Cytotoxicity and Antibacterial Studies of Newly Synthesized Novel Heterocylcic Pyridine Derivative and its Metal Complexes

2021 ◽  
Vol 6 (4) ◽  
pp. 243-249
Author(s):  
B.R. Chaitanya Kumar ◽  
K. Sudhakar Babu ◽  
J. Latha
Keyword(s):  
Metal Complexes ◽  
Cell Lines ◽  
Cancer Cell ◽  
Metal Ion ◽  
Analytical Data ◽  
Cancer Cell Lines ◽  
Diffusion Method ◽  
Pyridine Derivative ◽  
Bacterial Strains ◽  
Physico Chemical

A pyridine derivative 2-((E)-1-(2-hydrazinyl-4-methyl-6-phenyl-pyridine-3-carboyl)ethyl)pyridine-4- carbonitrile (CPHPC) ligand and its 3d-metal(II) complexes has been synthesized (where [M = Co(II), Ni(II) and Cu(II)]. The physico-chemical, analytical data, UV-Vis, FT-IR, 1H NMR and ESR spectrum methods were used to characterize all of the synthesized complexes. Spectral investigations of metal(II) complexes revealed that the metal ion is surrounded by an octahedral geometry. Low conductance values indicated that the metal(II) complexes behave as non-electrolyte. The cytotoxic activity on lung cancer cell lines and hepatic cancer cell lines A549 and HepG2, respectively, with the ligand and their metal complexes were tested with MTT assay. The ligand and its metal complexes were tested for diverse harmful bacterial strains using the agar well diffusion method on Gram-negative bacteria such as Pseudomonas desmolyticum, Escherichia coli and Klebsiella aerogenes, as well as Gram-positive bacteria Staphylococcus aureus.

scholarly journals THE METAL COMPLEXES OF NOVEL SCHIFF BASE CONTAINING ISATIN: CHARACTERIZATION, ANTIMICROBIAL, ANTIOXIDANT AND CATALYTIC ACTIVITY STUDY

2019 ◽  
pp. 206-210
Author(s):  
VAIRALAKSHMI M ◽  
PRINCESS R ◽  
JOHNSON RAJA S
Keyword(s):  
Catalytic Activity ◽  
Metal Complexes ◽  
1H Nmr ◽  
Metal Ion ◽  
Analytical Data ◽  
Free Ligand ◽  
Molar Conductance ◽  
Diffusion Method ◽  
Spectral Studies ◽  
Standard Drug

Objectives: The aim of our work was to synthesize novel mixed ligand-metal complexes and evaluation of antimicrobial, antioxidant assay, and analysis of catalytic oxidation of cyclohexane. Methods: The complexes were characterized by means of various physicochemical techniques such as elemental analysis, molar conductance, magnetic susceptibility, infrared (IR), electronic absorption, 1H NMR (proton magnetic resonance), and mass spectral studies. The antimicrobial screening study was done by disc diffusion method. The catalytic activity of the complexes was observed in the oxidation of cyclohexane using eco-friendly hydrogen peroxide as oxidant. Results: On comparing the 1H NMR and IR spectral data of free ligand and its complexes, it was found to be azomethine (CH=N) proton which is formed in the free ligand. During complexation, the azomethine proton is coordinated to the metal ion and the phenolic oxygen is coordinated to the metal ion by deprotonation. The analytical data and mass spectra of the ligand and the complexes confirm the stoichiometry of metal complexes as being of the (MLY)Cl type and the metal to ligand ratio is 1:1. The antimicrobial, antioxidant, and catalytic potential were evaluated and the result shows the better activity of the complexes than the ligand. Conclusion: It was found to be copper(II) and zinc(II) complexes which are effective against all the bacteria when compared to standard drug streptomycin. Copper(II) complex was found to be effective antibacterial agent against Aspergillus niger and Aspergillus flavus in comparison to the standard drug Nystatin. The zinc complex exhibited good catalytic activity.

scholarly journals Synthesis and Biological Evaluation of New Antitubulin Agents Containing 2-(3′,4′,5′-trimethoxyanilino)-3,6-disubstituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine Scaffold

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1690
Author(s):  
Romeo Romagnoli ◽  
Filippo Prencipe ◽  
Paola Oliva ◽  
Barbara Cacciari ◽  
Jan Balzarini ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Death ◽  
Cell Lines ◽  
Cancer Cell ◽  
Mononuclear Cells ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Pyridine Derivative ◽  
Tubulin Polymerization ◽  
Dependent Manner

Two novel series of compounds based on the 4,5,6,7-tetrahydrothieno[2,3-c]pyridine and 4,5,6,7-tetrahydrobenzo[b]thiophene molecular skeleton, characterized by the presence of a 3′,4′,5′-trimethoxyanilino moiety and a cyano or an alkoxycarbonyl group at its 2- or 3-position, respectively, were designed, synthesized, and evaluated for antiproliferative activity on a panel of cancer cell lines and for selected highly active compounds, inhibition of tubulin polymerization, and cell cycle effects. We have identified the 2-(3′,4′,5′-trimethoxyanilino)-3-cyano-6-methoxycarbonyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivative 3a and its 6-ethoxycarbonyl homologue 3b as new antiproliferative agents that inhibit cancer cell growth with IC50 values ranging from 1.1 to 4.7 μM against a panel of three cancer cell lines. Their interaction with tubulin at micromolar levels leads to the accumulation of cells in the G2/M phase of the cell cycle and to an apoptotic cell death. The cell apoptosis study found that compounds 3a and 3b were very effective in the induction of apoptosis in a dose-dependent manner. These two derivatives did not induce cell death in normal human peripheral blood mononuclear cells, suggesting that they may be selective against cancer cells. Molecular docking studies confirmed that the inhibitory activity of these molecules on tubulin polymerization derived from binding to the colchicine site.

Synthesis and Characterization of Some Metal Complexes of 4,5-Diazafluoren-9-one and their Biological Effects on Human Carcinoma Cells

2008 ◽  
Vol 61 (12) ◽  
pp. 975 ◽  
Author(s):  
Guo-Liang Lu ◽  
Cheuk-Lam Ho ◽  
Qiwei Wang ◽  
Wai-Yeung Wong ◽  
Chung-Hin Chui ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Inhibitory Effect ◽  
Ambient Conditions ◽  
Human Carcinoma ◽  
Human Cancer Cell Lines

Three new transition metal complexes of 4,5-diazafluoren-9-one, [(DAFO)PdCl2], [(DAFO)PtCl2], and [(DAFO)ZnCl2], were prepared in good yields by the reactions between appropriate metal chloride precursors and 4,5-diazafluoren-9-one under ambient conditions. The structures of these metal complexes were established by spectroscopic (Fourier-transform IR, NMR, and fast-atom bombardment mass spectrometry) techniques. The possible biological activity of these compounds on three human cancer cell lines including Hep3B, MDAMB-231, and SKHep-1 was investigated. The results obtained showed that both zinc- and platinum-containing compounds exhibit a similar growth inhibitory effect on these three cancer cell lines when compared with the prototypical cis-platin. In contrast, the corresponding palladium congener is virtually biologically inactive in these trials.

scholarly journals Cytotoxic Activity of Familact: A Probiotic Supplement

2018 ◽  
Vol 12 (4) ◽  
pp. 41-45
Author(s):  
Zahra Yahyavi ◽  
◽  
Mohammad Reza Fazeli ◽  
Mani Mirfeizi ◽  
Shima Aliebrahimi ◽  
...  
Keyword(s):  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Apoptotic Cell ◽  
Human Cancer ◽  
Complementary Therapy ◽  
Cancer Cell Lines ◽  
Dependent Manner ◽  
Bacterial Strains ◽  
Ht 29

Background: Lactobacillus and Bifidobacterium species are among the probiotics discussed due to their anti-cancer effects in the treatment of colorectal and breast cancers in recent studies. The aim of this study was to investigate the anticancer effect of Familact, a commercial probiotic capsule containing seven bacterial strains (L. casei, L. acidophilus, L. rhamnosus, L. bulgaricus, B. breve, B. longum and Streptococcus thermophilus). Methods: Various cancer cell lines including Caco-2, HT-29, T47D and normal cell line L929 were treated with different concentrations of Familact. Using MTT assay, the cytotoxicity effect was investigated for each cell line and then flow cytometry analysis of apoptosis was evaluated. Results: Familact demonstrated inhibitory effects on the proliferation of all tested cancer cell lines in a dose-dependent manner. Although Familact augmented apoptotic cell death in HT-29 human cancer cells, it was less effective in the case of Caco-2 and T47D cells. Moreover, exposure to Familact showed moderate cytotoxicity towards L929 mouse fibroblast cells. Conclusion: Familact could be considered as a complementary therapy in the treatment of cancers.

scholarly journals Newly Synthesized Benzothiazole Derived Ligand and its Co(III) and Ru(III) Complexes as Biological Potent Molecules: Chemical Preparation, Structure, Antimicrobial, in vitro and in vivo Cytotoxicity Studies

2021 ◽  
Vol 12 (6) ◽  
pp. 7817-7844
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
In Vivo Studies ◽  
Diffusion Method ◽  
Migration Behavior ◽  
Microbial Inhibition ◽  
Cytotoxicity Studies

Herein we describe the synthesis of 2-((E)-(2-(benzo[d]thiazol-2-yl)phenylimino)methyl)-5-methoxyphenol imine base (BMM) and its metal complexes such as [Co(BMM)2] C1, [Co(BMM)(ph)] C2, [Ru(BMM)2] C3 and [Ru(BMM)(ph)] C4. The ligand and its complexes were characterized by spectroscopic, TGA, Powder X-ray diffraction (XRD), and elemental analysis. The coordination number and geometry were confirmed by various experimental data. The Co(III) and Ru(III) complexes are assigned to be having octahedral geometry. Further, the experimental results revealed that complex C2 and C4 emerged as moderate DNA binding intercalators compared to standard intercalators and prominent nuclease activity compared with C1 and C3 complexes. The extent of interaction and intercalation mode was confirmed by monitoring electronic absorption studies, fluorescence quenching probe, and viscosity measurement. Furthermore, the complexes C1-C4 were investigated for their in vitro cytotoxic studies against a panel of human cancer cell lines, viz., A549, NIH3T3, MCF-7, and EAC. Also, the cell adhesion and migration behavior were carried out after administering the complex C2 and C4 to respective cancer cell lines. In mice, the toxicities and tolerabilities of the complex C2 and C4 were also investigated through in vivo studies. The resultant complexes were screened for their microbial inhibition studies through the good diffusion method. All the complexes display moderate microbial inhibition properties compared to their uncoordinated analog.

ACTIVITY OF Annona Squamosa PEELS EXTRACTS AGAINST TWO PATHOGENIC BACTERIA AND TWO BLOOD CANCER CELL LINES

2020 ◽  
Vol 51 (6) ◽  
pp. 496-1503
Author(s):  
Altaee & et al.
Keyword(s):  
Antibacterial Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Pathogenic Bacteria ◽  
Cancer Cell Lines ◽  
Diffusion Method ◽  
Annona Squamosa ◽  
Inhibitory Effects ◽  
Blood Cancer ◽  
Gram Positive Bacteria

This research project was designed to assess the antibacterial and antitcancer activity by using the crude extracts of fresh and dried peels of Annona squamosa fruit. The fresh and dried peels were extracted by using three solvents, inculded (water, ethanol, and methanol) at different concentrations (stock, 50, 25, 12.5, 6.25) µg/ml. The antibacterial activity was estimated against Gram-positive bacteria (Staphylococcus aureus) and Gram - negative bacteria (Pseudomonas aeruginosa) using agar well-diffusion method. Results showed the appearance of different regions of inhibition. Antibacterial activity of alcoholic solvent extracts of the dry and fresh peels showed noticeable inhibitory activity against both tested bacteria when comparing the last one with the aqueous extract of peels. The results of anticancer activity estimation against two hematological blood cancer cell lines showed that the three solvents for fresh and dried peels  caused a remarkable inhibitory effects and the ethanolic extracts of dried peels was the best. This encourage for the possibility of using  peels extracts of Annona. squamosa as a natural resources for growth inhibiting of different types of bacteria and cancer cells.

Thiosemicarbazone-metal complexes exhibiting cytotoxicity in colon cancer cell lines through oxidative stress

2020 ◽  
Vol 206 ◽  
pp. 110993
Author(s):  
Raquel Alcaraz ◽  
Pilar Muñiz ◽  
Mónica Cavia ◽  
Óscar Palacios ◽  
Katia G. Samper ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Colon Cancer ◽  
Metal Complexes ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Colon Cancer Cell ◽  
Colon Cancer Cell Lines

Identification of a pyridine derivative inducing senescence in ovarian cancer cell lines via P21 activation

2017 ◽  
Vol 45 (5) ◽  
pp. 452-460 ◽  
Author(s):  
Dongsheng Shang ◽  
Yanfang Wu ◽  
Ya Ding ◽  
Ziwen Lu ◽  
Yanting Shen ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Ovarian Cancer Cell ◽  
Cancer Cell Lines ◽  
Pyridine Derivative ◽  
Ovarian Cancer Cell Lines

scholarly journals Cytotoxic effects of steroidal glycosides isolated from the Paris vietnamensis plant on cancer cell lines and against bacterial strains

2019 ◽  
Vol 33 (1) ◽  
pp. 1516-1524 ◽  
Author(s):  
Thuy Thi Thu Vu ◽  
Lien Thi Kim Vu ◽  
Quan Huu Nguyen ◽  
Khang Van Pham ◽  
Dung Tien Nguyen ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Bacterial Strains ◽  
Cytotoxic Effects ◽  
Steroidal Glycosides

scholarly journals Parthenium hysterophorus:A Probable Source of Anticancer, Antioxidant and Anti-HIV Agents

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Shashank Kumar ◽  
Gousia Chashoo ◽  
Ajit K. Saxena ◽  
Abhay K. Pandey
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Metal Ion ◽  
Membrane Damage ◽  
Radical Scavenging ◽  
Liver Homogenate ◽  
Cancer Cell Lines ◽  
Aqueous Fraction ◽  
Antioxidant Agents ◽  
Anti Hiv

The present work reports the anticancer, antioxidant, lipo-protective, and anti-HIV activities of phytoconstituents present inP. hysterophorusleaf. Dried leaf samples were sequentially extracted with nonpolar and polar solvents. Ethanol fraction showed noticeable cytotoxic activity (81–85%) in SRB assay against MCF-7 and THP-1 cancer cell lines at 100 μg/ml concentration, while lower activity was observed with DU-145 cell line. The same extract exhibited 17–98% growth inhibition of HL-60 cancer cell lines in MTT assay, showing concentration dependent response. Ethanol extract caused 12% reduction in mitochondrial membrane potential and 10% increment in sub G1 population of HL-60 cell lines. Several leaf fractions, namely, ethyl acetate, ethanol, and aqueous fractions exhibited considerable reducing capability at higher concentrations. Most of the extracts demonstrated appreciable (>75%) metal ion chelating and hydroxyl radical scavenging activities at 200 µg/ml. All the extracts except aqueous fraction accounted for about 70–80% inhibition of lipid peroxidation in rat liver homogenate indicating protective response against membrane damage. About 40% inhibition of reverse transcriptase (RT) activity was observed in hexane fraction in anti-HIV assay at 6.0 µg/ml concentration. The study showed that phytochemicals present inP. hysterophorusleaf have considerable potential as cytotoxic and antioxidant agents with low to moderate anti-HIV activity.

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