アンフィフィリックポリメタクリlate誘導体は,抗微生物剤として使用されます

Kenichi Kuroda¹, William F DeGrado

¹Department of Biochemistry and Biophysics, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

Journal of the American Chemical Society

|March 24, 2005

まとめ

より小さなカチオンのポリマーは,抗微生物活性が低下し,低血解作用を示します. ブチル群の含有量が高くなると,細菌細胞の選択性が低下する.

科学分野:

ポリマー化学のポリマー化学について
抗微生物剤抗微生物剤抗微生物剤抗微生物剤
バイオマテリアルバイオマテリアル

背景:

カチオンのアンフィフィリックポリマーは,抗菌薬の応用のために調査されています.
構造活動関係は,ポリマーの性能を最適化するために不可欠です.
ポリメタクリlateの誘導体は,調節可能な性質を提供します.

研究の目的:

cationic amphiphilic polymethacrylate derivatesの構造活動関係を調査する. カチオンのアンフィフィリックポリメタクリlate誘導体の構造活動関係を調査する.
これらのポリマーの抗微生物および溶血作用を評価する.
ポリマーの性能に対する分子量と水性抵抗性の影響を決定する.

主な方法:

Bocで保護されたポリメタクリラート前駆体による合成.
三酸 (TFA) を用いて保護を解除し,カチオンの共ポリマーを生成する.
最低阻害濃度 (MIC) を決定するための抗菌剤測定法.
毒性を評価するための血液溶解測定法.

主要な成果:

分子重量2000Da未満のポリマーは,MICが最も低く,血解活性が低下しました.
ブチル基含有量 (水性) の増加は,細菌細胞に対する選択性の低下と相関する.
分子重量は,抗菌剤の効能と血解性可能性の両方に大きく影響します.

結論:

分子重量を最適化することは,より安全で効果的なキャチオン性抗菌ポリマーの開発の鍵です.
水嫌性は,ポリメタクリlate誘導体の細菌細胞に対する選択性に影響します.
構造-活性関係に関するさらなる研究は,標的型抗菌剤の設計を導くことができます.

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