Guiyun Cao*, Suqiao Han, Keke Li, Li Shen, Xiaohong Wang and Youbo Zhang Pages 67 - 73 ( 7 )
Background: Ferruginol (FRGN) exhibits a broad range of pharmacological properties which make it a promising candidate for chemoprevention. However, little is known about its absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties.
Methods: A rapid, sensitive and specific HPLC-DAD method was established to quantify FRGN in the plasma and tissues of Wistar rats. After extraction of FRGN with ethyl acetate (EtOAc), chromatographic separation was performed on a YMC ODS C18 column (250 × 4.6 mm I.D., 5 µm) with a mobile phase consisting of methanol-water (92:8, v/v) at a flow rate of 0.9 mL/min. Detection was conducted with a wavelength of 273 nm at 25 °C.
Results: The calibration curves for FRGN were linear in the concentration range of 0.5-20 µg/mL for plasma, 0.5-10 µg/mL for heart, liver, spleen, lung, kidney, stomach, intestine, brain and muscle. After three cycles of freezing and thawing, the concentration variations were within ± 7% of nominal concentrations, indicating no significant substance loss during repeated thawing and freezing. The assay was applied to pharmacokinetic and tissue distribution study in rats. Results suggested that lung, heart, liver, spleen and kidney were the major distribution tissues of FRGN in rats, and FRGN could permeate the blood-brain barrier to distribute in the brain of rats.
Conclusion: The information provided by this research is very useful for gaining knowledge of the pharmacokinetic process and tissue distribution of FRGN.
Ferruginol, pharmacokinetics, tissue distribution, HPLC-DAD, Wistar rats, calibration.
Jiangsu Key Laboratory of Experimental & Translational Non-coding, RNA Research, medical department, Yangzhou University, Yangzhou, 225001, Medical department, Yangzhou University, Yangzhou 225001, Medical department, Dalian University, Dalian 116622, Medical department, Yangzhou University, Yangzhou 225001, Jiangsu Key Laboratory of Experimental & Translational Non-coding, RNA Research, medical department, Yangzhou University, Yangzhou, 225001, State Key Laboratory of Natural and Biomimetic Drugs, Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, Beijing 100191