Sciadopitysin (Synonyms: NSC 45108)

Sciadopitysin is a biflavonoid originally isolated from G. biloba and has diverse biological activities.1,2,3,4 It reduces cytotoxicity induced by amyloid-β (1-42) in PC12 cells (EC50 = 9.84 μM).2 Sciadopitysin (0.1-10 μM) decreases methylglyoxal-induced insulin secretion, production of reactive oxygen species (ROS), cardiolipin peroxidation, and cytotoxicity in RIN-m5F pancreatic β-cells.3 It inhibits P-glycoprotein (P-gp; IC50 = 53.42 μM) and increases cellular toxicity of paraquat and paclitaxel in MDR1-MDCKII cells.5 Sciadopitysin inhibits RANKL-induced mRNA expression of the osteoclast-specific genes CTSK, TRAP, and MMP-9, activation of NF-κB, and osteoclastogenesis in a mouse model of LPS-induced bone loss.4

References
1. Brian•on-Scheid, F., Lobstein-Guth, A., and Anton, R. HPLC separation and quantitative determination of biflavones in leaves from ginkgo biloba. Planta Med. 49(12), 204-207 (1983).
2. Sasaki, H., Kitoh, Y., Tsukada, M., et al. Inhibitory activities of biflavonoids against amyloid-β peptide 42 cytotoxicity in PC-12 cells. Bioorg. Med. Chem. 25(14), 2831-2833 (2015).
3. Suh, K.S., Chon, S., and Choi, E.M. The protective effects of sciadopitysin against methylglyoxal-induced cytotoxicity in cultured pancreatic β-cells. J. Appl. Toxicol. 38(8), 1104-1111 (2018).
4. Cao, J., Lu, Q., Liu, N., et al. Sciadopitysin suppresses RANKL-mediated osteoclastogenesis and prevents bone loss in LPS-treated mice. Int. Immunopharmacol. 49, 109-117 (2017).
5. 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).