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    Tytuł:
    Design, synthesis and biological evaluation of some novel substituted quinazoline derivatives as antitumor agents.
    Autorzy:
    Ahmed, Marwa
    Magdy, Naja
    Powiązania:
    https://bibliotekanauki.pl/articles/895417.pdf
    Data publikacji:
    2018-06-30
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    cytotoxicity
    quinazoline
    Tyrosine kinases
    Opis:
    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.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 3
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    CYTOTOXIC ACTIVITY OF VARTHEMIA IPHIONOIDES ESSENTIAL OIL AGAINST VARIOUS HUMAN CANCER CELL LINES
    Autorzy:
    Abbas, Manal M.
    Abbas, Manal A.
    Kandil, Yasser I.
    Powiązania:
    https://bibliotekanauki.pl/articles/895451.pdf
    Data publikacji:
    2019-08-30
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    apoptosis
    cytotoxicity
    anticancer
    varthemia iphionoides
    Opis:
    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.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 4; 701-706
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY EVALUATION OF NEW QUINAZOLINE DERIVATIVES LINKED TO THIAZOLIDINONE, AZETIDINONE OR OXADIAZOL MOIETIES
    Autorzy:
    Ahmed, Marwa
    Magdy, Naja
    Powiązania:
    https://bibliotekanauki.pl/articles/895415.pdf
    Data publikacji:
    2018-12-31
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    cytotoxicity
    MCF-7
    quinazoline
    CASP3
    Opis:
    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.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 6; 1321-1328
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    SYNTHESIS, AND EVALUATION OF COUMARIN HYBRIDS AS ANTIMYCOBACTERIAL AGENTS
    Autorzy:
    Hassan, Mohd Z.
    ALSAYARI, ABDULRHMAN
    OSMAN, HASNAH
    ALI, MOHAMED A.
    MUHSINAH, ABDULLATIF B.
    AHSAN, MOHAMED J.
    Powiązania:
    https://bibliotekanauki.pl/articles/895509.pdf
    Data publikacji:
    2019-12-29
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    cytotoxicity
    Coumarin
    TB
    Thiazolopyrimidine
    HTS
    antimycobacterial
    Opis:
    A series of twelve hybrid coumarin analogues were synthesized and screened through HTS for their antimycobacterial activity against Mtb H37Rv. The hybrid molecules were efficiently synthesized by the reactions of 3-(bromoacetyl)coumarin with Biginelli products 2-mercapto-6-oxo-4-aryl-1,6-dihydropyrimidine-5-carbonitriles. Of the resulting twelve hybrids, the two compounds 7-(2,4-dichlorophenyl)-5-oxo-3-(2-oxo-2H-chromen-3-yl)-5H-thiazolo[3,2-a] pyrimidine-6-carbonitrile (3d) and 7-(4-nitrophenyl)-5-oxo-3-(2-oxo-2H-chromen-3-yl)-5H-thiazolo[3,2-a]pyrimidine-6-carbonitrile (3f) showed excellent antimycobacterial activity against Mtb (EC50 3.19 & 7.91 µM, respectively) and low cytotoxicity against the VERO cell line (IC50 > 62.5 µg/mL).
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 6; 1029-1036
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    ANTITUMOR EFFECTS OF VANILLIN BASED CHALCONE ANALOGUES IN VITRO
    Autorzy:
    Luković, Jovan
    Mitrović, Marina
    Popović, Suzana
    Milosavljević, Zoran
    Stanojević-Pirković, Marijana
    Anđelković, Marija
    Zelen, Ivanka
    Šorak, Marija
    Muškinja, Jovana
    Ratković, Zoran
    Nikolić, Ivana
    Powiązania:
    https://bibliotekanauki.pl/articles/895579.pdf
    Data publikacji:
    2020-02-29
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    Colorectal cancer
    apoptosis
    cytotoxicity
    Autophagy
    chalcones
    Opis:
    Chalcones, as a large group of organic compounds, are widely implemented in various types of anti-cancer therapeutics. These plant metabolites are present in fruits, vegetables, spices, and have anti-tumor, anti-inflammation, immunomodulation, antibacterial and anti-oxidative activities, as well as many other pharmacological and biological effects. The aim of the present study was to investigate cytotoxic effects, type of cell death and mechanism of action of the newly synthesized vanillin based chalcone analogues, (CH1) and (CH2) on human colon cancer HCT-116 and noncancerous (control) MRC-5 cell lines. In order to compare effects of vanillin based chalcone analogues on investigated cell lines, as reference substances cisplatin (cisPt) and dehydrozingerone (DHZ) were used. Investigation of antitumor effect of chalcone analogues on HCT-116 cells was carried out by three methods MTT assay, flow cytometry and immunofluorescence analysis. The result of our investigation indicated that newly synthesized vanillin based chalcone analogues expressed powerful antitumor effect on cancer cells (HCT-116 cell line), while their effect on healthy cells (MRC-5 cell line) was not statistically significant. Vanillin based chalcone analogues caused overexpression and activation of mitochondrial Bax protein and caspase-3 in HCT-116 cells, indicating that their mechanism of antitumor action was mediated through activation of inner apoptotic pathway. These results indicate possible usefulness of CH1 and CH2 in antitumor therapy whether through its direct cytotoxic effect or as adjuvant therapy. Our results indicate possible usefulness of CH1 and CH2 vanillin based chalcone analogues in antitumor therapy.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2020, 77, 1; 57-67
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Modulation of Doxorubicin Cytotoxicity by Isoliquiritin and Cynarin Combination on Different Cancer Cell Lines
    Autorzy:
    Al-AdamI, Salat G.
    Al-Khateeb, EKBAL H.
    NUMAN, NAWFAL A.
    ABBAS, Mannal M.
    Tawfiq, FATIMA A.
    Shakya, Ashok K.
    Powiązania:
    https://bibliotekanauki.pl/articles/895633.pdf
    Data publikacji:
    2020-06-29
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    cytotoxicity
    doxorubicin
    cancer cells
    Modulation
    Cynarin
    Isoliquiritin
    Opis:
    Natural polyphenolic compounds produced by plant exhibit many pharmacological effects including antioxidant, chemopreventive as well as anticancer properties. This study was conducted to investigate the effect of cynarin ( from Artichoke, Cynara scolymus) and isoliquiritin (from Licorice, Glycyrrhiza uralensis) on doxorubicin (positive control) cytotoxicity in different cell lines including normal (Fibroblasts MCR-5 and Myoblasts H9c2) and cancer (colorectal HCT-116 and hepatocellular HEP-G2) cell lines. The cytotoxic effect of doxorubicin, isoliquiritin and cynarin alone or in different combination was studied on cancer cell lines as well as normal cell lines. The results obtained indicated that both cynarin and isoliquiritin enhance the cytotoxicity of doxorubicin. Both cynarin and isoliquiritin also reduce the cardiotoxicity of doxorubicin on normal cardiac cell lines. The combination of the three compounds (cynarin, isoliquiritin and doxorubicin) result in decrease the cytotoxicity of doxorubicin, which may indicate the presence of interaction and/or antagonism effect between cynarin and isoliquiritin. Cynarin was found to enhance the growth of (HCT-116 and HEP-G2) this might suggest avoiding use of Artichoke in subjects’ susceptibility for these cancers. All results were evaluated using statistical path and showed significant findings. The mechanism of enhanced doxorubicin’s cytotoxicity by cynarin or isoliquiritin also require further investigation to explain the increasing and/or the decreasing effect of these polyphenolic compounds on cytotoxicity of doxorubicin. The current finding can help to start with safe minimum dose of two or three combination of compounds in the context of clinical trials and practice.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2020, 77, 3; 475-484
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    ANTI-INFLAMMATORY ACTIVITY AND CYTOTOXICITY OF DIOSGENIN ON LIPOPOLYSACCHARIDES INDUCED RAW 264.7 CELLS
    Autorzy:
    ning, jing
    chang, yu
    wang, ruxia
    lan, zhiwei
    ru, qing
    liu, mingchun
    tian, chunlian
    Powiązania:
    https://bibliotekanauki.pl/articles/895615.pdf
    Data publikacji:
    2020-04-29
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    Diosgenin
    Anti-inflammatory
    lipopolysaccharides
    cytotoxicity
    phagocytosis ability  
    Opis:
    Diosgenin is a steroidal sapogenin compound, and possesses multiple biological activities including anti-inflammatory, anticancer, immunological regulation, and anti-aging. The current study focused on its anti-inflammatory activities and cytotoxicity by analysis of NO production, phagocytosis activity, secretion of TNF-α and IL-6 and cell viability in LPS-induced RAW 264.7 cells. An IC50 value of diosgenin of 2.8 μM was calculated for diosgenin by regression of cell viability from concentrations ranging from 0.01 to 25 μM; this indicated that 0.01, 0.02, 0.04 μM diosgenin could reduce phagocytic activity very significantly (p<0.01) in a dose-dependent manner with no cytotoxic effect on the LPS-induced RAW 264.7 cells. However, there was no significant effect on NO content and secretion of TNF-α and IL-6 after diosgenin treatment. The research revealed that low concentrations diosgenin can directly inhibit cells phagocytosis, with no effect on the release of inflammatory mediators and cytokines. This lays a foundation for screening for a safe dose in research and developent of derivatives and new formulation of diosgenin for its anti-inflammatory effect.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2020, 77, 2; 313-317
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    PREPARATION AND CHARACTERIZATION OF SELF-MICROEMUSIFYING DRUG DELIVERY SYSTEM (SMEDDS) OF CISPLATIN FOR ORAL USE IN OVARIAN CANCER TREATMENT
    Autorzy:
    Akartas, Irfan
    Karasulu, Hatice Yeşim
    Powiązania:
    https://bibliotekanauki.pl/articles/895344.pdf
    Data publikacji:
    2020-02-29
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    cytotoxicity
    ovarian cancer
    cisplatin
    SMEDDS
    in vitro release
    Opis:
    Cisplatin is an antineoplastic drug, used for the treatment of ovarian cancer. SMEDDS has many advantages such as enhanced bioavailability, lymphatic targeting and ease of manufacture. The main objective of this study was to prepare and characterize Cisplatin loaded SMEDDS formulation and to evaluate antitumoral activity with cell viability studies. Cisplatin SMEDDS formulation was prepared and characterized physicochemically. In vitro release studies and cell viability studies were performed and evaluated. The mean droplet size of Cisplatin SMEDDS was measured as 25,4±1,9 nm and PDI was 0,241±0,018. Refractive index of the formulation was measured as 1,471±0,001. pH values of Cisplatin SMEDDS (dilution ratio 1:10 w) were measured as 5,84±0,09 and (dilution ratio 1:10 pH 6,8 PBS) 6,51±0,14. Viscosity of formulation was measured as 284 mPa. According to in vitro release studies, %78,17 of Cisplatin were released from Cisplatin SMEDDS. The formulation performed cytotoxic effect to A2780 cells; vitality was found 20,26% at 0,02 µg/mL. It was concluded that, Cisplatin SMEDDS could be beneficial for the treatment of ovarian cancer and it could be promising alternative due to its enhanced bioavailability.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2020, 77, 1; 183-193
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis and anticancer activity evaluation of some new derivatives of 2-(4-benzoyl-1-piperazinyl)-quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline.
    Autorzy:
    Kubica, Krzysztof P.
    Taciak, Przemyslaw P.
    Czajkowska, Agnieszka
    Sztokfisz-Ignasiak, Alicja
    Wyrebiak, Rafal
    Podsadni, Piotr
    Mlynarczuk-Bialy, Izabela
    Malejczyk, Jacek
    Mazurek, Aleksander P.
    Powiązania:
    https://bibliotekanauki.pl/articles/895388.pdf
    Data publikacji:
    2018-08-31
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    anticancer activity
    cytotoxicity assay
    2-quinoline
    cell migration assay
    Opis:
    In this study we designed and synthesized twenty new derivatives of 2-(4-benzoyl-1-piperazinyl)-quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline with potential anticancer activity. The structures of synthesized compounds were confirmed by 1H and 13C NMR spectroscopy and MS spectrometry. The activity of novel compounds was evaluated in the cell viability assay as well as in the wound healing assay. Presented data show that examined substances have anticancer activity in cell culture. Seven compounds which showed a high rate of cell growth inhibition were selected for further studies. Three of them strongly reduced growth of B16F10 cells. The novel compounds constitute a good base for further studies and optimization of structure for new therapeutically effective anti-cancerous drugs.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 4; 891-901
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis and anticancer activity evaluation of novel derivatives of 7-amino-4-methylquinolin-2(1H)-one
    Autorzy:
    Kubica, Krzysztof P.
    Taciak, Przemyslaw P.
    Czajkowska, Agnieszka
    Sztokfisz-Ignasiak, Alicja
    Wyrebiak, Rafal
    Mlynarczuk-Bialy, Izabela
    Malejczyk, Jacek
    Mazurek, Aleksander P.
    Powiązania:
    https://bibliotekanauki.pl/articles/895717.pdf
    Data publikacji:
    2018-08-31
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    anticancer activity
    cytotoxicity assay
    cell migration assay
    quinolin-2(1H)-one
    Opis:
    In this study we designed and synthesized sixteen new derivatives of 7-amino-4-methylquinolin-2(1H)-one with potential anticancer activity. The structures of synthesized compounds were confirmed by 1H and 13C NMR. The activity of novel substances was evaluated by cell viability assay and wound healing assay. In vitro tests for series of sixteen novel compounds were performed. The results showed that examined compounds are selective for cancer cells, but their activity for various types of cancer is different. Three of new compounds presented ability to inhibit cells migration. The novel compounds constitute a good starting point for further studies and optimization of structure for new therapeutically effective anti-cancerous drugs. Seven compounds, which showed the highest rate of cell inhibition, were selected for further studies.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 4; 903-910
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-10 z 10

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