Daphnetin

Daphnetin is a coumarin derivative that has been isolated from plants of the genus Daphne and has diverse biological activities, including kinase inhibitory, anti-proliferative, and antioxidative properties.^1,2,3 It inhibits the EGF receptor (EGFR), PKA, and PKC (IC₅₀s = 7.67, 9.33, and 25.01 µM, respectively, in kinase assays) and inhibits cell proliferation (IC₅₀ = 73 µM) and reduces cyclin D1 levels in MCF-7 breast carcinoma cells.^1,2 Daphnetin (5 and 10 µg/ml) decreases the generation of reactive oxygen species (ROS) and production of malondialdehyde (MDA) and increases superoxide dismutase (SOD) activity and the glutathione (GSH) to oxidized GSH (GSSG) ratio in RAW 264.7 cells.³ It also prevents cytotoxicity and ROS overproduction induced by t-butyl hydroperoxide (t-BHP) in wild-type, but not Nrf2^-/-, RAW 264.7 cells and increases the expression of proteins downstream of Nrf2, including HO-1, GCLM, GCLC, and NQO1.

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1. Yang, E.B., Zhao, Y.N., Zhang, K., et al. Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor. Biochem. Biophys. Res. Commun. 260(3), 682-685 (1999).

2. Jiménez-Orozco, F.A., Rosales, A.A., Vega-López, A., et al. Differential effects of esculetin and daphnetin on in vitro cell proliferation and in vivo estrogenicity. Eur. J. Pharmacol. 668(1-2), 35-41 (2011).

3. Lv, H., Liu, Q., Zhou, J., et al. Daphnetin-mediated Nrf2 antioxidant signaling pathways ameliorate tert-butyl hydroperoxide (t-BHP)-induced mitochondrial dysfunction and cell death. Free Radic. Biol. Med. 106, 38-52 (2017).