Synthesis of axially disubstituted silicon phthalocyanines and investigation of their in vitro cytotoxic/phototoxic anticancer activities

2020 ◽  
Vol 25 (01) ◽  
pp. 10-18
Author(s):  
Fatma Yurt ◽  
Ece Tugba Saka ◽  
Zekeriya Biyiklioglu ◽  
Ayça Tunçel ◽  
Derya Ozel ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Colon Adenocarcinoma ◽  
Nuclear Imaging ◽  
Fibroblast Cell ◽  
Target Tissue ◽  
Anticancer Activities ◽  
Human Lung Fibroblast ◽  
Ht 29

In this study, two SiPcs have been selected and the photodynamic therapy potentials were evaluated of the Pcs. Synthesis of Axially 2-decyn-1-oxy disubstituted Es-SiPc-2 was newly synthesized by the reaction of SiPcCl2 with 2-decyn-1-ol in the presence of NaH in toluene. Furthermore, their nuclear imaging potentials were evaluated in human colon adenocarcinoma (HT-29) and human lung fibroblast cell (WI-38) cell lines. The uptake results have indicated that Es-SiPc labeled with [Formula: see text]I radionuclide ([Formula: see text]I-Es-SiPc) was approximately 2-fold higher in the HT-29 cell line than the WI-38 cell line. In other words, the target/non-target tissue ratio is defined as two in the HT-29/WI-38 cell lines. Besides, the uptake values of [Formula: see text]I-Es-SiPc were found to be higher than [Formula: see text]I-Es-SiPc-2. [Formula: see text]I-Es-SiPc and [Formula: see text]I-Es-SiPc-2 are promising for imaging or treating colon adenocarcinoma. In vitrophotodynamic therapy (PDT) studies have shown that both compounds are suitable and can be used in this field. Also, Es-SiPc has been shown to have higher phototoxicity than Es-SiPc-2.

Evaluation of photodynamic therapy and nuclear imaging potential of subphthalocyanine integrated TiO2 nanoparticles in mammary and cervical tumor cells

2019 ◽  
Vol 23 (07n08) ◽  
pp. 908-915 ◽  
Author(s):  
Fatma Yurt ◽  
Kasim Ocakoglu ◽  
Ozge Er ◽  
Hale Melis Soylu ◽  
Mine Ince ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Nuclear Imaging ◽  
Target Tissue ◽  
Hela Cell Lines ◽  
Wi38 Cell

This study, subphthalocyanines (SubPc) and SubPc integrated TiO2 nanoparticles (SubPc-TiO[Formula: see text] were synthesized as novel photosensitizers. Their PDT effects were evaluated. Furthermore, nuclear imaging potential of [Formula: see text]I-labelled SubPc/SubPc-TiO2 were examined in mouse mammary carcinoma (EMT6) and cervix adenocarcinoma (HeLa) cell lines. The uptake results show that SubPc labelled with [Formula: see text]I radionuclide ([Formula: see text]I-SubPc) in EMT6 and HeLa cell lines was found to be approximately the same as in the WI38 cell line. However, the uptake values of SubPc-TiO2 labelled with [Formula: see text]I ([Formula: see text]I-SubPc-TiO[Formula: see text] in EMT6 and HeLa cell lines were determined to be two times higher than in the WI38 cell line. In other words, the target/non-target tissue ratio was identified as two in the EMT6 and HeLa cell lines. [Formula: see text]I-SubPc-TiO2 is promising for imaging or treatment of breast and cervix tumors. In vitro photodynamic therapy studies have shown that SubPc and SubPc-TiO2 are suitable agents for PDT. In addition, SubPc-TiO2 has higher phototoxicity than SubPc. As a future study, in vivo experiments will be held and performed in tumor-bearing nude mice.

Survival and Function of Fibroblasts Stored as Stock Cultures at a Non-freezing Temperature

1993 ◽  
Vol 21 (2) ◽  
pp. 206-209
Author(s):  
Anders H. G. Andrén ◽  
Anders P. Wieslander
Keyword(s):  
Cell Growth ◽  
Cell Line ◽  
Cell Lines ◽  
Fibroblast Cell ◽  
Freezing Temperature ◽  
Mouse Fibroblast ◽  
Toxic Response ◽  
Normal Manner ◽  
And Function

Cytotoxicity, measured as inhibition of cell growth of cultured cell lines, is a widely used method for testing the safety of biomaterials and chemicals. One major technical disadvantage with this method is the continuous routine maintenance of the cell lines. We decided to investigate the possibility of storing stock cultures of fibroblasts (L-929) in an ordinary refrigerator as a means of reducing the routine workload. Stock cultures of the mouse fibroblast cell line L-929 were prepared in plastic vials with Eagle's minimum essential medium. The vials were stored in a refrigerator at 4–10°C for periods of 7–31 days. The condition of the cells after storage was determined as cell viability, cell growth and the toxic response to acrylamide, measured as cell growth inhibition. We found that the L-929 cell line can be stored for 2–3, weeks with a viabilty > 90% and a cell growth of about 95%, compared to L-929 cells grown and subcultured in the normal manner. The results also show that the toxic response to acrylamide, using refrigerator stored L-929 cells, corresponds to that of control L-929 cells. We concluded that it is possible to store L-929 cells in a refrigerator for periods of up to 3 weeks and still use the cells for in vitro cytotoxic assays.

scholarly journals Phenolic Fractions from Vaccinium vitis-idaea L. and Their Antioxidant and Anticancer Activities Assessment

Antioxidants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1261
Author(s):  
Gabriele Vilkickyte ◽  
Lina Raudone ◽  
Vilma Petrikaite
Keyword(s):  
Antioxidant Activity ◽  
Biological Activity ◽  
Cell Lines ◽  
Radical Scavenging ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
Anticancer Activities ◽  
Cell Renal Cell Carcinoma ◽  
Human Malignant Melanoma ◽  
Ht 29

Lingonberry leaves and fruits are associated with a range of potential bioactivities related to their phenolic content and composition, but the identification of major biological activity markers remains limited. The present study aimed at the isolation of lingonberry phenolic fractions and biological activity evaluation of them. Crude dry extracts of lingonberry leaves and fruits were fractionated by chromatography using Sephadex LH-20 and analyzed by validated HPLC-PDA method. For each fraction, the anticancer activity against human clear cell renal cell carcinoma (CaKi-1), human colon adenocarcinoma (HT-29), and human malignant melanoma (IGR39) cell lines was determined using MTT assay, and the radical scavenging, reducing, and chelating activities were investigated using ABTS, FRAP, and FIC assays, respectively. Further, 28 phenolics were identified and quantified in the crude extract of lingonberry leaves and 37 in the extract of fruits. These compounds, during fractionation steps, were selectively eluted into active fractions, enriched with different groups of phenolics—monophenols, anthocyanins, phenolic acids, catechins, flavonols, or proanthocyanidins. Fractions of lingonberry leaves and fruits, obtained by the last fractionation step, proved to be the most active against tested cancer cell lines and possessed the greatest antioxidant activity. In this perspective, the predominant compounds of these fractions—polymeric and mainly A-type dimeric proanthocyanidins—also quercetin can be considered to be anticancer and antioxidant activity markers of lingonberries.

scholarly journals Design, Synthesis, Molecular Docking, ADME and Biological Evaluation Studies of Some New 1,3,4-oxadiazole Linked Benzimidazoles as Anticancer Agents and Aromatase Inhibitors

2021 ◽  
Author(s):  
ulviye acar çevik ◽  
Ismail Celik ◽  
Ayşen IŞIK ◽  
Yusuf Özkay ◽  
Zafer Asım Kaplancıklı
Keyword(s):  
Molecular Docking ◽  
Cell Line ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Evaluation Studies ◽  
Biological Evaluation ◽  
Binding Modes ◽  
Anticancer Activities ◽  
Mcf 7

Abstract In this study, due to the potential anticancer effects of the benzimidazole ring system, a series of benzimidazole-1,3,4-oxadiazole derivatives were synthesized and characterized by 1H NMR, 13C NMR, and MS spectra analyses. In the in vitro anticancer assay, all the compounds tested anticancer activities using MTT-based assay against five cancer cell lines (MCF-7, A549, HeLa, C6, and HepG2). Among them, compound 5a exhibited the most potent activity with IC50 values of 5,165±0,211 μM and 5,995±0,264 μM against MCF-7 and HepG2 cell lines. Compound 5a was included in the BrdU test to determine the DNA synthesis inhibition effects for both cell types. Furthermore, compound 5c was also found to be more effective than doxorubicin on the HeLa cell line. The selectivity of anticancer activity was evaluated in NIH3T3 (mouse embryo fibroblast cell line) cell line. In vitro, enzymatic inhibition assays of aromatase enzyme were performed for compound 5a acting on the MCF-7 cell line. For compound 5a, in silico molecular docking against aromatase enzyme was performed to determine possible protein-ligand interactions and binding modes.

Novel Chemical Method for Decreasing of Toxicity of Highly Cytotoxic Amidoximes by Introduction of Benzo[4,5]imidazo[2,1-b]thiazolyl Fragment

2018 ◽  
Vol 15 (8) ◽  
pp. 1154-1160
Author(s):  
Edgars Abele ◽  
Ramona Abele ◽  
Lena Golomba ◽  
Ilona Domracheva ◽  
Tatjana Beresneva ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Stereoselective Synthesis ◽  
Fibroblast Cell ◽  
Mouse Fibroblast ◽  
Cytotoxic Agents ◽  
Mouse Hepatoma ◽  
Ic50 Values ◽  
High Cytotoxicity

Aims and Objectives: The aim of the research is to obtain and to investigate the cytotoxicity of a novel class of non-toxic oximes – derivatives of N-(benzo[4,5]imidazo[2,1-b]thiazol-3-ylmethoxy)-ω- (hetarylsulfanyl)-alkanamidines. Materials and Methods: To assess the possible toxicity of the compounds, acute oral LD50 was calculated. The calculations were based on tested compounds IC50 values in relation to 3T3 (mouse fibroblast cell line) using NRU assay. Monolayer tumor cell lines HT-1080 (human fibrosarcoma, ATCC® CCL-121™), MH-22A (mouse hepatoma, ECACC code, 96121721) and NIH/3T3 (mouse Swiss Albino embryo fibroblasts, ATCC® CRL-1658™), were cultured in standard medium (Dulbecco`s modified Eagle`s medium) supplemented with 10% fetal bovine serum (“Sigma”). Results: E-Stereoselective synthesis of novel N-(benzo[4,5]imidazo[2,1-b]thiazol-3-ylmethoxy)-ω- (hetarylsulfanyl)alkanamidines as potential cytotoxic agents was carried out in three steps from corresponding thiones. N-(Benzo[4,5]imidazo[2,1-b]thiazol-3-ylmethoxy)-5-(benzothiazol-2-ylsulfanyl)-pentanamidine exhibits high activity in vitro on the monolayer tumour cell lines: MG-22A (mouse hepatoma) and HT-1080 (human fibrosarcoma). Besides this, the above compound exhibits low toxicity on the 3T3 cell line and low estimated acute oral LD50 (LD50 2759 mg/kg). Conclusion: In conclusion, such dramatic decreasing of expected acute toxicity and high cytotoxicity by the introduction of benzo[4,5]imidazo[2,1-b]thiazolyl fragment into N-hydroxy-ω-(hetarylsulfanyl)alkanamidines were demonstrated for the first time (see, for example, toxicity and cytotoxicity of compound 8b and corresponding unsubstituted oxime).

scholarly journals IN VITRO ANALYSIS OF ANTICANCER POTENTIAL OF TRIGONELLA FOENUM-GRAECUM

2019 ◽  
pp. 189-192
Author(s):  
SHIVSHARAN SINGH ◽  
SATISH K VERMA ◽  
SANTOSH SINGH
Keyword(s):  
Cell Lines ◽  
Bioactive Compounds ◽  
Plant Extract ◽  
Positive Control ◽  
Assay Method ◽  
Anticancer Activities ◽  
Trigonella Foenum Graecum ◽  
Percolation Method ◽  
Ht 29

Objective: The recent work was carried out to evaluate the presence of bioactive compounds and anticancer activities of selected plant Trigonella foenum-graecum extract. Methods: The crude extraction of whole plant was carried out using petroleum ether as a solvent by cold percolation as well as hot percolation method (Soxhlet method) both. The presence of phytochemicals was determined using standard protocols. The anticancer activities were evaluated by sulforhodamine B (SRB) dye assay method using Mitomycin-C (anticancer drug) as a positive control. Results: The qualitative analysis of plant extract showed the presence of bioactive compounds, namely, protein, alkaloids, steroids, phenolics, and flavonoids. The plant extract was tested for in vitro anticancer activity against human liver cancer (HEP-2) and colon cancer (HT-29) cell lines using SRB assay. The plant extract showed significant results against HT-29 and HEP-2 cancer cell lines. Conclusion: The study concluded that the extract of T. foenum-graecum can be further carefully used in herbal formulations for cancer therapy.

scholarly journals Novel N-Substituted Amino Acid Hydrazone-Isatin Derivatives: Synthesis, Antioxidant Activity and Anticancer Activity in 2D and 3D Models In Vitro

2021 ◽  
Vol 22 (15) ◽  
pp. 7799
Author(s):  
Ingrida Tumosienė ◽  
Ilona Jonuškienė ◽  
Kristina Kantminienė ◽  
Vytautas Mickevičius ◽  
Vilma Petrikaitė
Keyword(s):  
Antioxidant Activity ◽  
Colon Adenocarcinoma ◽  
3D Models ◽  
Anticancer Activities ◽  
Antioxidant Power ◽  
3D Cell Cultures ◽  
Ferric Reducing Antioxidant Power ◽  
2D And 3D ◽  
Ht 29

A series of novel mono and bishydrazones each bearing a 2-oxindole moiety along with substituted phenylaminopropanamide, pyrrolidin-2-one, benzimidazole, diphenylmethane, or diphenylamine fragments were synthesized, and their anticancer activities were tested by MTT assay against human melanoma A375 and colon adenocarcinoma HT-29 cell lines. In general, the synthesized compounds were more cytotoxic against HT-29 than A375. 3-((4-Methoxyphenyl)(3-oxo-3-(2-(2-oxoindolin-3-ylidene)hydrazinyl)propyl)amino)-N’-(2-oxoindolin-3-ylidene)propanehydrazide and (N’,N’’’)-1,1’-(methylenebis(4,1-phenylene))bis(5-oxo-N’-(2-oxoindolin-3-ylidene)pyrrolidine-3-carbohydrazide) were identified as the most active compounds against HT-29 in 2D and 3D cell cultures. The same compounds showed the highest antioxidant activity among the synthesized compounds screened by ferric reducing antioxidant power assay (FRAP). Their antioxidant activity is on par with that of a well-known antioxidant ascorbic acid.

scholarly journals Adherence of Group B Streptococci to Human Rectal and Vaginal Epithelial Cell Lines in Relation to Capsular Polysaccharides as well as Alpha-Like Protein Genes – Pilot Study

2013 ◽  
Vol 62 (1) ◽  
pp. 85-90 ◽  
Author(s):  
MALGORZATA BODASZEWSKA-LUBAS ◽  
MONIKA BRZYCHCZY-WLOCH ◽  
PAWEL ADAMSKI ◽  
TOMASZ GOSIEWSKI ◽  
MAGDALENA STRUS ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
Capsular Polysaccharides ◽  
Group B Streptococci ◽  
Significant Difference ◽  
Epithelial Cell Lines ◽  
Group B ◽  
Ht 29

Streptococcus agalactiae (Group B Streptococci, GBS) constitutes a risk factor for infections of the newborns born by colonized mothers. The adherence of GBS to epithelial cells has been proved to be an important factor in the colonization of mucus membranes of both human rectum and vagina. The objective of the study was to assess the adhesion of the selected GBS strains to the human colon adenocarcinoma cell line (HT-29) and human epidermoid vulvo-vaginal cells (A-431) in relation to the capsular polysaccharides and alpha-like protein genes. GBS strains from the human sources belonging to Ia, Ib, II, III and V serotypes possessing different surface alpha-like protein genes such as the alp 2, alp 3, bca, epsilon and rib in the conventional adherence assay were examined. The adherence of GBS strains to the HT-29 cell line was considerably higher than to the A-431 cell line. For GBS serotype Ia and III, a significant difference between the adhesion to the HT-29 and A-431 cell lines was presented. The adhesion of GBS strains to the HT-29 cell line depended on alpha-like protein genes. The most adhesive ones were the GBS strains containing the rib and alp 2 genes. The adherence of GBS strains to the A-431 cell line depended on both their serotype and alpha-like protein genes. Serotype III adhered to the A-431 cells most tightly, particularly the strains containing the rib and alp 2 genes. GBS strains containing the rib gene adhered to the HT-29 and A-431 cell lines more firmly than GBS strains containing other alpha-like protein genes.

scholarly journals Antiproliferative Effect of Epilobium parviflorum Extracts on Colorectal Cancer Cell Line HT-29

2021 ◽  
Vol 26 (6) ◽  
pp. 3120-3128
Author(s):  
M. AYDIN AKBUDAK ◽  
TEVHIDE SUT ◽  
NURANIYE ERUYGUR ◽  
ERSIN AKINCI
Keyword(s):  
Colon Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Fibroblast Cell ◽  
World Health ◽  
Colorectal Cancer Cell Line ◽  
Dependent Manner ◽  
Ht 29

The Epilobium species, rich in various active phytochemicals, have been widely used in folk medicine to treat several diseases including benign prostatic hyperplasia. Despite being demonstrated on some type of cancer cells such as prostate cancer, their potential anti-cancerous role on colorectal adenocarcinoma cells has not been studied yet. According to the World Health Organization (WHO), colon cancer is the third most common form of cancer, resulting over 800 000 deaths every year worldwide. The present study demonstrates the anti-cancerous activity of aqueous and ethanolic Epilobium parviflorum extracts in colon cancer cell line HT-29 cells in vitro. The both type of extracts reduced the cell viability of HT-29 cells in a dose dependent manner. Gene expression analysis of HT-29 cells demonstrated an increase at apoptotic genes, caspase 3 and caspase 8. Nuclear fragmentation of apoptotic cells was also demonstrated through TUNEL assay as well as immunostaining experiments. On the other hand, same lethal concentrations of E. parviflorum extracts were not profound on non-cancerous human fibroblast cell line BJ cells. Our results indicate that E. parviflorum may also be used as a therapeutic agent against colon cancers.

scholarly journals In vitro antimicrobial activity and cytotoxicity of nickel(II) complexes with different diamine ligands

2017 ◽  
Vol 82 (4) ◽  
pp. 389-398 ◽  
Author(s):  
Nenad Draskovic ◽  
Biljana Glisic ◽  
Sandra Vojnovic ◽  
Jasmina Nikodinovic-Runic ◽  
Milos Djuran
Keyword(s):  
Cell Line ◽  
Therapeutic Potential ◽  
Fibroblast Cell ◽  
Skin Wound ◽  
Significant Activity ◽  
Bacterial Strains ◽  
Negative Effects ◽  
Human Lung Fibroblast ◽  
Diamine Ligands

Three diamines, 1,3-propanediamine (1,3-pd), 2,2-dimethyl-1,3-propanediamine (2,2-diMe-1,3-pd) and (?)-1,3-pentanediamine (1,3-pnd), were used for the synthesis of nickel(II) complexes 1?3, respectively, of the general formula [Ni(L)2(H2O)2]Cl2. The stoichiometries of the complexes were confirmed by elemental microanalysis, and their structures were elucidated by spectroscopic (UV?Vis and IR) and molar conductivity measurements. The complexes 1?3, along with NiCl2?6H2O and the diamine ligands, were evaluated against a panel of microbial strains that are associated with skin, wound, urinary tract and nosocomial infections. The obtained results revealed no significant activity of 1?3 against the investigated bacterial strains. On the other hand, they showed good antifungal activity against pathogenic Candida strains, with minimum inhibitory concentration (MIC) values in the range from 15.6 to 62.5 ?g mL-1. The best anti-Candida activity was observed for complex 2 against C. parapsilosis, while the least susceptible to the effect of the complexes was C. krusei. The antiproliferative effect on normal human lung fibroblast cell line MRC-5 was also evaluated in order to determine the therapeutic potential of nickel(II) complexes 1?3. These complexes showed lower negative effects on the viability of the MRC-5 cell line than the clinically used nystatin and comparable selectivity indexes to that of this antifungal drug.

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