Controlling Plasma Protein Binding: Structural Correlates of Interactions of Hydrophobic Polyamine Endotoxin Sequestrants with Human Serum Albumin

2008 ◽  
Vol 5 (6) ◽  
pp. 1131-1137 ◽  
Author(s):  
Thuan B. Nguyen ◽  
E. V. K. Suresh Kumar ◽  
Diptesh Sil ◽  
Stewart J. Wood ◽  
Kelly A. Miller ◽  
...  
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Protein Binding ◽  
Human Serum ◽  
Plasma Protein Binding ◽  
Plasma Protein

Evaluation of the human serum albumin column as a discovery screening tool for plasma protein binding

2002 ◽  
Vol 15 (2) ◽  
pp. 209-215 ◽  
Author(s):  
Lisa Buchholz ◽  
Chun-Hua Cai ◽  
Larry Andress ◽  
Adriaan Cleton ◽  
Joanne Brodfuehrer ◽  
...  
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Protein Binding ◽  
Human Serum ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Screening Tool ◽  
Human Serum Albumin Column

scholarly journals Pharmacokinetics, Tissue Distribution, and Human Serum Albumin Binding Properties of Delicaflavone, a Novel Anti-Tumor Candidate

2021 ◽  
Vol 12 ◽  
Author(s):  
Bing Chen ◽  
Hongbin Luo ◽  
Weiying Chen ◽  
Qishu Huang ◽  
Kaifan Zheng ◽  
...  
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Protein Binding ◽  
Human Serum ◽  
Tissue Distribution ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Anticancer Agent ◽  
Dose Range ◽  
Binding Properties

Delicaflavone (DF), a natural active ingredient from Selaginella doederleinii Hieron, has been reported to have favorable anticancer effects and is thus considered a potential anticancer agent. However, its pharmacokinetics and plasma protein binding properties remain unknown. Here, we investigated the pharmacokinetic profile of DF in rats using a validated HPLC-MS/MS methods, as well as its human serum albumin (HSA) binding properties through multi-spectroscopic and in silico methods. The results showed that DF was rapidly eliminated and had a widespread tissue distribution after intravenous administration. DF showed linear dynamics in the dose range of 30–60 mg/kg and poor oral bioavailability. The major distribution tissues of DF were the liver, lungs, and kidneys. Ultraviolet and fluorescence spectroscopy and molecular docking demonstrated that DF had a static quenching effect on HSA, with one binding site, and relatively strong binding constants. Thermodynamic analysis of the binding data revealed that hydrogen bonding and van der Waals interactions played major roles in binding. The results of this study further our understanding of the pharmacokinetic and plasma protein binding properties of the potential anticancer agent DF and shed light on pharmacological strategies that may be useful for the development of novel cancer therapeutics.

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