Determination and Disposition Kinetics of Phellamurin Metabolites in Rat Brain
HUNG-YI CHEN1, TIAN-SHUNG WU2, YU-CHI HOU3, SHENG-CHU KUO1 AND PEI-DAWN LEE CHAO4*
1. Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan, R.O.C.
2. Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, R.O.C.
3. Jen-Te Junior College of Medicine, Nursing and Management, Miaoli, Taiwan, R.O.C.
4. Department of Pharmacy, China Medical College, 91 Hsueh-Shih Rd., Taichung, Taiwan 404, R.O.C.
Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan, R.O.C.Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan, R.O.C.
(Received: March 27, 2001; Accepted: May 15, 2001)
ABSTRACT
Phellamurin is a flavanone glycoside that is abundant in the leaves of Phellodendron wilsonii Hayata et Kanehira (Rutaceae). The disposition kinetics of phellamurin metabolites in rat brain was investigated in this study. Doses of 100 mg/kg and 200 mg/kg were orally administered to rats. At 0.33, 2, 4 and 6 hr after dosing, rats were dissected and the brain concentrations of the aglycone neophellamuretin were determined by an HPLC method prior to and after hydrolysis with β-glucuronidase. The mobile phase was acetonitrile: H2O (containing 1% acetic acid, 38:62, v/v). Our results indicated that neophellamuretin glucuronide might be able to cross the blood-brain barrier and its concentration in the brain was dose-dependent at the two doses investigated, whereas the aglycone neophellamuretin was present in a trace amount in the brain.
Key words: phellamurin, neophellamuretin, neophellamuretin glucuronides, brain distribution