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Wyświetlanie 1-15 z 19
Tytuł:
Effect of suberoylanilide hydroxamic acid on peripheral blood mononuclear cell cytotoxicity towards tumor cells in canines
Autorzy:
Oyamada, T.
Okano, S.
Powiązania:
https://bibliotekanauki.pl/articles/2087212.pdf
Data publikacji:
2021
Wydawca:
Polska Akademia Nauk. Czytelnia Czasopism PAN
Tematy:
antitumor effect
canines
cytotoxicity
NKG2D receptor
peripheral blood mononuclear cell
suberoylanilide hydroxamic acid
Źródło:
Polish Journal of Veterinary Sciences; 2021, 24, 1; 35-41
1505-1773
Pojawia się w:
Polish Journal of Veterinary Sciences
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Synthesis and characterization of diversely substituted pyrimidine-3-carboxamide and their antimicrobial evaluation
Autorzy:
Senjani, Hardik K.
Joshi, H. D.
Powiązania:
https://bibliotekanauki.pl/articles/1031771.pdf
Data publikacji:
2020
Wydawca:
Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
Tematy:
1-4-dihydropyrimidine
analgesic
anti-inflammatory
antibacterial
anticonvulsant
antifungal
antimicrobial
antituberculosis
antitumor
biginalli
dihydropyrimidine
insecticidal
multi-component reaction
pyrimidine
Opis:
Pyrimidine related fused heterocycles are attracted to every chemist during the last decade for their biological and chemotherapeutic importance. Pyrimidine derivatives play a vital role in their broad spectrum of biological activities including antituberculosis, anticonvulsant, anti-inflammatory, insecticidal, antifungal, analgesic, and antitumor properties and there of interest as potential bioactive molecules. The nitrogen-containing fragment may be an amidine, urea, thiourea, or guanidine, and adamantine homologs and aromatic aldehyde serve as an excellent illustrative example in that it readily undergoes as Biginali MCRs reaction. Pyrimidines and their derivatives are considered to be important for drugs and agricultural chemicals. Pyrimidine derivatives possess several interesting biological activities. Pyrimidine is a basic nucleus in DNA & RNA, it is associated with diverse biological activities so, we have designed and prepared a novel highly functionalized pyrimidine library of 1,4 DHP and DHPM via a one-pot multi-component (MCRs) synthesis and we screened for antimicrobial activity against various strains.
Źródło:
World Scientific News; 2020, 150; 39-77
2392-2192
Pojawia się w:
World Scientific News
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
THE INFLUENCE OF POLYETHER SUBSTITUENTS ON BIOLOGICAL ACTIVITY OF CURCUMIN DERIVATIVES
Autorzy:
Gruber, Beata M.
Tomasz, Deptuła
Adam, Krówczyński
Irena, Bubko
Powiązania:
https://bibliotekanauki.pl/articles/895397.pdf
Data publikacji:
2020-02-29
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Tematy:
Chemical synthesis
cytotoxic activity
curcumin derivatives
antitumor drugs
Opis:
Curcumin is reported as an anti proliferative and chemopreventive compound. However, it shows poor water solubility, low bioavailability, and rapid metabolism.. To address these problems, curcumin derivatives substituted with polyether chain were synthesised to improve the hydrophilicity of curcumin and thus its bioavailability. The biological activity of modified curcumin molecules were studied with human normal B-lymphocytes GM 14667 and human leukemia cells HL60 and covered: the denotation of IC50 values for each new compound with use of MTT test and the studies on apoptosis induction observed as morphological changes and the expression of apoptotic proteins, BAX, BCL-2 and survivin with use of Western Blot analysis. All effects were referenced to native curcumin. The derivatives with modified polyether chains number and the position of methoxy- groups were selected for further studies. As was shown, the solubility of the compound does not directly correlate with its cytotoxicity. The maintenance of the methoxy group in the meta position as well as the introduction of hydrophilic polyether chains but not the number of polyether chains may affect the cytotoxic activity of curcumin derivatives against cancer cells. Modifications of the curcumin molecule structure can determine its impact on the profile of pro or anti apoptotic proteins.
Źródło:
Acta Poloniae Pharmaceutica - Drug Research; 2020, 77, 1; 99-111
0001-6837
2353-5288
Pojawia się w:
Acta Poloniae Pharmaceutica - Drug Research
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
PHYTOCHEMICAL ANALYSIS AND BIOLOGICAL EVALUATION OF FORSSKAOLEA VIRIDIS AERIAL PARTS
Autorzy:
El-Bassossy, Taha A.
Ahmed, Fatma A.
El-Mesallamy, Amani M.
Powiązania:
https://bibliotekanauki.pl/articles/895657.pdf
Data publikacji:
2019-10-30
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Tematy:
antimicrobial
flavonoids
phenolics
antitumor
Forsskaolea viridis
Opis:
The chemical investigation of the chloroform and ethyl acetate extracts of the aerial parts of Forsskaolea viridis Ehrenb. ex Webb (Family: Urticaceae) led to isolation eight compounds for the first time from this plant, while two phenolic compounds, identified as p-coumaric and caffeic acids as well as six flavonoid compounds identified as 5-hydroxy-6,7,3',4'-tetramethoxy flavone, chrysoeriol, acacetin, chrysoeriol-7-O-β-D-glucoside, kaempferol-3-O-(2"-O-E--p-coumaroyl)-β-D-glucoside and isovetixin. The chemical structure of the isolated compounds was established by spectroscopic methods including UV, MS, 1H-NMR, and 13C-NMR. Antimicrobial, antioxidant and cytotoxic activities of the ethyl acetate and chloroform extracts were evaluated. The ethyl acetate extract exhibited strong antimicrobial activity (12-30 mm) against the tested strains. The ethyl acetate and chloroform extracts showed fair antioxidant and cytotoxicity.
Źródło:
Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 5; 815-823
0001-6837
2353-5288
Pojawia się w:
Acta Poloniae Pharmaceutica - Drug Research
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
SYNTHESIS, REACTIONS, AND APPLICATIONS OF HYDANTOIN AND 2-THIOHYDANTOIN DERIVATIVES
Autorzy:
Abd Elhady, Hebe
El Desoky, Somia
Al-Shareef, Hossa F.
El-mekawy, Rasha
Powiązania:
https://bibliotekanauki.pl/articles/895248.pdf
Data publikacji:
2019-12-29
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Tematy:
antimicrobial activity
antiviral activity
antitumor activity
Hydantoin
2-thiohydantoin
anxiolytic activity
Opis:
On account of the interesting pharmacological properties of hydantoin and 2-thiohydantoin derivatives, and other purposes such as textile printing, catalysts for polymerizations, their use in the production of resins and plastics, they have been the subject of chemical and biological studies. In this review article, we focused our interest on the most important methods for the synthesis of hydantoin and 2-thiohydantoin derivatives, different reactions and different application of them. We explored their antitumor, antimicrobial, antiviral, anxiolytic, antidiabetic, anticonvulsant activities, their utilities in treatment of vascular dysfunction, using them as an inhibitor of fatty acid amide hydrolase, using in hyperpigmentation applications, and utilities of them in the production of antimicrobial polyurethane coatings.
Źródło:
Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 6; 971-986
0001-6837
2353-5288
Pojawia się w:
Acta Poloniae Pharmaceutica - Drug Research
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Anticancer properties of Viburnum
Autorzy:
Stępień, Agnieszka
Aebisher, David
Bartusik-Aebisher, Dorota
Powiązania:
https://bibliotekanauki.pl/articles/454949.pdf
Data publikacji:
2018
Wydawca:
Uniwersytet Rzeszowski. Wydawnictwo Uniwersytetu Rzeszowskiego
Tematy:
antitumor activity
Viburnum species
cytotoxic activity
Opis:
Aim. The aim of this paper is to provide an overview of the anticancer properties of different species of Viburnum. Materials and methods. Forty nine papers that discuss the medicinal history and current research of Viburnum species as phytotherapeutic agent were used for this discussion. Literature analysis. The results of scientific research conducted in vitro indicate that the compounds present in the extracts of Viburnum significantly affect the development of cancer cells such as leukemia, cervical cancer, breast, colon, lung, skin and stomach. This indicates that they may be used as a therapeutic agent to support oncological therapies.
Źródło:
European Journal of Clinical and Experimental Medicine; 2018, 1; 47-52
2544-2406
2544-1361
Pojawia się w:
European Journal of Clinical and Experimental Medicine
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Tiosemikarbazony : właściwości koordynacyjne w aspekcie aktywności biologicznej
Thiosemicarbazones : coordination properties in relation to biological activity
Autorzy:
Ostrowska, M.
Toporivska, Y.
Pyrkosz-Bulska, M.
Gumienna-Kontecka, E.
Powiązania:
https://bibliotekanauki.pl/articles/171499.pdf
Data publikacji:
2018
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
tiosemikarbazony
czynniki przeciwnowotworowe
aktywność biologiczna
stałe trwałości
metale przejściowe
thiosemicarbazones
antitumor agents
biological activity
stability constants
transition metals
Opis:
Thiosemicarbazones are considered to be potential therapeutics, because they possess a broad range of biological properties including antitumor, antimalarial and antimicrobial activity. Generally, the tiosemicarbazones coordinate to the metal centre by means of an (N,S) bidentate mode, and when an additional coordinating group is present, more diversified binding modes can occur such as a tridentate (X,N,S) coordination fashion. The stability of the metal complexes formed with the tiosemicarbazoness strongly depends on the character of the metal ion, the X-donor atom of the additional functional group and the position and type of the substituents at the tiosemicarbazones. The most prominent representative of this family is the α(N)-heterocyclic Triapine (3-aminopyridine- 2-carbaldehyde thiosemicarbazone; 3-AP), which is currently undergoing different phase-I and -II clinical trials as an antitumor agent, and demonstrates promising activity. Triapine is a very strong inhibitor of ribonucleotide reductase, the rate determining enzyme in the supply of deoxyribonucleotides for DNA synthesis required for cell proliferation. The mechanism of action involves most probably the formation of an iron(II)–Triapine complex, which reacts with molecular oxygen to result in the generation of reactive oxygen species. Subsequently, these reactive oxygen species are responsible for the quenching of the active-site tyrosyl radical of ribonucleotide reductase required for the enzymatic activity. As a result, the coordination chemistry of iron complexes of tiosemicarbazones has been receiving considerable attention. This review describes the coordination chemistry of tiosemicarbazones, in particular analogs of Triapine. The coordination compounds of d-block elements are discussed with respect to their bonding and structures. Several of complexes are mononuclear, with distorted tetrahedral, square planar, square pyramid or octahedral as their common geometries. The metal-binding ability of STSC at physiological pH was compared and shown. Further, various biological applications with emphasis an anticancer activity of the ligands/complexes are discussed in brief so as to indicate the importance of ligands under consideration.
Źródło:
Wiadomości Chemiczne; 2018, 72, 7-8; 449-467
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Biological screening and assessment of certain substituted monoazo heterocycles containing sulphur and / or nitrogen and their seleno like moieties
Autorzy:
Khalifa, M. E.
Gobouri, A. A.
Powiązania:
https://bibliotekanauki.pl/articles/779055.pdf
Data publikacji:
2017
Wydawca:
Zachodniopomorski Uniwersytet Technologiczny w Szczecinie. Wydawnictwo Uczelniane ZUT w Szczecinie
Tematy:
thiophene
antioxidant activities
antitumor agents
pathogenic microorganisms
selenium
Opis:
The monoazo substituted five membered heterocycles, along with their seleno like moieties are still of interest in organic chemistry due to their medicinal and valuable applications. In continuation of our interest in the study of heterocyclic azo compounds containing sulphur and / or nitrogen heteroatoms, the synthesis of 5-aryl mono azo-thiazol-2-ylcarbamoyl-thiophene along with their seleno like derivatives of pyridine, pyridazine and quinolone, were accomplished. All the synthesized compounds were in vitro screening of their antioxidant activity, antitumor activity against Ehrlich ascites carcinoma cell EACC cell line and antimicrobial activity against various pathogenic microorganisms, such as Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli and Salmonella typhimurium) and fungi strains of Aspergillus flavus and Candida albicans. The structural–activity relationship was studied based on the obtained data.
Źródło:
Polish Journal of Chemical Technology; 2017, 19, 4; 28-35
1509-8117
1899-4741
Pojawia się w:
Polish Journal of Chemical Technology
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Grzyby nadrewnowe z rodzaju Ganoderma źródłem biologicznie aktywnych triterpenów
Wood Decay Mushrooms of The Genus Ganoderma as A Source of Biologically Active Triterpenes
Autorzy:
Sułkowska-Ziaja, Katarzyna
Piechaczek, Małgorzata
Pacławska, Aneta
Muszyńska, Bożena
Powiązania:
https://bibliotekanauki.pl/articles/1033575.pdf
Data publikacji:
2017
Wydawca:
Zakład Opieki Zdrowotnej Ośrodek Umea Shinoda-Kuracejo
Tematy:
Ganoderma sp.
anti-inflammatory
antitumor
terpenoids
Opis:
Species of the genus Ganoderma are an example of some of the most thoroughly studied representatives of Basidiomycota both in terms of chemical composition and biological activity. Among the compounds found in this kind, the therapeutic effect is primarily associated with the polysaccharides that are heteroglycans or β-D-glucans and terpenoids represented mainly by triterpenes. Triterpene compounds have a structure composed of 30 carbon atoms, usually forming a system of five six-membered rings. Characteristic of these structures are functional groups (hydroxyl, carboxyl or ketone) and double bonds. Mycochemical studies have led to the isolation of numerous triterpenes of the lanostane type (ganoderic acids, aldehydes, alcohols, esters), lucidenic acids and others from various species of the Ganoderma genus. The broad spectrum of biological activity determined by triterpene compounds includes anti- tumor, anti-inflammatory, antioxidant, hepatoprotective, antidiabetic, and antiviral effects. This work describes biologically active triterpenes in selected species of the genus Ganoderma: Ganoderma lucidum, Ganoderma applanatum, Ganoderma adspersum, Ganoderma pfeifferi, Ganoderma colossum and others. These species are sources of natural compounds valued for thousands of years in the traditional medicine of the Far East, while ongoing research has confirmed their medicinal properties nowadays.
Źródło:
Medicina Internacia Revuo; 2017, 28, 109; 237-245
0465-5435
Pojawia się w:
Medicina Internacia Revuo
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Synteza i badania oddziaływania z albuminą N,N-pdimetyloaminobenzylowej pochodnej tiosemikarbazonu i jej kompleksu z rutenem(II)
Synthesis and interaction with albumin of N,N-dimethylaminbenzyl derivative of thiosemicarbazone and its ruthenium(II) complex
Autorzy:
Łomzik, M.
Brindell, M.
Powiązania:
https://bibliotekanauki.pl/articles/142651.pdf
Data publikacji:
2013
Wydawca:
Stowarzyszenie Inżynierów i Techników Przemysłu Chemicznego. Zakład Wydawniczy CHEMPRESS-SITPChem
Tematy:
tiosemikarbazony
kompleksy rutenu
albumina
pomiary fluorescencyjne
stała Sterna-Volmera
terapia przeciwnowotworowa
thiosemicarbazones
ruthenium complexes
albumin
fluorescence measurements
Stern-Volmer's constant
antitumor therapy
Opis:
Z literatury wiadomo, że niektóre tiosemikarbazony wykazują działanie antynowotworowe jako inhibitory reduktazy rybonukleotydowej, a ich koordynacja do jonów Ru może prowadzić do wzmocnienia tej reaktywności. W artykule przedstawiono syntezę tiosemikarbazonu N,N-p-dimetyloaminobenzaldehydu oraz jego kompleksu z Ru(II). Zbadano oddziaływanie otrzymanych związków z albuminą przy użyciu metod spektrofluorymetrycznych. Wykazano, że po związaniu w kompleks ligand jest mniej reaktywny w stosunku do albuminy, co rokuje nadzieje na jego lepszą biodystrybucję.
Previous studies have shown that some thiosemicarbazones have antitumor activity as inhibitors of ribonucleotide reductase and their reactivity can be enhanced by coordination to Ru ion. The following paper describes the synthesis of N,N-p-dimethylaminbenzaldehyde thiosemicarbazone and its Ru(II) complex. In addition, the interaction of the obtained compounds with albumin was carried out using fluorescence spectroscopy. It has been shown that coordination of ligand to ruthenium decrease its reactivity towards albumin and therefore the better bioavailability is expected.
Źródło:
Chemik; 2013, 67, 2; 91-98
0009-2886
Pojawia się w:
Chemik
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Acaconin, a chitinase-like antifungal protein with cytotoxic and anti-HIV-1 reverse transcriptase activities from Acacia confusa seeds
Autorzy:
Lam, Sze
Ng, Tzi
Powiązania:
https://bibliotekanauki.pl/articles/1040370.pdf
Data publikacji:
2010
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
anti-HIV-1 reverse transcriptase
Acacia confusa
antifungal protein
antitumor
Opis:
From the seeds of Acacia confusa, a chitinase-like antifungal protein designated as acaconin that demonstrated antifungal activity toward Rhizoctonia solani with an IC50 of 30±4 µM was isolated. Acaconin demonstrated an N-terminal sequence with pronounced similarity to chitinases and a molecular mass of 32 kDa. It was isolated by chromatography on Q-Sepharose, SP-Sepharose and Superdex 75 and was not bound by either ion exchanger. Acaconin was devoid of chitinase activity. The antifungal activity against Rhizoctonia solani was completely preserved from pH 4 to 10 and from 0°C to 70°C. Congo Red staining at the tips of R. solani hyphae indicated inhibition of fungal growth. However, there was no antifungal activity toward Mycosphaerella arachidicola, Fusarium oxysporum, Helminthosporium maydis, and Valsa mali. Acaconin inhibited proliferation of breast cancer MCF-7 cells with an IC50 of 128±9 µM but did not affect hepatoma HepG2 cells. Its IC50 value toward HIV-1 reverse transcriptase was 10±2.3 µM. The unique features of acaconin include relatively high stability when exposed to changes in ambient pH and temperature, specific antifungal and antitumor actions, potent HIV-reverse transcriptase inhibitory activity, and lack of binding by strongly cationic and anionic exchangers.
Źródło:
Acta Biochimica Polonica; 2010, 57, 3; 299-304
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Metabolic transformations of antitumor imidazoacridinone, C-1311, with microsomal fractions of rat and human liver
Autorzy:
Wiśniewska, Anita
Chrapkowska, Agnieszka
Kot-Wasik, Agata
Konopa, Jerzy
Mazerska, Zofia
Powiązania:
https://bibliotekanauki.pl/articles/1040879.pdf
Data publikacji:
2007
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
antitumor drug
imidazoacridinone
C-1311
P450 isoenzymes
microsomes
Symadex
in vitro metabolism
Opis:
The imidazoacridinone derivative C-1311 is an antitumor agent in Phase II clinical trials. The molecular mechanism of enzymatic oxidation of this compound in a peroxidase model system was reported earlier. The present studies were performed to elucidate the role of rat and human liver enzymes in metabolic transformations of this drug. C-1311 was incubated with different fractions of liver cells and the reaction mixtures were analyzed by RP-HPLC. We showed that the drug was more sensitive to metabolism with microsomes than with cytosol or S9 fraction of rat liver cells. Incubation of C-1311 with microsomes revealed the presence of four metabolites. Their structures were identified as dealkylation product, M0, as well as a dimer-like molecule, M1. Furthermore, we speculate that the hydroxyl group was most likely substituted in metabolite M3. It is of note that a higher rate of transformation was observed for rat than for human microsomes. However, the differences in metabolite amounts were specific for each metabolite. The reactivity of C-1311 with rat microsomes overexpressing P450 isoenzymes, of CYP3A and CYP4A families was higher than that with CYP1A and CYP2B. Moreover, the M1 metabolite was selectively formed with CYP3A, whereas M3 with CYP4A. In conclusion, this study revealed that C-1311 varied in susceptibility to metabolic transformation in rat and human cells and showed selectivity in the metabolism with P450 isoenzymes. The obtained results could be useful for preparing the schedule of individual directed therapy with C-1311 in future patients.
Źródło:
Acta Biochimica Polonica; 2007, 54, 4; 831-838
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Strategies for overcoming ABC-transporters-mediated multidrug resistance (MDR) of tumor cells
Autorzy:
Borowski, Edward
Bontemps-Gracz, Maria
Piwkowska, Agnieszka
Powiązania:
https://bibliotekanauki.pl/articles/1041364.pdf
Data publikacji:
2005
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
antitumor cytostatics
antimetabolites
multidrug resistance
modulators
Opis:
The development of multidrug resistance (MDR) of tumors is a major cause of failure in antitumor chemotherapy. This type of crossresistance is due to the expression of ABC transporter glycoproteins actively effluxing the drug from the cells against the concentration gradient at the expense of metabolic energy, thus preventing the accumulation in cells of therapeutic concentration of active agents. In this review strategies for overcoming this adverse phenomenon are discussed. They comprise the control of expression of MDR glycoprotein transporters and control of the functioning of the expressed transporter proteins. The latter approach is discussed in more detail, comprising the following general strategies: (i) development of compounds that are not substrates of efflux pump(s), (ii) use of agents that inactivate (inhibit) MDR proteins, (iii) design of cytostatics characterized by fast cellular uptake, surpassing their mediated efflux, (iv) use of compounds competing with the drug for the MDR protein-mediated efflux. Positive and negative aspects of these strategies are analysed, with special attention put on strategy based on the use of MDR modulators in combination therapy, allowing the restoration of cytotoxic activity of clinical cytostatics towards resistant tumor cells.
Źródło:
Acta Biochimica Polonica; 2005, 52, 3; 609-627
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Similarity between enzymatic and electrochemical oxidation of 2-hydroxyacridinone, the reference compound of antitumor imidazoacridinones.
Autorzy:
Mazerska, Zofia
Powiązania:
https://bibliotekanauki.pl/articles/1043630.pdf
Data publikacji:
2003
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
peroxidase-mediated oxidation
antitumor acridinones
enzymatic activation
enzymatic and electrochemical transformations
Opis:
The present work is part of a wide research project aimed to elucidate the mechanism of the metabolic activation of the antitumor imidazoacridinone agent C-1311 selected for clinical trials. The objectives of the investigations presented here were: (i) to examine the enzymatic transformation of the reference compound 2-hydroxyacridinone and (ii) to test the similarity between enzymatic and electrochemical oxidation of acridinone compounds. This similarity was searched with respect to the usefulness of the electrochemical results for further studies on the metabolic oxidation of imidazoacridinone antitumor drugs. The enzymatic oxidation of 2-hydroxyacridinone was performed with a model system containing various amounts of horseradish peroxidase and hydrogen peroxide and was followed by UV-VIS spectroscopy and by HPLC. One product of the reaction was isolated and its chemical structure was identified. It was shown that 2-hydroxyacridinone was transformed by the studied system in a manner dependent on the amount of the enzyme and on the compound/H2O2 ratio. While under mild reaction conditions the transformation ran slowly to yield only one product, p1, independently of the reaction time, higher enzyme concentration resulted in several steps of transformation. Product p1 turned out to be a dimer: 1,1-bi(2-hydroxyacridinone). A comparison of the results of the enzymatic transformations of 2-hydroxyacridinone presented here with studies on the electrochemical oxidation reported earlier allowed us to show both transformations to be similar as far as the reaction pathway and two reaction products are concerned.
Źródło:
Acta Biochimica Polonica; 2003, 50, 2; 515-525
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
The ability to overcome multidrug resistance of tumor cell lines by novel acridine cytostatics with condensed heterocyclic rings.
Autorzy:
Bontemps-Gracz, Maria
Kupiec, Agnieszka
Antonini, Ippolito
Borowski, Edward
Powiązania:
https://bibliotekanauki.pl/articles/1043812.pdf
Data publikacji:
2002
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
acridine cytostatics
cytotoxic activity
multidrug resistance
antitumor compounds
Opis:
Two recently synthesized groups of acridine cytostatics containing fused heterocyclic ring(s): pyrazoloacridines (PAC) and pyrazolopyrimidoacridines (PPAC) were tested in regard to their in vitro cytotoxic activity towards a panel of sensitive and resistant human tumor cell lines. The obtained results corroborate our earlier hypothesis on the essential role of heterocyclic ring fused to the acridine moiety in the ability of acridine cytostatics to overcome multidrug resistance of tumor cells. The presence, location and kind of substituents considerably influenced both the cytotoxic activity of the derivatives and their ability to overcome multidrug resistance. The same factors also affected the cytostatics ability to differentiate between tumor cell lines with various types of drug exporting pumps.
Źródło:
Acta Biochimica Polonica; 2002, 49, 1; 87-92
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
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