Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line

Abstract Background In cancer cells, the intracellular antioxidant capacity and the redox homeostasis are mainly maintained by the glutathione- and thioredoxin-dependent systems which are considered as promising targets for anticancer drugs. Pyridazinones constitute an interesting source of heterocyclic compounds for drug discovery. The present investigation focused on studying the in-vitro antitumor activity of newly synthesized Pyridazin-3(2h)-ones derivatives against P815 (Murin mastocytoma) cell line. Methods The in-vitro cytotoxic activities were investigated toward the P815 cell line using tetrazolium-based MTT assay. Lipid peroxidation and the specific activities of antioxidant enzymes were also determined. Results The newly compounds had a selective dose-dependent cytotoxic effect without affecting normal cells (PBMCs). Apoptosis was further confirmed through the characteristic apoptotic morphological changes and DNA fragmentation. Two compounds (6f and 7h) were highly cytotoxic and were submitted to extend biological testing to determine the likely mechanisms of their cytotoxicity. Results showed that these molecules may induce cytotoxicity via disturbing the redox homeostasis. Importantly, the anticancer activity of 6f and 7h could be due to the intracellular reactive oxygen species hypergeneration through significant loss of glutathione reductase and thioredoxin reductase activities. This eventually leads to oxidative stress-mediated P815 cell apoptosis. Furthermore, the co-administration of 6f or 7h with Methotrexate exhibited a synergistic cytotoxic effect. Conclusions considering their significant anticancer activity and chemosensitivity, 6f and 7h may improve the therapeutic efficacy of the current treatment for cancer.

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3-(1,3-Dioxoisoindolin-2-yl)-N,N-dimethylpropan-1-ammonium perchlorate: Synthesis, crystal structure, docking study and in vitro anticancer activity against the human hepatomas cell line (Hep G2)

Journal of Molecular Structure ◽

10.1016/j.molstruc.2021.131006 ◽

2021 ◽

pp. 131006

Author(s):

Sahin Reja ◽

Deboshmita Mukherjee ◽

Purak Das ◽

Pranesh Kumar ◽

Rajesh Kumar Das

Keyword(s):

Crystal Structure ◽

Anticancer Activity ◽

Cell Line ◽

Ammonium Perchlorate ◽

Docking Study ◽

Hep G2

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Anticancer Activity of Tetrahydrocorysamine against Pancreatic Adenocarcinoma Cell Line PANC-1 In vitro and In vivo

Tropical Journal of Pharmaceutical Research ◽

10.4314/tjpr.v15i1.20 ◽

2016 ◽

Vol 15 (1) ◽

pp. 141 ◽

Cited By ~ 1

Author(s):

Jian-Bo Zhou ◽

Gang Peng ◽

Jun Li ◽

Yu-Cheng Jia ◽

Jia Wang ◽

...

Keyword(s):

Anticancer Activity ◽

Cell Line ◽

Pancreatic Adenocarcinoma ◽

Adenocarcinoma Cell Line ◽

Adenocarcinoma Cell ◽

Pancreatic Adenocarcinoma Cell Line

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SYNTHESIS, SPECTRAL CHARACTERIZATION AND ANTICANCER EVALUATION OF NEW DIAZENYL SCHIFF BASE DERIVATIVES

INDIAN DRUGS ◽

10.53879/id.54.02.10877 ◽

2017 ◽

Vol 54 (02) ◽

pp. 20-28

Author(s):

P. K. N. Sarangi ◽

◽

J. Sahoo ◽

S. K Paidesetty ◽

G. P. Mohanta

Keyword(s):

Schiff Base ◽

Anticancer Activity ◽

Cell Line ◽

Leukemia Cell ◽

Cancer Cell Line ◽

Leukemia Cell Line ◽

Primary Amines ◽

Schiff Base Derivatives ◽

Mcf 7

A series of several diazenyl Schiff base derivatives were designed and synthesized through azo coupling of diazotised primary amines with the novel synthesized Schiff base ligand (E)-N-((2-chloroquinolin-3-yl) methylene)-4-phenylthiazol-2-amine. All the synthesized compounds have been analysed by different spectral techniques such as elemental analysis, 1H NMR, FT-IR, UV-Vis and LC-MS for their structural confirmation. The above conjugates have been studied for their solvent effects by treating them with different solvents. The results of in vitro cytotoxic study of the synthesized compounds against MCF 7 (human breast cancer cell line) and K562 (Chronic Myeloid Leukemia cell line) revealed that some of the compounds show cytotoxic effect. However, the compounds (NZ)-N-(((4-bromo-3-methylphenyl) diazenyl) (2-chloroquinolin-3-yl) methylene)-4-phenylthiazol-2-amine: (5d) and 4-(((Z)-(2-chloroquinolin-3- yl)(4-phenylthiazol-2-ylimino)methyl)diazenyl)phenol (5e) showed potent cytotoxic activity in comparison to other compounds against MCF 7. Corroborating the results of anticancer activity, it is found to be observed that the compound 4- (((Z)- (2-chloroquinolin-3-yl) (4-phenylthiazol-2-ylimino)methyl) diazenyl) phenol (5e) showed excellent anticancer activity against MCF 7, which is further justified by the apoptosis study through Annexin V-FITC/PI analysis.

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IN VITRO ANTIOXIDANT AND ANTICANCER ACTIVITY OF ULVA LACTUCA L.USING MOLT-3 CELL LINE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i5.29825 ◽

2019 ◽

pp. 75-78 ◽

Cited By ~ 1

Author(s):

CHIDAMBARARAJAN P ◽

KEERTHANA V ◽

PRIYADHARSHINI K, ◽

SAKTHIVEL B

Keyword(s):

Anticancer Activity ◽

Cell Line ◽

Radical Scavenging ◽

Cancer Cell Line ◽

Ethanol Extract ◽

Maximum Growth ◽

Ulva Lactuca ◽

Cell Proliferation Inhibition ◽

Free Radical Scavenging Assay

Objective: The aim of the present investigation was to determine the in vitro antioxidant and anticancer activity of the ethanol extract of Ulva lactuca L. Methods: The present study was to investigate the antioxidant and anticancer activity of U. lactuca L. The extract of U. lactuca L. was extracted by ethanol and subject to analysis. An in vitro antioxidant activity of the ethanol extract of U. lactuca L. was performed by 1, 1-diphenyl-2-picrylhydrazyl free radical scavenging assay. Simultaneously anticancer activity was also performed using blood cancer (MOLT-3) cell line, and the species showed a strong selective cell proliferation inhibition of the cancer cell line. Results: The scavenging activity was measured and determined to be 78.5%. This might be due to high polyphenolic compounds and flavonoid contents of the extract, which showed maximum growth inhibition of 74.4%. Conclusion: Thus, the study concludes that the constituents of seaweeds can act as potent in treating various diseases and can be used as an alternative for therapeutic treatment.

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Description of a new hamster ventral prostate cell line containing androgen receptors

In Vitro ◽

10.1007/bf02615074 ◽

1977 ◽

Vol 13 (2) ◽

pp. 108-114 ◽

Cited By ~ 6

Author(s):

James S. Norris ◽

Charles Bowden ◽

P. O. Kohler

Keyword(s):

Cell Line ◽

Androgen Receptors ◽

Ventral Prostate ◽

Prostate Cell ◽

Prostate Cell Line

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Evaluation of Anticancer Activity of Olmesartan and Ramipril On A549 Cell Line

Biomedical & Pharmacology Journal ◽

10.13005/bpj/1498 ◽

2018 ◽

Vol 11 (3) ◽

pp. 1351-1357 ◽

Cited By ~ 1

Author(s):

E Gayathri ◽

K. Punnagai ◽

D. Darling Chellathai

Keyword(s):

Cell Cycle ◽

Flow Cytometry ◽

Anticancer Activity ◽

Cell Line ◽

A549 Cell ◽

Enzyme Inhibitor ◽

A549 Cell Line ◽

Ic50 Values

Angiotensin Converting Enzyme Inhibitor (ACEI) and Angiotensin II type 1 receptor antagonist (ARBs) are the most efficient cardiovascular drugs and exhibited efficient cytostatic activity in vitro in many malignant and normal cells1.OBJECTIVE: This study aims to assess the anticancer activity of these two drugs in a dose dependant manner using A549 cell line through MTT assay and Cell cycle analysis.. MATERIALS AND METHODS: Ramipril and Olmesartan were added to A549 at various concentrations ranging from 10⁻⁶ to 10mM.The dot plot of the cytotoxicity results were used to extrapolate the IC50 values. The dot plot of flow cytometry results were used to extrapolate the DNA percentage in phases of cell cycle. The plates were read at 570 nm by using a PERCLIN ELMER (multimode reader). Measurements for concentration required for 50% inhibition was noted. RESULTS: Ramipril and Olmesartan were added to A549 at various concentrations ranging from 10⁻⁶ to 10mM.The dot plot of the cytotoxicity results were used to extrapolate the IC50 values. The dot plot of flow cytometry results were used to extrapolate the DNA percentage in phases of cell cycle.

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