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CAS No.: 20069-09-4

Piperlongumine/荜茇酰胺 Catalog No. CSN11731

Synonyms: Piplartine;PPLGM;荜茇酰胺

Piperlongumine, a natural alkaloid from Piper longum L., increases the level of reactive oxygen species (ROS) and selectively kills cancer cells. It is a direct TrxR1 inhibitor with suppressive activity against gastric cancer and an inhibitor of CRM1 and is also an inhibitor of PI3K/Akt/mTOR in human breast cancer cells.

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生物活性

实验方案

技术信息

生物活性

描述Reactive Oxygen Species (ROS) can induce small molecules that use the altered redox state in cancer cells that will be more vulnerable than normal cells to agents with high levels of ROS as well as antioxidant enzymes. Piperlongumine(PL), a natural alkaloid from Piper longum L, can increase the level of ROS and selectively kills cancer cells, which is also a TrxR1 inhibitor with suppressive activity against gastric cancer and a novel inhibitor of CRM1 as well as an inhibitor of PI3K/Akt/mTOR in human breast cancer cells. The average IC50 value of piperlongumine in different cell types is about 5μM. Piperlongumine with concentration range of 0.1–20 μM induced a concentration and time-dependent decrease in the viability of PANC-1, MIA PaCa-2, and BxPC-3, with IC50 values of 4.2, 4.6, and 4.2 μM, respectively at 72 h. MIA PaCa-2 and BxPC-3 cells were particularly sensitive to piperlongumine, and no cells survived for the 5 and 10 μM treatments. PANC-1, MIA PaCa-2, and BxPC-3 cells treated with 10 μM PPLGM for 6 h followed by staining for 30 min, the production of ROS in all three cell lines increased. Three ovarian cancer cell lines A2780, OVCAR3, and SKOV3 and human embryonic kidney cell line HEK293T were treated with either DMSO or PL range from 1 to 100 μM for 72 hr, the IC50 values of PL afer 72 hr exposure were 6.18 μM, 6.20 μM, and 8.20 μM in A2780, OVCAR3, and SKOV3, respectively while it is 60.23 μM to HEK293T. In addition, PL treatment mostly induced apoptosis in OVCAR3 cells. OVCAR3 cells treated with PL (3 μM and 10 μM for 24 hr and 48 hr) showed that the subG1 and G2/M groups were dose- and time dependently increased. Furthermore, HepG2 cells were treated with 2 mM of PL to determine its ability to activate AMPK. PL increased Thr172 phosphorylation and led to a dose-dependent increase in phosphorylation of AMPK and acetyl-CoA carboxylase.
作用机制Piperlongumine can induce cell autophagy and cell death, inhibit cell proliferation and survival.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A375 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A375 cells after 72 hrs by MTT assay, EC50=6.17 μM	25826398
A549 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, EC50=12.2 μM	25826398
HaCaT cells	-	Proliferation assay	72 h	Antiproliferative activity against human HaCaT cells after 72 hrs by MTT assay, EC50=4.46 μM	25826398

更多
动物研究
剂量
Mice: 2.5 mg/kg, 5 mg/kg^[3] (i.p.), 1.5 mg/kg - 3.5 mg/kg^[4] (i.p.); 50 mg/kg^[5] (i.g.); 50 mg/kg, 100 mg/kg^[6] (p.o.)

给药途径
i.p., i.g., p.o.

动物研究
剂量	Mice: 2.5 mg/kg, 5 mg/kg^[3] (i.p.), 1.5 mg/kg - 3.5 mg/kg^[4] (i.p.); 50 mg/kg^[5] (i.g.); 50 mg/kg, 100 mg/kg^[6] (p.o.)
给药途径	i.p., i.g., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1512 mL
- 15.7561 mL
- 31.5123 mL
- 5 mM
- 0.6302 mL
- 3.1512 mL
- 6.3025 mL
- 10 mM
- 0.3151 mL
- 1.5756 mL
- 3.1512 mL

技术信息

CAS号

20069-09-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H19NO5

运输

蓝冰

分子量

317.34

别名

Piplartine;PPLGM;荜茇酰胺

溶解度

DMSO	300.0 mg/mL (945.4 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	6 mg/mL	clear
PO	0.5% CMC-Na	50 mg/mL	suspension

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A375 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A375 cells after 72 hrs by MTT assay, EC50=6.17 μM	25826398
A549 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, EC50=12.2 μM	25826398
HaCaT cells	-	Proliferation assay	72 h	Antiproliferative activity against human HaCaT cells after 72 hrs by MTT assay, EC50=4.46 μM	25826398
HCT116 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=6.04 μM	24937186
HFF1 cells	-	Proliferation assay	72 h	Antiproliferative activity against HFF1 cells after 72 hrs by MTT assay, EC50=13.1 μM	25826398
MA9.3 cells	-	Cytotoxicity assay	48 h	Cytotoxicity against human MA9.3 cells after 48 hrs by MTT assay, IC50=2 μM	25464887
MCF10A cells	-	Proliferation assay	72 h	Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay, EC50=18.1 μM	25826398
MDA-MB-231 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=8.46 μM	24937186
mouse RAW264.7 cells	-	Function assay	-	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50=3 μM	25453809
MRC5 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, IC50=35.04 μM	24937186
PANC1 cells	-	Cytotoxicity assay	24 h	Cytotoxicity against human PANC1 cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay, IC50=3.2 μM	25305718
SK-MEL-2 cells	-	Proliferation assay	72 h	Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by MTT assay, EC50=4.39 μM	25826398
WI38 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human WI38 cells after 72 hrs by MTT assay, IC50=26.78 μM	24937186
ZR75-30 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human ZR75-30 cells after 72 hrs by MTT assay, IC50=5.86 μM	24937186

Piperlongumine/荜茇酰胺 Catalog No. CSN11731

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