扁塑藤素

中文名称:

扁塑藤素

中文同义词:

扁塑藤素 (扁蒴藤素);扁蒴藤素;扁塑藤素;扁塑藤素 标准品;单酰基甘油脂肪酶(MGL)抑制剂(PRISTIMERIN);扁塑藤素对照品

英文名称:

pristimerin

英文同义词:

pristimerin;3-Hydroxy-2-oxo-24-nor-D:A-friedoolean-1(10),3,5,7-tetren-29-oic acid methyl ester;Celastrol-methylether;(9β,13α,14β,20α)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oicacidmethylester;(9b,13a,14b,20a)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tertraen-29-oic acid methyl ester;3-hydroxy-9β,13α-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid, methyl ester;Celastrol methyl ester;Pristimerin(NSC 99281)

CAS号:

1258-84-0

分子式:

C30H40O4

分子量:

464.64

EINECS号:

相关类别:

对照品,标准品;植物提取物;对照品;标准品;中药对照品;科研试剂;标准品-对照品;分析试剂标准品;细胞生物学试剂;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:

1258-84-0.mol

熔点 

219.5°C

沸点 

488.1°C (rough estimate)

密度 

1.0271 (rough estimate)

折射率 

1.4800 (estimate)

储存条件 

-20°C

溶解度 

DMSO: ≥5mg/mL

酸度系数(pKa)

8.60±0.70(Predicted)

形态

Red solid

颜色

orange

生物活性

Pristimerin是高效可逆的单酰基甘油脂肪酶(MGL)抑制剂，IC50值为93 nM。

靶点

IC50: 93 nM (MGL)

体外研究

Pristimerin inhibits the activity of purified MGL with an IC 50 of 93±8 nM and that of non-purified MGL (cell lysates of MGL-transfected HeLa cells) with an IC 50 of 398±68 nM. Pristimerin inhibits MGL through a mechanism that is rapid, reversible and non-competitive. The binding of pristimerin to MGL might be strengthened by formation of a polar interaction with a regulatory cysteine, possibly Cys 208 . Pristimerin inhibits HFLS-RA and HUVEC cell viability in a dose- and time-dependent manner. Pristimerin decreases VEGF-induced autophosphorylation of VEGFR2 and attenuates the activation of the VEGF-induced VEGFR2-mediated signaling pathway .

体内研究

Pristimerin inhibits inflammation and tumor angiogenesis. Pristimerin significantly reduces vessel density in synovial membrane tissues of inflamed joints and reduces the expression of pro-angiogenic factors in sera, including TNF-α, Ang-1, and MMP-9.

化学性质 

红色结晶，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于雷公藤。

用途 

抑制癌细胞、卵巢癌。

用途 

用于含量测定/鉴定/药理实验等

毒性

LD50 oral in mouse: 8gm/kg