Penta-O-Galloyl-β-D-Glucose Applications in Cancer Therapeutics

Penta-O-galloyl-β-D-glucose (PGG) is a naturally occurring gallotannin extracted from diverse plant sources. Preclinical studies have revealed its capacity to interfere with multiple hallmarks of cancer, including dysregulated proliferation, evasion of apoptosis, aberrant cell cycle progression, angiogenesis and metastatic spread. PGG exerts its effects by modulating key signalling axes such as p53, AMPK-ULK1, ERK/STAT3 and the PI3K/AKT pathway. These actions culminate in cell cycle arrest at G1 or S phase, induction of programmed cell death through both apoptotic and autophagic routes, and inhibition of DNA replication in tumour cells. In several xenograft models, oral or intraperitoneal administration of PGG markedly suppresses tumour growth without overt host toxicity. Furthermore, PGG enhances the efficacy of established chemotherapeutic and radiotherapy regimens, suggesting a role as an adjuvant agent. Despite these promising findings, comprehensive data on pharmacokinetics, bioavailability and long-term safety remain limited. Rigorous investigations into formulation, delivery systems and potential drug–drug interactions are essential to define the clinical utility of PGG in cancer therapeutics.

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Penta-O-Galloyl-β-D-Glucose Applications in Cancer Therapeutics publication trend

The graph below shows the total number of articles in penta-o-galloyl-β-d-glucose applications in cancer therapeutics across all publications each year (not limited to Nature Index journals).

Technical terms

Gallotannin: A class of polyphenolic compounds composed of gallic acid esters known for diverse bioactivities.

Apoptosis: Programmed cell death characterised by caspase activation, chromatin condensation and membrane blebbing.

Autophagy: Intracellular degradation pathway that sequesters cytoplasmic components in autophagosomes for lysosomal breakdown.

Cell cycle arrest: The halt of cell cycle progression at defined checkpoints (G1 or S phase) to prevent proliferation.

Xenograft: Transplantation of human tumour cells into immunocompromised animals to assess in vivo efficacy of anticancer agents.

Pharmacokinetics: The study of a compound’s absorption, distribution, metabolism and excretion within a biological system.

References

1. Pentagalloyl Glucose: A Review of Anticancer Properties, Molecular Targets, Mechanisms of Action, Pharmacokinetics, and Safety Profile. Molecules (2023).
2. Penta-O-galloyl-β-D-glucose induces G1arrest and DNA replicative S-phase arrest independently of P21 cyclin-dependent kinase inhibitor 1A, P27 cyclin-dependent kinase inhibitor 1B and P53 in human breast cancer cells and is orally active against triple-negative xenograft growth. Breast Cancer Research (2010).
3. Apoptotic and DNA Damage Effect of 1,2,3,4,6-Penta-O-galloyl-beta-D-glucose in Cisplatin-Resistant Non-Small Lung Cancer Cells via Phosphorylation of H2AX, CHK2 and p53. Cells (2022).
4. Penta-O-Galloyl-β-D-Glucose in Pistacia integerrima Targets AMPK-ULK1 and ERK/STAT3 Signaling Axes to Induce ROS-Independent Autophagic Cell Death in Human Lung Cancer Cells. Frontiers in Pharmacology (2022).