scholarly journals Concentration Gradient Constructions Using Inertial Microfluidics for Studying Tumor Cell–Drug Interactions

Micromachines ◽  
2020 ◽  
Vol 11 (5) ◽  
pp. 493
Author(s):  
Shaofei Shen ◽  
Fangjuan Zhang ◽  
Mengqi Gao ◽  
Yanbing Niu
Keyword(s):  
Tumor Cell ◽  
Drug Interactions ◽  
Cell Lines ◽  
Drug Concentration ◽  
Concentration Gradient ◽  
Breast Adenocarcinoma ◽  
Tumor Cell Lines ◽  
Concentration Gradients ◽  
Flow Rates ◽  
Wide Range

With the continuous development of cancer therapy, conventional animal models have exposed a series of shortcomings such as ethical issues, being time consuming and having an expensive cost. As an alternative method, microfluidic devices have shown advantages in drug screening, which can effectively shorten experimental time, reduce costs, improve efficiency, and achieve a large-scale, high-throughput and accurate analysis. However, most of these microfluidic technologies are established for narrow-range drug-concentration screening based on sensitive but limited flow rates. More simple, easy-to operate and wide-ranging concentration-gradient constructions for studying tumor cell–drug interactions in real-time have remained largely out of reach. Here, we proposed a simple and compact device that can quickly construct efficient and reliable drug-concentration gradients with a wide range of flow rates. The dynamic study of concentration-gradient formation based on successive spiral mixer regulations was investigated systematically and quantitatively. Accurate, stable, and controllable dual drug-concentration gradients were produced to evaluate simultaneously the efficacy of the anticancer drug against two tumor cell lines (human breast adenocarcinoma cells and human cervical carcinoma cells). Results showed that paclitaxel had dose-dependent effects on the two tumor cell lines under the same conditions, respectively. We expect this device to contribute to the development of microfluidic chips as a portable and economical product in terms of the potential of concentration gradient-related biochemical research.

Interaction of Human Tumor Cells with Human Platelets and the Coagulation System

1983 ◽  
Vol 50 (03) ◽  
pp. 726-730 ◽  
Author(s):  
Hamid Al-Mondhiry ◽  
Virginia McGarvey ◽  
Kim Leitzel
Keyword(s):  
Tumor Cell ◽  
Tumor Cells ◽  
Cell Lines ◽  
Human Tumor ◽  
Human Platelets ◽  
Factor Vii ◽  
Coagulation System ◽  
Breast Adenocarcinoma ◽  
Activate Factor ◽  
Tumor Cell Lines

SummaryThis paper reports studies on the interaction between human platelets, the plasma coagulation system, and two human tumor cell lines grown in tissue culture: Melanoma and breast adenocarcinoma. The interaction was monitored through the use of 125I- labelled fibrinogen, which measures both thrombin activity generated by cell-plasma interaction and fibrin/fibrinogen binding to platelets and tumor cells. Each tumor cell line activates both the platelets and the coagulation system simultaneously resulting in the generation of thrombin or thrombin-like activity. The melanoma cells activate the coagulation system through “the extrinsic pathway” with a tissue factor-like effect on factor VII, but the breast tumor seems to activate factor X directly. Both tumor cell lines activate platelets to “make available” a platelet- derived procoagulant material necessary for the conversion of prothrombin to thrombin. The tumor-derived procoagulant activity and the platelet aggregating potential of cells do not seem to be inter-related, and they are not specific to malignant cells.

Synthesis and Biological Evaluation of Novel 4,5,6,7-Tetrahydrobenzo[D]-Thiazol-2- Yl Derivatives Derived from Dimedone with Anti-Tumor, C-Met, Tyrosine Kinase and Pim-1 Inhibitions

2019 ◽  
Vol 19 (12) ◽  
pp. 1438-1453 ◽  
Author(s):  
Rafat M. Mohareb ◽  
Amr S. Abouzied ◽  
Nermeen S. Abbas
Keyword(s):  
Tyrosine Kinase ◽  
Tumor Cell ◽  
Cell Lines ◽  
Single Molecule ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
New Drugs ◽  
Tumor Cell Lines ◽  
Thiazole Derivatives ◽  
Wide Range

Background: Dimedone and thiazole moieties are privileged scaffolds (acting as primary pharmacophores) in many compounds that are useful to treat several diseases, mainly tropical infectious diseases. Thiazole derivatives are a very important class of compounds due to their wide range of pharmaceutical and therapeutic activities. On the other hand, dimedone is used to synthesize many therapeutically active compounds. Therefore, the combination of both moieties through a single molecule to produce heterocyclic compounds will produce excellent anticancer agents. Objective: The present work reports the synthesis of 47 new substances belonging to two classes of compounds: Dimedone and thiazoles, with the purpose of developing new drugs that present high specificity for tumor cells and low toxicity to the organism. To achieve this goal, our strategy was to synthesize a series of 4,5,6,7-tetrahydrobenzo[d]-thiazol-2-yl derivatives using the reaction of the 2-bromodimedone with cyanothioacetamide. Methods: The reaction of 2-bromodimedone with cyanothioacetamide gave the 4,5,6,7-tetrahydrobenzo[d]- thiazol-2-yl derivative 4. The reactivity of compound 4 towards some chemical reagents was observed to produce different heterocyclic derivatives. Results: A cytotoxic screening was performed to evaluate the performance of the new derivatives in six tumor cell lines. Thirteen compounds were shown to be promising toward the tumor cell lines which were further evaluated toward five tyrosine kinases. Conclusion: The results of antitumor screening showed that many of the tested compounds were of high inhibition towards the tested cell lines. Compounds 6c, 8c, 11b, 11d, 13b, 14b, 15c, 15g, 21b, 21c, 20d and 21d were the most potent compounds toward c-Met kinase and PC-3 cell line. The most promising compounds 6c, 8c, 11b, 11d, 13b, 14b, 15c, 15g, 20c, 20d, 21b, 21c and 21d were further investigated against tyrosine kinase (c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR). Compounds 6c, 11b, 11d, 14b, 15c, and 20d were selected to examine their Pim-1 kinase inhibition activity the results revealed that compounds 11b, 11d and 15c had high activities.

scholarly journals Desertomycin G, a New Antibiotic with Activity against Mycobacterium tuberculosis and Human Breast Tumor Cell Lines Produced by Streptomyces althioticus MSM3, Isolated from the Cantabrian Sea Intertidal Macroalgae Ulva sp.

Marine Drugs ◽  
2019 ◽  
Vol 17 (2) ◽  
pp. 114 ◽  
Author(s):  
Alfredo F. Braña ◽  
Aida Sarmiento-Vizcaíno ◽  
Ignacio Pérez-Victoria ◽  
Jesús Martín ◽  
Luis Otero ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Tumor Cell ◽  
Cell Lines ◽  
Antibiotic Activity ◽  
Breast Adenocarcinoma ◽  
Tumor Cell Lines ◽  
Human Breast ◽  
Antibiotic Resistant ◽  
Clinical Pathogens ◽  
Corynebacterium Urealyticum

The isolation and structural elucidation of a structurally new desertomycin, designated as desertomycin G (1), with strong antibiotic activity against several clinically relevant antibiotic resistant pathogens are described herein. This new natural product was obtained from cultures of the marine actinomycete Streptomyces althioticus MSM3, isolated from samples of the intertidal seaweed Ulva sp. collected in the Cantabrian Sea (Northeast Atlantic Ocean). Particularly interesting is its strong antibiotic activity against Mycobacterium tuberculosis clinical isolates, resistant to antibiotics in clinical use. To the best of our knowledge, this is the first report on a member of the desertomycin family displaying such activity. Additionally, desertomycin G shows strong antibiotic activities against other relevant Gram-positive clinical pathogens such as Corynebacterium urealyticum, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecium, Enterococcus faecalis, and Clostridium perfringens. Desertomycin G also displays moderate antibiotic activity against relevant Gram-negative clinical pathogens such as Bacteroides fragilis, Haemophilus influenzae and Neisseria meningitidis. In addition, the compound affects viability of tumor cell lines, such as human breast adenocarcinoma (MCF-7) and colon carcinoma (DLD-1), but not normal mammary fibroblasts.

scholarly journals Sorafenib fails to trigger ferroptosis across a wide range of cancer cell lines

2021 ◽  
Vol 12 (7) ◽  
Author(s):  
Jiashuo Zheng ◽  
Mami Sato ◽  
Eikan Mishima ◽  
Hideyo Sato ◽  
Bettina Proneth ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Renal Cell Carcinoma ◽  
Cell Death ◽  
Tumor Cell ◽  
Cell Lines ◽  
Kinase Inhibitor ◽  
Genetically Engineered ◽  
Tumor Cell Lines ◽  
Wide Range ◽  
Bona Fide

AbstractSorafenib, a protein kinase inhibitor approved for the treatment of hepatocellular carcinoma and advanced renal cell carcinoma, has been repeatedly reported to induce ferroptosis by possibly involving inhibition of the cystine/glutamate antiporter, known as system xc−. Using a combination of well-defined genetically engineered tumor cell lines and canonical small molecule ferroptosis inhibitors, we now provide unequivocal evidence that sorafenib does not induce ferroptosis in a series of tumor cell lines unlike the cognate system xc− inhibitors sulfasalazine and erastin. We further show that only a subset of tumor cells dies by ferroptosis upon sulfasalazine and erastin treatment, implying that certain cell lines appear to be resistant to system xc− inhibition, while others undergo ferroptosis-independent cell death. From these findings, we conclude that sorafenib does not qualify as a bona fide ferroptosis inducer and that ferroptosis induced by system xc− inhibitors can only be achieved in a fraction of tumor cell lines despite robust expression of SLC7A11, the substrate-specific subunit of system xc−.

scholarly journals Synthesis, Spectroscopic Characterization, Structural Studies, and In Vitro Antitumor Activities of Pyridine-3-carbaldehyde Thiosemicarbazone Derivatives

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Wilfredo Hernández ◽  
Fernando Carrasco ◽  
Abraham Vaisberg ◽  
Evgenia Spodine ◽  
Jorge Manzur ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Breast Adenocarcinoma ◽  
Significant Activity ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines ◽  
Biological Studies

Eight new thiosemicarbazone derivatives, 6-(1-trifluoroethoxy)pyridine-3-carbaldehyde thiosemicarbazone (1), 6-(4′-fluorophenyl)pyridine-3-carbaldehyde thiosemicarbazone (2), 5-chloro-pyridine-3-carbaldehyde thiosemicarbazone (3), 2-chloro-5-bromo-pyridine-3-carbaldehyde thiosemicarbazone (4), 6-(3′,4′-dimethoxyphenyl)pyridine-3-carbaldehyde thiosemicarbazone (5), 2-chloro-5-fluor-pyridine-3-carbaldehyde thiosemicarbazone, (6), 5-iodo-pyridine-3-carbaldehyde thiosemicarbazone (7), and 6-(3′,5′-dichlorophenyl)pyridine-3-carbaldehyde thiosemicarbazone (8) were synthesized, from the reaction of the corresponding pyridine-3-carbaldehyde with thiosemicarbazide. The synthesized compounds were characterized by ESI-Mass, UV-Vis, IR, and NMR (1H, 13C, 19F) spectroscopic techniques. Molar mass values and spectroscopic data are consistent with the proposed structural formulas. The molecular structure of 7 has been also confirmed by single crystal X-ray diffraction. In the solid state 7 exists in the E conformation about the N2-N3 bond; 7 also presents the E conformation in solution, as evidenced by 1H NMR spectroscopy. The in vitro antitumor activity of the synthesized compounds was studied on six human tumor cell lines: H460 (lung large cell carcinoma), HuTu80 (duodenum adenocarcinoma), DU145 (prostate carcinoma), MCF-7 (breast adenocarcinoma), M-14 (amelanotic melanoma), and HT-29 (colon adenocarcinoma). Furthermore, toxicity studies in 3T3 normal cells were carried out for the prepared compounds. The results were expressed as IC50 and the selectivity index (SI) was calculated. Biological studies revealed that 1 (IC50 = 3.36 to 21.35 μM) displayed the highest antiproliferative activity, as compared to the other tested thiosemicarbazones (IC50 = 40.00 to >582.26 μM) against different types of human tumor cell lines. 1 was found to be about twice as cytotoxic (SI = 1.82) than 5-fluorouracile (5-FU) against the M14 cell line, indicating its efficiency in inhibiting the cell growth even at low concentrations. A slightly less efficient activity was shown by 1 towards the HuTu80 and MCF7 tumor cell lines, as compared to that of 5-FU. Therefore, 1 can be considered as a promising candidate to be used as a pharmacological agent, since it presents significant activity and was found to be more innocuous than the 5-FU anticancer drug against the 3T3 mouse embryo fibroblast cells.

scholarly journals Evaluation of the antiproliferative activity of red propolis hydroalcoholic extract and its fractions obtained by partition

2020 ◽  
Vol 18 (2) ◽  
Author(s):  
Iara Squarisi ◽  
Karoline Soares De Freitas ◽  
Danieli Cristina Lemes ◽  
Gari Vidal Ccana Ccapatinta ◽  
Jennyfer Andrea Aldana Mejía ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Colorimetric Assay ◽  
Lung Fibroblasts ◽  
Breast Adenocarcinoma ◽  
Tumor Cell Lines ◽  
Hydroalcoholic Extract ◽  
Antitumor Potential ◽  
Significant Difference

Abstract. Squarisi IS, De Freitas KS, Lemes DC, Ccana-Ccapatinta GV, Mejia JAA, Bastos JK, Veneziani RCS, Ambrosio SR, Tavares DC. 2018. Evaluation of the antiproliferative activity of red propolis hydroalcoholic extract and its fractions obtained by partition. Biofarmasi J Nat Prod Biochem 18: 66-69. The present study aimed to evaluate the cytotoxicity of red propolis hydroalcoholic extract (RPHE) and its fractions obtained by partition, hexanes (HF), dichloromethane (DF), ethyl acetate (AF) and n-butanol (BF), on tumor and non-tumor cell lines. For this purpose, the XTT colorimetric assay was performed on human lung fibroblasts (GM07492A, non-tumor cell), breast adenocarcinoma (MCF-7), glioblastoma (U343) and cervix adenocarcinoma (HeLa) cells. The results showed that RPHE, HF and DF presented not only cytotoxic potential to all tumor cell lines but also to normal cell line, indicating selectivity absence. HF presented the lowest IC50 (half minimal inhibitory concentration; 33.8-133.3 µg/mL), with significant difference from those observed for RPHE (137.0-262.7 µg/mL). BF and AF revealed an IC50 which was higher than 1250 µg/mL in all cell lines. The results showed that red propolis has substances with antiproliferative activity, indicating that its hexanes fraction may have substances with antitumor potential.

scholarly journals β-Caryophyllene, a Compound Isolated from the Biblical Balm of Gilead (Commiphora gileadensis), Is a Selective Apoptosis Inducer for Tumor Cell Lines

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Eitan Amiel ◽  
Rivka Ofir ◽  
Nativ Dudai ◽  
Elaine Soloway ◽  
Tatiana Rabinsky ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Essential Oils ◽  
Cell Lines ◽  
Tumor Cell Lines ◽  
Dna Ladder ◽  
Normal Cells ◽  
Cytotoxic Compound ◽  
Wide Range ◽  
Food And Beverage ◽  
Apoptosis Inducer

The biblical balm of Gilead (Commiphora gileadensis) was investigated in this study for anticancerous activity against tumor cell lines. The results obtained from ethanol-based extracts and from essential oils indicated thatβ-caryophyllene (trans-(1R,9S)-8-methylene-4,11,11-trimethylbicyclo[7.2.0]undec-4-ene) is a key component in essential oils extracted from the balm of Gilead.β-Caryophyllene can be found in spice blends, citrus flavors, soaps, detergents, creams, and lotions, as well as in a variety of food and beverage products, and it is known for its anti-inflammatory, local anaesthetic, and antifungal properties. It is also a potent cytotoxic compound over a wide range of cell lines. In the current paper, we found thatCommiphora gileadensisstem extracts and essential oil have an antiproliferative proapoptotic effect against tumor cells and not against normal cells.β-caryophyllene caused a potent induction of apoptosis accompanied by DNA ladder and caspase-3 catalytic activity in tumor cell lines. In summary, we showed thatC. gileadensisstems contain an apoptosis inducer that acts, in a selective manner, against tumor cell lines and not against normal cells.

scholarly journals Synthesis and antiproliferative activity of various novel indole Mannich bases

2015 ◽  
Vol 1 (2) ◽  
Author(s):  
Mardia T El Sayed ◽  
Hoda A R Hussein ◽  
Khadiga M Ahmed ◽  
Nehal A Hamdy
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Human Tumor ◽  
Inhibitory Effect ◽  
Mannich Bases ◽  
Primary Amines ◽  
Breast Adenocarcinoma ◽  
Tumor Cell Lines

Various secondary and primary amines were converted into bis-indolyl Mannich bases with good to excellent yields via double condensation reactions with indole and glutaraldehyde. The expected bis-indolyl Mannich bases (2, 3 and 4) were formed by using piperazinehexahydrate and 4,4′-trimethylenedipiperidine. Whereas, the use of primary amines, phenylhydrazine, amino acids and primary diamine produced the corresponding bis-indolyl-1,2,6-trisubstituted pipridines (5a-e) and indolyl-quinolizine (6) and dibis-indolyl-1,2,6-trisubstituted pipridines (7). All analytical and spectral data of these bis-indolyl Mannich bases have been determined. Six of the synthesized bis-indolyl Mannich bases have been subjected for antiproliferative activity screening at National Cancer Institute (NCI), Egypt, towards three human tumor cell lines representing different tumor types: breast adenocarcinoma cell (MCF-7), non-small lung cancer cell (NCI-H460), and central nervous system (CNS) cancer cell (SF-268). Compound (4) indicated the best and highest inhibitory effect against all three tested tumor cell lines with inhibition of 50% concentration (IC<sub>50</sub>) for MCF<strong>-</strong>7 (0.08<strong> </strong>µmol/L), NCI<strong>-</strong>H460<strong> </strong>(0.05<strong> </strong>µmol/L) and SF<strong>-</strong>268 (0.01 µmol/L).

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