石蒜碱盐酸盐

石蒜碱盐酸盐

分类: 植物提取物 阅读
石蒜碱盐酸盐 用途与合成方法
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

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
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