Brusatol

一种具有多种生物活性的类苦素；对抗氯喹的恶性疟原虫分离株有效（EC50=7.58ng/ml）；在160nM时诱导3T3-L1脂肪细胞中的脂肪分解；在40nM时降低A549细胞中的Nrf2泛素化和降解以及Nrf2靶基因表达；在40nM时增强顺铂在A549细胞中诱导的细胞毒性，在2mg/kg时增强在A549小鼠异种移植模型中诱导的细胞毒性；在0.5和1mg/kg时减轻溃疡性结肠炎小鼠模型中的腹泻和组织病理学损伤的严重程度，并增加结肠中CAT、GSH和SOD的水平。A quassinoid with diverse biological activities; active against chloroquine-resistant isolates of P. falciparum (EC50 = 7.58 ng/ml); induces lipolysis in 3T3-L1 adipocytes at 160 nM; reduces Nrf2 ubiquitination and degradation and Nrf2 target gene expression in A549 cells at 40 nM; enhances cytotoxicity induced by cisplatin in A549 cells at 40 nM and in an A549 mouse xenograft model at 2 mg/kg; reduces diarrhea and the severity of histopathological injury, as well as increases colonic levels of CAT, GSH, and SOD in a mouse model of ulcerative colitis at 0.5 and 1 mg/kg.分子式C26H32O11分子量520.5O=C(OC)[C@]12[C@@]3([H])[C@]([C@]4([H])[C@@H](O)[C@@H]1O)(CO2)[C@@](OC([C@@H]3OC(/C=C(C)/C)=O)=O)([H])C[C@@]([C@]4(C)C5)([H])C(C)=C(O)C5=O