scholarly journals Synthesis and Preliminary Anticancer Activity Assessment of N-Glycosides of 2-Amino-1,3,4-thiadiazoles

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7245
Author(s):  
Katarzyna Żurawska ◽  
Marcin Stokowy ◽  
Patryk Kapica ◽  
Monika Olesiejuk ◽  
Agnieszka Kudelko ◽  
...  
Keyword(s):  
Hela Cells ◽  
Biological Response ◽  
Molecular Iodine ◽  
G1 Phase ◽  
Activity Assessment ◽  
Apoptotic Effect ◽  
Hct 116 ◽  
Thiadiazole Derivatives ◽  
Hct 116 Cells ◽  
Mcf 7

The addition of 2-amino-1,3,4-thiadiazole derivatives with parallel iodination of differently protected glycals has been achieved using a double molar excess of molecular iodine under mild conditions. The corresponding thiadiazole derivatives of N-glycosides were obtained in good yields and anomeric selectivity. The usage of iodine as a catalyst makes this method easy, inexpensive, and successfully useable in reactions with sugars. Thiadiazole derivatives were tested in a panel of three tumor cell lines, MCF-7, HCT116, and HeLa. These compounds initiated biological response in investigated tumor models in a different rate. The MCF-7 is resistant to the tested compounds, and the cytometry assay indicated low increase in cell numbers in the sub- G1 phase. The most sensitive are HCT-116 and HeLa cells. The thiadiazole derivatives have a pro-apoptotic effect on HCT-116 cells. In the case of the HeLa cells, an increase in the number of cells in the sub-G1- phase and the induction of apoptosis was observed.

scholarly journals Design, Syntheses, and Bioevaluations of Some Novel N2-Acryloylbenzohydrazides as Chemostimulants and Cytotoxic Agents

Medicines ◽  
2021 ◽  
Vol 8 (6) ◽  
pp. 27
Author(s):  
Kinjal Lakhani ◽  
Edgar A. Borrego ◽  
Karla G. Cano ◽  
Jonathan R. Dimmock ◽  
Renato J. Aguilera ◽  
...  
Keyword(s):  
Antineoplastic Agent ◽  
Cytotoxic Agents ◽  
Breast Cancer Cell Lines ◽  
Molecular Features ◽  
In Series ◽  
Hct 116 ◽  
Related Series ◽  
Hct 116 Cells ◽  
Related Compounds ◽  
Mcf 7

A series of novel N2-acryloylhydrazides 1a–m and a related series of compounds 6a–c were prepared as potential chemostimulants. In general, these compounds are cytotoxic to human HCT 116 colon cancer cells, as well as human MCF-7 and MDA-MB-231 breast cancer cell lines. A representative compound N1-(3,4-dimethoxyphenylcarbonyl)-N2-acryloylhydrazine 1m sensitized HCT 116 cells to the potent antineoplastic agent 3,5-bis(benzylidene)-4-piperidone 2a, and also to 5-fluorouracil. A series of compounds was prepared that incorporated some of the molecular features of 2a and related compounds with various N2-acryloylhydrazides in series 1. These compounds are potent cytotoxins. Two modes of action of representative compounds are the lowering of mitochondrial membrane potential and increasing the concentration of reactive oxygen species.

scholarly journals CYTOTOXIC LABDANE DITERPENOIDS FROM ANDROGRAPHIS PANICULATA (BURM.F.) NEES

2017 ◽  
Vol 10 (12) ◽  
pp. 99 ◽  
Author(s):  
Maria Carmens Tan ◽  
Glenn G Oyong ◽  
Chien Chang Shen ◽  
Consolacion Y Ragasa
Keyword(s):  
Dermal Fibroblasts ◽  
Multiple Comparison ◽  
Wild Type ◽  
Significant Difference ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Labdane Diterpenoids ◽  
Post Hoc ◽  
Ht 29 ◽  
Mcf 7

Objective: The primary objective of this study was to probe the cytotoxic capacity of the labdane diterpenoids andrographolide (1), 14-deoxyandrographolide (2), 14-deoxy-12-hydroxyandrographolide (3), and neoandrographolide (4) on mutant and wild-type immortalized cell lines.Methods: Breast adenocarcinoma (MCF-7), colon carcinomas (HCT-116 and HT-29), small cell lung carcinoma (H69PR), human acute monocytic leukemia (THP-1), and wild-type primary normal human dermal fibroblasts - neonatal cells (HDFn) were incubated with 1-4, and the degree of cytotoxicity was analyzed by employing the in vitro PrestoBlue® cell viability assay. Working solutions of 1-4 were prepared in complete cell culture medium to a final non-toxic dimethyl sulfoxide concentration of 0.2%. The plates were incubated at 37°C with 5% CO2 in a 98% humidified incubator throughout the assay. Nonlinear regression and statistical analyses were done to extrapolate the half maximal inhibitory concentration 50% (IC50). One-way ANOVA (p<0.05) and multiple comparison, Tukey’s post hoc test (p<0.05), were used to compare different pairs of data sets. Results were considered statistically significant at p<0.05.Results: The highest cytotoxicity index was exhibited by the H69PR and 1 trials which displayed the lowest IC50 value of 3.66 μg/mL, followed by HT-29 treated with 2, HCT-116 and 1 trials, and H69PR treated with 4 (IC50=3.81, 3.82, and 4.19 μg/mL, respectively). Only 1 and 4 were detrimental toward MCF-7, while 1, 3, and 4 were degenerative against H69PR. Tukey’s post hoc multiple comparison indicated no significant difference in the cytotoxicity of 1-4 on HCT-116 cells which afforded IC50 values ranging from 3.82 to 5.12 μg/mL. Evaluation of the two colon carcinoma cell lines showed that HCT-116 was categorically more susceptible to cellular damage caused by treatments with 1-4 than was HT-29. Cytotoxicity was not detected in THP-1 and HDFn cells (IC50>100 μg/mL).Conclusion: Diterpenoids 1-4 isolated from the dichloromethane extract of the leaves of A. paniculata exhibited different cytotoxic activities against MCF-7, HCT-116, HT-29, and H69PR. All constituents had comparable action on HCT-116 cells but were not found to be cytotoxic to normal HDFn cells and mutant THP-1 cells.

Immunological evaluation of the entirely carbohydrate-based Thomsen-Friedenreich – PS B conjugate

2016 ◽  
Vol 14 (13) ◽  
pp. 3350-3355 ◽  
Author(s):  
Kevin R. Trabbic ◽  
Jean-Paul Bourgault ◽  
Mengchao Shi ◽  
Matthew Clark ◽  
Peter R. Andreana
Keyword(s):  
T Cell ◽  
Tumor Antigen ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Immunological Evaluation ◽  
Mcf 7 ◽  
Zwitterionic Polysaccharide

PS B, a CD4+T-cell stimulating zwitterionic polysaccharide fromB. fragilis, was conjugated with aminooxy TF tumor antigen. Immunization revealed Ab specificity to TF. FACS revealed Ab binding to MCF-7 but not HCT-116 cells.

scholarly journals PHYTOCHEMICAL COMPOSITION AND ANTICANCER ACTIVITY OF SEAWEEDS ULVA LACTUCA AND EUCHEUMA COTTONII AGAINST BREAST MCF-7 AND COLON HCT-116 CELLS

2016 ◽  
Vol 9 (6) ◽  
pp. 115 ◽  
Author(s):  
Ade Arsianti Arsianti ◽  
Fadilah Fadilah ◽  
Kusmardi Suid ◽  
Fatmawaty Yazid ◽  
Lies Kurniati Wibisono ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Positive Result ◽  
Ethyl Acetate ◽  
Anticancer Activity ◽  
Ulva Lactuca ◽  
Phytochemical Composition ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Eucheuma Cottonii ◽  
Mcf 7

Objective: this study is aimed to develop marine resources which is focused on the determination of  phytochemical composition and exploration of seaweeds Ulva Lactuca and Eucheuma cotonii, as a potential  anti-breast cancer and anti-colorectal cancer agents. Methods: Seaweeds Ulva Lactuca collected from Parangtritis beach, Yogyakarta, Central Java, Indonesia. Whereas Eucheuma cottonii collected from Salemo island, South Sulawesi, Indonesia. Seaweeds U. lactuca and E. cottonii were macerated in organic solvents, n-hexane, chloroform, ethyl acetate and ethanol, respectively. After maceration for three days, the mixture was filtered, the filtrate was concentrated by rotary evaporator. The concentrated extract of n-hexane, ethyl acetate, ethanol and chloroform were then analyzed by thin layer chromatography. Phytochemical test of the concentrated extract were conducted to identify the metabolites containing in the seaweeds. Furthermore, the cytotoxic activity of the n-hexane, ethyl acetate, ethanol and chloroform extract of Ulva Lactuca and Eucheuma cotonii were evaluated as a growth inhibitor of breast MCF-7 and colorectal HCT-116 cancer cells by MTT cell proliferation assay. Results: Phytochemical test  for the  concentrated extracts of Ulva Lactuca showed the positive result for metabolites of  steroids, glycosides, flavonoid,and tannin. While  the concentrated extracts of E. cottonii showed positive result for metabolites of steroids, glycosides, and flavonoid. Both concentrated extracts of Ulva lactuca and Eucheuma cotonii exhibited anticancer activity against breast MCF-7 and colorectal HCT-116 cells with IC50 ranging of  21 µg/mL  to  99 µg/mL . Conclusion: Our results clearly demonstrate seaweeds Ulva Lactuca and Eucheuma cotonii as a promising candidates for the  new anti-breast and anti-colorectal cancer agents. Keywords: Phytochemistry, Ulva Lactuca, Eucheuma cotonii , anticancer, breast MCF-7, colorectal HCT-116

scholarly journals Inhibitory Effects of Peptide Lunasin in Colorectal Cancer HCT-116 Cells and Their Tumorsphere-Derived Subpopulation

2020 ◽  
Vol 21 (2) ◽  
pp. 537 ◽  
Author(s):  
Samuel Fernández-Tomé ◽  
Fei Xu ◽  
Yanhui Han ◽  
Blanca Hernández-Ledesma ◽  
Hang Xiao
Keyword(s):  
Colorectal Cancer ◽  
Cell Cycle ◽  
Kinase Inhibitor ◽  
G1 Phase ◽  
Inhibitory Effects ◽  
Cyclin Dependent Kinase Inhibitor ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Induced Apoptosis ◽  
Chemopreventive Activity

The involvement of cancer stem-like cells (CSC) in the tumor pathogenesis has profound implications for cancer therapy and chemoprevention. Lunasin is a bioactive peptide from soybean and other vegetal sources with proven protective activities against cancer and other chronic diseases. The present study focused on the cytotoxic effect of peptide lunasin in colorectal cancer HCT-116 cells, both the bulk tumor and the CSC subpopulations. Lunasin inhibited the proliferation and the tumorsphere-forming capacity of HCT-116 cells. Flow cytometry results demonstrated that the inhibitory effects were related to apoptosis induction and cell cycle-arrest at G1 phase. Moreover, lunasin caused an increase in the sub-GO/G1 phase of bulk tumor cells, linked to the apoptotic events found. Immunoblotting analysis further showed that lunasin induced apoptosis through activation of caspase-3 and cleavage of PARP, and could modulate cell cycle progress through the cyclin-dependent kinase inhibitor p21. Together, these results provide new evidence on the chemopreventive activity of peptide lunasin on colorectal cancer by modulating both the parental and the tumorsphere-derived subsets of HCT-116 cells.

scholarly journals Anti-Proliferative and Pro-Apoptotic Activities of Hederacolchiside A1 On MCF-7 Cells Via ROS Regulation and JAK2/STAT3 Inactivation

2021 ◽  
Author(s):  
Aijun Chen ◽  
Shushu Zhang ◽  
Dandan Zhang ◽  
Xingjiang Hu ◽  
Nana Xu ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Ros Generation ◽  
Caspase 9 ◽  
Apoptotic Pathway ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
Induced Apoptosis ◽  
Mcf 7

Abstract Many studies have shown that hederacolchiside A1 (HA1) is an important anticancer saponin, although its mechanism of action and in vivo investigations are still lacking. Our previous results revealed that HA1 may have the potential to treat breast cancer. Therefore, we attempted to verify the potential anti-breast cancer effect of HA1 in vitro and in vivo. MTT, flow cytometry, DCFH-DA fluorescence microscopy, and western blotting were used to evaluate the activities and mechanisms of action of HA1. Athymic nude mice were used to demonstrate the antitumor activity of HA1 in vivo. HA1 exhibited significant cytotoxic effects on HepG2, MCF-7, MDA-MB-231, SKBr-3, HT-29, and HCT-116 cells, especially MCF-7 cells. HA1 blocked the sub-G1 and G0/G1 phases, induced apoptosis, promoted reactive oxygen species (ROS) generation, and decreased the mitochondrial membrane potential of MCF-7 cells. HA1 upregulated Bax and downregulated Bcl-2 levels and activated caspase-9 and caspase-3 in MCF-7 cells Meanwhile, HA1 inhibited the phosphorylation of JAK2/STAT3 in MCF-7 cells. In addition, 50 and 100 mg/kg HA1 significantly inhibited the growth of transplanted tumors with inhibition rates of 46.95 ± 26.72% and 48.45 ± 22.36%, respectively. This preliminary study demonstrated that HA1 could inhibit proliferation and induce the apoptosis of MCF-7 cells via ROS-mediated activation of the mitochondrial apoptotic pathway and JAK2/STAT3 inactivation. HA1 may therefore be developed as a novel agent for breast cancer therapy.

scholarly journals The Potential of 9,10-Anthraquinone in Inhibiting Human Cancer Cells Growth

2021 ◽  
Vol 15 (1) ◽  
pp. 19
Author(s):  
Irmanida Batubara ◽  
Arif Rakhman Hakim ◽  
Silmi Mariya ◽  
Suminar Setiati Achmadi ◽  
Valentina Sokoastri Valentina Sokoastri ◽  
...  
Keyword(s):  
Gene Expression ◽  
Cell Growth ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Hela Cells ◽  
Human Cancer ◽  
Cancer Cell Growth ◽  
Human Cancer Cells ◽  
Hct 116 ◽  
Mcf 7

Background: 9,10-Anthraquinone (9,10-AQ) is a contaminant on some agricultural products and considered as carcinogenic based on EU Regulation No. 1146/2014. Except for little evidence on experimental rats, there is no strong proof regarding the carcinogenicity in humans. Therefore, it is essential to find a safe dose of this compound since the difference in 9,10-AQ levels will affect cancer cell growth. This research aims to find the 9,10-AQ concentration that does not proliferate the human cancer cells under in vitro study.Methods: In determining the 9,10-AQ concentration that does not proliferate the cancer cells growth, 0.01 to 500 mg/L 9,10-AQ was directly tested on four human cancer cells (colorectal carcinoma HCT 116, colon adenocarcinoma WiDr, breast cancer MCF-7, and cervical cancer HeLa), and the viability of the cells was counted via (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide) assay. In the gene expression level, the effects on a selected cancer cell line were determined by qRT-PCR against BAX, BCL-2, PCNA, and P53.Results: The result indicates that 9,10-AQ up to 500 mg/L concentration does not proliferate the cell’s growth but instead inhibits those four cancer cells’ growths. The concentration of 9,10-AQ that inhibits 50% the cancer cells growth (IC50) value was 321.8 mg/L (1.55 mM) against HCT 116 and above 500 mg/L (above 2.40 mM) against WiDr, MCF-7, and HeLa. The 9,10-AQ at 500 mg/L (or 2.40 mM) increases BAX expression and acts as an apoptotic agent on HeLa cells.Conclusions: The investigation has shown that 9,10-AQ up to 500 mg/L concentration does not proliferate the cancer cell growth; instead, it inhibits the HCT 116 and HeLa cells growth. We have preliminary evidence regarding the apoptotic mechanism of 9,10-AQ by increasing BAX gene expression on HeLa cells.

scholarly journals Naproxen Based 1,3,4-Oxadiazole Derivatives as EGFR Inhibitors: Design, Synthesis, Anticancer, and Computational Studies

2021 ◽  
Vol 14 (9) ◽  
pp. 870
Author(s):  
Mohammad Mahboob Alam ◽  
Syed Nazreen ◽  
Abdulraheem S. A. Almalki ◽  
Ahmed A. Elhenawy ◽  
Nawaf I. Alsenani ◽  
...  
Keyword(s):  
Docking Studies ◽  
Biological Data ◽  
Egfr Inhibitors ◽  
Design Synthesis ◽  
Standard Drug ◽  
Egfr Inhibition ◽  
Hct 116 ◽  
Oxadiazole Derivatives ◽  
Hct 116 Cells ◽  
Mcf 7

A library of novel naproxen based 1,3,4-oxadiazole derivatives (8–16 and 19–26) has been synthesized and screened for cytotoxicity as EGFR inhibitors. Among the synthesized hybrids, compound2-(4-((5-((S)-1-(2-methoxynaphthalen-6-yl)ethyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)phenol(15)was the most potent compound against MCF-7 and HepG2cancer cells with IC50 of 2.13 and 1.63 µg/mL, respectively, and was equipotent to doxorubicin (IC50 1.62 µg/mL) towards HepG2. Furthermore, compound 15 inhibited EGFR kinase with IC50 0.41 μM compared to standard drug Erlotinib (IC50 0.30 μM). The active compound induces a high percentage of necrosis towards MCF-7, HePG2 and HCT 116 cells. The docking studies, DFT and MEP also supported the biological data. These results demonstrated that these synthesized naproxen hybrids have EGFR inhibition effects and can be used as leads for cancer therapy.

scholarly journals Sildenafil (VIAGRATM): A Promising Anticancer Drug Against Certain Human Cancer Cell Lines

2021 ◽  
Vol 33 (6) ◽  
pp. 1420-1424
Author(s):  
Mohammed A. Hussein ◽  
Mohamed M. Salah El-Din ◽  
Esraa M. Saleh ◽  
Ahmed T. Mostafa ◽  
Mahmoud T. Abd-Elazziz ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Single Molecule ◽  
Hela Cells ◽  
Human Cancer ◽  
Structural Features ◽  
Mammalian Cell Lines ◽  
Hct 116 ◽  
Mcf 7

Sildenafil has been identified as the first agent for treating male erectile dysfunction and is a selective inhibitor of phosphodiesterase 5 (PDE5). Its chemical structure consists of three moieties named; 1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one, 5-(2-ethoxy-1-ylsulfonyl)phenyl and 4-methylpiperazine. Many articles are reported the cytotoxic activity of each moiety individually. The combination into a single molecule (sildenafil) of these three structural features could have promising anti-cancer and cytotoxic effects. The study evaluated sildenafil cytototoxic activity in vitro against mammalian cell lines: MCF-7, HCT-116, HeLa cells and A-549 cells with their IC50 values. Sildenafil showed considerable cytotoxic activity (IC50 = 28.2 ± 0.92, 45.2 ± 1.5, 30.5 ± 0.87 and 60.5 ± 3.2 μg/mL) against HCT-116, MCF-7, A-549 and HeLa cells, respectively. HCT-116 was the most sensitive cell line towards sildenafil followed by A-549, A375, MCF-7 and HeLa cells. These findings shed light on the antitumor activity of sildenafil and its possible impact on potentiating of cytokines, antitumor and anti-inflammatory markers in tumour cells. These effects might be related to the structure feature of sildenafil.

scholarly journals Cytotoxic Aporphines from Artabotrys Crassifolius

2016 ◽  
Vol 11 (3) ◽  
pp. 1934578X1601100
Author(s):  
Tan Kok Kwan ◽  
Fiona Shipton ◽  
Nadiah Syafiqah Nor Azman ◽  
Shahadat Hossan ◽  
Khoo Ten Jin ◽  
...  
Keyword(s):  
Chloroform Extract ◽  
Kidney Cells ◽  
Human Embryonic Kidney ◽  
Cytotoxic Effects ◽  
Human Embryonic Kidney Cells ◽  
Hct 116 ◽  
Ethanol Extracts ◽  
Hct 116 Cells ◽  
Mcf 7

Artabotrys crassifolius Hook. f. & Thomson is a medicinal plant used in Malaysia. The cytotoxic effects of the hexane, chloroform and ethanol extracts of the leaves and bark were examined in vitro against MCF-7, MDA-468 and HCT-116 cells. The chloroform extract of the bark inhibited the growth of all cell lines with GI50 values ranging from 4.2 μg/mL to 9.4 μg/mL. Silica gel column chromatography of this extract yielded artabotrine, liridine, atherospermidine and lysicamine. Artabotrine and lysicamine inhibited the growth of HCT-116 and MCF-7 cells with GI50 values ranging from 3.3 μM to 3.9 μM. These alkaloids were not toxic to human embryonic kidney cells (HEK297) up to a concentration of 50 μg/mL.

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