Synthesis and in vitro evaluation of 2,3-dibromo-3-methyl-1-phenylphospholane 1-oxide for potential anti-proliferative effects

A novel phospha sugar analogue, 2,3-dibromo-3-methyl-1-phenylphospholane 1-oxide (DBMPP), was prepared from 1-phenyl-3-methyl-2- phospholene 1-oxide and evaluated by in vitro MTT method forleukemia cells and microscopic observations forsolid tumor cells, e.g., stomach cancer cells. The evaluation re...

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Bibliographic Details
Published in:Journal of environmental biology 2009-11, Vol.30 (6), p.945-950
Main Authors: Fujie, Michio, Nakamura, Satoki, Asai, Kazuhide, Yamashita, Junko, Kiyofuji, Keita, Yamashita, Mitsuji
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Apoptosis - drug effects
Cell Line, Tumor
Humans
Neoplasms - drug therapy
Organophosphorus Compounds - chemical synthesis
Organophosphorus Compounds - pharmacology
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Summary:A novel phospha sugar analogue, 2,3-dibromo-3-methyl-1-phenylphospholane 1-oxide (DBMPP), was prepared from 1-phenyl-3-methyl-2- phospholene 1-oxide and evaluated by in vitro MTT method forleukemia cells and microscopic observations forsolid tumor cells, e.g., stomach cancer cells. The evaluation revealed clearly that the synthesized phospha sugar analogue DBMPP has competent potentials and excellent anti-cancer activities that killed selectively and specifically the leukemia cells of cell lines of K562 and U937 but did not give any damages on healthy leukocyte. Moreover it was revealed that DBMPP killed solid cancer cells such as stomach cancer cells and melanoma of cell lines of MKN45 and G361. Therefore, DBMPP should exert anti-proliferative effects for different kinds of tumor cells based on the in vitro evaluations. The cell cycle analyses by flow cytometry for K562 and U937 cells clearly demonstrated that the mechanism of the anti-proliferative effect on the human tumor cells is apoptosis induced by DBMPP.
ISSN:0254-8704