Genkwanin

Genkwanin is a flavonoid that has been found in T. kirilowii and has diverse biological activities.^1,2 It inhibits proliferation of MDA-MB-231 and MCF-7 breast cancer, Eca-109 esophageal carcinoma, and A549 lung adenocarcinoma cells (IC₅₀s = 58.54, 101.4, 98.2, and 120.77 µM, respectively).¹ It decreases the levels of PI3Kγ, as well as the levels of phosphorylated Akt, mTOR, p70 ribosomal S6 kinase (p70S6K) and ULK, and induces apoptosis and cell cycle arrest at the G₂/M phase in MDA-MB-231 cells. Genkwanin (20-40 µM) reverses increases in apoptosis, lactate dehydrogenase (LDH) release, and reactive oxygen species (ROS) production induced by 1-methyl-4-phenylpyridinium (MPP⁺) in an in vitro model of Parkinson’s disease inflammation using SH-SY5Y cells.² It also reduces protein levels of toll-like receptor 4 (TLR4), MyD88, NOD-like receptor protein 3 (NLRP3), and caspase-1 in SH-SY5Y cells.

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1. Zhang, H.-W., Hu, J.-J., Fu, R.-Q., et al. Flavonoids inhibit cell proliferation and induce apoptosis and autophagy through downregulation of PI3Kγ mediated PI3K/AKT/mTOR/p70S6K/ULK signaling pathway in human breast cancer cells. Sci. Rep. 8(1), 11255 (2018).

2. Li, Q., Zhang, P., and Cai, Y. Genkwanin suppresses MPP+-induced cytotoxicity by inhibiting TLR4/MyD88/NLRP3 inflammasome pathway in a cellular model of Parkinson’s disease. Neurotoxicology 87, 62-69 (2021).