| 論文名 |
New modified β-cyclodextrin derivatives as detoxifying agents of chemical warfare agents (II). In vitro detoxification of cyclosarin (GF): general screening and toxicokinetic aspects of OP scavengers. |
| 著者 |
Susanne M?ller
Fran?ois Estour
Raman Kumar Kalakuntla
Romain Le Provost
Olivier Lafont
Franz Worek
Horst Thiermann
Georg Reiter
|
| キーワード |
|
| 出版年月 |
1970年1月 |
| 発表先 |
Toxicol Lett. 2013 Feb 4;216(2-3):206-12. |
| WEBサイト |
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| 論文概要（和文） |
化学兵器の解毒剤としての新しい修飾β-シクロデキストリン誘導体（II）。 シクロサリン（GF）のin Vitro解毒：一般的なスクリーニングとOPスカベンジャーの毒性動態的側面。 |
| 論文概要（英文） |
As standard therapy of intoxication with organophosphorus (OP) compounds is still insufficient, developing new treatment strategies is urgently required. For evaluating potential of OP detoxification of several compounds correctly, different toxicodynamic impact of OP enantiomers has to be considered thoroughly. It has already been demonstrated that β-cyclodextrin (β-CD) derivatives with attached nucleophilic substituent iodosobenzoic acid (IBA) can be regarded as potent OP scavengers due to an accelerating effect on decay of different OP. Herein, six CD derivatives permethylated or not on CD torus as well as differently attached nucleophilic substituent IBA derivative were investigated regarding detoxification of GF as an OP model substance. Acceleration of GF detoxification could be detected for all compounds with highest rate constants for propylene chain linked nucleophilic substituents on CD derivative. In addition, fast initial binding of GF on CD could be observed and is ascribed to formation of CD complexes. Furthermore, terminal plateau phase was detected of about 1% of each enantiomer reflecting the necessity of a quantitative determination at low concentrations. Moreover, this molecular depot formation may represent an additional detoxification pathway for OP. |
