Cover Image

Ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (HL-60)

One of the major problems in cancer therapy is the lack of specificity of chemotherapeutic agents towards cancer cells, resulting in adverse side effects. One means to counter this is to selectively deliver the drug to the cancer cell. Cancer cells accumulate increased concentrations of polyamines...

Full description

Saved in:
Bibliographic Details
Main Authors: Rui, Traquete, Abdul Ghani, Radiah, Phanstiel, Otto, Heather, Wallace
Format: Article
Language:English
Published: Springer 2013
Subjects:
RM300 Drugs and their action
Online Access:http://irep.iium.edu.my/34725/1/Paper_2.pdf
http://irep.iium.edu.my/34725/
http://download.springer.com/static/pdf/187/art%253A10.1007%252Fs00726-012-1452-2.pdf?auth66=1390458631_bf7b320f472fb4848218748a72161e52&ext=.pdf
Tags: Add Tag
No Tags, Be the first to tag this record!
id my.iium.irep.34725
record_format dspace
spelling my.iium.irep.347252014-01-23T00:24:00Z http://irep.iium.edu.my/34725/ Ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (HL-60) Rui, Traquete Abdul Ghani, Radiah Phanstiel, Otto Heather, Wallace RM300 Drugs and their action One of the major problems in cancer therapy is the lack of specificity of chemotherapeutic agents towards cancer cells, resulting in adverse side effects. One means to counter this is to selectively deliver the drug to the cancer cell. Cancer cells accumulate increased concentrations of polyamines compared to normal cells, mainly through an increased uptake of preformed polyamines via the polyamine transport system (PTS). Furthermore, the nonstringent structural requirements of the PTS enable the transport of a range of polyamine-based molecules. Thus, the PTS can be used to transport compounds linked to polyamines selectively to cancer cells. In our laboratory, polyamine–anthracene conjugates have shown potent antitumour activity towards HL-60 cells. The aim of this study was to determine the cytotoxicity of Ant-4,4, a homospermidine–anthracene conjugate, and assess the long-term effects by determining whether cancer cells were able to recover from treatment. During exposure, Ant-4,4 was an effective growth-inhibitory agent in HL-60 cells decreasing viable cell number, protein and polyamine content. Evidence indicates concomitant cell-cycle arrest and increased apoptosis. Once the drug was removed, HL-60 cells recovered gradually over time. Increasing cell number, protein content and polyamine content, as well as diminished effects on cell-cycle and apoptotic stimuli were observed over time. These data suggest that, despite being an effective way of delivering anthracene, these polyamine conjugates do not exert long-lasting effects on HL-60 cells. Springer 2013-01-06 Article REM application/pdf en http://irep.iium.edu.my/34725/1/Paper_2.pdf Rui, Traquete and Abdul Ghani, Radiah and Phanstiel, Otto and Heather, Wallace (2013) Ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (HL-60). Amino Acids, 44 (4). pp. 1193-1203. ISSN 0939-4451 http://download.springer.com/static/pdf/187/art%253A10.1007%252Fs00726-012-1452-2.pdf?auth66=1390458631_bf7b320f472fb4848218748a72161e52&ext=.pdf
institution Universiti Islam Antarabangsa Malaysia
building IIUM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider International Islamic University Malaysia
content_source IIUM Repository (IREP)
url_provider http://irep.iium.edu.my/
language English
topic RM300 Drugs and their action
spellingShingle RM300 Drugs and their action
Rui, Traquete
Abdul Ghani, Radiah
Phanstiel, Otto
Heather, Wallace
Ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (HL-60)
description One of the major problems in cancer therapy is the lack of specificity of chemotherapeutic agents towards cancer cells, resulting in adverse side effects. One means to counter this is to selectively deliver the drug to the cancer cell. Cancer cells accumulate increased concentrations of polyamines compared to normal cells, mainly through an increased uptake of preformed polyamines via the polyamine transport system (PTS). Furthermore, the nonstringent structural requirements of the PTS enable the transport of a range of polyamine-based molecules. Thus, the PTS can be used to transport compounds linked to polyamines selectively to cancer cells. In our laboratory, polyamine–anthracene conjugates have shown potent antitumour activity towards HL-60 cells. The aim of this study was to determine the cytotoxicity of Ant-4,4, a homospermidine–anthracene conjugate, and assess the long-term effects by determining whether cancer cells were able to recover from treatment. During exposure, Ant-4,4 was an effective growth-inhibitory agent in HL-60 cells decreasing viable cell number, protein and polyamine content. Evidence indicates concomitant cell-cycle arrest and increased apoptosis. Once the drug was removed, HL-60 cells recovered gradually over time. Increasing cell number, protein content and polyamine content, as well as diminished effects on cell-cycle and apoptotic stimuli were observed over time. These data suggest that, despite being an effective way of delivering anthracene, these polyamine conjugates do not exert long-lasting effects on HL-60 cells.
format Article
author Rui, Traquete
Abdul Ghani, Radiah
Phanstiel, Otto
Heather, Wallace
author_facet Rui, Traquete
Abdul Ghani, Radiah
Phanstiel, Otto
Heather, Wallace
author_sort Rui, Traquete
title Ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (HL-60)
title_short Ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (HL-60)
title_full Ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (HL-60)
title_fullStr Ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (HL-60)
title_full_unstemmed Ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (HL-60)
title_sort ant 4,4, a polyamine-anthracene conjugate, induces cell death and recovery in human promyelogenous leukemia cells (hl-60)
publisher Springer
publishDate 2013
url http://irep.iium.edu.my/34725/1/Paper_2.pdf
http://irep.iium.edu.my/34725/
http://download.springer.com/static/pdf/187/art%253A10.1007%252Fs00726-012-1452-2.pdf?auth66=1390458631_bf7b320f472fb4848218748a72161e52&ext=.pdf
_version_ 1643610670227259392
score 13.211869

Similar Items