石蒜碱盐酸盐
| 中文名称 | 石蒜碱盐酸盐 |
|---|---|
| 中文同义词 | 石蒜碱盐酸盐;石蒜碱 HPL;石蒜鹼;水仙鹼;石蒜提取物.石蒜碱;LYCORINE 石蒜碱;石蒜碱(水仙碱);石蒜碱 |
| 英文名称 | LYCORINE |
| 英文同义词 | 2-beta-diol,3,3-alpha-didehydro-lycoran-1-alph;Amaryline;amarylline;Belamarine;galanthan-1,2-diol,3,12-didehydro-9,10-(methylenebis(oxy))-,(1-alpha,2-beta;galanthidine;narcissine;LYCORINE HPLC 98+% |
| CAS号 | 476-28-8 |
| 分子式 | C16H17NO4 |
| 分子量 | 287.31 |
| EINECS号 | 207-503-6 |
| 相关类别 | 中草药成分;中药对照品;植物提取物;对照品;标准品;Alkaloids;分析试剂标准品;对照品-中药对照品;生物碱;标准品 -中药标准品;标准品，对照品;通用生化试剂-天然产物 |
| Mol文件 | 476-28-8.mol |
| 结构式 |  |
石蒜碱盐酸盐 性质
| 熔点 | 253-255℃ (dec.) |
|---|---|
| 比旋光度 | D16 -129° (c = 0.16 in 98% alc) |
| 沸点 | 429.61°C (rough estimate) |
| 密度 | 1.53 |
| 折射率 | 1.5500 (estimate) |
| 储存条件 | 2-8°C |
| 溶解度 | 溶于氯仿、二氯甲烷、乙酸乙酯、DMSO、丙酮等。 |
| 酸度系数(pKa) | 13.55±0.40(Predicted) |
| 形态 | 粉末 |
Kd: 15.24 nM (SCAP)
Lycorine inhibits cell proliferation in a dose-dependent manner in the abovementioned 4 PCa cell lines, and the IC 50 ranged from 5 μM to 10 μM., it also shows Lycorine has little effects on PNT1A cell's proliferation.SCAP (SREBF chaperone) is an ER-toGolgi transport protein, undergoes a conformational change, and regulates/preserves SREBFs in the ER by forming a complex with INSIG1 (insulin induced gene 1).Lycorine (5-40 μM; 16 hours) significantly suppresses SREBFs activity (up to -70%) in a dosedependent manner and does not cause obvious cytotoxicity in cells.Lycorine (10-20 μM; 2-16 hours) dose- and time-dependently decreases the mature SREBF1 and SREBF2 proteins in HL-7702 cells.Lycorine (20 μM; 16 hours) neither activates NR1H3 transcription nor affect NR1H3 target genes, including ABCG5 and ABCG8, but Sterols activates NR1H3 transcription activity.Lycorine hydrochloride (0-25 μM; 48 hours) treatment markedly suppresses the expression of vascular endothelial (VE)-cadherin in a dose-dependent manner and also slightly diminishes the expression of Sema4D in C8161 cells. However, the expression of the other six genes is not affected.Lycorine hydrochloride (0-25 μM; 48 hours) treatment markedly reduces VE-cadherin protein levels in C8161 cells in a dose-dependent fashion.
Cell Viability Assay
| Cell Line: | HL-7702/SRE-Luc cells |
| Concentration: | 16 hours |
| Incubation Time: | 5 μM; 10 μM; 20 μM; 40 μM |
| Result: | Had no cytotoxicity on HL-7702 cells. |
Western Blot Analysis
| Cell Line: | HL-7702/SRE-Luc cells |
| Concentration: | 2 hours, 4 hours, 8 hours, 12 hours, 16 hours |
| Incubation Time: | 10 μM; 20 μM |
| Result: | Decreased p-SREBF1, m-SREBF1, p-SREBF2 and p-SREBF1 protein expression. |
RT-PCR
| Cell Line: | C8161 cells |
| Concentration: | 0 μM, 1.56 μM, 3.13 μM, 6.25 μM, 12.5 μM, 25 μM |
| Incubation Time: | 48 hours |
| Result: | Markedly suppressed the expression of VE-cadherin in a dose-dependent manner and also slightly diminished the expression of Sema4D in C8161 cells. |
Lycorine (oral chow; 15 mg/kg, 30 mg/kg; once daily) alleviates fat accumulation and metabolic syndrome, increases lipolysis and betaoxidation of fatty acid along with precursor and mature SREBFs in mice .
| Animal Model: | High-fat diet (HFD)-fed C57BL/6J mice |
| Dosage: | 15 mg/kg, 30 mg/kg |
| Administration: | Oral chow; once daily |
| Result: | Ameliorated high-fat diet-induced hyperlipidemia, hepatic steatosis, and insulin resistance in mice. |
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