荜茇酰胺

荜茇酰胺用途

Piperlongumine 是从荜茇中得到的生物碱[1],具有抗炎、抗菌、抗血管生成、抗氧化、抗肿瘤和抗糖尿病等活性[2]。在肿瘤细胞中,Piperlongumine 能够诱导 ROS 和凋亡[1]。Piperlongumine 具有抗心肌纤维化的作用,通过抑制 ERK1/2 信号通路抑制肌成纤维细胞的转化[2]。

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荜茇酰胺名称

[ CAS 号 ]:
20069-09-4

[ 中文名 ]:
荜茇酰胺

[ 英文名 ]:
Piplartine

[英文别名 ]:

Piperlongumine
(E)-Piplartine
piplartine

荜茇酰胺生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> MAPK/ERK信号通路 >> ERK

信号通路 >> 干细胞及 Wnt 通路 >> ERK

天然产物 >> 生物碱

研究领域 >> 癌症

研究领域 >> 心血管疾病

研究领域 >> 感染

[ 靶点 ]

ERK1

ERK2

[体外研究]

Piplartine(5,10和15μM)在处理24和48小时后显着降低786-O,SKBR3,Panc1,A549和L3.6pL癌细胞的细胞增殖,在5和5时诱导这些细胞系中的细胞凋亡和ROS。治疗3或9小时后10μM[1]。 Piplartine(5或10μM)诱导切割的PARP并下调Sp1,Sp3,Sp4和Sp调节的基因[1]。 Piplartine(20μM)降低心脏成纤维细胞(CFs)的活力。 Piplartine(0-10μM)通过抑制ERK1/2信号通路抑制肌成纤维细胞转化[2]。

[体内研究]

Piperlongumine(30 mg/kg /天,腹腔注射3周)在携带L3.6pL细胞且无体重减轻的无胸腺裸鼠中表现出有效的抗肿瘤作用[1]。

[参考文献]

[1]. Karki K, et al. Piperlongumine Induces Reactive Oxygen Species (ROS)-Dependent Downregulation of Specificity Protein Transcription Factors.

[2]. Wu X, e,t al. Piperlongumine inhibits angiotensin II-induced extracellular matrix expression in cardiac fibroblasts. J Cell Biochem. 2018 Dec;119(12):10358-10364

[相关活性小分子]

荜茇酰胺物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
475.6±45.0 °C at 760 mmHg

[ 熔点 ]:
124ºC

[ 分子式 ]:
C₁₇H₁₉NO₅

[ 分子量 ]:
317.336

[ 闪点 ]:
241.4±28.7 °C

[ 精确质量 ]:
317.126312

[ PSA ]:
65.07000

[ LogP ]:
2.34

[ 外观性状 ]:
white to beige

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.581

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: ≥5mg/mL at warmed to 60°C

荜茇酰胺MSDS

详细MSDS(安全技术说明书)

荜茇酰胺安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
UU7785850

[ 海关编码 ]:
2933399090

荜茇酰胺合成路线

详细合成路线

荜茇酰胺海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

荜茇酰胺文献

Serotonergic signalling suppresses ataxin 3 aggregation and neurotoxicity in animal models of Machado-Joseph disease.

Brain 138 , 3221-37, (2015)

Polyglutamine diseases are a class of dominantly inherited neurodegenerative disorders for which there is no effective treatment. Here we provide evidence that activation of serotonergic signalling is...

Piperlongumine induces apoptotic and autophagic death of the primary myeloid leukemia cells from patients via activation of ROS-p38/JNK pathways.

Acta Pharmacol. Sin. 36(3) , 362-74, (2015)

To investigate the effects of piperlongumine (PL), an anticancer alkaloid from long pepper plants, on the primary myeloid leukemia cells from patients and the mechanisms of action.Human BM samples wer...

Piperlongumine for Enhancing Oral Bioavailability and Cytotoxicity of Docetaxel in Triple-Negative Breast Cancer.

J. Pharm. Sci. 104 , 4417-26, (2016)

Very low oral bioavailability due to extensive pre-systemic metabolism and P-gp efflux has constrained the oral metronomic chemotherapy of docetaxel (DTX). There is tremendous need of compounds facili...

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