Isosinensetin

Isosinensetin is a polymethoxylated flavone that has been found in C. reticulata and has anticancer and anti-inflammatory activities.^1,2,3 It inhibits P-glycoprotein (P-gp; IC₅₀ = 4.2 µM) and increases the cytotoxicity of paraquat in MDR1-MDCKII cells and paclitaxel (Item No. 10461) in MX-1 breast and paclitaxel-resistant MX-1/T cancer cells.¹ Isosinensetin inhibits the proliferation of A549 lung, HL-60 leukemia, MCF-7 breast, and HO-8910 ovarian cancer cells (IC₅₀s = 23.6, 23.8, 15.1, and 12.5 µM, respectively).² It prevents decreases in cell viability and inhibits increases in IL-1β, TNF-α, and IL-6 levels and the production of reactive oxygen species (ROS) induced by fine particulate matter less than or equal to 2.5 µm (PM_2.5) in 16HBE bronchial epithelial cells when used at a concentration of 80 µg/ml.³

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1. Bai, J., Zhao, S., Fan, X., et al. Inhibitory effects of flavonoids on P-glycoprotein in vitro and in vivo: Food/herb-drug interactions and structure-activity relationships. Toxicol. Appl. Pharmacol. 369, 49-59 (2019).

2. Du, Q., and Chen, H. The methoxyflavones in Citrus reticulata Blanco cv. ponkan and their antiproliferative activity against cancer cells. Food Chem. 119(2), 567-572 (2010).

3. Zou, Y., Li, S., Li, X., et al. Isosinensetin alleviates the injury of human bronchial epithelial cells induced by PM2.5. Exp. Ther. Med. 22(6), 1435 (2021).