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;石蒜碱标准品;LYCORINE 石蒜碱 标准品
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+%
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;分析试剂标准品;对照品-中药对照品;Alkaloids;生物碱;标准品 -中药标准品;标准品,对照品
比旋光度
D16 -129° (c = 0.16 in 98% alc)
沸点
429.61°C (rough estimate)
酸度系数(pKa)
13.55±0.40(Predicted)
生物活性
Lycorine 是从金眼科植物科中提取的天然生物碱。Lycorine 是强效具有口服活性的 SCAP 抑制剂,Kd 值 15.24 nM。Lycorine 下调 SCAP 蛋白水平而不改变其转录。Lycorine 也是黑色素瘤血管生成抑制剂。Lycorine 有潜力用于前列腺癌和代谢疾病的研究。
体外研究
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 cells 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.
Cell Line:
HL-7702/SRE-Luc cells
Incubation Time:
5 μM; 10 μM; 20 μM; 40 μM
Result:
Had no cytotoxicity on HL-7702 cells.
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.
Concentration:
0 μM, 1.56 μM, 3.13 μM, 6.25 μM, 12.5 μM, 25 μM
Result:
Markedly suppressed the expression of VE-cadherin in a dose-dependent manner and also slightly diminished the expression of Sema4D in C8161 cells.
体内研究
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.
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.
化学性质
棱形大结晶。熔点275-280℃(分解)。溶于稀酸,难溶于醇、氯仿和石油醚,几乎水溶于水和碱类,对石蕊呈碱性反应。其盐酸盐为长针状结晶,熔点217℃(分解),带一分子结晶水的石蒜碱盐酸盐的熔点为206℃。可溶于20份水。
用途
石蒜碱经口给药或皮下注射有流涎、亚心及增加气管分泌的作用,故在一些时候曾用其制剂作祛痰剂。石蒜碱有较显著的催吐作用。效力比吐根碱强,但不如阿相吗啡。石蒜碱经氢化后生成二氢石蒜碱,后者具有较强的抗阿米巴痢的作用,且毒较小,已供临床使用。石蒜碱制成的内胺盐在动物上表现出抗种瘤作用。中药铁色箭、乌蒜具有祛痰催叶作用,其原因是含有石蒜碱。
生产方法
该品是广泛存在于石蒜科植物中的异喹啉生物碱,可从石蒜(Lycoris radiata)等的鳞茎中提取。
急性毒性
口服-小鼠 LD50: 10700 毫克/公斤; 皮下-小鼠LD50:145 毫克/公斤