"目录号: HY-14645 ee.: 100.00%

NF-κB-

(-)-DHMEQ是DHMEQ的优性异构体，是NF-kB 的抑制剂，能够抑制核里的kB,IC50值是20 ug/mL, 它的活性比(+)-DHMEQ (HY-14645A)强。

NF-κB

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生物活性

Description

(-)-DHMEQ, the eutomer of DHMEQ , is a newly developed NF-kB inhibitor, inhibits nuclear factor kB activation with IC50 value of 20 ug/mL, the activity is stronger than (+)-DHMEQ (HY-14645A).target: NF-kB [1]IC 50: 20 ug/mL [2]In vitro: (-)-DHMEQ significantly reduces eosinophilicairway inflammation and levels of Th2 cytokines in bronchoalveolar lavage fluid in theacute model. It also inhibits parameters of airway remodelling including mucus produc-tion, peribronchial fibrosis and the expression of a-smooth muscle actin.[1] (-)-DHMEQ strongly inhibits cyclin D1 and vascular en-dothelial growth factor (VEGF) promoter activity and decreased the levels of cyclin D1 protein and VEGF mRNA in KB cells。 (-)-DHMEQ strongly inhibits cyclin D1 and vascular en-dothelial growth factor (VEGF) promoter activity and decreasedthe levels of cyclin D1 protein and VEGF mRNA in KB cells.[2] (-)-DHMEQ suppresses the tumour growth and anti-inflammatory effects.[3] (-)-DHMEQ inhibits TPA-induced activation of NF-kB and differentiation of THP-1 cells into macrophages.[5]In vivo: When  (-)-DHMEQ is injects into mice 2 h before LPS injection, the survival of the LPS-injected mice was prolonged. When (-)-DHMEQ is injected twice (2 h before LPS injection and the day after LPS injection), all the mice are rescued. (-)-DHMEQ can be utilized for the prevention and treatment of endotoxin shock.[3]

References

[1].Matsumoto N et al. Synthesis of NF-kappaB activation inhibitors derived from epoxyquinomicin C. Bioorg Med Chem Lett. 2000 May 1;10(9):865-9.

[2].Yoshikazu Suzuki et al. Preparation and biological activities of optically active dehydroxymethylepoxyquinomicin, a novel NF-κB inhibitor. Tetrahedron. Tetrahedron 60 (2004) 7061-7066

[3].Shimizu K et al. Dehydroxymethylepoxyquinomicin (DHMEQ), a novel NF-kappaB inhibitor, inhibits allergic inflammation andairway remodelling in murine models of asthma. Clin Exp Allergy. 2012 Aug;42(8):1273-81.

[4].Ruan HY et al. Effects of a novel NF-kappaB inhibitor, dehydroxymethylepoxyquinomicin (DHMEQ), on growth, apoptosis,gene expression, and chemosensitivity in head and neck squamous cell carcinoma cell lines. Head Neck. 2006 Feb;28(2):158-65.

[5].Shimo T et al. Dehydroxymethylepoxyquinomicin (DHMEQ) can suppress tumour necrosis factor-α production inlipopolysaccharide-injected mice, resulting in rescuing mice from death in vivo. Clin Exp Immunol. 2011 Nov;166(2):299-306.