Podocarpusflavone A

Podocarpusflavone A is a biflavone that has been found in D. araucarioides and has diverse biological activities.^1,2,3,4 It inhibits dengue virus NS5 RNA-dependent RNA polymerase (DENV-NS5 RdRp; IC₅₀ = 0.75 μM).³ Podocarpusflavone A also inhibits cathepsin B with an IC₅₀ value of 1.68 μM and inhibits STAT3 in a reporter assay in a concentration-dependent manner.^1,2 It reduces the production of reactive oxygen species (ROS) and superoxide anions induced by phorbol 12-myristate 13-acetate in isolated human neutrophils when used at concentrations of 1 and 10 μM, respectively.⁴ Podocarpusflavone A also inhibits aggregation of amyloid-β (1-40) peptide in a cell-free assay with an IC₅₀ value of 4.9 μM.⁵ Podocarpusflavone A (20 μM) decreases viability of A375, MALME-3M, SK-MEL-1, and SK-MEL-5 melanoma cells and reduces tumor growth in an A375 mouse xenograft model when administered at doses of 20 and 40 mg/kg.²

1.Zhang, Y., Tan, N.S., Huang, H., et al.Three bioactive biflavones isolated from Taxodium mucronatumYunnan Zhiwu Yanjiu27(1)107-110(2005) 2.Meng, H., Pang, Y., Liu, G., et al.Podocarpusflavone A inhibits cell growth of skin cutaneous melanoma by suppressing STAT3 signalingJ. Dermatol. Sci.100(3)201-208(2020) 3.Coulerie, P., Nour, M., Maciuk, A., et al.Structure-activity relationship study of biflavonoids on the Dengue virus polymerase DENV-NS5 RdRpPlanta Med.79(14)1313-1318(2013) 4.Arwa, P.S., Zeraik, M.L., Ximenes, V.F., et al.Redox-active biflavonoids from Garcinia brasiliensis as inhibitors of neutrophil oxidative burst and human erythrocyte membrane damageJ. Ethnopharmacol.174410-418(2015) 5.Sirimangkalakitti, N., Juliawaty, L.D., Hakim, E.H., et al.Naturally occurring biflavonoids with amyloid β aggregation inhibitory activity for development of anti-Alzheimer agentBioorg. Med. Chem. Lett.29(15)1994-1997(2019)