Pentagalloylglucose

Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is an orally active gallic tannin compound and an inducer of apoptosis and autophagy. Pentagalloglucose induces cell apoptosis and autophagy through the GSK3β/β-catenin pathway. Pentagalloylglucose inhibits UBE2T-mediated p53 ubiquitination, upregulates p53, downregulates RRM1/RRM2 in pancreatic cancer organoids. Pentagalloglucose has antioxidant, anti mutagenic, anti-inflammatory, anticonvulsant, cardioprotective, anti allergic, cholesterol lowering, and anti-tumor activities^{[1][2][3][4][5][6]}. In Vitro:Pentagalloylglucose (1 μM, 5 days) inhibits the proliferation and survival of breast cancer cells and medulloblastoma cells, with IC₅₀ values of 3.24 μM and 1.47 μM, respectively^[1].
Pentagalloylglucose (10-20 μM, 24 h) reduces AGE induced inflammation by activating Nrf2/HO-1 in mesangial cells and inhibiting the JAK2/STAT3 pathway^[2].
Pentagalloylglucose (40 μM, 24 h) inhibits the growth and migration of human nasopharyngeal carcinoma cells through the GSK3β/β - catenin pathway, blocks the cell cycle, and induces apoptosis and autophagy^[3].
Pentagalloylglucose (100 nM) inhibits UBE2T-mediated p53 ubiquitination, upregulates p53, downregulates RRM1/RRM2 in pancreatic cancer organoids^[6].
In Vivo:Pentagalloylglucose (10 mg/kg, three times a week, i.v.) enhances tumor sensitivity to PARP inhibitors and radiotherapy by disrupting the PALB2-BRCA2 interaction in MDA-MB-231 xenograft nude mice^[1].
Pentagalloylglucose (10, 20 mg/kg, once every two days, i.p.) reduces tumor lung metastasis and exhibits anti-tumor activity in a CNE2 cell xenograft nude mouse model^[3].
Pentagalloylglucose (5, 10 mg/kg, 7 days, i.p.) has an improving effect on the Ischemia and reperfusion-induced brain injury in rats^[4].
Pentagalloylglucose (10 mg/kg, 28 days, p.o.) increases T regulatory cell populations and inhibits IgE production in ovalbumin sensitized mice through immunosuppressive activity^[5].
Pentagalloylglucose (20 mg/kg, p.o., daily, 6 weeks) shows potent anti-tumor efficacy in KPC mice (LSL-Kras^G12D/+, LSL-Trp53R^172H/+, Pdx1-Cre) when combined with Gemcitabine (HY-17026)^[6].