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 1μg/mL in mouse plasma was 70.0±1.3% (n=5). The limit of detection (LOD) for PGG was approximately 0.2μg/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 3-4μM at a dose of 0.5mg per mouse (∼20mg/kg) at 2h post-injection (T max).
|Original language||English (US)|
|Number of pages||6|
|Journal||Journal of Pharmaceutical and Biomedical Analysis|
|State||Published - Feb 20 2011|
Bibliographical noteFunding Information:
The authors thank Professor Ann Hagerman, Department of Chemistry and Biochemistry, Miami University, Oxford OH 45056 for providing initial protocol, reference compounds and valuable advices. The assistance of Ellen Kroc and animal facility staff and Todd Schuster of Shared Instruments Core facility is gratefully acknowledged. This work was supported by NIH grant CA136953 .
- Acidic methanolysis
- Liquid-liquid extraction
- Mouse plasma
- Penta-galloyl glucose