Anti-cancer, anti-diabetic and other pharmacologic and biological activities of penta-galloyl-glucose

Jinhui Zhang, Li Li, Sung Hoon Kim, Ann E. Hagerman, Junxuan Lü

Research output: Contribution to journalReview article

161 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)2066-2080
Number of pages15
JournalPharmaceutical Research
Volume26
Issue number9
DOIs
StatePublished - Sep 1 2009

Fingerprint

Prostaglandins G
Rubiaceae
Bioactivity
Glucose
Neoplasms
Toxicity
Polyphenolic compounds
Gallic Acid
Pharmacokinetics
Transcription Factor AP-1
Polyphenols
Tea
Medical problems
Matrix Metalloproteinases
S Phase
Metabolism
Apoptosis
Inflammation

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)

Cite this

Zhang, Jinhui ; Li, Li ; Kim, Sung Hoon ; Hagerman, Ann E. ; Lü, Junxuan. / Anti-cancer, anti-diabetic and other pharmacologic and biological activities of penta-galloyl-glucose. In: Pharmaceutical Research. 2009 ; Vol. 26, No. 9. pp. 2066-2080.
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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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Anti-cancer, anti-diabetic and other pharmacologic and biological activities of penta-galloyl-glucose. / Zhang, Jinhui; Li, Li; Kim, Sung Hoon; Hagerman, Ann E.; Lü, Junxuan.

In: Pharmaceutical Research, Vol. 26, No. 9, 01.09.2009, p. 2066-2080.

Research output: Contribution to journalReview article

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