scholarly journals Effect of Selected Silyl Groups on the Anticancer Activity of 3,4-Dibromo-5-Hydroxy-Furan-2(5H)-one Derivatives

2021 ◽  
Vol 14 (11) ◽  
pp. 1079
Author(s):  
Radoslaw Kitel ◽  
Anna Byczek-Wyrostek ◽  
Katarzyna Hopko ◽  
Anna Kasprzycka ◽  
Krzysztof Walczak
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Systematic Investigation ◽  
Silyl Group ◽  
Silyl Groups ◽  
Clonogenic Potential ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Silicon Based ◽  
The Impact

The pharmacological effects of carbon to silicon bioisosteric replacements have been widely explored in drug design and medicinal chemistry. Here, we present a systematic investigation of the impact of different silyl groups on the anticancer activity of mucobromic acid (MBA) bearing furan-2(5H)-one core. We describe a comprehensive characterization of obtained compounds with respect to their anticancer potency and selectivity towards cancer cells. All four novel compounds exert stronger antiproliferative activity than MBA. Moreover, 3b induce apoptosis in colon cancer cell lines. A detailed investigation of the mechanism of action revealed that 3b activity stems from the down-regulation of survivin and the activation of caspase-3. Furthermore, compound 3b attenuates the clonogenic potential of HCT-116 cells. Interestingly, we also found that depending on the type of the silyl group, compound selectivity towards cancer cells could be precisely controlled. Collectively, we demonstrated the utility of silyl groups for adjusting both the potency and selectivity of silicon-containing compounds. These data reveal a link between the types of silyl group and compound potency, which could have bearings for the design of novel silicon-based anticancer drugs.

scholarly journals Limonene and BEZ 235 inhibits growth of COLO-320 and HCT-116 colon cancer cells

2016 ◽  
Vol 8 (3) ◽  
pp. 89 ◽  
Author(s):  
Raja Ratna Reddy Yakkanti ◽  
P Chandra Sekhar ◽  
K Bharath Nandhan Reddy ◽  
S Ramamoorthy ◽  
S Ranga Suresh ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Cancer Cells ◽  
Colon Cancer Cells ◽  
Wild Type ◽  
Anticancer Effects ◽  
Clonogenic Potential ◽  
Hct 116 ◽  
Cancer Types ◽  
Hct 116 Cells ◽  
Preclinical And Clinical Studies

<p>D-Limonene is a dietary monoterpene with significant anticancer activity against many cancer types in preclinical and clinical studies. The study is designed to investigate synergistic anticancer effects of limonene and BEZ235 combination in COLO-320 and HCT-116 colon cancer cells. Cells were treated with both the drugs alone and in combination and the effects on cell viability; cell migration and clonogenic potential were examined. Results show that both drugs exhibited dose and time dependant cytotoxicity on the cell lines tested. CompuSyn analysis of the drug combination effects revealed the strong synergistic interaction of the combination. Our results also indicate that COLO-320 cells were more sensitive for anticancer effects of the drugs than HCT-116 cells. The presence of Ras and PI3K mutations in HCT-116 cells could possibly be one of the main reasons for the observed outcome as compared to the wild type expressions of them in COLO-320 cells.</p>

scholarly journals Ultrasound-enhanced biosynthesis of uniform ZnO nanorice using Swietenia macrophylla seed extract and its in vitro anticancer activity

2021 ◽  
Vol 10 (1) ◽  
pp. 572-585
Author(s):  
Darren Yi Sern Low ◽  
Camille Keisha Mahendra ◽  
Janarthanan Supramaniam ◽  
Loh Teng Hern Tan ◽  
Learn Han Lee ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Hexagonal Wurtzite Structure ◽  
Colon Cancer Cells ◽  
Swietenia Macrophylla ◽  
Zno Nps ◽  
Human Colon Cancer ◽  
Hct 116

Abstract In this study, ultrasonically driven biosynthesis of zinc oxide nanoparticles (ZnO NPs) using Swietenia macrophylla seed ethyl acetate fraction (SMEAF) has been reported. X-ray powder diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR) analyses confirmed the presence of a pure hexagonal wurtzite structure of ZnO. Field emission scanning electron microscope images revealed the formation of uniquely identifiable uniform rice-shaped biologically synthesized ZnOSMEAF particles. The particle sizes of the biosynthesized NPs ranged from 262 to 311 nm. The underlying mechanisms for the biosynthesis of ZnOSMEAF under ultrasound have been proposed based on FTIR and XRD results. The anticancer activity of the as-prepared ZnOSMEAF was investigated against HCT-116 human colon cancer cell lines via methyl thiazolyl tetrazolium assay. ZnOSMEAF exhibited significant anticancer activity against colon cancer cells with higher potency than ZnO particles prepared using the chemical method and SMEAF alone. Exposure of HCT-116 colon cancer cells to ZnOSMEAF promoted a remarkable reduction in cell viability in all the tested concentrations. This study suggests that green sonochemically induced ZnO NPs using medicinal plant extract could be a potential anticancer agent for biomedical applications.

Phytochemical analysis and anticancer activity of seaweed Eucheuma Sp. against colon HCT-116 cells

2019 ◽  
Author(s):  
Priscilla Aya Maheswari Subroto ◽  
Ade Arsianti ◽  
Trivani Putri ◽  
Elvira Lesmana
Keyword(s):  
Anticancer Activity ◽  
Phytochemical Analysis ◽  
Hct 116 ◽  
Hct 116 Cells

Induction of p53 contributes to apoptosis of HCT-116 human colon cancer cells induced by the dietary compound fisetin

2009 ◽  
Vol 296 (5) ◽  
pp. G1060-G1068 ◽  
Author(s):  
Do Y. Lim ◽  
Jung Han Yoon Park
Keyword(s):  
Colon Cancer ◽  
Cancer Cells ◽  
Death Receptor ◽  
Parp Cleavage ◽  
Caspase 8 ◽  
Colon Cancer Cells ◽  
Protein Levels ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Induced Apoptosis

Fisetin, or 3,3′,4′,7-tetrahydroxyflavone, is present in fruits and vegetables and has been previously reported to inhibit the proliferation of a variety of cancer cells (Lu X, Jung J, Cho HJ, Lim do Y, Lee HS, Chun HS, Kwon DY, Park JH. J Nutr 135: 2884–2890, 2005). We have demonstrated in a previous work that 20–60 μmol/l fisetin inhibits cyclin-dependent kinase activities resulting in cell cycle arrest in HT-29 colon cancer cells. In the present study, we attempted to characterize the mechanisms by which fisetin induces apoptosis in HCT-116 cells. DNA condensations, cleavage of poly(ADP-ribose) polymerase (PARP), and cleavage of caspases 9, 7, and 3 were induced in HCT-116 cells treated with 5–20 μmol/l of fisetin. Fisetin induced a reduction in the protein levels of antiapoptotic Bcl-xL and Bcl-2 and an increase in the levels of proapoptotic Bak and Bim. Fisetin did not affect the Bax protein levels, but induced the mitochondrial translocation of this protein. Fisetin also enhanced the permeability of the mitochondrial membrane and induced the release of cytochrome c and Smac/Diablo. Additionally, fisetin caused an increase in the protein levels of cleaved caspase-8, Fas ligand, death receptor 5, and TNF-related apoptosis-inducing ligand, and the caspase-8 inhibitor Z-IETD-FMK suppressed fisetin-induced apoptosis and the activation of caspase-3. Furthermore, fisetin increases p53 protein levels, and the inhibition of p53 expression by small interference RNA resulted in a decrease in the fisetin-induced translocation of Bax to the mitochondria, release of mono- and oligonucleosome in the cytoplasm, and PARP cleavage. These results show that fisetin induces apoptosis in HCT-116 cells via the activation of the death receptor- and mitochondrial-dependent pathway and subsequent activation of the caspase cascade. The induction of p53 results in the translocation of Bax to the mitochondria, which contributes to fisetin-induced apoptosis in HCT-116 cells.

scholarly journals Suppression of ID1 expression in colon cancer cells increases sensitivity to 5-fluorouracil

2017 ◽  
Vol 64 (2) ◽  
Author(s):  
Tomasz Przybyła ◽  
Monika Sakowicz-Burkiewicz ◽  
Izabela Maciejewska ◽  
Hanna Bielarczyk ◽  
Tadeusz Pawełczyk
Keyword(s):  
Colon Cancer ◽  
Cancer Cells ◽  
Thymidine Phosphorylase ◽  
Dihydropyrimidine Dehydrogenase ◽  
Mrna Level ◽  
Colon Cancer Cells ◽  
Altered Expression ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Ht 29

Adjuvant chemotherapy with 5-fluorouracil remains the basic treatment for patients with advanced colorectal carcinoma. The major obstacle in successful treatment is an ability of CRC cells to acquire chemoresistance. Here we examined the impact of ID1 silencing on the sensitivity of CRC cells to 5-FU. To suppress ID1 expression in HT-29 and HCT-116 cells the cells were transduced with a lentiviral vector carrying the ID1 silencing sequence. Cells with silenced ID1 showed altered expression of epithelial and mesenchymal markers and exhibited increased proliferation rate compared to the parental cells. HCT-116 cells with suppressed ID1 became sensitized to 5-FU and this was not observed in HT-29 cells. Silencing ID1 resulted in altered expression of genes encoding enzymes metabolizing 5-FU. HT-29 cells with suppressed ID1 had significantly reduced mRNA level for thymidine phosphorylase, uridine-cytydine kinase 2 and dihydropyrimidine dehydrogenase. ID1 suppression in HCT-116 cells resulted in an increase of mRNA level for thymidine phosphorylase, thymidyne kinase and uridine-cytydine kinase 2 with concurrent drop of dihydropyrimidine dehydrogenase and thymidylate synthetase mRNA levels. In conclusion ID1 expression impacts the sensitivity of colon cancer cells to 5-FU and may be considered as potential predictive marker in CRC treatment.

scholarly journals Potentiation of Cisplatin Activity in Colorectal Cancer Cells by Lovastatin

2019 ◽  
pp. 1-6 ◽  
Author(s):  
Sameer E. Alharthi
Keyword(s):  
Colorectal Cancer ◽  
Cancer Cells ◽  
Cellular Uptake ◽  
Glycoprotein P ◽  
P Glycoprotein ◽  
Colorectal Cancer Cells ◽  
Cytocidal Effect ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Lovastatin Treatment

Cisplatin (CIS) is an anticancer drugs used in the treatment of several solid tumors with nephrotoxicity as its main toxic effect. The current study was directed to assess the role of hypolipidemic drug (lovastatin) on sensitization of human colorectal cancer cells (HCT -116) to the action of CIS. This study assessed the action of lovastatin on sensitization of colorectal cancer cells to       cisplatin by examining cisplatin cytotoxicity, cisplatin cellular uptake and P-glycoprotein (P-gp) activity in presence and absence of Lovastatin 10 and 30 ug/ml. Lovastatin treatment at dose level of 10 and 30 µg/ml potentiated the cytocidal effect of cisplatin against the growth of HCT-116 cells with IC50 7.3 and 5.4 µg/ml, respectively compare to 18 µg/ml after treatment with cisplatin      alone. Moreover, lovastatin increased the uptake of cisplatin into colorectal cancer cells with marked inhibition of P-glycoprotein pump. On conclusion Lovastatin treatment increases the antiproliferative activity of cisplatin against the growth of colorectal cancer cells due to inhibition the activity P-glycoprotein pump with marked increase in its cellular uptake.

scholarly journals ID: 1029 Effects of carnosine on regulation of migration and invasion in human colorectal cancer cells

2017 ◽  
Vol 4 (S) ◽  
pp. 104 ◽  
Author(s):  
Po-Yu Lai ◽  
Shu-Chen Hsieh ◽  
Chih-Chung Wu ◽  
Shu-Ling Hsieh
Keyword(s):  
Colorectal Cancer ◽  
Colon Cancer ◽  
Cancer Cells ◽  
Human Colon ◽  
Migration And Invasion ◽  
Colon Cancer Cells ◽  
Human Colon Cancer ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Human Colon Cancer Cells

Colorectal cancer is the third most commonly diagnosed cancer in the word. Carnosine is an endogenous dipeptide found in vertebrate skeletal muscles. It is known to have anti-fatigue, antioxidative, antihypertensive, antidiabetic, and cancer inhibiting effects. However, little research has been done regarding its influence on the metastasis of colon cancer. This study cultivated HCT-116 human colon cancer cells as a test model in order to investigate the impact of carnosine on the migration and invasion of human colon cancer cells. The results showed that 48-hour treatments of HCT-116 cells with 0.5, 1, or 5 mM carnosine each significantly inhibited the migration ability of the cells (P < 0.05). The 48-hour treatments with 0.5, 1, or 5 mM carnosine were also found to significantly reduce MMP-9 activity (P < 0.05), but not MMP-2 expression. Furthermore, when HCT-116 cells treated with 1 or 5 mM carnosine, invasion ability are significantly decreased and significantly increased E-cadherin expression (P < 0.05). On the other hand, the protein of TIMP-1, an inhibitor of MMP-9, is signification increased after 1 or 5 mM carnosine treatment (P<0.05). In addition, the u-PA protein level are significantly decreased after carnosine treatment. The results indicate that carnosine can regulate the migration and invasion by regulating MMPs and its regulator molecular expression in HCT-116 cells.

scholarly journals Activations of Both Extrinsic and Intrinsic Pathways in HCT 116 Human Colorectal Cancer Cells Contribute to Apoptosis through p53-Mediated ATM/Fas Signaling byEmilia sonchifoliaExtract, a Folklore Medicinal Plant

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Yu-Hsuan Lan ◽  
Jo-Hua Chiang ◽  
Wen-Wen Huang ◽  
Chi-Cheng Lu ◽  
Jing-Gung Chung ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Cancer Cells ◽  
Major Constituent ◽  
Herbaceous Plant ◽  
Human Colorectal Cancer ◽  
Colorectal Cancer Cells ◽  
Fas Signaling ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Human Colorectal Cancer Cells

Emilia sonchifolia(L.) DC (Compositae), an herbaceous plant found in Taiwan and India, is used as folk medicine. The clinical applications include inflammation, rheumatism, cough, cuts fever, dysentery, analgesic, and antibacteria. The activities ofEmilia sonchifoliaextract (ESE) on colorectal cancer cell death have not been fully investigated. The purpose of this study explored the induction of apoptosis and its molecular mechanisms in ESE-treated HCT 116 human colorectal cancer cellsin vitro. The methanolic ESE was characterized, and γ-humulene was formed as the major constituent (63.86%). ESE induced cell growth inhibition in a concentration- and time-dependent response by MTT assay. Apoptotic cells (DNA fragmentation, an apoptotic catachrestic) were found after ESE treatment by TUNEL assay and DNA gel electrophoresis. Alternatively, ESE stimulated the activities of caspase-3, -8, and -9 and their specific caspase inhibitors protected against ESE-induced cytotoxicity. ESE promoted the mitochondria-dependent and death-receptor-associated protein levels. Also, ESE increased ROS production and upregulated the levels of ATM, p53, and Fas in HCT 116 cells. Strikingly, p53 siRNA reversed ESE-reduced viability involved in p53-mediated ATM/Fas signaling in HCT 116 cells. In summary, our result is the first report suggesting that ESE may be potentially efficacious in the treatment of colorectal cancer.

Anticancer Activity of Mixed Doxorubicin and Pravastatin in Nanoemulsions Against HCT 116 Colon Cancer Cells

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Mayson Alkhatib ◽  
Retnowati . ◽  
Amalia F.
Keyword(s):  
Colon Cancer ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Therapeutic Potential ◽  
Morphological Changes ◽  
Weight Ratio ◽  
Nuclear Staining ◽  
Colon Cancer Cells ◽  
Fixed Weight ◽  
Hct 116

Combining drugs with different mechanism of action in nanocarriers is becoming a promising strategy in cancer therapy. In the present study, the anticancer activity of the combination of doxorubicin (DOX) and pravastatin (PRV) loaded in nanoemulsions (NEs) was evaluated in HCT 116 colon cancer cells. The NE formulas (NEa and NEb) consisted of different weight fractions of the surfactant mixture of Eumulgin HRE 40/ Soya phosphatidylcholine/ sodium oleate at a fixed weight ratio of 3.5:3.0:3.5, cholesterol (CHO), Tris- HCl buffer (pH 7.22), and 1-octanol. The cytotoxicity of the drug formulas, loaded in either water or NEs, was assessed through 3-(4, 5 Dimethylthiazole- 2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay, while the mechanism of cell death was determined by observing the morphological changes of treated cells under light microscope and identifying apoptosis by using the ApopNexin FITC kit and DAPI nuclear staining. It has been found that reducing the concentration of DOX from 15 to 7.5µM by formulating it with 7.5µM of PRV in NEa (NEa (1 DOX:1 PRV)) has preserved its cytotoxicity against HCT-116 cancer cells. The present study proved that the combination of the PRV and DOX loaded in NEa formulations improved the therapeutic potential of both of PRV and DOX as anticancer drugs.

Unexpected Growth-Promoting Effect of Oxaliplatin in Excision Repair Cross-Complementation Group 1 Transfected Human Colon Cancer Cells

Pharmacology ◽  
2018 ◽  
Vol 102 (3-4) ◽  
pp. 161-168 ◽  
Author(s):  
Lars Petter Jordheim ◽  
Kamel Chettab ◽  
Emeline Cros-Perrial ◽  
Eva-Laure Matera ◽  
Charles Dumontet
Keyword(s):  
Cancer Cells ◽  
Excision Repair ◽  
Complementation Group ◽  
Human Colon Cancer ◽  
Repair Capacity ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Group 1

The nucleotide excision repair protein excision repair cross-complementation group 1 (ERCC1) has been repeatedly shown to be involved in the sensitivity of cancer cells to platinum derivatives. In order to better understand this process, we transfected HCT-116 cells with a plasmid encoding ERCC1 and studied their in vitro and in vivo behaviour. No main differences were observed for sensitivity to platinum drugs, DNA repair capacity and clonogenicity in vitro. However, ­ERCC1-transfected HCT-116 cells showed paradoxical behaviour in vivo with increased growth in mice treated with oxaliplatin as compared to untreated mice. The Trop2 protein was identified as being potentially involved in the underlying mechanism for these observations, as it was overexpressed in transfected cells. Our results suggest complex regulation of signalling in cancer cells exposed to cancer drugs.

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