Chebulinic acid is an ellagitannin that has been found in T. chebula and has diverse biological activities.1,2,3,4,5 It is an inhibitor of protein tyrosine phosphatase non-receptor 9 (PTPN9) and PTPN11 (IC50s = 34 and 37 nM, respectively).2 Chebulinic acid (5 ?M) increases glucose uptake in 3T3-L1 preadipocytes. It induces apoptosis of HL-60 and NB4 acute promyelocytic leukemia (APL), but not K562 chronic myelogenous leukemia (CML), cells (IC50s = 7.5, 5, and >60 ?M, respectively).1 Chebulinic acid (25 ?M) reduces the production of reactive oxygen species (ROS) induced by glyceraldehyde-related advanced glycation end products (glycer-AGEs) in human umbilical vein endothelial cells (HUVECs) and reduces glutamate-induced ROS production and cell death in HT22 mouse hippocampal cells.3,4 It inhibits H+/K+-ATPase activity (IC50 = 65.01 ?g/ml) and reduces free and total gastric acidity, as well as increases gastric mucin secretion, in various rat models of gastric ulcer.5
1.Chhabra, S., Mishra, T., Kumar, Y., et al.Chebulinic acid isolated from the fruits of Terminalia chebula specifically induces apoptosis in acute myeloid leukemia cellsPhytother. Res.31(12)1849-1857(2017) 2.Yoon, S.-Y., Kang, H.J., Ahn, D., et al.Identification of chebulinic acid as a dual targeting inhibitor of protein tyrosine phosphatases relevant to insulin resistanceBioorg. Chem.90103087(2019) 3.Lee, H.-S., Koo, Y.-C., Suh, H.J., et al.Preventive effects of chebulic acid isolated from Terminalia chebula on advanced glycation endproduct-induced endothelial cell dysfunctionJ. Ethnopharmacol.131(3)567-574(2010) 4.Song, J.H., Shin, M.-S., Hwang, G.S., et al.Chebulinic acid attenuates glutamate-induced HT22 cell death by inhibiting oxidative stress, calcium influx and MAPKs phosphorylationBioorg. Med. Chem. Lett.28(3)249-253(2018) 5.Mishra, V., Agrawal, M., Onasanwo, S.A., et al.Anti-secretory and cyto-protective effects of chebulinic acid isolated from the fruits of Terminalia chebula on gastric ulcersPhytomedicine20(6)506-511(2013)