Brazilein

Brazilein is a phytochemical that has been found in C. sappan and has diverse biological activities.^1,2,3,4 It is active against E. coli, P. aeruginosa, and methicillin-susceptible S. aureus (MSSA; MICs = 32, 512, and 512 µg/ml), as well as a panel of 10 clinical isolates of methicillin-resistant S. aureus (MRSA; MIC₅₀s = 16-32 µg/ml).¹ Brazilein (10 µM) inhibits LPS-induced nitric oxide (NO) production in J774A.1 cells.² It is cytotoxic to HepG2, Hep3B, MDA-MB-231, MCF-7, A549, and Ca9-22 cancer cells (IC₅₀s = 3.15, 3.42, 2.36, 3.96, 9.68, and 8.63 µg/ml, respectively).³ Brazilein (1-10 µg/ml) also inhibits the proliferation of isolated mouse spleen lymphocytes induced by concanavalin A .⁴

1.Zuo, G.Y., Han, Z.Q., Hao, X.Y., et al.Synergy of aminoglycoside antibiotics by 3-benzylchroman derivatives from the chinese drug Caesalpinia sappan against clinical methicillin-resistant Staphylococcus aureus (MRSA)Phytomedicine21(7)936-941(2014) 2.Sasaki, Y., Hosokawa, T., Nagai, M., et al.In vitro study for inhibition of NO production about constituents of Sappan LignumBiol. Pharm. Bull.30(1)193-196(2007) 3.Yen, C.-T., Nakagawa-Goto, K., Hwang, T.-L., et al.Antitumor agents. 271: Total synthesis and evaluation of brazilein and analogs as anti-inflammatory and cytotoxic agentsBioorg. Med. Chem. Lett.20(3)1037-1039(2010) 4.Ye, M., Xie, W.-D., Lei, F., et al.Brazilein, an important immunosuppressive component from Caesalpinia sappan LInt. Immunopharmacol.6(3)426-432(2006)