パラジアム,金,銀のN-ヘテロサイクリックカルベンの複合体に基づく抗癌および抗微生物金属製薬剤

Sriparna Ray¹, Renu Mohan, Jay K Singh

¹Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai 400 076, India.

Journal of the American Chemical Society

|November 9, 2007

まとめ

新しいパラジウム,金,銀複合体とN-ヘテロサイクリックカルベンが合成されました. パラジウム複合体は,シスプラチンよりも強力な抗がん活性を示し,金銀複合体は,抗菌特性を示しています.

科学分野:

有機金属化学有機金属化学
薬用化学薬用化学について
マテリアルサイエンス材料科学

背景:

N-ヘテロサイクリックカルベン (NHCs) は,協調化学における多用途リガンドである.
NHCの金属複合体は,生物医学的な応用において有望であることが示されています.

研究の目的:

1-ベンジル-3-テルト-ブチリミダゾール-2-イリデンのリガンドを含む新しいパラジウム,金,銀複合体を合成し,特徴づけること.
これらの金属複合体の抗がんおよび抗菌作用を評価する.

主な方法:

金属複合体の合成は,直接反応または伝送反応による.
X線微分法を用いた構造の解明.
抗増殖および抗微生物活性に関するインビトロ評価.

主要な成果:

2つのパラジウム複合体 (1a,1b),1つの金複合体 (1c),1つの銀複合体 (1d) が成功して合成され,構造的に特徴づけられました.
パラジウム複合体1bは,子宮頸がん,乳がん,結腸がんの細胞系に対する有意な抗増殖活性を示し,シスプラチンよりも高い.
複合体1bが誘発したG2細胞サイクル停止と,p53依存経路によるプログラム細胞死.
ゴールド複合体1cとシルバー複合体1dは,バチルス・サブティリスに対する抗菌活性を示し,1cは1dの2倍に強力であった.

結論:

合成されたパラジウム複合体は強力な抗がん性を持ち,がん治療のためのさらなる調査を正当化しています.
金と銀の複合体は,有望な抗菌活性を示し,細菌感染症との闘いにおける潜在的な応用を示唆しています.

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