通过抑制IKKβ的活化来防止NF-κB活化,Withaferin A 是从南非醉茄中分离到的甾体内酯,可以抑制 NF-kB 的活性,靶作用于波形蛋白 (vimentin),具有抗炎,抗肿瘤等功效。
生物活性
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
性状
Solid
IC50 & Target[1][2]
NFκB
体外研究(In Vitro)
Withaferin A has antiinflammatory activity, and potently inhibits NF-kB activation by preventing the TNF-induced activation of Ik-B kinase beta via a thioalkylation-sensitive redox mechanism. Withaferin A also has anticancer activity. Withaferin A targets the IF protein vimentin, causes aggregation of vimentin filaments in bovine aortic endothelial cells (BAECs) at 3 μM, and induces vimentin fragmentation in endothelial cells at 10 μM. Withaferin A (0.5, 1.5 μM) alone or incombination with cisplatin (CIS) dose-dependently reduces tumorigenic potential of ALDH1 positive cancer stem cells (CSCs).
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Withaferin A (2 mg/kg, i.p.) shows potent angiogenesis inhibitory activity via vimentin in mice. Withaferin A (2 mg/kg) combined with cisplatin (CIS) regulates the expression of ALDH1 marker, and downregulates the expression of securin in tumors collected from mice.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.