Dimethylamino-micheliolide (DMAMCL) is a prodrug form of the sesquiterpene lactone micheliolide .[1] It inhibits migration and invasion of, and vascular formation by, U-118 MG glioma cells when used at a concentration of 10 µM. DMAMCL enhances cell death induced by the DNA-cross-linking agent cisplatin in U-118 MG cells. In vivo, DMAMCL (200 mg/kg) reduces tumor volume and slows the tumor growth rate in a U-118 MG mouse xenograft model when administered in combination with cisplatin. It also prevents proteinuria and renal failure in a db/db mouse model of diabetic nephropathy.[2]
References:
[1].Xi, X., Liu, N., Wang, Q., et al.ACT001, a novel PAI-1 inhibitor, exerts synergistic effects in combination with cisplatin by inhibiting PI3K/AKT pathway in gliomaCell Death Dis.10(10)757(2019).
[2].Liu, W., Chen, X., Wang, Y., et al.Micheliolide ameliorates diabetic kidney disease by inhibiting Mtdh-mediated renal inflammation in type 2 diabetic db/db micePharmacol. Res.150104506(2019).