Studies on the cytostatic and cytotoxic effects and mode of action of 8-nitro-7-hydroxycoumarin.

  title={Studies on the cytostatic and cytotoxic effects and mode of action of 8-nitro-7-hydroxycoumarin.},
  author={Denise A. Egan and Philippe James and D. L. Cooke and Richard O'Kennedy},
  journal={Cancer letters},
  volume={118 2},
A derivative of coumarin, 8-nitro-7-hydroxycoumarin (8-NO2-7-OHC), was synthesised, purified and characterised. The cytostatic and cytotoxic nature of this compound was determined using both human and animal cell lines grown in vitro for 96 h in the presence of drug (0-500 microM, equivalent to 0-104 microg/ml). 8-NO2-7-OHC was shown to be cytotoxic to three cell lines, but cytostatic to all cell lines tested. With K562 and HL-60 cells, cell death was found to occur by apoptosis. This cytotoxic… Expand
In vitro cytotoxic potential and mechanism of action of selected coumarins, using human renal cell lines.
Results would suggest that 6-NO(2)-7- OHC and 7,8-OHC might have a therapeutic role to play in the treatment of renal cell carcinoma. Expand
A study of the role of cell cycle events mediating the action of coumarin derivatives in human malignant melanoma cells.
These and other nitro-derivatives of 7-OHC may represent novel therapeutic agents for the treatment of malignant melanoma as they are capable of selective and irreversible cytotoxicity. Expand
Investigation of intracellular signalling events mediating the mechanism of action of 7-hydroxycoumarin and 6-nitro-7-hdroxycoumarin in human renal cells.
6-NO2-7-OHC may represent a novel therapeutic agent for the treatment of RCC's and modulated signalling events associated with cellular differentiation and apoptosis, suggesting its mechanism of action may be the promotion of cellular maturation and/or death. Expand
In vitro cytotoxicity of benzopyranone derivatives with basic side chain against human lung cell lines.
In vitro cytotoxicity of new coumarin-based benzopyranone derivatives containing diethylaminoethoxy and piperidinylethoxy showed anticancer activity against lung cancer cell lines, while compound 6 showed highly selective antic cancer activity. Expand
An in vitro investigation of the induction of apoptosis and modulation of cell cycle events in human cancer cells by bisphenanthroline-coumarin-6,7-dioxacetatocopper(II) complex.
[Cu(cdoa)(phen)(2)] has been shown to be a more potent anti-proliferative agent than either the ligand or cisplatin, and is capable of altering key biochemical events leading to the execution of apoptotic and/or necrotic cell death, suggesting that it is worthy of further investigation. Expand
Cytotoxic Effects of Hydroxy Coumarin Derivatives on Mouse Neuroblastoma N2a Cell Line
Neuroblastoma is one of the nervous system cancers, which approximately consists of 9% of childhood cancers. In this study, we evaluated the toxic effects of prenyl hydroxy coumarin derivatives onExpand
Cytotoxic Properties of Three Isolated Coumarin-hemiterpene Ether Derivatives from Artemisia armeniaca Lam.
Considering multiple reports on cytotoxic activity of the Artemisia genus and its phytochemicals, in the current study A. armeniaca Lam. and the three components isolated from the plant wereExpand
Study of the in vitro cytotoxic potential of natural and synthetic coumarin derivatives using human normal and neoplastic skin cell lines
The cytotoxic potential of coumarins appears to be highly dependent on the nature and position of the functional group, suggesting that these nitro-derivatives may have a chemotherapeutic role in the future. Expand
Role of cell cycle events and apoptosis in mediating the anti-cancer activity of a silver(I) complex of 4-hydroxy-3-nitro-coumarin-bis(phenanthroline) in human malignant cancer cells.
Taking together, [Ag(hnc)(phen)(2)] has been shown to be a more potent anti-proliferative agent than cisplatin, capable of altering key biochemical events leading to cell death. Expand
Activation of mitogen activated protein kinase pathways and melanogenesis by novel nitro-derivatives of 7-hydroxycomarin in human malignant melanoma cells.
  • G. Finn, B. Creaven, D. Egan
  • Biology, Medicine
  • European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
  • 2005
It is established that exposure of human malignant melanoma cells to these drugs leads to a modulation of p38 MAP kinase phosphorylation, which implies that these drugs may function by altering both melanogenesis and cellular differentiation. Expand


Inhibition of Chemical Carcinogen-induced Neoplasia by Coumarins and α-Angelicalactone
Coumarin, umbelliferone (7-hydroxycoumarin), scopoletin (7-hydroxy-6-methoxycoumarin), and limettin (5,7-dimethoxycoumarin), four naturally occurring plant constituents, were studied for theirExpand
Antiproliferative effect of esculetin on vascular smooth muscle cells: possible roles of signal transduction pathways.
The results suggest that the antiproliferative effect of esculetin on vascular smooth muscle cells may be partly mediated through inhibition of protein tyrosine kinase and modulated by inhibition of lipoxygenase. Expand
Suppression of 7,12-Dimethylbenz(α) Anthracene-Induced Breast Carcinoma by Coumarin in the Rat
The effect of oral administration of coumarin on the induction of breast tumors brought about by DMBA has been studied in female Wistar rats. Coumarin given before DMBA caused a significantExpand
Induction of apoptosis (programmed cell death) in human leukemic HL-60 cells by inhibition of RNA or protein synthesis.
The results suggest that certain dividing cell populations do not require RNA or protein synthesis to undergo apoptosis and further, that continuous transcription and translation of some regulatory protein(s) may be required to maintain control over the apoptotic "machinery" of such cells. Expand
Coumarins : biology, applications, and mode of action
List of contributors. Preface. History of the Development and Applications of Coumarin and Coumarin--related Compounds (I. Weinmann). The Chemistry and Occurrence of Coumarins (G. Keating & R. OaExpand
Induction of apoptosis in cells of the immune system by cytotoxic stimuli.
  • T. Cotter
  • Chemistry, Medicine
  • Seminars in immunology
  • 1992
It is shown that when cells of the immune system are exposed to a range of cytotoxic agents, such as the RNA synthesis inhibitor actinomycin D, the DNA polymerase inhibitor aphidicolin or the topoisomerase I inhibitor campthothecin, they rapidly undergo cell death via apoptosis. Expand
Detection of P-glycoprotein in multidrug-resistant cell lines by monoclonal antibodies
Monoclonal antibodies whose binding to plasma membranes of different multidrug-resistant mammalian cells correlates with the degree of drug resistance are produced and might serve as diagnostic reagents for clinically unresponsive tumours16. Expand
Prevention of tumorigenesis of oncogene-transformed rat fibroblasts with DNA site inhibitors of poly(ADP ribose) polymerase.
  • A. Tseng, W. Lee, +5 authors E. Kun
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
  • 1987
Poly(ADP ribose) polymerase was inhibited by the drug in both untreated and dexamethasone-treated cells both in vitro and in vivo to the same extent, but biological consequences of enzyme inhibition were manifest only when the cells were in the transformed tumorigenic state. Expand
Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays.
  • T. Mosmann
  • Biology, Medicine
  • Journal of immunological methods
  • 1983
A tetrazolium salt has been used to develop a quantitative colorimetric assay for mammalian cell survival and proliferation and is used to measure proliferative lymphokines, mitogen stimulations and complement-mediated lysis. Expand
The pharmacology, metabolism, analysis, and applications of coumarin and coumarin-related compounds.
(1990). The Pharmacology, Metabolism, Analysis, and Applications of Coumarin and Coumarin-Related Compounds. Drug Metabolism Reviews: Vol. 22, No. 5, pp. 503-529.