水仙环素

中文名称:

水仙环素

中文同义词:

水仙环素;水仙环素?, 99.9%;水仙环素标准品;水仙环素对照品

英文名称:

narciclasine

英文同义词:

Narciclasin;Narciclasine, 99.9%;narciclasine;(13β)-1,19-Didehydro-2α,3β,4β,7-tetrahydroxy-11,12-dinor-5,19-secocrinan-6-one;(2S)-3,4,4aβ,5-Tetrahydro-2α,3β,4β,7-tetrahydroxy[1,3]dioxolo[4,5-j]phenanthridin-6(2H)-one;Lycorcidinol;(2S,3R,4S,4aR)-3,4,4a,5-Tetrahydro-2,3,4,7-tetrahydroxy-(1,3)dioxolo(4,5-j)phenanthridin-6(2H)-one;(2S-(2-alpha,3-beta,4-beta,4a-beta))-3,4,4a,5-tetrahydro-2,3,4,7-tetrahydroxy-(1,3)Dioxolo(4,5-j)phenanthridin-6(2H)-one

CAS号:

29477-83-6

分子式:

C14H13NO7

分子量:

307.26

EINECS号:

相关类别:

中药对照品;标准品;对照品;植物提取物;细胞周期;标准品-对照品;对照品-中药对照品;标准品 -中药标准品;标准品，对照品

Mol文件:

29477-83-6.mol

熔点 

250-252℃

沸点 

447.77°C (rough estimate)

密度 

1.85±0.1 g/cm3 (20 ºC 760 Torr)

折射率 

1.5300 (estimate)

储存条件 

Store at -20°C

溶解度 

DMSO: ≥10mg/mL

酸度系数(pKa)

7.72±0.70(Predicted)

颜色

white to off-white

作用

水仙环素能够高选择性地作用于多形性成胶质细胞瘤，其通过显著减少有丝分裂速度而发挥作用，而不是诱导细胞凋亡来抑制多形性成胶质细胞瘤；同时水仙环素也能调节Rho/Rho激酶/LIM激酶/肌动蛋白素信号通路，增强GTP酶RhoA的活性，同时诱导肌动蛋白应力纤维的形成。

生物活性

Narciclasine是一种植物生长调节剂。 Narciclasine调节Rho/Rho 激酶/LIM 激酶/cofilin信号传导途径，大大增加GTP酶RhoA活性以及以RhoA依赖性方式诱导肌动蛋白应力纤维形成。

靶点

ROCK

ROCK

体外研究

Narciclasine activates Rho and stress fibers in glioblastoma multiforme cells. The mean IC 50 of ~50 nM calculated on the 6 human glioblastoma multiforme (U373, Hs683, GL19, GL5, GL16, GL17), The mean IC 50 value of 47 nM for Narciclasine across a panel of 60 cancer cell lines. Bioassay-guided fractionation of the A. belladonna extract resulted in the identification of lycorine as the bio-active compound. The IC 50 measured for radicle growth inhibition is 0.1 µM for Narciclasine.

体内研究

The i.v. regimen of Narciclasine at 1 mg/kg significantly (P=0.02) increases the survival of GL19 glioblastoma multiforme-bearing mice. Narciclasine when given orally at the same dose five times a week for 5 consecutive weeks also significantly increases animal survival in this model (P=0.008). Oral treatment with Narciclasine at 1 mg/kg significantly increases the survival (P=0.004) of Hs683 glioblastoma multiforme-bearing mice. Increasing the number of doses administered per week does not increase the survival of these Hs683 glioblastoma multiforme-bearing mice. Narciclasine appears to show similar increased survival in these models to temozolomide but at appreciable lower doses and following both oral and i.v. administration.

化学性质 

白色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于水仙。

用途 

水仙环素具有抗肿瘤，抗脑瘤，细胞毒作用。

危险品标志 

Xn

危险类别码 

46

安全说明 

36