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1

The influence of acupuncture TENS currents on the proliferation of cancer cells tested in vitro

100%

Pełczyńska M., Milczarek M., Maciejewska M., Wietrzyk J.

Medical Rehabilitation

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2019

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vol. 23(4)

42-46

PL

Wstęp: Przezskórna elektrostymulacja nerwów (TENS) jest szeroko stosowaną niefarmakologiczną metodą leczenia przeciwbólowego. Jednak wiedza na temat wpływu tej metody na proces nowotworowy jest fragmentaryczna. Dlatego też zastosowanie jej w leczeniu pacjentów po przebytej chorobie nowotworowej jest bardzo ograniczone. Niestety, w literaturze nie ma wielu wyników badań odnoszących się bezpośrednio do takich metod. Tym bardziej, że znacznie trudniej jest wykluczyć pronowotworową aktywność tych metod, niż ją potwierdzić. Cel pracy: Celem badań było sprawdzenie hipotezy o pobudzającym wpływie prądu TENS na proliferację komórek nowotworowych w warunkach in vitro. Materiał i metody: Badania przeprowadzono w oparciu o 96 godzinny test SRB proliferacji in vitro dla komórek linii nowotworowych: A549 (rak płuc); ES-2 (rak jajnika); HT29 (rak jelita grubego); MCF-7 (rak piersi). Komórki zostały poddane działaniu prądu TENS akupunkturowego o parametrach: 0,1 mA, 1 mA i 10 mA na dołek, czas impulsu 200μs, symetryczny, częstotliwość 2 Hz, stała, czas ekspozycji 20 min, w pojedynczej dawce po 24 godzinach lub w serii trzech ekspozycji po 24, 48 i 72 godzinach od początku eksperymentu. Wyniki: W wyniku przeprowadzonych badań uzyskano niewielkie zmiany proliferacji w badanych komórkach. Żadna ze zmian nie była statystycznie istotna, w szczególności nie obserwowano istotnego statystycznie przyspieszenia proliferacji. Wnioski: Ani pojedyncza ekspozycja na prąd TENS akupunkturowy, ani seria trzykrotnej ekspozycji nie powoduje istotnego przyspieszenia proliferacji komórek nowotworowych.

EN

Introduction: Transcutaneous Electrical Nerve Stimulation (TENS) is a very popular, non-pharmacological antianalgetic method. Nonetheless, knowledge on using this method is very limited in the treatment of patients with cancer anamnesis. Unfortunately, there are not many results of research referring to the application of this method. It is much more difficult to exclude the possibility of proneoplastic activity regarding these methods than to confirm this action. Aim: The aim of the study was to evaluate the influence of TENS currents on the proliferation of cancer cells tested in vitro. Materials and methods: The following human cell lines were used - A549, ES-2, HT29, MCF-7. The cells were plated 24 h before treatment. Then, the cells were exposed to AL-TENS currents (0.1 mA, 1.0 mA and 10 mA), t imp. 200μs; f 2 Hz, constant; duration: 20 min. The in vitro cytotoxic effects were examined after 96 h in SRB assay. In the other experiment, there were three expositions – 24, 48 and 72 hours from the beginning of the experiment. Results: In this assay, the acceleration of cancer cell proliferation after single or triple-dose expositions to AL-TENS currents was not observed. Conclusions: The AL-TENS current after repeated doses did not accelerate proliferation of cancer cells in in vitro conditions.

2

Isophosphoramide mustard analogues as prodrugs for anti-cancer gene-directed enzyme-prodrug therapy (GDEPT).

88%

Misiura K., Szymanowicz D., Kuśnierczyk H., Wietrzyk J., Opolski A.

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2002

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vol. 49

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issue 1

169-176

EN

Two types of prodrugs, benzyl analogues of isophosphoramide mustard (iPAM), activated by cytochrome P450, and acylthioethyl analogues, activated by esterases, were designed. In contrast to iPAM that hydrolyse rapidly, the examined compounds are stable in phosphate-buffered saline and Tris buffer. Benzyl analogues of iPAM are poor substrates for cytochrome P450, are not cytotoxic and posses no antitumour activity. Acylthioethyl analogues of iPAM are good substrates for pig liver esterase, are cytotoxic and exert antitumour activity against L1210 leukaemia in mice. The observed correlation for iPAM analogues between their susceptibility to hydrolysis and cytotoxicity and antitumour activity suggests possible application of these compounds as the prodrugs in gene-directed enzyme-prodrug therapy.

3

Design, Efficient Synthesis, Mechanism of Reaction and Antiproliferative Activity Against Cancer And Normal Cell Lines of A Novel Class of Fused Pyrimidine Derivatives

76%

roaiah h. F., Rashdan H. R., soliman a., Muhammed Z., Wietrzyk J., Milczarek M.

Acta Poloniae Pharmaceutica - Drug Research

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2018

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vol. 75

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issue 3

EN

This work concentrated on the utility of hydrazonoyl halides in synthesis of bioactive heterocycles like triazoles, pyrazoles, pyrimidines and their fused derivatives which have a wide spectrum of pharmaceutical value. Herein we discussed the synthesis of new heterocyclic compounds containing fused pyrimidine rings derived from hydrazonoyl halides and their significant pharmaceutical importance as anticancer agents. New fused pyrimidine derivatives bearing 1,2,3-triazole moiety were prepared via reaction of enaminone 2 with and 6-amino-2-thioxo-pyrimidin-4-one and then with hydrazonoyl chlorides 6a-h. In addition 3-amino-6-(2-oxo-2H-chromen-3-yl)pyridine-2-carbonitrile (12) was submitted to react with carbon dioxide to afford 3-(1,2,3,4-tetrahydro-2,4-dithioxopyrido[2,3-d]pyrimidin-7-yl)-2H-chromen-2-one (15), which act as key molecule for synthesis of new series of fused prymidinethione derivatives containing coumarine moiety via its reaction with different selected derivatives of hydrazonoyl halides 6a-h. Structures of the newly synthesized compounds were confirmed using spectral data (IR, H1NMR and Mass spectrometry) and microanalytical methods. Also, they screened for their anticancer activity.

4

DESIGN, SYNTHESIS AND ANALYSIS OF ANTICANCER ACTIVITY OF NEW SAR-BASED S16020 DERIVATIVES

76%

Tylińska B., Jasztold-Howorko R., Kowalczewska K., Szczaurska-Nowak K., Gębarowski T., Wietrzyk J.

Acta Poloniae Pharmaceutica - Drug Research

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2018

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vol. 75

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issue 6

1313-1320

EN

A novel set of S16020 derivatives was designed applying structure activity relationships (SAR). The newly synthesized compounds were subjected to in vitro cytostatic activity screening against human kidney cancer (cell line A498), human lung cancer (cell line A549) and normal human dermal fibroblasts (cell line NHDF). Two 6H-pyrido[4,3-b]carbazole derivatives exhibited stronger potency against both investigated cell lines than the reference compounds ellipticine and doxorubicin.

5

Synthesis and antiproliferative activity in vitro of new 2-aminobenzimidazole derivatives. Reaction of 2-arylideneaminobenzimidazole with selected nitriles containing active methylene group

76%

Nowicka A., Liszkiewicz H., Nawrocka W., Wietrzyk J., Kempińska K., Dryś A.

Open Chemistry

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2014

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vol. 12

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issue 10

1047-1055

EN

A series of pyrimido[1,2-a]benzimidazole and α-cyanocinnamic acid derivatives have been synthesized in the reactions of Schiff bases 2–7 with selected nitriles containing an active methylene group: malononitrile 8–12, cyanoacetamide 13–16, benzyl cyanide 17–21, benzoylacetonitrile 22–24, cyanoacetate methyl ester 25–28 and benzylacetamide 29. The structures 8–29 were confirmed by the results of elementary analysis and their IR, 1H-, 13C-NMR and MS spectra. The products 8–29 of various chemical structure pyrimido[1,2-a] benzimidazole 8–12, 14–16, 17–21, 23–24, 26 and α-cyanocinnamic acid derivatives 13, 22, 25, 27, 28 were obtained, which are of interest for biological studies or which can be substrates for further synthesis. The selected compounds 10, 13, 14, 17, 19, 21, 23–25 and 28 were screened for their antiproliferative activity in vitro against neoplastic and normal cell lines. The most active two compounds were: 2-(o-bromophenylene)-3-cyano-4-phenyl-1,2-dihydropyrimido[1,2-a]benzimidazole (24) and 3-cyano-4-phenyl-2-(2,4-dimethoxyphenyl)-1,2-dihydropyrimido[1,2-a]benzimidazole (23). However, similarly like cisplatin used as the control, they showed no selectivity towards cancer cells, by inhibiting proliferation of normal mouse fibroblasts in similar manner.

6

Synthesis and biological evaluation of 4'-O-acetyl-isoxanthohumol and its analogues as antioxidant and antiproliferative agents

76%

Stompor M., Świtalska M., Podgórski R., Uram Ł., Aebisher D., Wietrzyk J.

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2017

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vol. 64

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issue 3

577-583

EN

Isoxanthohumol (2) and its 4'-O-monoacylated (3) and 7,4'-O-diacetylated (4) derivatives were synthesized and evaluated in vitro for their cytotoxic activity against several cancer cell lines of various origins: MCF-7 (breast), A549 (lung), MESSA (uterine sarcoma), LoVo (colon), drug-resistant human cancer cells (MESSA/DX and LoVo/DX), glioblastoma (U-118 MG), and also towards the non-cancerous cell line MCF-10A (normal breast cells). An antiproliferative assay indicates that 7,4'-di-O-acylisoxanthohumol (4) has similar cytotoxicity to its precursor, isoxanthohumol (2), against selected cell lines (A549, MES-SA, MES-SA/5DX, and U-118 MG). Compound 4 was only slightly more cytotoxic to lung, colon, breast (cancerous and normal) and uterine sarcoma (drug sensitive and drug resistant) cell lines compared to its monoacylated derivative (3). Both acylated isoxanthohumols showed preferential activity against tumor cells (MCF-7) and low cytotoxicity to normal cells (MCF-10A), which suggests selectivity of the acylated isoxanthohumols towards cancer cells. Additionally, the activity of the acylated isoxanthohumols was higher than for 2. To the best of our knowledge this is the first report on bioactivity of monoacylated isoxanthohumol (3) and its ester derivatives as antiproliferative compounds in drug resistant cell cultures. Acylation of 2 decreased the antioxidant activity determined by the DPPH method in the order isoxanthohumol (2) >4'-O-acetylisoxanthohumol (3) >7,4'-di-O-acetylisoxanthohumol (4).

Refine search results

The influence of acupuncture TENS currents on the proliferation of cancer cells tested in vitro

Isophosphoramide mustard analogues as prodrugs for anti-cancer gene-directed enzyme-prodrug therapy (GDEPT).

Design, Efficient Synthesis, Mechanism of Reaction and Antiproliferative Activity Against Cancer And Normal Cell Lines of A Novel Class of Fused Pyrimidine Derivatives

DESIGN, SYNTHESIS AND ANALYSIS OF ANTICANCER ACTIVITY OF NEW SAR-BASED S16020 DERIVATIVES

Synthesis and antiproliferative activity in vitro of new 2-aminobenzimidazole derivatives. Reaction of 2-arylideneaminobenzimidazole with selected nitriles containing active methylene group

Synthesis and biological evaluation of 4'-O-acetyl-isoxanthohumol and its analogues as antioxidant and antiproliferative agents