New Quinoline Based Sulfonamide Derivatives: Cytotoxic and Apoptotic Activity Evaluation Against Pancreatic Cancer Cells

2018 ◽  
Vol 18 (8) ◽  
pp. 1122-1130 ◽  
Author(s):  
Leyla Yurttaş ◽  
Gülşen A. Çiftçi
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Flow Cytometric Analysis ◽  
Protein Kinase Inhibitors ◽  
Standard Drug ◽  
Activity Evaluation ◽  
Pancreatic Cancer Cells ◽  
Cytotoxicity Studies ◽  
Induced Apoptosis ◽  
Phenyl Moiety

Background: Quinoline is a privileged scaffold especially known with antimalarial and antibacterial drugs before, presently followed anticancer efficiency with a new group of protein kinase inhibitors. Objective: In this work, combining quinoline ring, hydrazone and sulphonamide groups, we have synthesized N'-arylidene-2-[4-(quinolin-8-ylsulfonyl)piperazin-1-yl]acetohydrazide derivatives (3a-o) and evaluated their in vitro anticancer activity against cancerous cell lines PANC-1, CAPAN-1, and healthy cell line hTERT-HPNE. Method: Fifteen compounds were synthesized a simple, well-known three-step synthetic procedure starting from 8-quinolinesulfonylchloride. Cytotoxicity studies were performed according to the conventional MTT method. As a second stage, flow cytometric analysis was done to the nine most cytotoxic compounds for determining the mechanism of action which could be apoptosis and/or necrosis. </P><P> Results/Conclusion: According to anticancer activity evaluation, compound 3b bearing 4-methyl phenyl moiety exhibited significant cytotoxicity which has an IC50 value nearly four-fold lower than cisplatin displayed, whereas compound 3f bearing 4-trifluoromethyl phenyl moiety showed two-fold potency of the standard drug against PANC-1 cell line. Compounds 3h, 3k and 3n against CAPAN-1 also showed significant cytotoxicity, selectively. The most active compounds 3b, 3c, 3d, 3f, 3g, 3h, 3k and 3n against PANC-1 and compounds 3f, 3g, 3h, 3k and 3n against CAPAN-1 were selected to be studied in flow cytometry. Compound 3b induced apoptosis of PANC-1 cells with a percentage of 16.0%, whereas compound 3h induced apoptosis of CAPAN-1 cells with a value of 20.6%.

scholarly journals Synthesis and Anticancer Activity Evaluation of Azepinobisindoles; the Isomeric Iheyamine A Derivatives

2019 ◽  
Vol 35 (2) ◽  
pp. 723-731
Author(s):  
Weerachai Phutdhawong ◽  
Sopita Rattanopas ◽  
Jitnapa Sirirak ◽  
Thongchai Taechowisan ◽  
Waya S. Phutdhawong
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Human Cancer ◽  
Docking Study ◽  
Inhibitory Effect ◽  
Molecular Docking Study ◽  
Human Cancer Cell Lines ◽  
Activity Evaluation ◽  
Cancer Line

Azepinobisindole derivatives, the isomeric Iheyamine skeleton, was prepared and its anticancer activity evaluation were investigated against two human cancer cell lines, Hepatocellular carcinoma (HepG2) and human cervical cancer line (Hela) as well as the normal cell line (Vero cell line) using MTT assay. The anticancer activity results indicated that 2-methoxy-5-methyl-5H-azepino[2,3-b:4,5-bʹ]diindole was the most active derivative against tested cell lines. Additionally, molecular docking study in silico the possible inhibitory effect of cyclin-dependent kinase 2 (CDK2) by the azepinoindole revealed that all synthesized compounds fit well in the binding cavity of CDK2.

One-pot synthesis and biological evaluation of novel 3-(5-((aryl) methyl) isoxazol-3-yl)-4H-chromen-4-one derivatives as potent antibacterial and anticancer agents

2021 ◽  
Vol 25 (11) ◽  
pp. 80-85
Author(s):  
Rani Janapatla Uma ◽  
Babu H. Ramesh ◽  
M. Prashanthi
Keyword(s):  
Antibacterial Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Cell Line Hela ◽  
Aryl Methyl ◽  
Mcf 7

In search of better antibacterial and anticancer agents, a series of novel 3-(5-((aryl) methyl) isoxazol-3-yl)-4Hchromen- 4-one derivatives was synthesized (4a-4l) by using 4-oxo-4H-chromene-3-carbaldehyde and alkyne via in situ generated nitrile oxide and evaluated for their antibacterial and anticancer activity in vitro. Antibacterial activity was evaluated against three G+ bacterial strains and anticancer activity against breast cancer cell line (MCF-7) and cervical carcinoma cell line (HeLa). Among all the tested compounds, 4j and 4g exhibited potent antibacterial activity against tested grampositive bacterial strains. 4g, 4i and 4j exhibited potent cytotoxic activity against MCF-7 with IC50 values nearer to the standard drug doxorubicin.

Protective Effects of Wuyaoshunqisan Against H2O2-Induced Apoptosis on Hippocampal Cell Line HiB5

2002 ◽  
Vol 30 (04) ◽  
pp. 561-570 ◽  
Author(s):  
Jeong-Jin Je ◽  
Hyun-Taeg Shin ◽  
Seok-Hee Chung ◽  
Jong-Soo Lee ◽  
Sung-Soo Kim ◽  
...  
Keyword(s):  
Cell Line ◽  
Flow Cytometric Analysis ◽  
Terminal Deoxynucleotidyl Transferase ◽  
Protective Effects ◽  
Flow Cytometric ◽  
Hippocampal Cell ◽  
Diphenyltetrazolium Bromide ◽  
The Central Nervous System ◽  
Biochemical Analyses ◽  
Induced Apoptosis

Oxidative stress has been implicated in the pathogenesis of different neurodegenerative disorders. To investigate the protective effects of Wuyaoshunqisan against H 2 O 2-induced apoptosis in the central nervous system, the 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay, the terminal deoxynucleotidyl transferase (TdT)-mediated dUTP nick end-labeling (TUNEL) method, flow cytometric analysis, and the DNA fragmentation assay were performed on cells of the hippocampal cell line HiB5. Through the morphological and biochemical analyses, it was shown that HiB5 cells treated with H 2 O 2 exhibit classical apoptotic features, while the occurrence of such changes is reduced in cells pre-treated with Wuyaoshunqisan prior to H 2 O 2 exposure.

scholarly journals Apoptosis and Antioxidant Activities of Catharanthus rosues [L] G.Don Extract on Breast Cancer Cell Line

2010 ◽  
Vol 1 (2) ◽  
pp. 99
Author(s):  
Wahyu Widowati ◽  
Tjandrawati Mozef ◽  
Chandra Risdian ◽  
Hana Ratnawati ◽  
Susi Tjahyani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Catharanthus Roseus ◽  
Breast Cancer Cell Line ◽  
Cancer Cell Line ◽  
Induced Apoptosis

Tapak dara or Madagascar Periwinkle (Catharanthus roseus [L] G.Don), a natural plant, is empirically reported to have promising anticancer activity. To elucidate its mechanism, a research was conducted to investigate the possible ethanol extract of  C. roseus in inducing apoptosis on breast cancer cell line (T47D). Antioxidant activity of C. roseus was investigated as well. Sub-G1 flowcytometric apoptotic analysis result showed that extract of C. roseus at 6.25 μg/mL induced apoptosis for 26.365%. Increasing extract concentration resulted an increasing apoptotic level as well, extract at concentration of 12.5 μg/mL induced apoptosis for 22.235%.  Meanwhile doxorubicin at concentration of 10 μg/mL induced apoptosis for 36.055%. The antioxidant activity was determined by using in vitro assay: inhibition of  2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity. Antioxidant activity of C. roseus extract were compared to quercetin and butylated hydroxyanisol (BHA), as positive controls.  The results showed that DPPH IC50 of C. roseus extract, quercetin and BHA were 358.411 μg/mL, 19.200 μg/mL  and  94.178 μg/mL, respectively. We suggest that C. roseus extract had a potential anticancer activity by inducing apoptosis.Key words : antioxidant, DPPH, Catharanthus roseus, apoptosis, breast cancer, T47D

scholarly journals Synergistic Effect of the Combination of Polyphenols with Gemcitabineon Pancreatic Cancer Cell line AsPC-1

2017 ◽  
Vol 2 (1) ◽  
Keyword(s):  
Pancreatic Cancer ◽  
Cell Line ◽  
Efflux Pump ◽  
Flow Cytometric Analysis ◽  
Pancreatic Cancer Cell Line ◽  
Cancer Cell Line ◽  
Human Pancreatic Cancer ◽  
Pancreatic Cell ◽  
Pancreatic Cancer Cells

In our diet, polyphenols are micronutrients with an important role in the prevention of degenerative diseases such as cancer and cardiovascular diseases. Particularly, Pancreatic cancer is one of the most aggressive cancers, with only about 5% of patients surviving 5 years past the initial diagnosis. Despite advances with current chemotherapy combinations, overall survival outcomes are still require novel therapeutic approaches. Here, we examined the efficacy of combined treatments of polyphenols and gemcitabine the standard of treatment for patients with metastatic pancreatic cancer in human pancreatic cancer cells. For that purpose, the pro-apoptic effects of gemcitabine were studied on the human pancreatic cell line AsPC1 in presence or absence of several polyphenols, in order to evaluate if they latter are able to potentialize gemcitabine cytotoxicity. Our study aims to investigate the implication of MDR1 (multidrug transporter)in resistance to gemcitabine and if the studied polyphenol could target this drug efflux pump in AsPC-1 cells by flow cytometric analysis. We observed that 5µg/ml gemcitabine in combination with 15 µg/ml of selected polyphenol (Catechin, Quercetin, Bergamottin, Rhamnetin) was more effective than gemcitabine alone, by increased in the percentage of dead cells up to 60%. Morever our results demonstrated that some polyphenols (Quercetin) inhibit the efflux activity of MDR1. Our study in vitro suggests therefore that chemotherapy with gemcitabine might be significantly increased upon combination with specific polyphenol. In conclusion, polyphenols may be promising agents for novel combination therapy since they potentialize the cytotoxic activity of gemcitabine to eradicate pancreatic cancer and therefore the cellular resistance.

scholarly journals Metformin-induced ROS upregulation as amplified by apigenin causes profound anticancer activity while sparing normal cells

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Madhuri Shende Warkad ◽  
Chea-Ha Kim ◽  
Beom-Goo Kang ◽  
Soo-Hyun Park ◽  
Jun-Sub Jung ◽  
...  
Keyword(s):  
Dna Damage ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Mitochondrial Membrane ◽  
Dermal Fibroblasts ◽  
Minimal Effect ◽  
Related Factors ◽  
Pancreatic Cancer Cells ◽  
Induced Apoptosis ◽  
Hdf Cells

AbstractMetformin increased cellular ROS levels in AsPC-1 pancreatic cancer cells, with minimal effect in HDF, human primary dermal fibroblasts. Metformin reduced cellular ATP levels in HDF, but not in AsPC-1 cells. Metformin increased AMPK, p-AMPK (Thr172), FOXO3a, p-FOXO3a (Ser413), and MnSOD levels in HDF, but not in AsPC-1 cells. p-AMPK and p-FOXO3a also translocated from the cytosol to the nucleus by metformin in HDF, but not in AsPC-1 cells. Transfection of si-FOXO3a in HDF increased ROS levels, while wt-FOXO3a-transfected AsPC-1 cells decreased ROS levels. Metformin combined with apigenin increased ROS levels dramatically and decreased cell viability in various cancer cells including AsPC-1 cells, with each drug used singly having a minimal effect. Metformin/apigenin combination synergistically decreased mitochondrial membrane potential in AsPC-1 cells but to a lesser extent in HDF cells. Metformin/apigenin combination in AsPC-1 cells increased DNA damage-, apoptosis-, autophagy- and necroptosis-related factors, but not in HDF cells. Oral administration with metformin/apigenin caused dramatic blocks tumor size in AsPC-1-xenografted nude mice. Our results suggest that metformin in cancer cells differentially regulates cellular ROS levels via AMPK-FOXO3a-MnSOD pathway and combination of metformin/apigenin exerts anticancer activity through DNA damage-induced apoptosis, autophagy and necroptosis by cancer cell-specific ROS amplification.

Synthesis, Anticancer and Antibacterial Studies of Benzylidene Bearing 5-substituted and 3,5-disubstituted-2,4-Thiazolidinedione Derivatives

2020 ◽  
Vol 16 ◽  
Author(s):  
Navjot Singh Sethi ◽  
Deo Nandan Prasad ◽  
Rajesh K. Singh
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Cell Line ◽  
Hepg2 Cell ◽  
Antiproliferative Activity ◽  
Human Lung Cancer ◽  
Hepg2 Cell Line ◽  
Standard Drug ◽  
Cytotoxicity Studies ◽  
Mcf 7

Aim: To develop novel compounds having potent anticancer and antibacterial activities. Background: Several studies have proved that benzylidene analogues of clinical 2,4-TZDs such as troglitazone and ciglitazone have more potent antiproliferative activity than their parent compounds. Literature studies also revealed that attachment of more heterocyclic rings containing nitrogen on 5th position of 2,4-TZD can enhance the antimicrobial activity. Hence, attachment of various moieties on benzylidene ring may produce safe and effective compounds in future. Objective: The objective of the present study is to synthesize a set of novel benzylidene ring containing 5- and 3- substituted-2,4-thiazolidinedione derivatives and evaluated for their anticancer and antibacterial activity. Method: The synthesized compounds were characterized by IR, NMR, mass and elemental studies. The in vitro cytotoxicity studies were performed for human breast cancer (MCF-7) and human lung cancer (A549) cells and HepG2 cell-line and compared to standard drug doxorubicin by MTT assay. Antimicrobial activity of the synthesized 2,4-thiazolidinediones derivatives was carried out using the cup plate method with slight modification. Result: The results obtained showed that TZ-5 and TZ-13 exhibited good antiproliferative activity against A549 cancer cell-line whereas TZ-10 exhibited moderate antiproliferative activity against HepG2 cell-line when compared to standard drug doxorubicin. TZ-5 also exhibited reasonable activity against MCF-7 cell-line against doxorubicin as standard. TZ-4, TZ-5, TZ-6, TZ-7 and TZ-16 exhibited remarkable antibacterial activity against Gram +ive and moderate activity against Gram –ive bacteria against standard drug ciprofloxacin. Conclusion: Attachment of heterocyclic rings containing nitrogen as the hetero atom improves the anticancer and antimicrobial potential. Attachment of electronegative element like halogens can also enhance the antimicrobial activity. Further structure modifications may lead to the development of more potent 2,4-TZD leads that can be evaluated for further advanced studies.

Pyrrolo[2,3-b]Pyridinic Derivatives Induce Cell Growth Inhibition of the Myeloblastic HL-60 Cell Line.

Blood ◽  
2006 ◽  
Vol 108 (11) ◽  
pp. 4400-4400
Author(s):  
Maylis Decrop ◽  
Claire Espanel ◽  
Jerome Guillard ◽  
Elodie Boissier ◽  
Nathalie Gallay ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Growth ◽  
Cell Line ◽  
Therapeutic Potential ◽  
Biological Effects ◽  
Flow Cytometric Analysis ◽  
Leukemic Cells ◽  
Trypan Blue Exclusion ◽  
Viable Cells ◽  
Induced Apoptosis

Abstract Cytokins, N6-subsitued adenine derivatives play an important role in many different processes in plant development (Mok et al, Annu Rev Plant. Physiol Plant Mol Biol2001, 52:89–118), including the cell growth and division control, the vegetable cell differentiation with auxin and the storage of various metabolites as alkaloids (Yahia et al, Plant Science1998, 133:9–15). Furthermore, several studies suggest that cytokinins and their purin derivated are able to control mammalian cell apoptosis and differentiation of human leukemic cells (HL-60 myeloblastic cell line) into mature granulocytes (Ishii et al, Cell Growth Differ2002, 13: 19–26). All these compounds exert their biological activity via Cyclin-Dependant Kinase (CDK) inhibition and particulary CDK1 and CDK2. The aim of our study was the synthesis of new 7-azaindole derivates as cytokinin analogues and the evaluation of their biological effects on HL-60 cells. Eight analogues of 7-azaindole were prepared by the condension of (N-methyl-)4-chloropyrrolo[2,3-b]pyridine with corresponding amines using palladium-catalyzed reaction (Hartwig et al, Angew Chem IN Ed1998, 37: 2046–2067). The four derivates from 1H-pyrrolo[2,3-b]pyridine were 4-phenylamino-7-azaindole, 4-benzylamino-7-azaindole, 4-phenethylamino-7-azaindole and 4-phenylpiperazylamino-7-azaindole. The four derivates from 1-methyl-pyrrolo[2,3-b]pyridine were 4-phenylamino-N-methyl-7-azaindole, 4-benzylamino-N-methyl-7-azaindole, 4-phenetylamino-N-methyl-7-azaindole and 4-phenylpiperazylamino-N-methyl-7-azaindole. HL-60 cells were exposed to three concentrations of these compounds (10–100–500 μM) during 72h at 37°C. The number of viable cells was determined by Trypan blue exclusion, and the cell cycle was assessed by propidium iodide staining followed by flow cytometric analysis. All these compounds decreased the number of viable cells. The compounds of the NH serie were more active than their methyl-analogues, especially 4-phenylamino-N-methyl-7-azaindole and 4-phenethylamino-7-azaindole which presented an estimated IC50 of 2 μM. Moreover, when used at 10 μM, 4-phenylamino-N-methyl-7-azaindole induced apoptosis whereas 4-phenethylamino-7-azaindole promoted inhibition of the cell cycle without pro-apoptotic effect. These results suggest that cytokinin analogues derived from 1H-pyrrolo[2,3-b]pyridine may present interesting therapeutic potential as cytostatic agents. Further studies will clarify their biological effects on leukemic cells.

scholarly journals Synthesis and Anticancer Activity of Novel Benzofurancarboxamides

2020 ◽  
Vol 10 (6) ◽  
pp. 6597-6609
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
National Cancer Institute ◽  
Efficient Synthesis ◽  
Anticancer Activities ◽  
Developmental Therapeutics Program ◽  
Activity Evaluation ◽  
Developmental Therapeutics

In our present work, we presented an efficient synthesis and anticancer activity evaluation of some novel benzofurancarboxamides. Our proposed approaches provide the possibility to design benzofurans diversity with a considerable chemical novelty. The synthesized substances were selected by the National Cancer Institute (NCI) Developmental Therapeutics Program for the in vitro cell line screening to investigate their anticancer activity. The compounds with significant levels of anticancer activities have been found that can be used for further optimization.

Sign in / Sign up

Export Citation Format

Share Document