scholarly journals The Synthesis of Unsymmetrical Urea from Substituted Phenethylamine and the Investigation of its Antibacterial, Anticancer, and Antioxidant Properties

2021 ◽  
Vol 12 (5) ◽  
pp. 7052-7063
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Biological Activities ◽  
Small Cell Lung Carcinoma ◽  
Antioxidant Properties ◽  
Moderate Activity ◽  
Bacterial Strains ◽  
Human Neuroblastoma ◽  
Cell Lung Carcinoma

There are numerous derivatives having urea scaffold in the literature, and these have many biological activities such as anticancer, antioxidant, antibacterial. Therefore, it aimed to synthesize urea derivatives containing substituted phenethylamine rings and investigate their biological properties such as anticancer, antimicrobial, and antioxidant. The antibacterial activity was carried out against four different bacterial strains (Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, and Pseudomonas aeruginosa ATCC 27853) by disc diffusion test. The synthesized compound was analyzed for their in vitro anticancer activity on SH-SY5Y (human neuroblastoma), HeLa (human cervical cancer), and A549 (non-small cell lung carcinoma) cell lines by using MTT, and LDH assays. The compound was inactive against all tested bacterial strains. The anticancer activity studies revealed that the unsymmetrical urea compound had remarkable activity against the tested cell lines, especially against the HeLa cell line with 50,61 µg/ml IC50 value. The compound was also analyzed for its antioxidant capacity by DPPH, ABTS, and CUPRAC methods. According to the results, the compound showed good to moderate activity against standard antioxidants. Therefore, this compound may be considered an anticancer and antioxidant agent in treating cancer and other related diseases.

Extraction, Chemical Composition, Antioxidant Property and In vitro Anticancer Activity of Silymarin from Silybum Marianum On Kb and A549 Cell Lines

2020 ◽  
Vol 17 ◽  
Author(s):  
Mojgan Azadpour ◽  
Mohammad Mehdi Farajollahi ◽  
Ali Mohammad Varzi ◽  
Pejman Hashemzadeh ◽  
Hossein Mahmoudvand ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
A549 Cell ◽  
Hplc Analysis ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antioxidant Property ◽  
Silybum Marianum ◽  
Stable Free Radical

Introduction: This study aimed to evaluate the antioxidant property of silymarin (SM) extracted from the seed of Silybum marianum and its anticancer activity on KB and A549 cell lines following 24, 48, and 72 h of treatment. Methods: Ten grams of powdered S. marianum seeds were defatted using n-hexane for 6 hours and then extracted by methanol. The silymarin extracted of extraction components The extracted components of silymarin were measured by spectrophotometric assay and HPLC analysis. 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, phenol content, total flavonoid content, and total antioxidant capacity were measured to detect the antioxidant properties of SM. The anticancer activity of the SM on cell lines evaluated by MTT. Results: In HPLC analysis, more than 50% of the peaks were related to silibin A and B. SM was reducedDPPH (the stable free radical) with a 50% inhibitory concentration (IC50) of 6.56 μg/ ml in comparison with butylated hydroxyl toluene (BHT), which indicated an IC50 of ~3.9 μg/ ml.The cytotoxicity effect of SM on the cell lines was studied by MTT assay. The cytotoxicity effect of the extracted silymarin on KB and A549 cell lines was observed up to 80 and 70% at 156 and 78 µg/ml, respectively. The IC50 value of the extracted SM on KB and A549 cell lines after 24 hours of treatment was seen at 555 and 511 µg/ml, respectively. Conclusion: Due to the good antioxidant and anticancer properties of the isolated silymarin, its use as an anticancer drug is suggested.

scholarly journals Viburnum opulus L. Fruit Extracts Protect Human Neuroblastoma SH-SY5Y Cells against Hydrogen Peroxide-Induced Cytotoxicity

Proceedings ◽  
2019 ◽  
Vol 40 (1) ◽  
pp. 5 ◽  
Author(s):  
Paşayeva ◽  
Arslan ◽  
Kararenk
Keyword(s):  
Oxidative Stress ◽  
Hydrogen Peroxide ◽  
Biological Activities ◽  
Iridoid Glycosides ◽  
Antioxidant Properties ◽  
Ethanol Extract ◽  
Anticancer Activities ◽  
Viburnum Opulus ◽  
Human Neuroblastoma

Viburnum L., is one of the most diverse genera of Caprifoliaceae family. There are 4 species of this genus in Turkey. One of them is Viburnum opulus L. The fruits of V. opulus have been used as an antidiabetic in Turkish folk medicine and a traditional drink named “gilaburu” in Middle Anatolia. Oxidative stress is involved in the cell degenerative changes in the pathogenesis of a wide variety of human chronic diseases, such as cancer. Some of the studies carried out on the V. opulus extracts revealed the presence of phenolic acids, flavonoids, hydroxybenzoic acids, tannins, coumarins, cathechols, iridoid glycosides, antocyanins, and some others. Most of these polyphenols have various biological activities, including antioxidant, cancer chemopreventive, and anticancer activities. This study aimed to assess the in vitro antioxidant properties of the ethanol extract (VOE), decoction (VOD) and fruit juice (VOFJ) from the fruits of V. opulus against hydrogen peroxide (H2O2)-induced oxidative stress in human SH-SY5Y neuronal cells. Our study revealed that the VOE, VOD and VOFJ provided neuroprotection against H2O2-induced oxidative stress. In conclusion, VOE, VOD and VOFJ can be used as a functional dietary ingredient that might help in reducing health problems associated with various oxidative stress insults.

scholarly journals Hypoxia-induced Tie1 Drives Stemness and Cisplatin Resistance in Non-small Cell Lung Carcinoma Cells

2020 ◽  
Author(s):  
Chaojie Li ◽  
Nannan Yang ◽  
Zhijin Chen ◽  
Ning Xia ◽  
Qungang Shan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Lung Carcinoma ◽  
Cisplatin Resistance ◽  
Small Cell Lung Carcinoma ◽  
Small Cell ◽  
Nsclc Cell ◽  
Luciferase Reporter ◽  
Small Cell Lung ◽  
Cell Lung Carcinoma

Abstract Background: Drug resistance and metastasis involving hypoxic tumor environment and persistent stem cell populations are detrimental to the survival of patients with non-small cell lung carcinoma (NSCLC). Tie1 is upregulated in hypoxia and is believed to counteract the effectiveness of platinum agents, by promoting the stemness properties in cells. We have investigated the association of Tie1 with HIF-1α and cisplatin resistance in NSCLC cell lines. Methods: Expression of Tie1 in a pulmonary microvascular endothelial cell line (HPMEC) and in NSCLC cell lines was detected using qRT-PCR and western blot. The effect of Tie1 on cell stemness and migration was examined by sphere-forming assay and transwell assay in NSCLC cells with Tie1 silenced. The regulation of Tie1 by HIF-1α was evaluated by a dual-luciferase reporter assay and chromatinImmune precipitation (ChIP) analysis.Results: We found that hypoxia could induce stemness and cisplatin resistance in vitro. Tie1 was expressed at low levels in NSCLC cells when compared with human pulmonary microvascular endothelial cells, however, its expression was increased by hypoxia. Additionally, Tie1 knockdown could reduce the stemness properties and increase sensitivity to cisplatin in vitro and in a xenograft mouse model. The promoter of Tie1 contains two predicted hypoxia-response elements (HREs). We mutated both HRE sites and conducted chromatin immune-precipitation and promoter luciferase reporter assays and were able to conclude that the induction of Tie1 by hypoxia was HIF-1α-dependent. Conclusions: Our findings indicated that Tie1 is upregulated in a hypoxic environment by HIF-1α and contributes to tumorigenesis and cisplatin resistance through the promotion of stemness in NSCLC cells.

scholarly journals Synthesis and Evaluation of Biological Activities of Bis(spiropyrazolone)cyclopropanes: A Potential Application against Leishmaniasis

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4960
Author(s):  
Olalla Barreiro-Costa ◽  
Gabriela Morales-Noboa ◽  
Patricio Rojas-Silva ◽  
Eliana Lara-Barba ◽  
Javier Santamaría-Aguirre ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
In Silico ◽  
Potential Application ◽  
Mammalian Cells ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Therapeutic Use ◽  
Derivatives Of

This work focuses on the search and development of drugs that may become new alternatives to the commercial drugs currently available for treatment of leishmaniasis. We have designed and synthesized 12 derivatives of bis(spiropyrazolone)cyclopropanes. We then characterized their potential application in therapeutic use. For this, the in vitro biological activities against three eukaryotic models—S. cerevisiae, five cancer cell lines, and the parasite L. mexicana—were evaluated. In addition, cytotoxicity against non-cancerous mammalian cells has been evaluated and other properties of interest have been characterized, such as genotoxicity, antioxidant properties and, in silico predictive adsorption, distribution, metabolism, and excretion (ADME). The results that we present here represent a first screening, indicating two derivatives of bis(spiropyrazolone)cyclopropanes as good candidates for the treatment of leishmaniasis. They have good specificity against parasites with respect to mammalian cells.

Design, Synthesis of novel coumarin conjugated acetamides as promising anticancer agents: An in-silico and in-vitro approach.

2020 ◽  
Vol 20 ◽  
Author(s):  
Mamatha S. V ◽  
S. L. Belagali ◽  
Mahesh Bhat ◽  
Vijay M. Kumbar
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Anticancer Agents ◽  
In Silico ◽  
Active Sites ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Mcf 7

Background: Coumarin and benzophenone possess a vast sphere of biological activities whereas thiazoles display various pharmacological properties. Hence we focused on incorporation of coumarin and thiazole core to the benzophenone skeleton to enhance the bioactivity anticipating their interesting biological properties. Objective: The objective of the current work is synthesis and biological evaluation of a novel series of coumarin fused thiazole derivatives. Methods: A novel series of Coumarin conjugated thiazolyl acetamide hybrid derivatives were synthesized by multistep reaction sequence and were characterized by the FT-IR, LCMS and NMR spectral techniques. The newly synthesized compounds were screened for anticancer activity by in-silico and in-vitro methods. The cytotoxicity of the synthesized unique compounds had been executed for two different cancer cell lines MCF-7 (Breast cancer) and KB (Oral cancer) in comparison with standard paclitaxel by MTT assay. Results: The compound 7f is the potent motif with an acceptable range of IC 50 values for anticancer activity were 63.54 µg/ml and 55.67 µg/ml, against the MCF-7 and KB cell lines, respectively. Molecule docking model revealed that this compound formed three conventional hydrogen bonds with the active sites of the amino acids MET 769, ARG 817 and LYS 721. Conclusion: Compound 7f with two methyl groups on the phenoxy ring and one 4-position methoxy group on the benzoyl ring, showed a significant cytotoxic effect. An advantageous level of low toxicity against normal cell line (L292) by MTT assay was determined.

scholarly journals Synthesis, characterization, molecular docking and in vitro anticancer activity of 3-(4-methoxyphenyl)-5-substituted phenyl-2-pyrazoline-1- carbothioamide

2021 ◽  
Vol 12 (2) ◽  
pp. 1648-1658
Author(s):  
Benupani Sahu ◽  
Rajapandi R ◽  
Avik Maji ◽  
Abhik Paul ◽  
Tanushree Singha ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Liver Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Breast Adenocarcinoma ◽  
Moderate Activity ◽  
Hep G2 ◽  
Molegro Virtual Docker ◽  
Mcf 7

In the present study, eight numbers of new 3- (4-methoxy phenyl)-5-substituted phenyl-2-pyrazoline-1-carbothioamide (5a-h) have been synthesized from 1- (4-methoxy phenyl)-3- (substituted phenyl)-prop-2-en-1-one (3a-h) and structurally characterized by using FT-IR, 1H NMR, 13C NMR, Mass and Elemental analysis. The synthesized molecules were biologically evaluated for their in vitro anticancer activity against human breast adenocarcinoma (MCF-7), liver cancer (Hep-G2) and leukaemia cancer (K-562) cell line using Sulforhodamine B (SRB) bioassay technique. From the all synthesized compounds 5a, 5c, 5d, and 5e exhibited potent anticancer activity (GI50= <10µg/ml) as compared to the controlled drug 5-Fluorouracil (5-FU) (GI50=44.5µg/ml) and Adriamycin (ADR) (GI50= <10µg/ml) on MCF-7 cell lines. Besides this, all the synthesized compounds have exhibited moderate activity against human liver cancer (Hep-G2) and leukaemia cancer (K-562) cell lines. In addition, molecular docking studies were also explored in order to study the probable binding specificity into the active site of Epidermal Growth Factor Receptor tyrosine kinase (EGFR) (PDB ID: 1M17) using Molegro Virtual Docker Evaluation 2013 6.0.1 (MVD). Based on the molecular docking result, it was found that compound 5a exhibited the best interaction with the above target (i.e., EGFR) by interacting with specific amino acid residues such as: Thr 766, Gin 767, Thr 830, Cys 575, Ala 719 and Met 769.

scholarly journals Hypoxia-induced Tie1 drives stemness and cisplatin resistance in non-small cell lung carcinoma cells

2020 ◽  
Author(s):  
Chaojie Li ◽  
Nannan Yang ◽  
Zhijin Chen ◽  
Ning Xia ◽  
Qungang Shan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Lung Carcinoma ◽  
Cisplatin Resistance ◽  
Small Cell Lung Carcinoma ◽  
Small Cell ◽  
Nsclc Cell ◽  
Luciferase Reporter ◽  
Small Cell Lung ◽  
Cell Lung Carcinoma

Abstract Background: Drug resistance and metastasis involving hypoxic tumor environments and persistent stem cell populations are detrimental to the survival of patients with non-small cell lung carcinoma (NSCLC). Tie1 is upregulated in hypoxia and is believed to counteract the effectiveness of platinum agents by promoting the stemness properties in cells. We have investigated the association of Tie1 with HIF-1α and cisplatin resistance in NSCLC cell lines.Methods: The expression of Tie1 in a pulmonary microvascular endothelial cell line (HPMEC) and NSCLC cell lines was detected using qRT-PCR and western blotting. The effect of Tie1 on cell stemness and migration was examined by sphere-forming and transwell assays in NSCLC cells with Tie1 silenced. The regulation of Tie1 by HIF-1α was evaluated by a dual-luciferase reporter assay and chromatin immunoprecipitation.Results: We found that hypoxia could induce stemness and cisplatin resistance in vitro. Tie1 was expressed at low levels in NSCLC cells when compared with human pulmonary microvascular endothelial cells, however, its expression was increased by hypoxia. Additionally, Tie1 knockdown could reduce stemness properties and increase sensitivity to cisplatin in vitro and in a xenograft mouse model. The promoter of Tie1 contains two predicted hypoxia-response elements (HREs). We mutated both HRE sites and conducted chromatin immune-precipitation and promoter luciferase reporter assays and were able to conclude that the induction of Tie1 by hypoxia was HIF-1α-dependent.Conclusions: Our findings indicated that Tie1 is upregulated in a hypoxic environment by HIF-1α and contributes to tumorigenesis and cisplatin resistance through the promotion of stemness in NSCLC cells.

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