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Anti-Cancer, Anti-Diabetic and Other Pharmacologic and Biological Activities of Penta-Galloyl-Glucose

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Abstract

1, 2, 3, 4, 6-penta-O-galloyl-β-D-glucose (PGG) is a polyphenolic compound highly enriched in a number of medicinal herbals. Several in vitro and a handful of in vivo studies have shown that PGG exhibits multiple biological activities which implicate a great potential for PGG in the therapy and prevention of several major diseases including cancer and diabetes. Chemically and functionally, PGG appears to be distinct from its constituent gallic acid or tea polyphenols. For anti-cancer activity, three published in vivo preclinical cancer model studies with PGG support promising efficacy to selectively inhibit malignancy without host toxicity. Potential mechanisms include anti-angiogenesis; anti-proliferative actions through inhibition of DNA replicative synthesis, S-phase arrest, and G1 arrest; induction of apoptosis; anti-inflammation; and anti-oxidation. Putative molecular targets include p53, Stat3, Cox-2, VEGFR1, AP-1, SP-1, Nrf-2, and MMP-9. For anti-diabetic activity, PGG and analogues appear to improve glucose uptake. However, very little is known about the absorption, pharmacokinetics, and metabolism of PGG, or its toxicity profile. The lack of a large quantity of highly pure PGG has been a bottleneck limiting in vivo validation of cancer preventive and therapeutic efficacies in clinically relevant models.

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GRANT SUPPORT

This work was supported, in parts, by The Hormel Foundation, NIH grant CA136953 and by MRC grant (No. 2009-0063466) from Korea Ministry of Education, Science and Technology.

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Authors and Affiliations

  1. The Hormel Institute, University of Minnesota, 801 16th Avenue NE, Austin, MN, 55912, USA

    Jinhui Zhang, Li Li, Sung-Hoon Kim & Junxuan Lü

  2. Cancer Preventive Material Development Research Center and Institute, College of Oriental Medicine, Kyunghee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul, 130-701, Republic of Korea

    Sung-Hoon Kim

  3. Department of Chemistry & Biochemistry, Miami University, Oxford, OH, 45056, USA

    Ann E. Hagerman

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  1. Jinhui Zhang
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  2. Li Li
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  4. Ann E. Hagerman
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  5. Junxuan Lü
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Correspondence to Sung-Hoon Kim or Junxuan Lü.

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Zhang, J., Li, L., Kim, SH. et al. Anti-Cancer, Anti-Diabetic and Other Pharmacologic and Biological Activities of Penta-Galloyl-Glucose. Pharm Res 26, 2066–2080 (2009). https://doi.org/10.1007/s11095-009-9932-0

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  • DOI: https://doi.org/10.1007/s11095-009-9932-0

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