Absence in amphotericin B‐spiked human plasma of the free monomeric drug, as detected by SERS

FEBS Letters

Bolard, Jacques¹  Ridente, Yara¹  Aubard, Jean² 

[1] Laboratoire de Physicochimie Biomoléculaire et Cellulaire (LPBC) (ESA CNRS 7033), Case 138, Université Pierre et Marie Curie, 75252 Paris Cedex 05, France;Institut de Topologie et de Dynamique des Systèmes (ITODYS) (ESA CNRS 7086), Université Denis Diderot, 1 rue Guy de la Brosse, 75005 Paris, France

关键词: Amphotericin B;    Lipoprotein;    Low density lipoprotein;    Plasma;    Surface enhanced Raman spectroscopy;   

DOI  :  10.1016/S0014-5793(99)00238-0

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Using surface enhanced Raman spectroscopy (SERS) which enables us to specifically detect traces of monomeric amphotericin B (AmB), we were able to show that in a 10⁻⁵ M AmB suspension, the concentration of free drug was below 10⁻⁸ M in the presence of low density lipoproteins (LDL) or plasma. The affinity constant of AmB for LDL determined from electronic absorption data, was found to be 4×10⁶ M⁻¹. Therefore, since AmB appears to be in the majority bound to lipoproteins under in vivo conditions, its toxicity should not result from the induction of host-cell transmembrane permeability but rather from the internalization of the AmB-LDL complex.

【 授权许可】

Unknown