Brusatol

Brusatol is a quassinoid that has been found in B. javanica and has diverse biological activities, including antimalarial, lipolytic, antioxidative, anticancer, and anti-inflammatory properties.^1,2,3,4 It is active against chloroquine-resistant isolates of P. falciparum (EC₅₀ = 7.58 ng/ml) and induces lipolysis in 3T3-L1 adipocytes when used at a concentration of 160 nM.^1,2 Brusatol (40 nM) reduces nuclear erythroid 2-related factor 2 (Nrf2) ubiquitination and degradation and Nrf2 target gene expression in A549 lung cancer cells.³ It enhances cytotoxicity induced by cisplatin (Item No. 13119) in A549 cells when used at a concentration of 40 nM in vitro and in an A549 mouse xenograft model when administered at a dose of 2 mg/kg. Brusatol also inhibits LPS-induced production of TNF-α, pro-IL-1β, prostaglandin E₂ (Item No. 14010), and nitric oxide (NO) in RAW 264.7 macrophages. It reduces diarrhea and the severity of histopathological injury, as well as increases colonic levels of catalase (CAT), glutathione (GSH), and superoxide dismutase (SOD), in a mouse model of ulcerative colitis when administered at doses of 0.5 and 1 mg/kg.⁴

WARNING This product is not for human or veterinary use.

1. Lee, K.-H., Tani, S., and Imakura, Y. Antimalarial agents, 4. Synthesis of a brusatol analog and biological activity of brusatol-related compounds. J. Nat. Prod. 50(5), 847-851 (1987).

2. Lahrita, L., Moriai, K., Iwata, R., et al. Quassinoids in Brucea javanica are potent stimulators of lipolysis in adipocytes. Fitoterapia 137, 104250 (2019).

3. Ren, D., Villeneuve, N.F., Jiang, T., et al. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Proc. Natl. Acad. Sci. USA 108(4), 1433-1438 (2011).

4. Zhou, J., Wang, T., Dou, Y., et al. Brusatol ameliorates 2, 4, 6-trinitrobenzenesulfonic acid-induced experimental colitis in rats: Involvement of NF-κB pathway and NLRP3 inflammasome. Int. Immunopharmacol. 64, 264-274 (2018).