Background:
Dehydrocostus Lactone is a major sesquiterpene lactone isolated from the roots of Saussurea lappa.IC50 value:Target:In vitro: Dehydrocostus Lactone promoted apoptosis with increased activation of caspases 8, 9, 7, 3, enhanced PARP cleavage, decreased Bcl-xL expression and increased levels of Bax, Bak, Bok, Bik, Bmf, and t-Bid. We have demonstrated that Dehydrocostus Lactone inhibits cell growth and induce apoptosis in DU145 cells [1]. Dehydrocostus Lactone inhibits NF-kappaB activation by preventing TNF-alpha-induced degradation and phosphorylation of its inhibitory protein I-kappaB alpha in human leukemia HL-60 cells and that dehydrocostus lactone renders HL-60 cells susceptible to TNF-alpha-induced apoptosis by enhancing caspase-8 and caspase-3 activities [2]. Dehydrocostus Lactone inhibited the production of NO in lipopolysaccharide (LPS)-activated RAW 264.7 cells by suppressing inducible nitric oxide synthase enzyme expression.In vivo: Dehydrocostus Lactone decreased the TNF-alpha level in LPS-activated systems in vivo [3].
参考文献:
[1]. Eun Ji Kim, et al. Apoptosis of DU145 human prostate cancer cells induced by dehydrocostus lactone isolated from the root of Saussurea lappa. Food and Chemical ToxicologyVolume 46, Issue 12, December 2008, Pages 3651–3658
[2]. Oh GS, et al. Dehydrocostus lactone enhances tumor necrosis factor-alpha-induced apoptosis of human leukemia HL-60 cells. Immunopharmacol Immunotoxicol. 2004 May;26(2):163-75.
[3]. Lee HJ, et al. A sesquiterpene, dehydrocostus lactone, inhibits the expression of inducible nitric oxide synthase and TNF-alpha in LPS-activated macrophages. Planta Med. 1999 Mar;65(2):104-8.
[4]. Taniguchi M, et al. COSTUNOLIDE AND DEHYDROCOSTUS LACTONE AS INHIBITORS OF KILLING FUNCTION OF CYTOTOXIC T LYMPHOCYTES. Bioscience, Biotechnology, and Biochemistry, 1995, 59 (11): 2064-2067
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