Aminopterin-human serum albumin conjugate (AP-HSA): uptake and cytotoxic effects in tumor cell lines

2002 ◽  
Vol 40 (12) ◽  
pp. 564-566 ◽  
Author(s):  
N. Eschen ◽  
U. Bauder-Wüst ◽  
E. Frei ◽  
H.-H. Schrenk ◽  
H. Sinn ◽  
...  
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Tumor Cell ◽  
Human Serum ◽  
Cell Lines ◽  
Tumor Cell Lines ◽  
Cytotoxic Effects

scholarly journals Heat Shock Protein Inhibitor 17-Allyamino-17-Demethoxygeldanamycin, a Potent Inductor of Apoptosis in Human Glioma Tumor Cell Lines, Is a Weak Substrate for ABCB1 and ABCG2 Transporters

2021 ◽  
Vol 14 (2) ◽  
pp. 107
Author(s):  
Nikola Pastvova ◽  
Petr Dolezel ◽  
Petr Mlejnek
Keyword(s):  
Heat Shock ◽  
Heat Shock Protein ◽  
Tumor Cell ◽  
Cell Lines ◽  
Single Agent ◽  
Heat Shock Protein 90 ◽  
Genetic Alterations ◽  
Tumor Cell Lines ◽  
Cytotoxic Effects ◽  
Glioma Tumor

Glioblastoma multiforme (GBM) is the most common primary brain tumor in adults and has a poor prognosis. Complex genetic alterations and the protective effect of the blood–brain barrier (BBB) have so far hampered effective treatment. Here, we investigated the cytotoxic effects of heat shock protein 90 (HSP90) inhibitors, geldanamycin (GDN) and 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin), in a panel of glioma tumor cell lines with various genetic alterations. We also assessed the ability of the main drug transporters, ABCB1 and ABCG2, to efflux GDN and 17-AAG. We found that GDN and 17-AAG induced extensive cell death with the morphological and biochemical hallmarks of apoptosis in all studied glioma cell lines at sub-micro-molar and nanomolar concentrations. Moderate efflux efficacy of GDN and 17-AAG mediated by ABCB1 was observed. There was an insignificant and low efflux efficacy of GDN and 17-AAG mediated by ABCG2. Conclusion: GDN and 17-AAG, in particular, exhibited strong proapoptotic effects in glioma tumor cell lines irrespective of genetic alterations. GDN and 17-AAG appeared to be weak substrates of ABCB1 and ABCG2. Therefore, the BBB would compromise their cytotoxic effects only partially. We hypothesize that GBM patients may benefit from 17-AAG either as a single agent or in combination with other drugs.

scholarly journals Interaction of Arylidenechromanone/Flavanone Derivatives with Biological Macromolecules Studied as Human Serum Albumin Binding, Cytotoxic Effect, Biocompatibility Towards Red Blood Cells

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3172 ◽  
Author(s):  
Angelika A. Adamus-Grabicka ◽  
Magdalena Markowicz-Piasecka ◽  
Michał B. Ponczek ◽  
Joachim Kusz ◽  
Magdalena Małecka ◽  
...  
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Red Blood Cells ◽  
Human Serum ◽  
Cell Line ◽  
Cell Lines ◽  
Blood Cells ◽  
Cytotoxic Effect ◽  
Human Leukemia ◽  
Ic50 Values

The aim of this study was to determine the cytotoxic effect of 3-arylidenechromanone (1) and 3arylideneflavanone (2) on HL-60 and NALM-6 cell lines (two human leukemia cell lines) and a WM-115 melanoma cell line. Both compounds exhibited high cytotoxic activity with higher cytotoxicity exerted by compound 2, for which IC50 values below 10 µM were found for each cell line. For compound 1, the IC50 values were higher than 10 µM for HL-60 and WM-115 cell lines, but IC50 < 10 µM was found for the NALM-6 cell line. Both compounds, at the concentrations close to IC50 (concentration range: 5–24 µM/L for compound 1 and 6–10 µM/L for compound 2), are not toxic towards red blood cells. The synthesized compounds were characterized using spectroscopic methods 1H- and 13C-NMR, IR, MS, elemental analysis, and X-ray diffraction. The lipophilicity of both synthesized compounds was determined using an RP-TLC method and the logP values found were compared with the theoretical ones taken from the Molinspiration Cheminformatics (miLogP) software package. The mode of binding of both compounds to human serum albumin was assessed using molecular docking methods.

Human serum albumin capsulated hydrophobic carbon nanodots as staining agent on HeLa tumor cell

2020 ◽  
Vol 239 ◽  
pp. 122266
Author(s):  
Mochamad Zakki Fahmi ◽  
Denika Liyan Nor Wibowo ◽  
Satya Candra Wibawa Sakti ◽  
Hwei Voon Lee ◽  
Isnaeni
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Tumor Cell ◽  
Human Serum ◽  
Carbon Nanodots

Cytotoxic Effects of 24/R,25-Dihydroxycholecalciferol on the Proliferation of Various Tumor Cell Lines in vitro and Its Antitumor Effects in vivo

Oncology ◽  
1988 ◽  
Vol 45 (3) ◽  
pp. 206-209 ◽  
Author(s):  
Yuji Maeda ◽  
Tohru Hirai ◽  
Hideyuki Yamato ◽  
Noriko Kobori ◽  
Ken-ichi Matsunaga ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Tumor Cell Lines ◽  
Antitumor Effects ◽  
Cytotoxic Effects

Efficacy markers for cisplatin and S-1 in biliary tract carcinoma.

2015 ◽  
Vol 33 (3_suppl) ◽  
pp. 334-334
Author(s):  
Yasunari Sakamoto ◽  
Hidenori Ojima ◽  
Chigusa Morizane ◽  
Seri Yamagishi ◽  
Hiroko Hosoi ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Biliary Tract ◽  
Mtt Assay ◽  
Biliary Tract Carcinoma ◽  
Tumor Cell Lines ◽  
Cytotoxic Effects ◽  
First Choice ◽  
Ercc1 Expression ◽  
Mtt Assays

334 Background: Gemcitabine (GEM) + cisplatin (CDDP) combination chemotherapy is the first choice for advanced biliary tract carcinoma (BTC). In Japan, the GEM + S-1 therapy has shown promise for the treatment of BTC. Our aim was to investigate the cytotoxic effects of GEM, CDDP and S-1 on BTC cell lines and find an immunohistochemical marker for predicting the efficacy of chemotherapy. Methods: We evaluated the efficacy of GEM, CDDP, and S-1 by means of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay of 17 BTC cell lines. Furthermore, we subdivided the cell lines into sensitive and insensitive groups on the basis of the sensitivity of each drug. Moreover, pairwise studies were conducted using the MTT assay, Bliss additivism model, and Combination Index for analysis. Immunohistochemical expression analysis of excision repair cross-complementation group 1 (ERCC1), thymidylate synthase (TS), dihydropyrimidine dehydrogenase (DPD), orotate phosphoribosyltransferase (OPRT), and thymidine phosphorylase (TP) were also performed in each cell line to compare the results of the cytotoxic effects of CDDP and S-1. Results: In the single-agent MTT assays, among the 17 tumor cell lines, 11 were sensitive to GEM, 13 to CDDP, and 11 to S-1. In 5 cell lines, <30% of the cells showed ERCC1 expression; these lines belonged to the CDDP-sensitive group. Conversely, the cell lines with >30% ERCC1-positive cells mostly belonged to the CDDP-insensitive group. CDDP IC50 correlated with the percentage of ERCC1-positive cells (P <.05). In contrast, none of the immunohistochemical markers could be used to select a cutoff level that would point to the sensitivity to S-1. In pairwise MTT assays (combination therapy), we demonstrated the synergy of GEM with CDDP in 9 tumor cell lines (53%) and the synergy of GEM with S-1 in 4 tumor cell lines(24%). Although 3 cell lines with the synergy of GEM with CDDP showed <30% ERCC1-positive cells, there was no correlation between them. Conclusions: ERCC1 expression in <30% of cells may help to identify CDDP-sensitive tumors; however, it is unknown whether expression of ERCC1 can help to predict efficacy of treatment with GEM + CDDP.

Cytotoxic effects of pyocin S2 produced by Pseudomonas aeruginosa on the growth of three human cell lines

2004 ◽  
Vol 50 (5) ◽  
pp. 375-381 ◽  
Author(s):  
A Abdi-Ali ◽  
E A Worobec ◽  
A Deezagi ◽  
F Malekzadeh
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Tumor Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Human Cell ◽  
Human Tumor ◽  
Exchange Chromatography ◽  
Tumor Cell Lines ◽  
Inhibitory Effects ◽  
Cytotoxic Effects

Pyocin typing of 82 Pseudomonas aeruginosa strains, collected from different Iranian clinical sources, revealed that one isolate, P. aeruginosa 42A, produced pyocin S2, a protease-sensitive bacteriocin. Pyocin S2 production was induced by mitomycin C (2 µg/mL) in the pyocin S2 producer P. aeruginosa 42A. Pyocin S2 was purified using ion exchange chromatography with CM-Sepharose CL-6B and sodium phosphate buffer (pH 8) from an 80% ammonium sulfate precipitate of whole-cell lysates. Pyocin activity of the fractions was detected using the Govan spot testing method. The purity of the active fraction was confirmed by SDS–PAGE, where a single band with a molecular mass of 74 kDa was detected. Cytotoxic effects of purified pyocin S2 and partially purified pyocin from P. aeruginosa 42A on the human tumor cell lines HepG2 and Im9 and the normal human cell line HFFF (Human Foetal Foreskin Fibroblast) were studied by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The results demonstrated that partially purified pyocin and pyocin S2 exhibited substantial inhibitory effects on the growth of the tumor cell lines HepG2 and Im9, while no inhibitory effects were observed on the normal cell line HFFF. Pure lipopolysaccharide was used as a control and was found to have no inhibitory effect on any of the cell lines tested.Key words: Pseudomonas aeruginosa, pyocin, cytotoxicity, MTT assay.

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