scholarly journals Identification of Spiro-Fused Pyrrolo[3,4-a]pyrrolizines and Tryptanthrines as Potential Antitumor Agents: Synthesis and In Vitro Evaluation

2021 ◽  
Vol 22 (21) ◽  
pp. 11997
Author(s):  
Diana. K. Latypova ◽  
Stanislav V. Shmakov ◽  
Sofya A. Pechkovskaya ◽  
Alexander S. Filatov ◽  
Alexander V. Stepakov ◽  
...  
Keyword(s):  
Hela Cell ◽  
Cell Line ◽  
Cervical Carcinoma ◽  
Hela Cells ◽  
Antitumor Agents ◽  
Hela Cell Lines ◽  
M Phase ◽  
Induced Apoptosis ◽  
Potential Antitumor

A series of heterocyclic compounds containing a spiro-fused pyrrolo[3,4-a]pyrrolizine and tryptanthrin framework have been synthesized and studied as potential antitumor agents. Cytotoxicity of products was screened against human erythroleukemia (K562) and human cervical carcinoma (HeLa) cell lines. Among the screened compounds. 4a, 4b and 5a were active against human erythroleukemia (K562) cell line, while 4a and 5a were active against cervical carcinoma (HeLa) cell line. In agreement with the DNA cytometry studies, the tested compounds have achieved significant cell-cycle perturbation with higher accumulation of cells in G2/M phase and induced apoptosis. Using confocal microscopy, we found that with 4a and 5a treatment of HeLa cells, actin filaments disappeared, and granular actin was distributed diffusely in the cytoplasm in 76–91% of cells. We discovered that HeLa cells after treatment with compounds 4a and 5a significantly reduced the number of cells with filopodium-like membrane protrusions (from 63 % in control cells to 29% after treatment) and a decrease in cell motility.

Interaction of Candida albicans with genital mucosa: effect of sex hormones on adherence of yeasts in vitro

1988 ◽  
Vol 34 (3) ◽  
pp. 224-228 ◽  
Author(s):  
Aliza Kalo ◽  
Esther Segal
Keyword(s):  
Candida Albicans ◽  
Hela Cell ◽  
Sex Hormones ◽  
Hela Cells ◽  
Cell Types ◽  
Vaginal Candidiasis ◽  
Genital Mucosa ◽  
Hela Cell Lines ◽  
I Cells

Findings from our previous studies revealed a correlation between the level of adherence in vitro of Candida albicans to human exfoliated vaginal epithelial cells (VEC) and the hormonal status of the cell donors. In the present study we investigated the effect of the sex hormones estradiol, estriol, progesterone, and testosterone on the binding of the yeasts to HeLa cell lines and VEC in vitro. Monolayers of HeLa cells were exposed to the hormones and yeasts under controlled conditions. The number of adherent yeasts per square millimetre of HeLa cell monolayers and the percentage of VEC with adherent yeasts was estimated by microscopic counts. The results showed that the tested sex hormones affected at various degrees the adhesion of yeasts to HeLa cells or VEC. Progesterone had the most marked effect, leading to a significant increase in the number of adherent yeasts to HeLa cells or in the percentage of adhesion of VEC. In addition, VEC were separated on Percoll gradients into the two cell types: superficial (S) and intermediate (I), cell types which appear physiologically under increased serum levels of estradiol or progesterone, respectively. Adhesion assays with the separated cell populations revealed an increased binding capacity of the I cells. The finding that progesterone increased the adherence of yeasts to genital mucosa and that VEC of the I type have a higher capacity to adhere the yeasts is compatible with our previous observation that increased numbers of I cells, appearing under high level of progesterone, are found in situations known to have predisposition to vaginal candidiasis. Thus, our data point to a possible involvement of the hormone progesterone in the adherence of C. albicans to genital epithelium.

An in vitro study of biological safety of condoms and their additives

2003 ◽  
Vol 22 (12) ◽  
pp. 659-664 ◽  
Author(s):  
N A Motsoane ◽  
M J Bester ◽  
E Pretorius ◽  
P J Becker
Keyword(s):  
Hela Cell ◽  
Cell Viability ◽  
Cell Line ◽  
Tumor Cell Line ◽  
Toxic Effects ◽  
Specific Cell ◽  
Epithelial Tumor ◽  
Hela Cell Lines ◽  
Cell Line Hela

The use of condoms to prevent sexually transmitted diseases, especially HIV, is widely encouraged. Condoms contain latex, nonspermicidal lubricants (such as dimethylsiliconium) and other nonspecified compounds, such as colorants and flavorings. Latex causes allergy reaction in susceptible individuals but little is known regarding the cytotoxic effects of other additives. The objective of this study was to develop a sensitive in vitrosystem to determine the toxic effects of condom material. The modified L929 FDA method and a more specific cell type, such as the cervical epithelial tumor cell line HeLa, was used. Lubricated (LC), lubricated and flavored (LFC), and lubricated, flavored and colored condoms (LFCC) were evaluated. Washings containing condom surface material were prepared by washing condom fragments in medium for different time intervals. Changes in cell number, viability and lysosome integrity in the L929 and HeLa cell lines was determined using the Crystal Violet, MTT and Neutral Red assays, respectively. The condom type affected cell viability and lysosome integrity, with LC inducing an increase in cell viability and LFC a decrease in lysosome integrity. The HeLa cell line in combination with the MTT and NR assay was the most sensitive in vitro system to determine the toxic effects of condom material.

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.

scholarly journals Identification of Spiro-Fused [3-azabicyclo[3.1.0]hexane]oxindoles as Potential Antitumor Agents: Initial In Vitro Evaluation of Anti-Proliferative Effect and Actin Cytoskeleton Transformation in 3T3 and 3T3-SV40 Fibroblast

2021 ◽  
Vol 22 (15) ◽  
pp. 8264
Author(s):  
Nickolay A. Knyazev ◽  
Stanislav V. Shmakov ◽  
Sofya A. Pechkovskaya ◽  
Alexander S. Filatov ◽  
Alexander V. Stepakov ◽  
...  
Keyword(s):  
Cell Line ◽  
Antitumor Agents ◽  
Tumor Cell Line ◽  
Proliferative Effect ◽  
In Silico Admet ◽  
Murine Fibroblast ◽  
Membrane Protrusions ◽  
Erythroleukemic Cell ◽  
Potential Antitumor

Novel heterocyclic compounds containing 3-spiro[3-azabicyclo[3.1.0]hexane]oxindole framework (4a, 4b and 4c) have been studied as potential antitumor agents. The in silico ADMET (adsorption, distribution, metabolism, excretion and toxicity) analysis was performed on 4a–c compounds with promising antiproliferative activity, previously synthetized and screened against human erythroleukemic cell line K562 tumor cell line. Cytotoxicity of 4a–c against murine fibroblast 3T3 and SV-40 transformed murine fibroblast 3T3-SV40 cell lines were evaluated. The 4a and 4c compounds were cytotoxic against 3T3-SV40 cells in comparison with those of 3T3. In agreement with the DNA cytometry studies, the tested compounds have achieved significant cell-cycle perturbation with higher accumulation of cells in G0/G1 phase. Using confocal microscopy, we found that with 4a and 4c treatment of 3T3 cells, actin filaments disappeared, and granular actin was distributed diffusely in the cytoplasm in 82–97% of cells. The number of 3T3-SV40 cells with stress fibers increased to 7–30% against 2% in control. We discovered that transformed 3T3-SV40 cells after treatment with compounds 4a and 4c significantly reduced the number of cells with filopodium-like membrane protrusions (from 86 % in control cells to 6–18% after treatment), which indirectly suggests a decrease in cell motility. We can conclude that the studied compounds 4a and 4c have a cytostatic effect, which can lead to a decrease in the number of filopodium-like membrane protrusions.

scholarly journals Design, synthesis and pharmacological evaluation of new 2-oxo-quinoline derivatives containing α-aminophosphonates as potential antitumor agents

MedChemComm ◽  
2017 ◽  
Vol 8 (6) ◽  
pp. 1158-1172 ◽  
Author(s):  
Yan-Cheng Yu ◽  
Wen-Bin Kuang ◽  
Ri-Zhen Huang ◽  
Yi-Lin Fang ◽  
Ye Zhang ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Hepg2 Cell ◽  
Antitumor Agents ◽  
Mitochondrial Pathway ◽  
Quinoline Derivatives ◽  
Design Synthesis ◽  
Pharmacological Evaluation ◽  
M Phase ◽  
Induced Apoptosis ◽  
Potential Antitumor

Novel 2-oxo-quinoline derivatives containing α-aminophosphonates were synthesized as antitumor agents. Compound 5b blocked HepG2 cell cycle at G2/M phase and induced apoptosis in mitochondrial pathway.

scholarly journals Chemopreventive Effect of β-Cryptoxanthin on Human Cervical Carcinoma (HeLa) Cells Is Modulated through Oxidative Stress-Induced Apoptosis

Antioxidants ◽  
2019 ◽  
Vol 9 (1) ◽  
pp. 28 ◽  
Author(s):  
Enkhtaivan Gansukh ◽  
Arti Nile ◽  
Iyyakkannu Sivanesan ◽  
Kannan R. R. Rengasamy ◽  
Doo-Hwan Kim ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Dna Damage ◽  
Cervical Carcinoma ◽  
Hela Cells ◽  
Caspase 3 ◽  
Nuclear Condensation ◽  
Physiological Concentration ◽  
Human Cervical Carcinoma ◽  
Induced Apoptosis

The present study was aimed to assess cellular and molecular events involved in the chemopreventive activities of β-cryptoxanthin derived from mandarin oranges (Citrus unshiu Marc.) on human cervical carcinoma (HeLa) cells. In vitro experiments established that β-cryptoxanthin significantly inhibited the proliferation of HeLa cells with the IC50 value of 4.5 and 3.7 µM after 24 and 48 h of treatments, respectively. β-cryptoxanthin-treated HeLa cells exhibited enhanced levels of oxidative stress correlated with significant downregulation of anti-apoptotic Bcl-2, and upregulation of pro-apoptotic Bax mRNA expression. Moreover, β-cryptoxanthin triggered nuclear condensation and disruption of the integrity of the mitochondrial membrane, upregulated caspase-3, -7, and -9 mRNA, and enhanced activation of caspase-3 proteins, resulting in nuclei DNA damage and apoptosis of HeLa cells. Remarkably, TUNEL assay carried out to detect nuclei DNA damage showed 52% TUNEL-positive cells after treatment with a physiological concentration of β-cryptoxanthin (1.0 μM), which validates its potential as an anticancer drug of natural origin.

Mapping the distribution of Golgi enzymes involved in the construction of complex oligosaccharides

1995 ◽  
Vol 108 (4) ◽  
pp. 1617-1627 ◽  
Author(s):  
C. Rabouille ◽  
N. Hui ◽  
F. Hunte ◽  
R. Kieckbusch ◽  
E.G. Berger ◽  
...  
Keyword(s):  
Golgi Apparatus ◽  
Hela Cell ◽  
Cell Line ◽  
Cell Lines ◽  
Hela Cells ◽  
Stable Expression ◽  
Hela Cell Line ◽  
Specific Antibodies ◽  
Hela Cell Lines ◽  
Golgi Network

The distribution of beta 1,2 N-acetylglucosaminyltransferase I (NAGT I), alpha 1,3-1,6 mannosidase II (Mann II), beta 1,4 galactosyltransferase (GalT), alpha 2,6 sialyltransferase (SialylT) was determined by immuno-labelling of cryo-sections from HeLa cell lines. Antibody labelling in the HeLa cell line was made possible by stable expression of epitope-tagged forms of these proteins or forms from species to which specific antibodies were available. NAGT I and Mann II had the same distribution occupying the medial and trans cisternae of the stack. GalT and SialylT also had the same distribution but they occupied the trans cisterna and the trans-Golgi network (TGN). These results generalise our earlier observations on the overlapping distribution of Golgi enzymes and show that each of the trans compartments of the Golgi apparatus in HeLa cells contains unique mixtures of those Golgi enzymes involved in the construction of complex, N-linked oligosaccharides.

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

Design, Synthesis, In vitro and In silico Evaluation of New Hydrazonebased Antitumor Agents as Potent Akt Inhibitors

2020 ◽  
Vol 17 (11) ◽  
pp. 1380-1392
Author(s):  
Emine Merve Güngör ◽  
Mehlika Dilek Altıntop ◽  
Belgin Sever ◽  
Gülşen Akalın Çiftçi
Keyword(s):  
Cell Line ◽  
Anticancer Agents ◽  
In Silico ◽  
Antitumor Agents ◽  
Colorimetric Assay ◽  
Fibroblast Cell ◽  
Lipinski’S Rule ◽  
In Silico Docking ◽  
Embryonic Fibroblast

Background: Akt is overexpressed or activated in a variety of human cancers, including gliomas, lung, breast, ovarian, gastric and pancreatic carcinomas. Akt inhibition leads to the induction of apoptosis and inhibition of tumor growth and therefore extensive efforts have been devoted to the discovery of potent antitumor drugs targeting Akt. Objectives: The objective of this work was to identify potent anticancer agents targeting Akt. Methods: New hydrazone derivatives were synthesized and investigated for their cytotoxic effects on 5RP7 H-ras oncogene transformed rat embryonic fibroblast and L929 mouse embryonic fibroblast cell lines. Besides, the apoptotic effects of the most active compounds on 5RP7 cell line were evaluated using flow cytometry. Their Akt inhibitory effects were also investigated using a colorimetric assay. In silico docking and Absorption, Distribution, Metabolism and Excretion (ADME) studies were also performed using Schrödinger’s Maestro molecular modeling package. Results and Discussion: Compounds 3a, 3d, 3g and 3j were found to be effective on 5RP7 cells (with IC50 values of <0.97, <0.97, 1.13±0.06 and <0.97 μg/mL, respectively) when compared with cisplatin (IC50= 1.87±0.15 μg/mL). It was determined that these four compounds significantly induced apoptosis in 5RP7 cell line. Among them, N'-benzylidene-2-[(4-(4-methoxyphenyl)pyrimidin- 2-yl)thio]acetohydrazide (3g) significantly inhibited Akt (IC50= 0.5±0.08 μg/mL) when compared with GSK690693 (IC50= 0.6±0.05 μg/mL). Docking studies suggested that compound 3g showed good affinity to the active site of Akt (PDB code: 2JDO). According to in silico ADME studies, the compound also complies with Lipinski's rule of five and Jorgensen's rule of three. Conclusion: Compound 3g stands out as a potential orally bioavailable cytotoxic agent and apoptosis inducer targeting Akt.

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