Preparation of penta-O-galloyl-β-d-glucose from tannic acid and plasma pharmacokinetic analyses by liquid-liquid extraction and reverse-phase HPLC

Li Li, Ahmad Ali Shaik, Jinhui Zhang, Katai Nhkata, Lei Wang, Yong Zhang, Chengguo Xing, Sung Hoon Kim, Junxuan Lü

Research output: Contribution to journalArticlepeer-review

38 Scopus citations

Abstract

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 languageEnglish (US)
Pages (from-to)545-550
Number of pages6
JournalJournal of Pharmaceutical and Biomedical Analysis
Volume54
Issue number3
DOIs
StatePublished - Feb 20 2011

Bibliographical note

Funding 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 .

Keywords

  • Acidic methanolysis
  • HPLC
  • Liquid-liquid extraction
  • Mouse plasma
  • Penta-galloyl glucose
  • Pharmacokinetics

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