Geraniin, a TNF-α releasing inhibitor with an IC50 value of 43μM, exhibits numerous activities including anticancer, anti-inflammatory, and anti-hyperglycemic activities[1]. Geraniin can induce the nuclear translocation of nuclear factor Nrf2 and enhance glutathione (GSH) levels, thus reducing intracellular ROS levels in cells [2]. Geraniin has been widely used in cell and animal models to inhibit tumor growth and interfere with mitochondrial function[3].
In vitro, Geraniin treatment for 48 hours significantly inhibited the viability of OVCAR3 and SKOV3 cells with IC50 values of 34.5μM and 23.6μM, respectively[4]. Geraniin treatment at 36µM for 24h abrogated HT-29 cell growth and induced nuclear morphological changes and DNA fragmentation[5]. Treatment of T24 cells with 20µM Geraniin for 24 hours induced cell cycle arrest, decreased the proportion of T24 cells in S phase, promoted cell apoptosis, and regulated the PI3K/AKT signaling pathway[6].
In vivo, Geraniin (20mg/kg/day) administered daily by gavage for 14 days alleviated lipopolysaccharide (LPS)-induced cognitive impairment, ameliorated LPS-induced nerve/synaptic damage, and reduced Aβ production in mice[7]. Daily gavage administration of Geraniin (8mg/kg/day) for 10 consecutive weeks could reduce the body weight of ApoE−/− mice on a high-fat diet, and lower the levels of serum triglycerides (TG) and low-density lipoprotein cholesterol (LDL-C)[8].
References:
[1] Okabe S, Suganuma M, Imayoshi Y, et al. New TNF-α releasing inhibitors, geraniin and corilagin, in leaves of Acer nikoense, Megusurino-ki[J]. Biological and Pharmaceutical Bulletin, 2001, 24(10): 1145-1148.
[2] Cheng H S, Ton S H, Abdul Kadir K. Ellagitannin geraniin: a review of the natural sources, biosynthesis, pharmacokinetics and biological effects[J]. Phytochemistry reviews, 2017, 16(1): 159-193.
[3] Li J, Wang S, Yin J, et al. Geraniin induces apoptotic cell death in human lung adenocarcinoma A549 cells in vitro and in vivo[J]. Canadian Journal of Physiology and Pharmacology, 2013, 91(12): 1016-1024.
[4] Wang X, Chen Z, Li X, et al. Geraniin suppresses ovarian cancer growth through inhibition of NF‐κB activation and downregulation of Mcl‐1 expression[J]. Journal of Biochemical and Molecular Toxicology, 2017, 31(9): e21929.
[5] Chan C K, Tang L Y, Goh B H, et al. Targeting apoptosis via inactivation of PI3K/Akt/mTOR signaling pathway involving NF-κB by geraniin in HT-29 human colorectal adenocarcinoma cells[J]. Progress in Drug Discovery & Biomedical Science, 2019, 2(1).
[6] Xu J, Qin N, Yao Y, et al. Geraniin inhibits bladder cancer cell growth via regulation of PI3K/AKT signaling pathways[J]. Tropical Journal of Pharmaceutical Research, 2020, 19(2): 253-257.
[7] Wang D, Dong X, Wang B, et al. Geraniin attenuates lipopolysaccharide-induced cognitive impairment in mice by inhibiting toll-like receptor 4 activation[J]. Journal of Agricultural and Food Chemistry, 2019, 67(36): 10079-10088.
[8] Xie Y, Liu S, Wei Z, et al. Geraniin Alleviates High‐Fat Diet‐Induced Atherosclerosis in ApoE−/− Mice[J]. Food Science & Nutrition, 2025, 13(7): e70693.