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

Preparation of penta-O-galloyl-β-D-glucose from tannic acid and plasma pharmacokinetic analyses by liquid-liquid extraction and reverse-phase HPLC.
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DOI:
10.1016/j.jpba.2010.09.028
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发表时间:
2011-02-20
影响因子:
3.4
通讯作者:
Lü J
Lü J
中科院分区:
医学3区
文献类型:
--
作者:
Li L;Shaik AA;Zhang J;Nhkata K;Wang L;Zhang Y;Xing C;Kim SH;Lü J

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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 (Cmax) were approximately 3–4 μM at a dose of 0.5 mg per mouse (~20 mg/kg) at 2 h post-injection (Tmax).
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