scholarly journals A Novel Dermaseptin Isolated from the Skin Secretion of Phyllomedusa tarsius and Its Cationicity-Enhanced Analogue Exhibiting Effective Antimicrobial and Anti-Proliferative Activities

Biomolecules ◽  
2019 ◽  
Vol 9 (10) ◽  
pp. 628 ◽  
Author(s):  
Li ◽  
Xi ◽  
Ma ◽  
Chen ◽  
Zhou ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Membranes ◽  
Human Cancer ◽  
Antimicrobial Effect ◽  
Human Cell Line ◽  
Haemolytic Activity ◽  
Human Cancer Cells ◽  
Proliferative Effect ◽  
Lysine Residues ◽  
Normal Human Cell

A novel dermaseptin peptide, dermaseptin-PT9 (DPT9), was isolated and identified from Phyllomedusa tarsius by the combination of molecular cloning and LC-MS analysis. Chemically synthesised DPT9 was broadly effective against the tested microorganisms through the disruption of cell membranes and showed weak haemolytic activity towards horse erythrocytes. It also exhibited anti-proliferative effect against various human cancer cells. Moreover, an analogue with enhanced cationicity, K8, 23-DPT9, in which Asp8 and Glu23 were substituted by lysine residues, had a markedly increased antimicrobial effect against all tested microorganisms and disrupted microbial cell membranes. This analogue also showed no haemolysis at its effective antimicrobial concentrations. In addition, K8, 23-DPT9 displayed an enhanced anti-proliferative effect against cancer cells, while displayed weak activity against the normal human cell line, HMEC-1.

Study on anti-proliferative effect of benzoxathiole derivatives through inactivation of NF-κB in human cancer cells

2012 ◽  
Vol 22 (14) ◽  
pp. 4523-4527 ◽  
Author(s):  
Eeda Venkateswararao ◽  
Hoang Le Tuan Anh ◽  
Vinay K. Sharma ◽  
Ki-Cheul Lee ◽  
Niti Sharma ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Human Cancer Cells ◽  
Proliferative Effect

scholarly journals Identification and Characterization of the Caspase-Mediated Apoptotic Activity of Teucrium mascatense and an Isolated Compound in Human Cancer Cells

Molecules ◽  
2019 ◽  
Vol 24 (5) ◽  
pp. 977 ◽  
Author(s):  
Neena Panicker ◽  
Sameera Balhamar ◽  
Shaima Akhlaq ◽  
Mohammed Qureshi ◽  
Tania Rizvi ◽  
...  
Keyword(s):  
Cell Death ◽  
Cancer Cells ◽  
Apoptotic Cell ◽  
Human Cancer ◽  
Annexin V ◽  
Dependent Manner ◽  
Human Cancer Cells ◽  
Cell Death Pathways ◽  
Proliferative Effect ◽  
Mcf 7

Plants of the genus Teucrium (Lamiaceae or Labiatae family) are known historically for their medicinal value. Here, we identify and characterize the anticancer potential of T. mascatense and its active compound, IM60, in human cancer cells. The anti-proliferative effect of a T. mascatense methanol extract and its various fractions were analyzed in MCF-7 and HeLa cells in a dose- and time dependent manner. The dichloromethane fraction (TMDF) was observed to be the most effective with cytotoxicity against a more expanded series of cell lines, including MDA-MB-231. A time and dose-dependent toxicity profile was also observed for IM60; it could induce rapid cell death (within 3 h) in MCF-7 cells. Activation of caspases and PARP, hallmarks of apoptotic cell death pathways, following treatment with TMDF was demonstrated using western blot analysis. Inversion of the phosphatidylserine phospholipid from the inner to the outer membrane was confirmed by annexin V staining that was inhibited by the classical apoptosis inhibitor, Z-VAK-FMK. Changes in cell rounding, shrinkage, and detachment from other cells following treatment with TMDF and IM60 also supported these findings. Finally, the potential of TMDF and IM60 to induce enzymatic activity of caspases was also demonstrated in MCF-7 cells. This study, thus, not only characterizes the anticancer potential of T. mascatense, but also identifies a lead terpenoid, IM60, with the potential to activate anticancer cell death pathways in human cancer cells.

Anti-proliferative effect of chalcone derivatives through inactivation of NF-κB in human cancer cells

2014 ◽  
Vol 22 (13) ◽  
pp. 3386-3392 ◽  
Author(s):  
Eeda Venkateswararao ◽  
Vinay K. Sharma ◽  
Jieun Yun ◽  
Youngsoo Kim ◽  
Sang-Hun Jung
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Chalcone Derivatives ◽  
Human Cancer Cells ◽  
Proliferative Effect

Stattic enhances the anti-proliferative effect of docetaxel via the Bax/Bcl-2/cyclin B axis in human cancer cells

2018 ◽  
Vol 69 ◽  
pp. 188-196 ◽  
Author(s):  
Jamal Mohammadian ◽  
Ommoleila Molavi ◽  
Mohammad Bagher Pirouzpanah ◽  
Ali Akbar Rahim Rahimi ◽  
Nasser Samadi
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Cyclin B ◽  
Human Cancer Cells ◽  
Proliferative Effect

scholarly journals Cytotoxic activity of bromodomain inhibitor NVS-CECR2-1 on human cancer cells

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Seul Gi Park ◽  
Daye Lee ◽  
Hye-Ran Seo ◽  
Shin-Ai Lee ◽  
Jongbum Kwon
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Human Cancer ◽  
Chromosome Region ◽  
Human Cancer Cells ◽  
Cat Eye Syndrome ◽  
Promising Therapeutic Target ◽  
Maximum Inhibition ◽  
Lysine Residues ◽  
First Time

Abstract Bromodomain (BRD), a protein module that recognizes acetylated lysine residues on histones and other proteins, has recently emerged as a promising therapeutic target for human diseases such as cancer. While most of the studies have been focused on inhibitors against BRDs of the bromo- and extra-terminal domain (BET) family proteins, non-BET family BRD inhibitors remain largely unexplored. Here, we investigated a potential anticancer activity of the recently developed non-BET family BRD inhibitor NVS-CECR2-1 that targets the cat eye syndrome chromosome region, candidate 2 (CECR2). We show that NVS-CECR2-1 inhibits chromatin binding of CECR2 BRD and displaces CECR2 from chromatin within cells. NVS-CECR2-1 exhibits cytotoxic activity against various human cancer cells, killing SW48 colon cancer cells in particular with a submicromolar half maximum inhibition value mainly by inducing apoptosis. The sensitivity of the cancer cells to NVS-CECR2-1 is reduced by CECR2 depletion, suggesting that NVS-CECR2-1 exerts its activity by targeting CECR2. Interestingly, our data show that NVS-CECR2-1 also kills cancer cells by CECR2-independent mechanism. This study reports for the first time the cancer cell cytotoxic activity for NVS-CECR2-1 and provides a possibility of this BRD inhibitor to be developed as an anticancer therapeutic agent.

scholarly journals BISBENZOXAZOLE DERIVATIVES HAD ANTI-PROLIFERATIVE EFFECT ON HUMAN CANCER CELLS

2019 ◽  
Vol 8 (2) ◽  
pp. 203-211
Author(s):  
Furkan AYAZ ◽  
Qadar Ahmed Isse ◽  
Rusmeenee Kheeree ◽  
Ronak Haj Ersan ◽  
Oztekin Algul
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Human Cancer Cells ◽  
Proliferative Effect

scholarly journals Cytotoxicity of Frutalin on Distinct Cancer Cells Is Independent of Its Glycosylation

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4712
Author(s):  
Carla Oliveira ◽  
Ana Isabel Freitas ◽  
Nair Campos ◽  
Lucília Saraiva ◽  
Lucília Domingues
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Active Form ◽  
High Yield ◽  
Human Cancer Cells ◽  
Proliferative Effect ◽  
Recombinant Production ◽  
Tetrameric Structure ◽  
Spectroscopy Studies ◽  
Purification Protocol

Frutalin is a plant lectin with beneficial immunobiological action, although the access to its active form is still restricted. Moreover, there is a knowledge gap on isoform activity and glycosylation impact on its bioactivity, and recombinant production protocols were seen as ineffective. Here, a simpler and faster production and purification protocol was developed, attaining a yield of purified frutalin 3.3-fold higher than that obtained previously. Hemagglutination assays confirmed that this frutalin isoform could not agglutinate rabbit erythrocytes, while maintaining the native tetrameric structure, as indicated by DLS analysis, and strong interaction with methyl-alpha-galactose, in fluorescence spectroscopy studies. The cytotoxicity of the recombinant frutalin isoform was shown in a broad panel of human cancer cells: colon (HCT116), melanoma (A375), triple-negative breast cancer (MDA-MB-231), and ovarian (IGROV-1). Treatment with 8.5–11.8 μM TrxFTL reduced proliferation of all cancer cells to half in 48 h. This anti-proliferative effect encompasses the p53 pathway since it was significantly reduced in p53-null colon cancer cells (HCT116 p53−/−; GI50 of 25.0 ± 3.0 μM), when compared to the isogenic p53-positive cells (HCT116 p53+/+; GI50 of 8.7 ± 1.8 μM; p < 0.002). This recombinantly produced frutalin isoform has relevant cytotoxic effect and its biological activity is not dependent on glycosylation. The developed E. coli production and purification protocol generates high yield of non-glycosylated frutalin isoform with potent cytotoxic activity, enabling the development of novel anticancer p53-targeting therapies.

Indirubin derivatives inhibit SFKs/Stat signaling associated with apoptosis in human cancer cells

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
S Nam ◽  
R Buettner ◽  
X Liu ◽  
J Turkson ◽  
D Kim ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Human Cancer Cells ◽  
Stat Signaling
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