anticancer activity of aziridinyl-quinones is mainly attributed to their NAD(P)H:quinone oxidoreductase 1 (NQO1)-catalyzed two-electron reduction into DNA-alkylating products. However, little is known about their cytotoxicity in primary cells, which may be important in understanding their side effects. We found that the cytotoxicity of aziridinyl-unsubstituted quinones (n = 12) in mice splenocytes with a low amount of NQO1, 4 nmol × mg-1 × min-1, was caused mainly by the oxidative stress. Aziridinyl-benzoquinones (n = 6) including a novel anticancer agent RH1 were more cytotoxic than aziridinyl-unsubstituted ones with the similar redox properties, and their cytotoxicity was not decreased by an inhibitor of NQO1, dicumarol. The possible reasons for their enhanced cytotoxicity are discussed.
2
Content available NEW CHITOSAN WOUND DRESSING – FIRST STEP - THE CYTOTOXICITY EVALUATION
100%
Karuga E. , Zając A. , Rybak Z. , Hanuza J.
Progress on Chemistry and Application of Chitin and its Derivatives
|
2015
|
tom 20
97-109
EN
The cytotoxicity of chitosan with polyvinox (PCH) and crosslinked chitosan (CH) was studied and analyzed. Cell viability was determined by thiazolyl blue formazan (MTT) assay and cell morphology observations were carried out during cell culturing and MTT tests. Crosslinked chitosan was used as a protective foil (scaffold) for skin wounds. Studies in vitro and the other obtained in this work results prove that the studied materials CH and PCH do not cause cytotoxic activity to Balb 3T3 mouse fibroblasts. CH and PCH are promising biomaterials with prospective application as wound healing dressings.
3
Content available remote Redox properties and prooxidant cytotoxicity of a neuroleptic agent 6,7-dinitrodihydroquinoxaline-2,3-dione (DNQX)
100%
Šarlauskas J. , Nemeikaitė-Čėnienė A. , Misevičienė L. , Krikštopaitis K. , Anusevičius Ž. , Čėnas N.
Acta Biochimica Polonica
|
2013
|
tom 60
|
nr 2
227-231
EN
In order to characterize the possible mechanism(s) of cytotoxicity of a neuroleptic agent 6,7-dinitrodihydroquinoxaline-2,3-dione (DNQX) we examined the redox properties of DNQX, and its mononitro- (NQX) and denitro- (QX) derivatives. The irreversible electrochemical reduction of the nitro groups of DNQX was characterized by the reduction peak potentials (Ep,7) of -0.43 V and -0.72 V vs. Ag/AgCl at pH 7.0, whereas NQX was reduced at Ep,7 = -0.67 V. The reactivities of DNQX and NQX towards the single-electron transferring enzymes NADPH:cytochrome P-450 reductase and NADPH:adrenodoxin reductase/adrenodoxin complex were similar to those of model nitrobenzenes with the single-electron reduction potential (E17) values of -0.29 V - -0.42 V. DNQX and NQX also acted as substrates for two-electron transferring mammalian NAD(P)H:quinone oxidoreductase (DT-diaphorase). The cytotoxicity of DNQX in bovine leukemia virus-transformed lamb kidney fibroblasts (line FLK) was prevented by antioxidants and an inhibitor of NQO1, dicoumarol, and was enhanced by the prooxidant alkylating agent 1,3-bis(2-chloromethyl)-1-nitrosourea. A comparison with model nitrobenzene compounds shows that the cytotoxicity of DNQX and NQX reasonably agrees with the ease of their electrochemical reduction, and/or their reactivities towards the used enzymatic single-electron reducing systems. Thus, our data imply that the cytotoxicity of DNQX in FLK cells is exerted mainly through oxidative stress.
4
Content available remote A preliminary assessment of singlet oxygen scavenging, cytotoxic and genotoxic properties of Geranium macrorrhizum extracts
100%
Venskutonis P. R. , Dedonytė V. , Lazutka J. , Slapšytė G. , Marozienė A. , Nemeikaitė-Čėnienė A. , Čėnas N. , Miliauskas G.
Acta Biochimica Polonica
|
2010
|
tom 57
|
nr 2
157-163
EN
Strong radical-scavenging activity of Geranium macrorrhizum extracts isolated by using various solvent systems has been reported previously. This study aimed at expanding the knowledge on the bioactivities of antioxidatively active G. macrorrhizum butanol fraction, which was isolated from ethanolic extract (EB), and water fraction, which was isolated from water extract (WW) by measuring their singlet oxygen scavenging properties, as well as preliminary assessment of cytotoxicity and genotoxicity toward mammalian cells. The cytotoxicity (necrosis induction) of the extracts in bovine leukemia virus-transformed lamb kidney fibroblasts (line FLK) was partly prevented by antioxidants and stimulated by the prooxidant BCNU (N,N'-bis(2-chloroethyl)-N-nitrosourea). This indicates that the cytotoxicity of G. macrorrhizum extracts is at least partly attributed to their prooxidant action, presumably due to the formation of quinoidal products of their (auto)oxidation. The latter was evidenced by the nature of the peroxidase-catalyzed oxidation products, which supported DT-diaphorase-catalyzed oxidation of NADPH and participated in conjugation reactions with reduced glutathione. The genotoxic properties were studied using chromosome aberration (CA) and sister chromatid exchange (SCE) tests in human lymphocytes in vitro and Drosophila melanogaster somatic mutation and recombination test (SMART) in vivo. In the CA test, only the highest doses of both fractions significantly increased chromosome aberration frequency. In the SCE test, both fractions induced SCEs in a clear dose-dependent manner. G. macrorrhizum extracts were not genotoxic in the SMART test in vivo. Our data indicate that in spite of the possible beneficial (antioxidant) effects of Geranium extracts, the possibilities of their use as ingredients of functional foods and/or food supplements should be further examined due to their cyto- and genotoxic effects resulting mainly from the action of quercetin-derived components abundant in the extracts.
5
Synthesis and Properties of a Trinuclear Copper(II) Complex with Trithiocyanurate Bridge
100%
Kopel P. , Čermáková S. , Dolezal K. , Kalińska B. , Bieńko A. , Mroziński J.
|
2007
|
tom Vol. 81, nr 3
327-335
EN
Mixed-ligand trinuclear Cu(II) complex involving trithiocyanurate(3-) anion (ttc3-) and N,N,N',N' , N'-pentamethyldiethylenetriamine (pmdien) in the coordination sphere of composition [Cu3(pmdien)3(mi-ttc)](ClO4)3 has been prepared. The complex has been characterized by EA, IR, UV-Vis, and mass spectroscopy. We can assume, that the complex is trinuclear with central atoms connected by trithiocyanurate(3-) bridges. Each central atom is in deformed trigonal bypiramidal arrangement formed by chelating S,N atoms of ttc(3-) and by three N atoms of pmdien. Temperature dependence of magnetic susceptibility and EPR spectroscopy have also been employed to characterize the compound. Magnetic susceptibility measurements over the 1.8-300 K temperature range revealed antiferromagnetic interactions among central atoms. The antitumor activity in vitro against G-361 (human malignant melanoma), HOS (human osteogenic sarcoma), K-562 (human chronic myelogenous leukaemia) and MCF-7 (human breast adenocarcinoma) tumor cell lines have been tested but unfortunately the complexes showed no cytotoxic activity against the four cell lines.
6
Content available Design, synthesis and biological evaluation of some novel substituted quinazoline derivatives as antitumor agents.
100%
Ahmed M. , Magdy N.
Acta Poloniae Pharmaceutica - Drug Research
|
2018
|
tom 75
|
nr 3
EN
New series of 6,8-dibromo-2-(4-chlorophenyl)quinazolin-4-yloxy derivatives were synthesized and their cytotoxic activity on MCF7, HEPG2 and HCT116 cell lines were evaluated. Compound XI and XIIIb were two times more active than doxorubicin on MCF7 cancer cell line. Compound VIIIa was 3 times more active than doxorubicin on HEPG2 cancer cell line. While compounds XII, XIIIa and XIIIb were more potent than doxorubicin on HCT116 cancer cell line. IC50 of all newly synthesized compounds were evaluated in vitro for thier inhibition to EGFR tyrosine kinase. All compound show good inhibitory activity on EGFR tyrosine kinase with IC50 range (6.19-19.87) µM.
7
Content available DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY EVALUATION OF NEW QUINAZOLINE DERIVATIVES LINKED TO THIAZOLIDINONE, AZETIDINONE OR OXADIAZOL MOIETIES
100%
Ahmed M. , Magdy N.
Acta Poloniae Pharmaceutica - Drug Research
|
2018
|
tom 75
|
nr 6
1321-1328
EN
Novel series of 4-substituted 6,8-dibromo-2-(4-chloro-phenyl)-quinazoline have been designed and synthesized. All new derivatives were tested in vitro against MCF-7. Compounds Xc and XIb exerted powerful cytotoxic activity with low IC50 (6.3 and 6.9 µM) compared to doxorubicin 7.72 µM. Compounds Xa, IXb and IXc showed moderate cytotoxic effects with IC50 range (10.0 – 16.7) µM, respectively. Compounds IXa, XIc, XIa, VIIb, VIIIc, Xb and VIIIa showed promising cytotoxic effects with IC50 range (20.3 – 40 µM, respectively. ). Exploring their apoptotic effect; all compounds activated apoptotic cascade in MCF-7. Compounds Xc and XIb increased CASP3 activity more than doxorubicin.
8
Synthesis, Spectral Characteristics and Antitumor Activity of Tungstosilicic Polyoxometalate Containing 5-Fluorouracil
100%
Feng C. G. , Wang S. S. , Liu X.
|
2009
|
tom Vol. 83, nr 12
2079-2087
EN
A novel polyoxometalate com pound with 5-fluorouracil C4H4FN2O2H3SiW12O40ź12H2O (FSW) was synthesized and its structure was analyzed using IR spectra, X-ray powder diffraction (XRD), 183W NMR and TG. IR spectra and XRD indicate that FSW has a Keggin structure of heteropolyanion with a ring structure of 5-fluorouracil as expected. It was found by the analysis of the 183W NMR spectra that the W atoms of FSW remain in the same chemical environment. The results of TG show that the compound has two weight-losing steps with certain degree of thermal stability. The present study uses 5-fluorouracil as the positive control group in the cytotoxicity tests of FSW on human renal embryonic cell HEK293 and the antitumor activity tests in cervical cancer cell Hela using the methyl thiazolyl tetrazolium method. The results obtained show that the therapeutic index of the new polyoxometalate compound is 0.75, higher than that of 5-fluoro-uracil.
9
Content available Novel Synthesis, spectral, characterization of 4,5-diphenyl-1-((tetrahydrofuran-2-yl)methyl)-2-(3,4,5-trichlorophenyl)-1H-imidazole and its applications of molecular docking, anticancer activity
100%
Dhineshkumar E. , doss M. A. , Uma D.
World News of Natural Sciences
|
2020
|
tom 30
|
nr 2
203-212
EN
In the present study of 4,5-diphenyl-1-((tetrahydrofuran-2-yl)methyl)-2-(3,4,5-trichlorophenyl)-1H-imidazole 1 was synthesized. The synthesized imidazole compound 1 has been characterized by FT-IR, 1H, 13C NMR and ESI-Mass spectral studies. Molecular docking is also performed in order to explain the over-expression of estrogen receptor in 70% of liver cancer. The imidazole scaffold is a privileged scaffold for exploration of anticancer agents. The objective of the present study is to evaluate the anticancer activity of imidazole 1 in human liver cancer cell lines HepG2.
10
Content available The use of in vitro assays for the assessment of cytotoxicity on the example of MTT test
100%
Twarużek M. , Zastempowska E. , Soszczyńska E. , Ałtyn I.
Acta Universitatis Lodziensis. Folia Biologica et Oecologica
|
2018
|
tom 14
23-32
PL
Testy biologiczne oparte na hodowlach komórkowych z powodzeniem stosowane są do oceny cytotoksyczności leków, artykułów spożywczych, pasz. Testy in vitro stają się uzupełnieniem konwencjonalnych metod chemicznych, a także alternatywą dla badań przeprowadzanych na zwierzętach. Na podstawie badań własnych można stwierdzić, że test MTT jest czułą metodą diagnostyczną przydatną w ocenie cytotoksyczności nie tylko mikotoksyn, pestycydów, bakterii, pleśni, żywności, pasz, ale także próbek uzyskanych z materiałów budowlanych.
EN
In recent years, biological tests have been developed based on cell cultures and successfully used to the hygienic assess of a variety of samples. In vitro assays become the complement of conventional chemical methods. They do not narrow the results only to the quantitative and qualitative information on toxic substances, but also increase knowledge on the direct impact on the organism. They are also an alternative for animal testing, which are currently given up for ethical reasons. At present, the market is steadily increasing in the number of tests and bio-assay techniques. Based on our own studies we conclude that the MTT test is perfect as a diagnostic method for evaluating the cytotoxicity of materials of different composition such as mycotoxins, pesticides, bacterial cultures, moulds isolates, food, feed, as well as a vast spectrum of other environmental samples.
11
Content available remote Correlation between mammalian cell cytotoxicity of flavonoids and the redox potential of phenoxyl radical/phenol couple
100%
Marozienė A. , Nemeikaitė-Čėnienė A. , Vidžiūnaitė R. , Čėnas N.
Acta Biochimica Polonica
|
2012
|
tom 59
|
nr 2
299-306
EN
Flavonoids exhibit prooxidant cytotoxicity in mammalian cells due to the formation of free radicals and oxidation products possessing quinone or quinomethide structure. However, it is unclear how the cytotoxicity of flavonoids depends on the ease of their single-electron oxidation in aqueous medium, i.e., the redox potential of the phenoxyl radical/phenol couple. We verified the previously calculated redox potentials for several flavonoids according to their rates of reduction of cytochrome c and ferricyanide, and proposed experimentally-based values of redox potentials for myricetin, fisetin, morin, kaempferol, galangin, and naringenin. We found that the cytotoxicity of flavonoids (n=10) in bovine leukemia virus-transformed lamb kidney fibroblasts (line FLK) and murine hepatoma (line MH-22a) increases with a decrease in their redox potential of the phenoxyl radical/phenol couple and an increase in their lipophilicity. Their cytotoxicity was decreased by antioxidants and inhibitors of cytochromes P-450, α-naphthoflavone and isoniazide, and increased by an inhibitor of catechol-O-methyltransferase, 3,5-dinitrocatechol. It shows that although the prooxidant action of flavonoids may be the main factor in their cytotoxicity, the hydroxylation and oxidative demethylation by cytochromes P-450 and O-methylation by catechol-O-methyltransferase can significantly modulate the cytotoxicity of the parent compounds.
12
Content available CYTOTOXIC ACTIVITY OF VARTHEMIA IPHIONOIDES ESSENTIAL OIL AGAINST VARIOUS HUMAN CANCER CELL LINES
100%
Abbas M. M. , Abbas M. A. , Kandil Y. I.
Acta Poloniae Pharmaceutica - Drug Research
|
2019
|
tom 76
|
nr 4
701-706
EN
Varthemia iphionoides is a perennial plant that belongs to Asteraceae family. This study investigates the cytotoxic effect of V. iphionoides essential oil on breast (MCF7), prostate (PC3), and chronic myelogenous leukemia (K562) and normal human fibroblast cell lines using MTT assay and flow cytometric analysis. In addition, GC-MS of the oil was carried out. The IC50 values for PC3, MCF7, K562 and fibroblast were 145.3, 188.8, 87.88 and 173.3 µg/ml, respectively. V. iphionoides essential oil was most effective against K562. Flow cytometric results for IC50 dose of V. iphionoides oil on K562 cells showed 32.2 % apoptosis in 24 h. GC-MS analysis resulted in the identification of 25 compounds. 1,8-Cineole, borneol, and α-cadinol were the major constituents of V. iphionoides volatile oil. In conclusion, this study reveals for the first time the cytotoxic activity of V. iphionoides essential oil on K562 cell line which may occur through apoptosis induction.
13
Content available remote Enzymatic redox reactions of the explosive 4,6-dinitrobenzofuroxan (DNBF): implications for its toxic action.
100%
Nemeikaitė-Čėnienė A. , Šarlauskas J. , Misevièienė L. , Anusevièius Ž. , Marozienė A. , Čėnas N.
Acta Biochimica Polonica
|
2004
|
tom 51
|
nr 4
1081-1086
EN
With an aim to understand the toxicity mechanisms of the explosive 4,6-dinitro- benzofuroxan (DNBF), we studied its single-electron reduction by NADPH:cytochrome P450 reductase and ferredoxin:NADP+ reductase, and two- electron reduction by DT-diaphorase and Enterobacter cloacae nitroreductase. The enzymatic reactivities of DNBF and another explosive 2,4,6-trinitrotoluene (TNT) were similar, except for the much lower reactivity of DNBF towards nitroreductase. DNBF was less cytotoxic in FLK cells than TNT. However, their action shared the same mechanisms, oxidative stress and activation by DT-diaphorase. The lower cytotoxicity of DNBF may be explained by the negative electrostatic charge of its adduct with water which may impede cellular membrane penetration, and by the formation of its less reactive adducts with intracellular reduced glutathione.
14
Content available remote Sensitivity of Vi phages III to γ-radiation in the presence of cisplatin
100%
Dabrowski T. , Kwiatkowski B.
Acta Biochimica Polonica
|
2005
|
tom 52
|
nr 2
545-550
EN
In this study we determined Vi bacteriophage III sensitivity to native cisplatin, γ radiation (60Co) or to irradiated cisplatin, and checked the possibility of enhanced Vi bacteriophage III inactivation under combined exposure to cisplatin and γ radiation. We used highly purified phage suspensions in 0.9% NaCl solution or phosphate-buffered saline. Phage suspensions were titrated using a double agar layer method. Our study implies that survival of Vi bacteriophage III shows an exponential inverse correlation with cisplatin concentration in the incubation medium and the time of phage incubation in the presence of cisplatin. The use of irradiated cisplatin reduces phage survival in comparison with suspensions containing non-irradiated cisplatin. Irradiation of phage suspension with cisplatin causes a significant increase of phage inactivation in comparison with either treatment alone. Our results suggest that presence of cisplatin in irradiated medium enhances the radiobiological effect on Vi bacteriophages III.
15
New Amino Acid Derivatives of 6H-Indolo[2,3-b]quinolines
100%
Sidoryk K. , Kaczmarek Ł. , Szczepek W. J. , Wietrzyk J. , Świtalska M. , Peczyńska-Czoch W.
|
2008
|
tom Vol. 82, nr 11
2095-2105
EN
Some of alkyl, dialkylaminoalkyl and saccharide derivatives of 6H- indolo[2,3-b]quinoline manifest a cytotoxic activity. A wider application of these compounds is limited because of their low water solubility. Attaching aminoacids and peptides to a drug can increase its solubility, selectivity, and bioavailability. A series of novel 6H- in dolo[2,3- b]quinoline derivatives, substituted at C-2 or C-9 with an aminoacid, was designed and synthesized. These compounds were evaluated in vitro for their cytotoxic activity against KB cells (human cervix carcinoma). Gly, His, Pro, and Ser derivatives revealed cytotoxic activity.
16
Content available remote Cytostatic and cytotoxic effects of (E)-2'-deoxy-2'-(fluoromethylene)-cytidine on a solid tumor and a leukemia cell line.
100%
Grieb P. , Koronkiewicz M. , Skierski J. S.
Acta Biochimica Polonica
|
2000
|
tom 47
|
nr 1
165-171
EN
(E)-2'-deoxy-2'-(fluoromethylene)-cytidine (FMdC), a deoxycytidine analog displaying a very high toxicity toward a variety of solid tumor cell lines and xenografts, is activated intracellularly by deoxycytidine kinase (dCK). We have compared cytotoxicity of FMdC towards a human promyeolocytic leukemia line HL-60 and a human colorectal carcinoma line COLO-205. Despite dCK activity being by far the highest in cells of lymphoid origin, the effects of FMdC were detectable at the lowest drug concentration only in a solid tumor cell line, and at higher concentrations they were qualitatively similar in the two tumor lines (increased cell protein content, cell cycle block and apoptosis). Apparently, low dCK activity in solid tumor cells sufficiently activates FMdC to yield cytotoxic effects, while high dCK activity in leukemia cells does not increase its cytotoxicity.
17
Content available remote Photodynamic effect of protoporphyrin diarginate (PPArg2) on methicillin-resistant Staphylococcus aureus and human dermal fibroblasts
88%
Grinholc M. , Kawiak A. , Kurlenda J. , Graczyk A. , Bielawski K. P.
Acta Biochimica Polonica
|
2008
|
tom 55
|
nr 1
85-90
EN
The worldwide rise in the antibiotic resistance of bacteria forces the development of alternative antimicrobial treatments. A potential approach is photodynamic inactivation (PDI). The aim of the present study was to determine the phototoxicity of protoporphyrin diarginate (PPArg2) against methicillin-resistant Staphylococcus aureus and human dermal fibroblasts. Different concentrations (0 to 20 µM) of PPArg2 and light dose of 6 J cm-2 were tested. Cell viability was evaluated using the methylthiazoletetrazolium (MTT) assay. Incubation with 10 µM followed by illumination yielded a 3.6 log10-unit reduction in the viable count for Staphylococcus aureus. At the same experimental conditions, only 22.5% of the fibroblasts were photoinactivated. Protoporphyrin diarginate at concentrations up to 20 µM demonstrated no toxicity towards S. aureus or fibroblasts when not irradiated. These results suggest that the protoporphyrin diarginate exerts a high bactericidal effect against methicillin-resistant S. aureus strain without harming eukaryotic cells.
18
Content available remote Cytotoxic activity of ethanolic extracts of Eleutherococcus species cultivated in Poland on HL60 leukemia cell line
88%
Zaluski D. , Smolarz H. D. , Bogucka-Kocka A.
Current Issues in Pharmacy and Medical Sciences
|
2014
|
tom 27
|
nr 1
41-45
EN
The Eleutherococcus species including 40 species native to Asia are medicinal plants widely used in traditional medicine. Some of these species are cultivated at the botanical gardens in Europe. On the basis on our earlier studies it was concluded that the extracts of analyzed species act as antioxidants, inhibitors of MMPs, and cytotoxic against Jurkat 45 leukemia cell line. In this study, the anti-leukemic potential of roots and leaves from six Eleutherococcus species cultivated in Poland was determined. The in vitro cytotoxic activity towards human promyelotic leukemia cell line HL60 using trypan blue assay was evaluated. The induction of apoptosis in stimulated leukemia cells was determined by AnnexinV method. Morphological changes in treated cells were observed by microscopic investigations. The results showed that ethanolic extracts from the roots and the leaves of E. senticosus, E. setchuensis, E. sessiliflorus, E.gracilistylus, E. henryi and E. divaricatus exhibit cytotoxic effect towards leukemic HL60 cells. The received IC50 values for roots ranged from 49- 208 μg/mL and for the leaves from 116-518 μg/mL. The ethanol extract from the roots of E. divaricatus showed the highest cytotoxic and proapoptotic effect on HL60 human lymphoid leukemia cell line.
19
Content available Dendrimer-paclitaxel complexes for efficient treatment in ovarian cancer: study on OVCAR-3 and HEK293T cells
88%
Yao H. , Ma J.
Acta Biochimica Polonica
|
2018
|
tom 65
|
nr 2
219-225
EN
The present paper investigates the enhancement of the therapeutic effect of Paclitaxel (a potent anticancer drug) by increasing its cellular uptake in the cancerous cells with subsequent reduction in its cytotoxic effects. To fulfill these goals the Paclitaxel (PTX)-Biotinylated PAMAM dendrimer complexes were prepared using biotinylation method. The primary parameter of Biotinylated PAMAM with a terminal HN2 group - the degree of biotinylation - was evaluated using HABA assay. The basic integrity of the complex was studied using DSC. The Drug Loading (DL) and Drug Release (DR) parameters of Biotinylated PAMAM dendrimer-PTX complexes were also examined. Cellular uptake study was performed in OVCAR-3 and HEK293T cells using fluorescence technique. The statistical analysis was also performed to support the experimental data. The results obtained from HABA assay showed the complete biotinylation of PAMAM dendrimer. DSC study confirmed the integrity of the complex as compared with pure drug, biotinylated complex and their physical mixture. Batch 9 showed the highest DL (12.09%) and DR (70%) for 72 h as compared to different concentrations of drug and biotinylated complex. The OVCAR-3 (cancerous) cells were characterized by more intensive cellular uptake of the complexes than HEK293T (normal) cells. The obtained experimental results were supported by the statistical data. The results obtained from both experimental and statistical evaluation confirmed that the biotinylated PAMAM NH2 dendrimer-PTX complex not only displays increased cellular uptake but has also enhanced release up to 72 h with the reduction in cytotoxicity.
20
Content available remote Antiviral activity of novel oseltamivir derivatives against some influenza virus strains
88%
Kocik J. , Kołodziej M. , Joniec J. , Kwiatek M. , Bartoszcze M.
Acta Biochimica Polonica
|
2014
|
tom 61
|
nr 3
509-513
EN
The aim of this study was to investigate the in vitro cytotoxicity of oseltamivir derivatives and determine their activity against A/H1N1/PR/8/34 and A/H3N2/HongKong/8/68 - strains of influenza virus. Antiviral activity of these compounds was determined by using two methods. MTT staining was used to assess the viability of MDCK cells infected with influenza viruses and treated with various concentrations of drugs. In parallel, the effect of drugs on viral replication was assessed using the hemagglutination test. The most toxic compounds were: OS-64, OS-35, OS-29, OS-27 and OS-25, whereas OS-11, OS-20 and OS-23 were the least toxic ones. Statistically significant antiviral effect at a higher virus dose was shown by compounds: OS-11, OS-20, OS-27, OS-35, and OS-64. H3N2 virus was sensitive to 10-times lower concentrations of OS-11 and OS-35 than H1N1. At a lower infection dose, the antiviral activity was observed for OS-11, OS 27, OS-35 and OS-20. OS-64 turned out to be effective only at a high concentration. OS-23 showed no antiviral effect.
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