Sparstolonin B is an isocoumarin that has been found in Spaganium stoloniferum and has diverse biological activities.1,2,3,4 It inhibits increases in TNF-α, IL-6, and IL-1β levels induced by the toll-like receptor 4 (TLR4) agonist LPS, TLR2 agonist Pam3CSK4 , or TLR2/6 agonist FSL-1 but not the TLR3 agonist poly(I:C) or TLR9 agonist ODN1668 in primary mouse macrophages when used at a concentration of 100 ?M.1 Sparstolonin B (1-10 ?M) reduces HIV-1 p24 antigen levels in the culture supernatant of human peripheral blood mononuclear cells (PBMCs) infected with HIV-1, indicating inhibition of HIV replication.2 It induces apoptosis, cell cycle arrest at the G2/M phase, and production of reactive oxygen species (ROS) in SH-SY5Y neuroblastoma cells when used at a concentration of 10 ?M.3 Sparstolonin B (3 and 9 mg/kg) protects mice from lethal endotoxin shock.4
1.Liang, Q., Wu, Q., Jiang, J., et al.Characterization of sparstolonin B, a chinese herb-derived compound, as a selective toll-like receptor antagonist with potent anti-inflammatory propertiesJ. Biol. Chem.286(30)26470-26479(2011) 2.Deng, X., Zhang, Y., Jiang, F., et al.The chinese herb-derived sparstolonin B suppresses HIV-1 transcriptionVirol. J.12108(2015) 3.Kumar, A., Fan, D., Dipette, D.J., et al.Sparstolonin B, a novel plant derived compound, arrests cell cycle and induces apoptosis in N-myc amplified and N-myc nonamplified neuroblastoma cellsPLoS One9(5)e96343(2014) 4.Liang, Q., Dong, S., Lei, L., et al.Protective effects of Sparstolonin B, a selective TLR2 and TLR4 antagonist, on mouse endotoxin shockCytokine75(2)302-309(2015)