A Fluorescent Alkyllysophospholipid Analog Exhibits Selective Cytotoxicity Against the Hormone-Insensitive Prostate Cancer Cell Line PC3

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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A Fluorescent Alkyllysophospholipid Analog Exhibits Selective Cytotoxicity Against the Hormone-Insensitive Prostate Cancer Cell Line PC3



Anti-Cancer Agents in Medicinal Chemistry, 14(4): 528-538.

Author(s): Pranati Samadder, Hoe-Sup Byun, Robert Bittman and Gilbert Arthur.

Affiliation: Department of Biochemistry and Medical Genetics, University of Manitoba, 754 Bannatyne Avenue, Winnipeg, Manitoba, Canada R3E 0J9.

Abstract

A fluorescent analog of ET-18-OCH3, 1-O-(7’-N,N-dimethylamino-3’-pentadecanoyl-1’-naphthyl)-2-O-methyl-sn-glycerophosphocholine (1), was synthesized and its bioactivity was screened against 12 human cancer cell lines. The bioactivity of 1 was found to differ markedly from that of ET-18-OCH3. Growth of two prostate cell lines (PC3 and DU145) and a glioma cell line (U251) was significantly affected by 1, with IC50 values of 2, 6, and 12 µM, respectively. Compound 1 was cytotoxic to PC3 cells by caspasedependent apoptosis. The subcellular distribution of 1 differed from that reported for a phenyl-polyene analog of ET-18-OCH3; 1 was found to be localized in the endoplasmic reticulum, mitochondria, and lysosomes but not in the plasma membrane or nucleus of PC3 cells. However, no differences in accumulation of 1 were found between PC3 and cells that were not affected by the compound, implying that the selective PC3 cytotoxicity is a consequence of specific molecular components of PC3 cells.

Keywords:

Antitumor ether lipids, edelfosine, fluorescent alkylphospholipid analog, naphthol-edelfosine, PC3 cells, selective toxicity.



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Article Details

Volume: 14
Issue Number: 4
First Page: 528
Last Page: 538
Page Count: 11
DOI: 10.2174/1871520614666140309223603
Price: $58
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