石蒜碱盐酸盐
- CAS号:476-28-8
- 英文名:LYCORINE
- 中文名:石蒜碱盐酸盐
- CBNumber:CB6226644
- 分子式:C16H17NO4
- 分子量:287.31
- MOL File:476-28-8.mol
- 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 :Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
- 酸度系数(pKa) :13.55±0.40(Predicted)
- 形态 :powder
- 颜色 :White to off-white
- 旋光性 (optical activity) :-12916 (c 0.16, 98% ethanol)
石蒜碱盐酸盐性质、用途与生产工艺
- 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。
-
靶点
Kd: 15.24 nM (SCAP)
-
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 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. -
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. - 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。
- 类别 有毒物品
- 毒性分级 中毒
- 急性毒性 口服-小鼠 LD50: 10700 毫克/公斤; 皮下-小鼠LD50:145 毫克/公斤
- 可燃性危险特性 可燃;燃烧产生有毒氮氧化物烟雾
- 储运特性 库房通风低温干燥
- 灭火剂 干粉、泡沫、砂土、二氧化碳, 雾状水
- 更新日期：2024/11/11
- 产品编号：XW47628801
- 产品名称：石蒜碱 Lycorine
- CAS编号：
- 包装：20mg
- 价格：113元
- 更新日期：2024/11/08
- 产品编号：HY-N0288
- 产品名称：石蒜碱盐酸盐 Lycorine
- CAS编号：476-28-8
- 包装：50mg
- 价格：800元
- 公司名称：CFMOT-PHYTO
- 联系电话：--
- 电子邮件：
- 国家：德国
- 产品数：1136
- 优势度：62
- 公司名称：Service Chemical Inc.
- 联系电话：--
- 电子邮件：sales@chemos-group.com
- 国家：德国
- 产品数：6350
- 优势度：71
