Hispidulin is a flavonoid compound that acts as a Pim-1 inhibitor (IC₅₀=2.71μM). Hispidulin can induce apoptosis through mitochondrial dysfunction and inhibit the production of inflammatory cytokines. Hispidulin is applicable for research in various cancers (including renal cancer, liver cancer, glioblastoma, acute myeloid leukemia, etc.) and inflammation-related diseases[1-4].
In vitro, MG63 and 143B human osteosarcoma cells were treated with Hispidulin (7.5–30μM) for 24–72 hours. Hispidulin significantly inhibited cell proliferation, colony formation, migration, and invasion, and induced G2/M phase arrest and apoptosis[5]. MCF-7 and HCC38 human breast cancer cells were co-treated with Hispidulin (1.25–2.5μM) and TGF-β1 (10ng/ml) for 24 hours. Hispidulin significantly increased the expression of E-cadherin and occludin, decreased vimentin expression, and inhibited TGF-β1-induced Smad2/3 phosphorylation and cell migration[6].
In vivo, C57BL/6J mice undergoing aortic banding surgery were intraperitoneally injected with Hispidulin (20mg/kg/day) starting from one day before surgery until four weeks after surgery. Hispidulin significantly alleviated pressure overload-induced cardiac hypertrophy and improved cardiac function[7]. C57BL/6 mice were intraperitoneally injected with Hispidulin (50mg/kg; single injection) one hour after endotoxin (10mg/kg) injection. Hispidulin significantly ameliorated endotoxin-induced acute kidney injury[8].
References:
[1] Chao SW, Su MY, Chiou LC, et al. Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene Kinase Pim-1. J Nat Prod. 2015 Aug 28;78(8):1969-76.
[2] Gao H, Wang H, Peng J. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Cell Biochem Biophys. 2014 May;69(1):27-34.
[3] Zhou R, Wang Z, Ma C. Hispidulin exerts anti-osteoporotic activity in ovariectomized mice via activating AMPK signaling pathway. Cell Biochem Biophys. 2014 Jun;69(2):311-7.
[4] Lin TY, Lu CW, Wang SJ, et al. Protective effect of hispidulin on kainic acid-induced seizures and neurotoxicity in rats. Eur J Pharmacol. 2015 May 15;755:6-15.
[5] Yuan X, Yu S, Zeng Z, et al. Hispidulin suppresses osteosarcoma by directly targeting FABP4 to disrupt lipid metabolism and inhibit the PI3K/AKT pathway. J Transl Med. 2025 Oct 7;23(1):1062.
[6] Kim HA, Lee J. Hispidulin modulates epithelial-mesenchymal transition in breast cancer cells. Oncol Lett. 2021 Feb;21(2):155.
[7] Wang Y, Xie Z, Jiang N, et al. Hispidulin Attenuates Cardiac Hypertrophy by Improving Mitochondrial Dysfunction. Front Cardiovasc Med. 2020 Nov 26;7:582890.
[8] Kim K, Leem J. Hispidulin Ameliorates Endotoxin-Induced Acute Kidney Injury in Mice. Molecules. 2022 Mar 21;27(6):2019.