竹柏内酯 B

生物活性靶点体外研究体内研究竹柏内酯 B 试剂级价格

竹柏内酯 B

CAS号:19891-51-1
英文名:(1S)-1,2,3,3a,5aβ,6,10b,10cβ-Octahydro-1,2α,6α-trihydroxy-3aβ,10bα-dimethyl-7-isopropyl-4H,9H-furo[2',3',4':4,5]naphtho[2,1-c]pyran-4,9-dione
中文名:竹柏内酯 B
CBNumber:CB92270118
分子式:C19H24O7
分子量:364.39
MOL File:19891-51-1.mol

竹柏内酯 B化学性质

熔点 :258-261℃
沸点 :644.6±55.0 °C(Predicted)
密度 :1.42±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :Soluble in DMSO
形态 :Solid
酸度系数(pKa) :12.23±0.70(Predicted)
颜色 :White to off-white

竹柏内酯 B性质、用途与生产工艺

生物活性 Nagilactone B，是从 Podocarpus nagi 根皮中提取的，是一种肝 X 受体 (LXR) 激动剂。
靶点

LXR
体外研究

RAW264.7 cells are co-incubated with oxLDL (20 μg/mL) and Nagilactone B (0.02, 0.1, and 0.5 μM) for 24 h. Oil Red O (ORO) staining reveals significant lipid accumulation and foam cell formation in RAW264.7 cells following oxLDL treatment. Nagilactone B (NLB) significantly ameliorates intracellular lipid accumulation. ORO positive areas are reduced by 30.05±7.49 (P<0.01), 47.25±5.39 (P<0.001), and 48.65±7.44% (P<0.001) in Nagilactone B (0.02, 0.1, and 0.5 μM)-treated groups, respectively. The effects of Nagilactone B are evaluated ton cholesterol efflux. Nagilactone B (0.02, 0.1, and 0.5 μM) markedly promotes cholesterol efflux to extracellular apolipoprotein A-I (apoA-I) and high density lipoprotein (HDL) with maximal 5.72- (P<0.05) and 2.34-fold (P<0.01), respectively.
体内研究

Nagilactone B (NLB) suppresses atherosclerosis in apoE ^-/- mice by inducing ATP-binding cassette transporter A1 (ABCA1) and G1 (ABCG1) mediated cholesterol efflux in macrophages. Male apoE-deficient mice on C57BL/6J background receive Nagilactone B (10 and 30 mg/kg) for 12 weeks. Compared with the model group, Nagilactone B treatment (10 and 30 mg/kg) significantly reduces en face lesions of total aorta areas. Six-week-old male apoE ^-/- mice on an HFD are randomized to receive Atorvastatin (10 mg/kg/day), Nagilactone B (10 and 30 mg/kg/day), or CMC-Na for 12 weeks. Mice on chow diet are administered CMC-Na as the normal diet control group. En face aortic lesion areas are evaluated with Sudan IV staining and lesion areas in the aortic sinus monitored via ORO staining. Atherosclerosis developes slowly in the normal diet group, whereas lesions in the HFD model group are significantly increased in en face aortas. Nagilactone B treatment (10 and 30 mg/kg/day) significantly reduces en face aortic lesions, compared with the HFD group by 54.96±10.06% (P<0.01), 71.50±15.37% (P<0.001) in both NLB (L) and NLB (H) groups. In particular, Nagilactone B markedly attenuates atherosclerotic plaque lesion areas in the aortic arch aorta, thoracic aorta, and abdominal aorta [P<0.01 in NLB (H) group].