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.

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 In VitroCytotoxic Potential of Essential Oils ofEucalyptus benthamiiand Its Related Terpenes on Tumor Cell Lines

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Patrícia Mathias Döll-Boscardin ◽  
Adilson Sartoratto ◽  
Beatriz Helena Lameiro de Noronha Sales Maia ◽  
Josiane Padilha de Paula ◽  
Tomoe Nakashima ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Essential Oils ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cytotoxic Effect ◽  
Herbal Remedy ◽  
Jurkat Cells ◽  
Tumor Cell Lines ◽  
Hela Cell Lines

EucalyptusL. is traditionally used for many medicinal purposes. In particular, someEucalyptusspecies have currently shown cytotoxic properties. Local Brazilian communities have used leaves ofE. benthamiias a herbal remedy for various diseases, including cancer. Considering the lack of available data for supporting this cytotoxic effect, the goal of this paper was to study thein vitrocytotoxic potential of the essential oils from young and adult leaves ofE. benthamiiand some related terpenes (α-pinene, terpinen-4-ol, andγ-terpinene) on Jurkat, J774A.1 and HeLa cells lines. Regarding the cytotoxic activity based on MTT assay, the essential oils showed improved results thanα-pinene andγ-terpinene, particularly for Jurkat and HeLa cell lines. Terpinen-4-ol revealed a cytotoxic effect against Jurkat cells similar to that observed for volatile oils. The results of LDH activity indicated that cytotoxic activity of samples against Jurkat cells probably involved cell death by apoptosis. The decrease of cell DNA content was demonstrated due to inhibition of Jurkat cells proliferation by samples as a result of cytotoxicity. In general, the essential oils from young and adult leaves ofE. benthamiipresented cytotoxicity against the investigated tumor cell lines which confirms their antitumor potential.

Cytotoxic potential of essential oils of Eucalyptus benthamii and its related terpenes on tumor cell lines

Planta Medica ◽  
2015 ◽  
Vol 81 (11) ◽  
Author(s):  
PV Farago ◽  
PM Döll-Boscardin ◽  
CC Kanunfre ◽  
JM Budel
Keyword(s):  
Tumor Cell ◽  
Essential Oils ◽  
Cell Lines ◽  
Tumor Cell Lines ◽  
Cytotoxic Potential

scholarly journals The effect of the essential oils from five different Lippia species on the viability of tumor cell lines

2013 ◽  
Vol 23 (6) ◽  
pp. 895-902 ◽  
Author(s):  
Mayna da S. Gomide ◽  
Fernanda de O. Lemos ◽  
Miriam T.P. Lopes ◽  
Tânia M. de A. Alves ◽  
Lyderson F. Viccini ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Essential Oils ◽  
Cell Lines ◽  
Tumor Cell Lines

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.

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 Antimicrobial Activity of Essential Oils againstStreptococcus mutansand their Antiproliferative Effects

2012 ◽  
Vol 2012 ◽  
pp. 1-12 ◽  
Author(s):  
Lívia Câmara de Carvalho Galvão ◽  
Vivian Fernandes Furletti ◽  
Salete Meyre Fernandes Bersan ◽  
Marcos Guilherme da Cunha ◽  
Ana Lúcia Tasca Góis Ruiz ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Tumor Cell ◽  
Essential Oils ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Human Tumor ◽  
Gas Chromatography Mass Spectrometry ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

This study aimed to evaluate the activity of essential oils (EOs) againstStreptococcus mutansbiofilm by chemically characterizing their fractions responsible for biological and antiproliferative activity. Twenty EO were obtained by hydrodistillation and submitted to the antimicrobial assay (minimum inhibitory (MIC) and bactericidal (MBC) concentrations) againstS. mutansUA159. Thin-layer chromatography and gas chromatography/mass spectrometry were used for phytochemical analyses. EOs were selected according to predetermined criteria and fractionated using dry column; the resulting fractions were assessed by MIC and MBC, selected as active fractions, and evaluated againstS. mutansbiofilm. Biofilms formed were examined using scanning electron microscopy. Selected EOs and their selected active fractions were evaluated for their antiproliferative activity against keratinocytes and seven human tumor cell lines. MIC and MBC values obtained for EO and their active fractions showed strong antimicrobial activity. Chemical analyses mainly showed the presence of terpenes. The selected active fractions inhibitedS. mutansbiofilm formation (P<0.05) did not affect glycolytic pH drop and were inactive against keratinocytes, normal cell line. In conclusion, EO showed activity at low concentrations, and their selected active fractions were also effective against biofilm formed byS. mutansand human tumor cell lines.

scholarly journals Transcriptional downregulation of gap-junction proteins blocks junctional communication in human mammary tumor cell lines.

1992 ◽  
Vol 118 (5) ◽  
pp. 1213-1221 ◽  
Author(s):  
S W Lee ◽  
C Tomasetto ◽  
D Paul ◽  
K Keyomarsi ◽  
R Sager
Keyword(s):  
Cell Cycle ◽  
Tumor Cell ◽  
Gap Junction ◽  
Tumor Cells ◽  
Cell Lines ◽  
Mammary Tumor ◽  
Northern Analysis ◽  
Tumor Cell Lines ◽  
Mammary Tumor Cell ◽  
Normal Cells

Subtractive hybridization, selecting for mRNAs expressed in normal human mammary epithelial cells (NMECs) but not in mammary tumor cell lines (TMECs), led to the cloning of the human gap junction gene connexin 26 (Cx26), identified by its sequence similarity to the rat gene. Two Cx26 transcripts derived from a single gene are expressed in NMECs but neither is expressed in a series of TMECs. Northern analysis using rat Cx probes showed that Cx43 mRNA is also expressed in the normal cells, but not in the tumor lines examined. Connexin genes Cx31.1, Cx32, Cx33, Cx37, and Cx40 are not expressed in either normal cells or the tumor lines examined. In cell-cell communication studies, the normal cells transferred Lucifer yellow, while tumor cells failed to show dye transfer. Both Cx26 and Cx43 proteins were immunolocalized to membrane sites in normal cells but were not found in tumor cells. Further analysis demonstrated that Cx26 is a cell-cycle regulated gene expressed at a moderate level during G1 and S, and strongly up-regulated in late S and G2, as shown with lovastatin-synchronized NMECs. Cx43, on the contrary is constitutively expressed at a uniform low level throughout the cell cycle. Treatment of normal and tumor cells with a series of drugs: 5dB-cAMP, retinoic acid, okadaic acid, estradiol, or TGFb had no connexin-inducing effect in tumor cells. However, PMA induced re-expression of the two Cx26 transcripts but not of Cx43 in several TMECs. Thus Cx26 and Cx43 are both downregulated in tumor cells but respond differentially to some signals. Modulation of gap-junctional activity by drug therapy may have useful clinical applications in cancer.

scholarly journals A Lipoaminopeptaibol Secreted by Alkalophilic Fungus Emericellopsis alkalina Demonstrates a Strong Cytotoxic Effect against Tumor Cell Lines

Proceedings ◽  
2019 ◽  
Vol 22 (1) ◽  
pp. 4
Author(s):  
Eugene Rogozhin ◽  
Vera Sadykova
Keyword(s):  
Tumor Cell ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cytotoxic Effect ◽  
Antimicrobial Effect ◽  
Antitumor Antibiotic ◽  
Tumor Cell Lines ◽  
Normal Cells ◽  
Hela Cell Lines

Soil fungi are known to produce and secrete antibiotics with a strong antimicrobial effect towards eukaryotic organisms. In many occasions, these compounds belong to peptides that are products of non-ribosomal biosynthesis and are called peptaibols. Many peptaibols are cytotoxic and some of them suppress tumor cell lines much better than normal cells by inducing calcium-mediated apoptosis. The main antimicrobial lipoaminopeptaibol—emericellipsin A—isolated from the fungus Emericellopsis alkalina strain VKPM F-1428, which demonstrates promising antifungal activity against different fungal taxons,has been found to exhibit selective cytotoxic activity against HepG2 and Hela cell lines (EC50 2.8 and 0.5 μM, respectively) in MTT assays in vitro. This result corresponds to the standard antitumor antibiotic doxorubicin, which has an EC50 value of 440 nM. In a fibroblast toxicity test, emericellipsin A exhibited less cytotoxic activity than doxorubicin (EC50 14 and 0.34 μM, respectively). Therefore, it is less toxic to normal cells than doxirubicin (~40 times), but it yields a more potent cytotoxic effect on tumor cell lines. That is why emericellipsin A can be considered for future more detailed investigations to be an effective antitumor substance.

Sign in / Sign up

Export Citation Format

Share Document