1,2,3,4,6-Penta-O-galloyl-β-D-glucopyranose, a natural product isolated and purified from the peel of Punica granatum L., suppresses interleukin (IL)-4 induced signal pathway in B cell, and inhibits IgE production partially caused by increasing a population of Treg cells in conjunction with Treg-inducing factors[3]. 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose is a large polyphenol that has been shown to be effective at inhibiting aggregation of full-length Aβ1-40 and Aβ1-42, but has the opposite effect on the C-terminal fragment Aβ25-35[4]. PGG (1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose) is a CMG2 inhibitor with antiangiogenic activity. PGG inhibits CMG2 with a submicromolar IC50 and it also inhibits the migration of human dermal microvascular endothelial cells at similar concentrations in vitro. Oral or intraperitoneal administration of PGG inhibits angiogenesis in the mouse corneal micropocket assay in vivo[5]. Cell cycle was blocked in S phase at lower dose (25 μM PGG), and G1 phase at higher dose (50 or 75 μM PGG). PGG affected cell cycle- or apoptosis-related proteins such as cyclin D1, Bcl-2 and Bax[6]. 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose (PGG) inhibits biofilm formation by S. aureus by preventing the initial attachment of the cells to a solid surface and reducing the production of polysaccharide intercellular adhesin (PIA)[7].
1,2,3,4,6-O-pentagalloylglucose 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Peripheral blood mononuclear cells (PBMCs)
20 µM
PGG significantly inhibited the levels of IFN-β, TNF-α, IL-6, and CXCL10
Mol Med. 2024 Sep 27;30(1):160.
THP-1 cells
5, 10, 20 µM
2 h
PGG reduced the expression of p-IRF3 and p-STING protein and inhibited the expression of IFN-β, TNF-α, IL-6, and CXCL10
Mol Med. 2024 Sep 27;30(1):160.
Bone marrow-derived macrophages (BMDMs)
5, 10, 20 µM
2 h
PGG gradient inhibited the phosphorylation of IRF3 and STING and reduced the mRNA expression of IFN-β, TNF-α, IL-6, ISG15, and CXCL10
Mol Med. 2024 Sep 27;30(1):160.
TRAMP-C2 cells
25 μM
24 h
PGG significantly inhibited the growth of TRAMP-C2 cells and induced caspase-independent programmed cell death and autophagic features
Mol Cancer Ther. 2009 Oct;8(10):2833-43.
PC-3 cells
50, 75 μM
4 days
PGG significantly decreased the number of adherent PC-3 cells and induced autophagic features and caspase-independent programmed cell death
Mol Cancer Ther. 2009 Oct;8(10):2833-43.
BHK-21 cells
10 μM
24 h
PGG significantly downregulated the level of phosphorylated STAT3 (p-STAT3) and upregulated SOCS3 whether PGG was used with or without CVS-11 infection, and, as expected, PGG induced significant inhibition of virus replication at the levels of all proteins and mRNAs and virus titers.
J Virol. 2019 Aug 28;93(18):e00539-19.
MC3T3-E1 cells
1×10−3 µM
24 h
PGG significantly enhanced cell viability and decreased cell apoptosis by restoring mitochondrial function, attenuating reactive oxygen species levels, decreasing the mitochondrial membrane potential, and enhancing ATP production.
Molecules. 2024 Oct 29;29(21):5110.
1,2,3,4,6-O-pentagalloylglucose 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Acetaminophen-induced acute liver injury model
Intraperitoneal injection
20 and 40 mg/kg
Single administration, lasting 24 hours
PGG reduced serum ALT, AST, and ALP levels, improved liver tissue damage and apoptosis, and inhibited acetaminophen-induced cGAS-STING pathway activation
Mol Med. 2024 Sep 27;30(1):160.
Sprague Dawley rats
LPS-induced acute lung injury model
Intraperitoneal injection
60 and 30 mg/kg
Administered 48, 24, and 1 hour before LPS, lasting for 3 days
PGG inhibited inflammation and oxidative stress by activating the AMPK/PI3K/Akt/Nrf2 pathway, significantly alleviating pulmonary edema and histological changes, reducing total leukocyte count and pro-inflammatory cytokines IL-6 and IL-1β production, and decreasing oxidative stress markers MDA formation and SOD depletion.
Int J Mol Sci. 2022 Nov 20;23(22):14423
Nude mice
Human DU145 and PC-3 prostate cancer xenograft models
20 mg/kg
Daily administration
PGG suppressed the growth of human DU145 and PC-3 prostate cancer xenografts in nude mice, suggesting potential utility as a PCa chemotherapeutic or chemopreventive agent
Mol Cancer Ther. 2009 Oct;8(10):2833-43.
Sprague Dawley (SD) male rats
LPS-induced acute lung injury model
Oral
17.16 mg/kg
Administered 48, 24, and 1 hour before LPS, lasting for 12 hours
PGG significantly inhibited lung edema, attenuated pulmonary histological changes, and reduced the number of total cells and neutrophils in BALF.
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