Search

Your search keyword '"Stevens, M F G"' showing total 273 results
Start Over Author "Stevens, M F G"
273 results on '"Stevens, M F G"'

2. Summary of Poster-Sessions

Author

Bonmassar, E., Gescher, A., Newell, D. R., Stevens, M. F. G., Giraldi, Tullio, editor, Connors, Thomas A., editor, and Cartei, Giuseppe, editor

Published
1990
Full Text
View/download PDF

14. Benzylidene derivatives of andrographolide inhibit growth of breast and colon cancer cells in vitro by inducing G1 arrest and apoptosis

Author

Jada, Srinivasa Rao, Matthews, Charlie, Saad, Mohd Said, Hamzah, Ahmad Sazali, Lajis, Md Nordin, Stevens, M. F. G., Stanslas, J., Jada, Srinivasa Rao, Matthews, Charlie, Saad, Mohd Said, Hamzah, Ahmad Sazali, Lajis, Md Nordin, Stevens, M. F. G., and Stanslas, J.

Abstract

Background and purpose: Andrographolide, the major phytoconstituent of Andrographis paniculata, was previously shown by us to have activity against breast cancer. This led to synthesis of new andrographolide analogues to find compounds with better activity than the parent compound. Selected benzylidene derivatives were investigated for their mechanisms of action by studying their effects on the cell cycle progression and cell death. Experimental approach: Microculture tetrazolium, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and sulphorhodamine B (SRB) assays were utilized in assessing the in vitro growth inhibition and cytotoxicity of compounds. Flow cytometry was used to analyse the cell cycle distribution of control and treated cells. CDK1 and CDK4 levels were determined by western blotting. Apoptotic cell death was assessed by fluorescence microscopy and flow cytometry. Key results: Compounds, in nanomolar to micromolar concentrations, exhibited growth inhibition and cytotoxicity in MCF-7(breast) and HCT-116 (colon) cancer cells. In the NCI screen, 3,19-(2-bromobenzylidene) andrographolide (SRJ09) and 3,19-(3-chloro-4-fluorobenzylidene) andrographolide (SRJ23) showed greater cytotoxic potency and selectivity than andrographolide. SRJ09 and SRJ23 induced G1 arrest and apoptosis in MCF-7 and HCT-116 cells, respectively. SRJ09 downregulated CDK4 but not CDK1 level in MCF-7 cells. Apoptosis induced by SRJ09 and SRJ23 in HCT-116 cells was confirmed by annexin V-FITC/PI flow cytometry analysis. Conclusion and implications: The new benzylidene derivatives of andrographolide are potential anticancer agents. SRJ09 emerged as the lead compound in this study, exhibiting anticancer activity by downregulating CDK4 to promote a G1 phase cell cycle arrest, coupled with induction of apoptosis.

Published
2008

15. Semisynthesis and in vitro anticancer activities of andrographolide analogues

Author

Jada, Srinivasa Rao, Subur, Genevieve Suseno, Matthews, Charlie, Hamzah, Ahmad Sazali, Lajis, Md Nordin, Saad, Mohammad Said, Stevens, M. F. G., Stanslas, Johnson, Jada, Srinivasa Rao, Subur, Genevieve Suseno, Matthews, Charlie, Hamzah, Ahmad Sazali, Lajis, Md Nordin, Saad, Mohammad Said, Stevens, M. F. G., and Stanslas, Johnson

Abstract

The plant Andrographis paniculata found throughout Southeast Asia contains Andrographolide 1, a diterpenoid lactone, which has antitumour activities against in vitro and in vivo breast cancer models. In the present study, we report on the synthesis of andrographolide derivatives, 3,19-isopropylideneandrographolide (2), 14-acetyl-3,19-isopropylideneandrographolide (3) and 14-acetylandrographolide (4), and their in vitro antitumour activities against a 2-cell line panel consisting of MCF-7 (breast cancer cell line) and HCT-116 (colon cancer cell line). Compounds 2 and 4 were also screened at the US National Cancer Institute (NCI) for their activities against a panel of 60 human cancer cell lines derived from nine cancer types. Compound 2 was found to be selective towards leukaemia and colon cancer cells, and compound 4 was selective towards leukaemia, ovarian and renal cancer cells at all the dose-response parameters. Compounds 2 and 4 showed non-specific phase of the cell cycle arrest in MCF-7 cells treated at different intervals with different concentrations. NCI’s COMPARE and SOM mechanistic analyses indicated that the anticancer activities of these new class of compounds were not similar to that of standard anticancer agents, suggesting novel mechanism(s) of action.

Published
2007

Catalog

Books, media, physical & digital resources
See catalog results