Preparation of penta-O-galloyl-β-D-glucose from tannic acid and plasma pharmacokinetic analyses by liquid-liquid extraction and reverse-phase HPLC.
The gallotannin penta-O-galloyl-beta-D-glucose (PGG) has many biological activities including in vivo anti-cancer efficacy. We present in this paper a scaled-up protocol for its preparation in high purity from tannic acid by acidic methanolysis with typical yield of 15%. We also describe a method for the analysis of PGG in mouse plasma by HPLC and its application in preliminary pharmacokinetic studies. A liquid-liquid extraction (LLE) protocol was optimized for the extraction of PGG from mouse plasma. The extraction efficiency for PGG at 1 μg/mL in mouse plasma was 70.0±1.3% (n=5). The limit of detection (LOD) for PGG was approximately 0.2 μg/mL. Preliminary pharmacokinetic parameters of PGG following a single i.p. injection with 5% ethanol/saline vehicle in mice were established. The peak plasma PGG concentrations (C(max)) were approximately 3-4 μM at a dose of 0.5 mg per mouse (∼20 mg/kg) at 2 h post-injection (T(max)).
Li
Li
L
The Hormel Institute, University of Minnesota, 801 16th Avenue NE, Austin, MN 55912, USA.
Shaik
Ahmad Ali
AA
Zhang
Jinhui
J
Nhkata
Katai
K
Wang
Lei
L
Zhang
Yong
Y
Xing
Chengguo
C
Kim
Sung-Hoon
SH
Lü
Junxuan
J
D000818:Animals; D002138:Calibration; D002851:Chromatography, High Pressure Liquid; D005260:Female; D047348:Hydrolyzable Tannins / Q000097:blood / Q000302:isolation & purification* / Q000493:pharmacokinetics*; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D013634:Tannins / Q000737:chemistry*
D047348:Hydrolyzable Tannins; D013634:Tannins; C435084:pentagalloylglucose