scholarly journals Structures of the free and inhibitors-bound forms of bromelain and ananain from Ananas comosus stem and in vitro study of their cytotoxicity

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Mohamed Azarkan ◽  
Erik Maquoi ◽  
François Delbrassine ◽  
Raphael Herman ◽  
Nasiha M’Rabet ◽  
...  
Keyword(s):  
Cell Lines ◽  
Complex Mixture ◽  
In Vitro Study ◽  
Cysteine Proteases ◽  
Ananas Comosus ◽  
Adherent Cell ◽  
High Discrimination ◽  
Protease Substrate ◽  
Case Sequence

Abstract The Ananascomosus stem extract is a complex mixture containing various cysteine ​​proteases of the C1A subfamily, such as bromelain and ananain. This mixture used for centuries in Chinese medicine, has several potential therapeutic applications as anti-cancer, anti-inflammatory and ecchymosis degradation agent. In the present work we determined the structures of bromelain and ananain, both in their free forms and in complex with the inhibitors E64 and TLCK. These structures combined with protease-substrate complexes modeling clearly identified the Glu68 as responsible for the high discrimination of bromelain in favor of substrates with positively charged residues at P2, and unveil the reasons for its weak inhibition by cystatins and E64. Our results with purified and fully active bromelain, ananain and papain show a strong reduction of cell proliferation with MDA-MB231 and A2058 cancer cell lines at a concentration of about 1 μM, control experiments clearly emphasizing the need for proteolytic activity. In contrast, while bromelain and ananain had a strong effect on the proliferation of the OCI-LY19 and HL-60 non-adherent cell lines, papain, the archetypal member of the C1A subfamily, had none. This indicates that, in this case, sequence/structure identity beyond the active site of bromelain and ananain is more important than substrate specificity.

Effect of black seeds (Nigella sativa) volatile oil on the cervical cancer: In vitro study, on Hela cell lines

2019 ◽  
Vol 7 (4) ◽  
pp. 91-96
Author(s):  
Isra'a Al-sobhi ◽  
◽  
Rawan Al-Ghabban ◽  
Soad Shaker Ali ◽  
Jehan Al-Amri ◽  
...  
Keyword(s):  
Cervical Cancer ◽  
Hela Cell ◽  
Cell Lines ◽  
Nigella Sativa ◽  
In Vitro Study ◽  
Volatile Oil ◽  
Vitro Study ◽  
Hela Cell Lines ◽  
Black Seeds

scholarly journals The Modulation of PCSK9 and LDLR by Supercritical CO2 Extracts of Mentha longifolia and Isolated Piperitone Oxide, an In Vitro Study

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3886
Author(s):  
Stefania Sut ◽  
Irene Ferrarese ◽  
Maria Giovanna Lupo ◽  
Nicola De Zordi ◽  
Elisa Tripicchio ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Cell Lines ◽  
Hepatoma Cell ◽  
Density Lipoprotein ◽  
In Vitro Study ◽  
Volatile Constituent ◽  
Dependent Manner ◽  
Human Hepatoma Cell ◽  
Concentration Dependent Manner

In the present study the ability of supercritical carbon dioxide (SCO2) extracts of M. longifolia L. leaves to modulate low-density lipoprotein receptor (LDLR) and proprotein convertase subtilisin/kexin type 9 (PCSK9) expression was evaluated in cultured human hepatoma cell lines Huh7 and HepG2. Two SCO2 extracts, one oil (ML-SCO2) and a semisolid (MW-SCO2), were subjected to detailed chemical characterization by mono- and bidimensional nuclear magnetic resonance (1D, 2D-NMR), gas chromatography coupled with mass spectrometry (GC-MS) and liquid chromatography coupled with mass spectrometry (LC-MS). Chemical analysis revealed significant amounts of fatty acids, phytosterols and terpenoids. ML-SCO2 was able to induce LDLR expression at a dose of 60 µg/mL in HuH7 and HepG2 cell lines. Furthermore, ML-SCO2 reduced PCSK9 secretion in a concentration-dependent manner in both cell lines. Piperitone oxide, the most abundant compound of the volatile constituent of ML-SCO2 (27% w/w), was isolated and tested for the same targets, showing a very effective reduction of PCSK9 expression. The overall results revealed the opportunity to obtain a new nutraceutical ingredient with a high amount of phytosterols and terpenoids using the SCO2 extraction of M. longifolia L., a very well-known botanical species used as food. Furthermore, for the first time we report the high activity of piperitone oxide in the reduction of PCSK9 expression.

Ellagic Acid Cytotoxic and Metalloproteinases Inhibitory Effects Against Oral Squamous Cell Carcinoma: An in Vitro Study

2021 ◽  
Author(s):  
Patricia Maria Wiziack Zago ◽  
Luiza Rodrigues Hellmeister ◽  
Lucas Novaes Teixeira ◽  
Rui Barbosa de Brito Junior ◽  
Elizabeth Ferreira Martinez
Keyword(s):  
Oral Cancer ◽  
Cell Lines ◽  
Ellagic Acid ◽  
Normal Cell ◽  
In Vitro Study ◽  
Significance Level ◽  
Viability Analysis ◽  
Anticancer Properties

Abstract ObjectivesThis study aimed to evaluate the in vitro antitumoral potential of different concentrations of EA against two OSCC cell lines with distinct tissue invasiveness profiles. Material and methodsNormal keratinocytes (NOK) and OSCC´s cells CAL-27 and SCC-9 were treated with concentrations of EA varying from 5 to 662 µM during 24, 48 or 72h. After each time of treatment, cells were submitted to viability analysis using MTT and the secretion of metalloproteinases (MMP-2 and MMP-9) and tissue metalloproteinases inhibitors (TIMP-1 and TIMP-2) were performed by Enzyme-Linked Immunoassay (ELISA). Data were submitted to ANOVA, followed by Bonferroni´s test, considering 5% as significance level. ResultsEA was cytotoxic to OSCC cells in all exposure times, rarely affecting normal cell viability, except for concentrations higher than 82 µM and after 72h treatment. For OSCC cells, EA decreased MMPs and increased TIMPs´s expression without effect on those enzymes for normal cell lines during all times of exposure. ConclusionEA is a promising therapeutic adjuvant to treat oral cancer, however, further in vivo studies are required to clinically validate its potential. Clinical RelevanceThe in vitro anticancer properties showed by Ellagic acid, a phenolic compound that could easily be accessed by oral cancer patients, provides data to base future clinical studies intended to develop a safe topical oral anticancer product.

Irinotecan Resistance – In Search of New Markers in CRC.

2021 ◽  
Author(s):  
Jakub Kryczka ◽  
Joanna Boncela
Keyword(s):  
Drug Resistance ◽  
Cell Lines ◽  
Expression Profiles ◽  
Resistance Mechanism ◽  
Interaction Network ◽  
In Vitro Study ◽  
Cancer Drug ◽  
New Genes

Abstract Colorectal cancer (CRC) is one of the most prominent causes of cancer death worldwide. Chemotherapeutic regimens consisting of different drugs combinations such as 5-fluorouracil, and oxaliplatin (FOLFOX) or irinotecan (FOLFIRI) have been proven successful in the treatment of CRC. However, chemotherapy often leads to the acquisition of cancer drug resistance followed by metastasis and in the aftermath therapeutic failure. The molecular mechanism responsible for drug resistance is still unclear. The systemic search for new biomarkers of this phenomenon may identify new genes and pathways. To understand the drug resistance mechanism in CRC, the in vitro study based on the molecular analysis of drug-sensitive cells lines vs drug-resistant cells lines has been used. In our study to bridge the gap between in vitro and in vivo study, we compared the expression profiles of cell lines and patient samples from the publicly available database to select the new candidate genes for irinotecan resistance. Using The Gene Expression Omnibus (GEO) database of CRC cell lines (HT29, HTC116, LoVo, and their respective irinotecan-resistant variants) and patient samples (GSE42387, GSE62080, and GSE18105) we compared the changes in the mRNA expression profile of the main genes involved in irinotecan body’s processing, such as transport out of the cells and metabolism. Furthermore, using a protein-protein interaction network of differently expressed genes between FOLFIRI resistant and sensitive CRC patients, we have selected top networking proteins (upregulated: NDUFA2, SDHD, LSM5, DCAF4, and COX10, downregulated: RBM8A, TIMP1, QKI, TGOLN2, and PTGS2). Our analysis provided several potential irinotecan resistance markers, previously not described as such.

scholarly journals Investigating the impact of alpha/beta and LET d on relative biological effectiveness in scanned proton beams: An in vitro study based on human cell lines

2020 ◽  
Vol 47 (8) ◽  
pp. 3691-3702 ◽  
Author(s):  
Elisabeth Mara ◽  
Monika Clausen ◽  
Suphalak Khachonkham ◽  
Simon Deycmar ◽  
Clara Pessy ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cell ◽  
Relative Biological Effectiveness ◽  
In Vitro Study ◽  
Vitro Study ◽  
Human Cell Lines ◽  
Biological Effectiveness ◽  
Alpha Beta ◽  
The Impact

Anticancer potential of docetaxel-loaded cobalt ferrite nanocarrier: an in vitro study on MCF-7 and MDA-MB-231 cell lines

2020 ◽  
Vol 38 (1) ◽  
pp. 36-46
Author(s):  
Jnanranjan Panda ◽  
Bhabani Sankar Satapathy ◽  
Bidisha Mandal ◽  
Ramkrishna Sen ◽  
Biswajit Mukherjee ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cobalt Ferrite ◽  
In Vitro Study ◽  
Vitro Study ◽  
Mcf 7

scholarly journals Aminolevulinic Acid-Mediated Photodynamic Therapy of Human Meningioma: An in Vitro Study on Primary Cell Lines

2015 ◽  
Vol 16 (12) ◽  
pp. 9936-9948 ◽  
Author(s):  
Mustafa El-Khatib ◽  
Carolin Tepe ◽  
Brigitte Senger ◽  
Maxine Dibué-Adjei ◽  
Markus Riemenschneider ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Cell Lines ◽  
Aminolevulinic Acid ◽  
In Vitro Study ◽  
Vitro Study ◽  
Primary Cell ◽  
Human Meningioma ◽  
Primary Cell Lines

scholarly journals The Selection of NFκB Inhibitors to Block Inflammation and Induce Sensitisation to FasL-Induced Apoptosis in HNSCC Cell Lines Is Critical for Their Use as a Prospective Cancer Therapy

2019 ◽  
Vol 20 (6) ◽  
pp. 1306 ◽  
Author(s):  
Mario Scheurer ◽  
Roman Brands ◽  
Mohamed El-Mesery ◽  
Stefan Hartmann ◽  
Urs Müller-Richter ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Cell Lines ◽  
In Vitro Study ◽  
Keratinocyte Cell Line Hacat ◽  
Keratinocyte Cell ◽  
Nfκb Pathway ◽  
Induced Apoptosis ◽  
Selection Of ◽  
Hnscc Cell

Inflammation is a central aspect of tumour biology and can contribute significantly to both the origination and progression of tumours. The NFκB pathway is one of the most important signal transduction pathways in inflammation and is, therefore, an excellent target for cancer therapy. In this work, we examined the influence of four NFκB inhibitors—Cortisol, MLN4924, QNZ and TPCA1—on proliferation, inflammation and sensitisation to apoptosis mediated by the death ligand FasL in the HNSCC cell lines PCI1, PCI9, PCI13, PCI52 and SCC25 and in the human dermal keratinocyte cell line HaCaT. We found that the selection of the inhibitor is critical to ensure that cells do not respond by inducing counteracting activities in the context of cancer therapy, e.g., the extreme IL-8 induction mediated by MLN4924 or FasL resistance mediated by Cortisol. However, TPCA1 was qualified by this in vitro study as an excellent therapeutic mediator in HNSCC by four positive qualities: (1) proliferation was inhibited at low μM-range concentrations; (2) TNFα-induced IL-8 secretion was blocked; (3) HNSCC cells were sensitized to TNFα-induced cell death; and (4) FasL-mediated apoptosis was not disrupted.

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