Halofuginone (RU-19110, RU19110),又称常山酮或卤夫酮,Febrifugine的衍生物,是一种竞争性的脯氨酰-tRNA合成酶(prolyl-tRNA synthetase)抑制剂,Ki为18.3 nM,表现出抗炎、抗癌、抗寄生虫、抗纤维化等活性。Halofuginone也是一种新型的广谱抗球虫药,具有高效、低毒、不易产生耐药性等特点。
参考文献
1.Tsuchida K, et al. Halofuginone enhances the chemo-sensitivity of cancer cells by suppressing NRF2 accumulation. Free Radic Biol Med. 2017 Feb;103:236-247.
2.Nelson EF, et al. Halofuginone down-regulates Smad3 expression and inhibits the TGFbeta-induced expression of fibrotic markers in human corneal fibroblasts. Mol Vis. 2012;18:479-87.
3.Cui Z, et al. Halofuginone attenuates osteoarthritis by inhibition of TGF-β activity and H-type vessel formation in subchondral bone. Ann Rheum Dis. 2016 Sep;75(9):1714-21.
4.Tracy L McGaha, et al. Halofuginone, an inhibitor of type-I collagen synthesis and skin sclerosis, blocks transforming-growth-factor-beta-mediated Smad3 activation in fibroblasts. J Invest Dermatol. 2002 Mar;118(3):461-70.
冰袋运输。粉末直接保存于-20℃,有效期3年。建议分装后-20℃干燥保存,避免反复冻融。