Nomilin 是一种柠檬苦素类化合物,从柑桔类提取物中获得,是抗肥胖症和降糖药。
产品描述
Nomilin is naturally occurring triterpenoids, have immunomodulatory activity.
体外活性
Administration of Nomilin significantly retarded endothelial cell proliferation, invasion, migration and tube formation. It also possesses anti-proliferative activity against the number of human cancer cell lines including leukemia (HL-60), ovary (SKOV-3), liver (Hep G2), cervix (HeLa), stomach (NCI-SNU-1), and breast (MCF-7)[2]. Nomilin significantly decreased TRAP-positive multinucleated cell numbers compared with the control and exhibited no cytotoxicity. It decreases bone resorption activity and downregulates osteoclast-specific genes, NFATc1 and TRAP mRNA levels. Furthermore, Nomilin suppressed MAPK signaling pathways. Thus, Nomilin has inhibitory effects on osteoclastic differentiation in vitro[3].
体内活性
Nomilin is an effective inducer of gluthathione S-transferase activity in mice and to inhibit carcinogenesis in the hamster buccal pouch assay. Nomilin can shorten anaesthetic-induced sleeping time in mice, probably through a stimulant action on the central nervous system [1]. Nomilin significantly inhibited tumour-directed capillary formation. Serum proinflammatory cytokines such as IL-1β, IL-6, TNF-α and GM-CSF and also serum NO levels were significantly reduced by the treatment of nomilin. Administration of Nomilin significantly reduced the serum level of VEGF, a proangiogenic factor and increased the antiangiogenic factors TIMP-1 and IL-2 [2].
细胞实验
Cell lines: HUVECs. Concentrations: 5 μg-500 μg/ml. Incubation Time: 48 h. Method:. HUVECs were seeded (5000 cells/well) in 96-well flat-bottomed titer plate and incubated for 24 h at 37 °C in 5% CO2 atmosphere. Different concentrations of Nomilin (5 μg-500 μg/ml) were added and incubated further for 48 h. Before 4 h completion of incubation, 20 μl MTT (5 mg/ml) was added. Percentage of dead cells was determined using an ELISA plate reader set to record absorbance at 570 nm.
动物实验
Animal Models: Four to six week old male C57BL/6 mice. Formulation: light paraffin oil. Dosages: 6 mg/kg, I.P.
Cas No.
1063-77-0
分子式
C28H34O9
分子量
514.571
储存和溶解度
Ethanol:Insoluble
DMSO:50 mg/mL
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years