Determination of pinostilbene in rat plasma by LC-MS/MS: Application to a pharmacokinetic study.

摘要: Pinostilbene (3-methoxyresveratrol or trans-3,4'-dihydroxy-5-methoxystilbene) is a naturally occurring monomethylether analogue of resveratrol (trans-3,5,4'-trihydroxystilbene) that exhibits various pharmacological activities. To further examine its medicinal potential, sensitive LC-MS/MS method was developed and validated for the determination pinostilbene in rat plasma. Heavy Isotope labelled used as an internal standard. The ESI operated negative ion mode while were measured by multiple reaction monitoring (MRM) using precursor-to-product transitions m/z 241→181 233→191, respectively. This had excellent selectivity, sensitivity (LLOQ=1ng/ml), accuracy (both intra- interday analytical recovery within 100±15%) precision RSD < 15%). matrix effect insignificant. pharmacokinetics subsequently profiled Sprague-Dawley rats. Upon intravenous administration (5 10mg/kg), displayed rapid clearance (Cl=129±42 107±31ml/min/kg) extremely short mean transit time (MTT=6.24±0.41 8.52±1.38min). After oral dosing (50mg/kg), bioavailability limited but highly erratic (F=1.87±2.67%). Pharmacokinetic comparison among pinostilbene, some analogues suggested stilbenes with meta-hydroxyl group(s) may be associated metabolic instability suffer from low bioavailability. information obtained this study will facilitate exploration on well other analogues.