Gossypin

Gossypin is a flavonoid glycoside originally isolated from H. vitifolius that has diverse biological activities.^1,2,3,4,5 It inhibits RANKL-induced osteoclastogenesis in RAW 264.7 cells when used at a concentration of 5 ?M.¹ Gossypin inhibits Aurora B kinase (IC₅₀ = 11.07 ?M in a cell-free assay using the human enzyme), as well as Aurora A kinase and p90 ribosomal S6 kinase 2 (RSK2) at 20 ?M.^2,3 It induces cell cycle arrest at the G₂/M phase and apoptosis in HGC-27 gastric cancer cells.³ Gossypin decreases lactate dehydrogenase (LDH) release induced by the glutathione-depleting agent D,L-buthionine (S,R)-sulfoximine in primary rat cortical cells (IC₅₀ = 7.4 ?g/ml).⁴ It reduces acetic acid-induced writhing in mice, an effect that can be reversed by the opioid antagonist naloxone, in a dose-dependent manner.⁵

1.Kunnumakkara, A.B., Nair, A.S., Ahn, K.S., et al.Gossypin, a pentahydroxy glucosyl flavone, inhibits the transforming growth factor beta-activated kinase-1-mediated NF-κB activation pathway, leading to potentiation of apoptosis, suppression of invasion, and abrogation of osteoclastogenesisBlood109(12)5112-5121(2007) 2.Jung, Y., Shin, S.Y., Yong, Y., et al.Plant-derived flavones as inhibitors of aurora B kinase and their quantitative structure-activity relationshipsChem. Biol. Drug Des.85(5)574-585(2015) 3.Wang, L., Wang, X., Chen, H., et al.Gossypin inhibits gastric cancer growth by direct targeting of AURKA and RSK2Phytother. Res.33(3)640-650(2019) 4.Yoon, I., Lee, K.H., and Cho, J.Gossypin protects primary cultured rat cortical cells from oxidative stress- and beta-amyloid-induced toxicityArch. Pharm. Res.27(4)454-459(2004) 5.Viswanathan, S., Sambantham, P.T., Reddy, K., et al.Gossypin-induced analgesia in miceEur. J. Pharmacol.98(2)289-291(1984)