Asperglaucide

Asperglaucide is an amide originally isolated from P. aurantiacum that has diverse biological activities, including anti-inflammatory, antibacterial, antioxidant, and anticancer properties.^1,2,3,4 Asperglaucide inhibits production of nitric oxide (NO), prostaglandin E₂ , and IL-1β in LPS-stimulated BV-2 microglial cells (IC₅₀s = 49.7, 51.5, and 40.4 µM, respectively).² It is active against Gram-negative bacteria (MICs = 0.05-0.10 mg/ml) and has antioxidant activity in 2,2-diphenyl-1-picrylhydrazyl and Trolox equivalent antioxidant capacity (TEAC) assays (EC₅₀s = 9.51-78.81 µg/ml).³ Asperglaucide decreases viability of U87 and U251 cancer cells in vitro when used at concentrations ranging from 10 to 100 µM and reduces tumor growth when administered at a dose of 1 mg via intratumoral injection in a U87 mouse xenograft model.⁴

1.Banerji, A., and Ray, R.Aurantiamides: A new class of modified dipeptides from Piper aurantiacumPhytochemistry20(9)2217-2220(1981) 2.Yoon, C.S., Kim, D.C., Lee, D.S., et al.Anti-neuroinflammatory effect of aurantiamide acetate from the marine fungus Aspergillus sp. SF-5921: Inhibition of NF-κB and MAPK pathways in lipopolysaccharide-induced mouse BV2 microglial cellsInt. Immunopharmacol.23(2)568-574(2014) 3.Tamokou, J.D., Simo Mpetga, D.J., Keilah Lunga, P., et al.Antioxidant and antimicrobial activities of ethyl acetate extract, fractions and compounds from stem bark of Albizia adianthifolia (Mimosoideae)BMC Complement. Altern. Med.1299(2012) 4.Yang, Y., Zhang, L.H., Yang, B.X., et al.Aurantiamide acetate suppresses the growth of malignant gliomas in vitro and in vivo by inhibiting autophagic fluxJ. Cell. Mol. Med.19(5)1055-1064(2015)