石蒜碱盐酸盐

生物活性靶点体外研究体内研究石蒜碱盐酸盐试剂级价格

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

石蒜碱盐酸盐化学性质

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 :Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
酸度系数(pKa) :13.55±0.40(Predicted)
形态 :powder

安全信息

危险品标志 :T
危险类别码 :25
安全说明 :45
危险品运输编号 :UN 2811 6.1/PG 3
WGK Germany :3

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