Database Query Results : Piperlongumine, ,

PL, Piperlongumine: Click to Expand ⟱

Features:

Piperlongumine (also called Piplartine), an alkaloid from long pepper fruit
-Piperlongumine is a bioactive alkaloid derived from the long pepper (Piper longum)
– Piperlongumine has been shown to selectively increase ROS levels in cancer cells.
-NLRP3 inhibitor?
-TrxR inhibitor (major antioxidant system) to increase ROS in cancer cells
-ic50 cancer cells maybe 2-10uM, normal cells maybe exceeding 20uM.

Available from mcsformulas.com
-(Long Pepper, 500mg/Capsule)- 1 capsule 3 times daily with food
-Piperlongumine Pro Liposomal, 40 mg-take 1 capsule daily with plenty of water, after a meal

-Note half-life 30–60 minutes
BioAv poor aqueous solubility and bioavailability
Pathways:
- induce ROS production in cancer cells likely at any dose. Effect on normal cells is inconclusive.
- ROS↑ related: MMP↓(ΔΨm), ER Stress↑, UPR↑, Cyt‑c↑, Caspases↑, DNA damage↑, cl-PARP↑, Prx,
- Lowers some AntiOxidant markers/ defense in Cancer Cells: but mostly raises NRF2 (raises antiO defense), TrxR↓(*important), GSH↓ Catalase↓ HO1↓ GPx↓
- Very little indication of raising AntiOxidant defense in Normal Cells: GSH↑,
- lowers Inflammation : NF-kB↓, COX2↓, conversely p38↑, Pro-Inflammatory Cytokines : NLRP3↓, IL-1β↓, TNF-α↓, IL-6↓, IL-8↓
- inhibit Growth/Metastases : TumMeta↓, TumCG↓, EMT↓, MMP2↓, MMP9↓, VEGF↓, NF-κB↓, CXCR4↓, ERK↓
- reactivate genes thereby inhibiting cancer cell growth : HDAC↓(few reports), DNMT1↓, DNMT3A↓, EZH2↓, P53↑, HSP↓, Sp proteins↓,
- cause Cell cycle arrest : TumCCA↑, cyclin D1↓, CDK2↓, CDK4↓, CDK6↓,
- inhibits Migration/Invasion : TumCMig↓, TumCI↓, ERK↓, EMT↓,
- small indication of inhibiting glycolysis : HIF-1α↓, cMyc↓, LDH↓, HK2↓,
- inhibits angiogenesis↓ : VEGF↓, HIF-1α↓, EGFR↓,
- Others: PI3K↓, AKT↓, JAK↓, STAT↓, β-catenin↓, ERK↓, JNK,
- Synergies: chemo-sensitization, RadioSensitizer, Others(review target notes), Neuroprotective, Cognitive, Hepatoprotective, CardioProtective,

- Selectivity: Cancer Cells vs Normal Cells

Rank	Pathway / Target Axis	Direction	Primary Effect	Notes / Cancer Relevance	Ref
1	Transformation-linked oxidative stress dependence	↑ ROS	Cancer-selective stress overload	Landmark study: piperlongumine selectively kills cells with a cancer genotype by elevating ROS; antioxidant rescue blocks killing	(ref)
2	GSTP1 redox buffering (glutathione S-transferase π)	↓ GSTP1 function / ↑ ROS	Disables antioxidant buffering	Biochemical/structural work describing GSTP1 as a piperlongumine target and linking PL exposure to increased ROS and decreased GSH	(ref)
3	ER stress / UPR via PRDX4 (Peroxiredoxin 4)	↓ PRDX4 activity / ↑ ER stress	Proteotoxic stress, preferential glioma killing	Piperlongumine inactivates PRDX4, exacerbates ER stress, increases ROS, and preferentially kills high-grade glioma cells	(ref)
4	Mitochondrial disruption + stress MAPK (JNK)	↓ ΔΨm / ↑ JNK	Mitochondrial apoptosis signaling	Example mechanistic paper: piperlongumine induces ROS-mediated mitochondrial disruption and activates JNK associated with apoptosis	(ref)
5	DNA damage response	↑ DNA damage	Checkpoint activation, death signaling	Piperlongumine elevates ROS and causes DNA damage in pancreatic cancer models; antioxidant reverses DNA damage and killing	(ref)
6	STAT3 signaling	↓ STAT3 activity (↓ pSTAT3 / ↓ STAT3 function)	Reduced survival & stem-like growth	Drug-repositioning study identifies piperlongumine as a direct STAT3 inhibitor; shows reduced STAT3 activation and mammosphere inhibition	(ref)
7	NF-κB signaling	↓ NF-κB DNA binding / ↓ nuclear translocation	Reduced inflammatory & anti-apoptotic transcription	Piperlongumine down-regulates NF-κB DNA-binding activity and decreases nuclear translocation of p50/p65 in prostate cancer cells	(ref)
8	PI3K–AKT–mTOR pathway	↓ PI3K/AKT/mTOR signaling	Growth suppression; promotes apoptosis/autophagy	Paper explicitly reporting piperlongumine induces apoptosis and autophagy through inhibition of PI3K/Akt/mTOR in lung cancer cells	(ref)
9	p38 signaling (stress kinase)	↑ p38 signaling	Stress response; autophagy involvement	Mechanistic study showing piperlongumine induces autophagy by targeting p38 signaling	(ref)
10	Cell cycle regulation	↑ G2/M arrest	Proliferation block	Demonstrates piperlongumine induces G2/M cell-cycle arrest in MCF-7 cells (cell cycle distribution shift shown)	(ref)
11	EMT / migration / invasion	↓ EMT / ↓ migration & invasion	Anti-metastatic phenotype	Reports piperlongumine inhibits TGF-β–induced EMT and reduces migration/invasion in cancer cells	(ref)
12	Ferroptosis (iron-dependent oxidative death)	↑ ferroptosis	Non-apoptotic killing modality	Shows piperlongumine-induced cancer cell death is inhibited by ferroptosis inhibitors and iron chelation, supporting ferroptosis involvement	(ref)

Scientific Papers found: Click to Expand⟱

2964-

PL,

Preformulation Studies on Piperlongumine

Analysis,

Nor,

"highlight2" >*BioAv↓, "highlight2" >*BioAv↑, "highlight2" >*other↝, "highlight2" >*eff↓,

2951-

PL,

AF,

Synergistic Dual Targeting of Thioredoxin and Glutathione Systems Irrespective of p53 in Glioblastoma Stem Cells

in-vitro,

GBM,

U87MG

"highlight2" >GSH↓, "highlight2" >eff↑, "highlight2" >GSTP1/GSTπ↓,

2952-

PL,

Piperlongumine suppresses bladder cancer invasion via inhibiting epithelial mesenchymal transition and F-actin reorganization

in-vitro,

Bladder,

T24/HTB-9

2.5, 5, 10 and 20 μM, 24 h

10–20 μM

in-vivo,

Bladder,

"highlight2" >TumCP↓, "highlight2" >TumCCA↑, "highlight2" >TumCMig↓, "highlight2" >TumCI↓, "highlight2" >ROS↑, "highlight2" >Slug↓, "highlight2" >β-catenin/ZEB1↓, "highlight2" >Zeb1↓, "highlight2" >N-cadherin↓, "highlight2" >F-actin↓, "highlight2" >GSH↓, "highlight2" >EMT↓, "highlight2" >CLDN1↓, "highlight2" >ZO-1↓,

2953-

PL,

Piperlongumine Acts as an Immunosuppressant by Exerting Prooxidative Effects in Human T Cells Resulting in Diminished TH17 but Enhanced Treg Differentiation

in-vitro,

Nor,

10 μM PL up to 24 h

nvestigated the effects of PL on the survival and function of primary human peripheral blood T cells (PBTs

"highlight2" >*ROS↑, "highlight2" >*GSTA1↓, "highlight2" >eff↝, "highlight2" >*toxicity↓, "highlight2" >ROS↑, "highlight2" >*Hif1a↓,

2954-

PL,

The metabolites from traditional Chinese medicine targeting ferroptosis for cancer therapy

Review,

Var,

"highlight2" >NRF2↑, "highlight2" >ROS↑, "highlight2" >ER Stress↑, "highlight2" >MAPK↑, "highlight2" >CHOP↑, "highlight2" >selectivity↑, "highlight2" >Keap1↝, "highlight2" >HO-1↑, "highlight2" >Ferroptosis↑,

2955-

PL,

Heme Oxygenase-1 Determines the Differential Response of Breast Cancer and Normal Cells to Piperlongumine

in-vitro,

BC,

MCF-7

in-vitro,

Nor,

MCF10

"highlight2" >ROS?, "highlight2" >*ROS∅, "highlight2" >other⇅, "highlight2" >HO-1↑, "highlight2" >*HO-1↑, "highlight2" >NRF2↑, "highlight2" >Keap1↓, "highlight2" >cl‑PARP↑, "highlight2" >selectivity↑, "highlight2" >GSH↓, "highlight2" >GSSG↑,

2956-

PL,

Piperlongumine rapidly induces the death of human pancreatic cancer cells mainly through the induction of ferroptosis

in-vitro,

PC,

"highlight2" >ROS↑, "highlight2" >Ferroptosis↓, "highlight2" >GSH↓, "highlight2" >GPx↓, "highlight2" >cl‑PARP∅, "highlight2" >cl‑Casp3∅, "highlight2" >eff↑, "highlight2" >eff↑,

2957-

PL,

Piperlongumine Induces Cell Cycle Arrest via Reactive Oxygen Species Accumulation and IKKβ Suppression in Human Breast Cancer Cells

in-vitro,

BC,

MCF-7

10–40 μM

"highlight2" >TumCP↓, "highlight2" >TumCMig↓, "highlight2" >TumCCA↑, "highlight2" >ROS↑, "highlight2" >H2O2↑, "highlight2" >GSH↓, "highlight2" >IKKα↓, "highlight2" >NF-kB↓, "highlight2" >P21↑, "highlight2" >eff↓,

2958-

PL,

Natural product piperlongumine inhibits proliferation of oral squamous carcinoma cells by inducing ferroptosis and inhibiting intracellular antioxidant capacity

in-vitro,

Oral,

HSC3

14.71 µM (48 hr),

"highlight2" >TumCP↓, "highlight2" >lipid-P↑, "highlight2" >ROS↑, "highlight2" >DNMT1↑, "highlight2" >FTH1↓, "highlight2" >GPx4↓, "highlight2" >eff↓, "highlight2" >GSH↓, "highlight2" >Ferroptosis↑, "highlight2" >MDA↓,

2959-

PL,

Piperlongumine mitigates LPS-induced inflammation and lung injury via targeting MD2/TLR4

in-vivo,

Nor,

"highlight2" >*Inflam↓,

2960-

PL,

Synthesis of Piperlongumine Analogues and Discovery of Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators as Potential Neuroprotective Agents

Analysis,

Nor,

"highlight2" >NRF2↑, "highlight2" >neuroP↑,

2961-

PL,

Piperlongumine inhibits esophageal squamous cell carcinoma in vitro and in vivo by triggering NRF2/ROS/TXNIP/NLRP3-dependent pyroptosis

in-vitro,

ESCC,

KYSE-30

28.55 μM

"highlight2" >Pyro↑, "highlight2" >TumCP↓, "highlight2" >TumCMig↓, "highlight2" >TumCI↓, "highlight2" >ASC↑, "highlight2" >cl‑Casp1↑, "highlight2" >NLRP3↑, "highlight2" >GSDMD↑, "highlight2" >ROS↑, "highlight2" >NRF2↓, "highlight2" >TXNIP↑,

2962-

PL,

Synthesis of Piperlongumine Analogues and Discovery of Nuclear Factor Erythroid 2‑Related Factor 2 (Nrf2) Activators as Potential Neuroprotective Agents

in-vitro,

Nor,

PC12

"highlight2" >*GSH↑, "highlight2" >*NQO1↑, "highlight2" >*Trx↑, "highlight2" >*TrxR↑, "highlight2" >*NRF2↑, "highlight2" >*NRF2⇅, "highlight2" >*eff↑, "highlight2" >*BioAv↑, "highlight2" >*ROS↓,

2963-

PL,

Piperlongumine activates Sirtuin1 and improves cognitive function in a murine model of Alzheimer’s disease

in-vitro,

AD,

HEK293

50 mg/kg/day for 2.5 months

mice

"highlight2" >*SIRT1↑, "highlight2" >*cognitive↑, "highlight2" >*Aβ↓, "highlight2" >*Inflam↓, "highlight2" >*neuroP↑, "highlight2" >memory↑, "highlight2" >Dose↓, "highlight2" >NAD↑,

2950-

PL,

Overview of piperlongumine analogues and their therapeutic potential

Review,

Var,

"highlight2" >AntiAg↑, "highlight2" >neuroP↑, "highlight2" >Inflam↓, "highlight2" >NO↓, "highlight2" >PGE2↓, "highlight2" >MMP3↓, "highlight2" >MMP13↓, "highlight2" >TumCMig↓, "highlight2" >TumCI↓, "highlight2" >p38↑, "highlight2" >JNK↑, "highlight2" >NF-kB↑, "highlight2" >ROS↑, "highlight2" >FOXM1↓, "highlight2" >TrxR1↓, "highlight2" >GSH↓, "highlight2" >Trx↓, "highlight2" >cMyc↓, "highlight2" >Casp3↑, "highlight2" >Bcl-2↓, "highlight2" >Mcl-1↓, "highlight2" >STAT3↓, "highlight2" >AR↓, "highlight2" >DNAdam↑,

2965-

PL,

docx,

Piperlongumine for enhancing oral bioavailability and cytotoxicity of docetaxel in triple negative breast cancer

Analysis,

Var,

"highlight2" >BioEnh↑, "highlight2" >eff↑,

2966-

PL,

A strategy to improve the solubility and bioavailability of the insoluble drug piperlongumine through albumin nanoparticles

in-vitro,

LiverDam,

"highlight2" >*Half-Life↑, "highlight2" >*BioAv↑, "highlight2" >eff↑, "highlight2" >ROS↑,

2967-

PL,

Piperlongumine and its derivatives against cancer: A recent update and future prospective

Review,

Var,

"highlight2" >BioAv↓, "highlight2" >BioAv↑,

2968-

PL,

Chit,

Preparation of piperlongumine-loaded chitosan nanoparticles for safe and efficient cancer therapy

in-vitro,

GC,

AGS

"highlight2" >eff↑, "highlight2" >Dose↝, "highlight2" >ROS↑, "highlight2" >BioAv↑,

2969-

PL,

Piperlongumine induces autophagy by targeting p38 signaling

in-vitro,

OS,

U2OS

in-vitro,

Cerv,

HeLa

"highlight2" >p38↑, "highlight2" >ROS↑, "highlight2" >GPx1∅, "highlight2" >SOD∅, "highlight2" >Catalase∅,

2970-

PL,

Piperlongumine induces apoptosis and autophagy in leukemic cells through targeting the PI3K/Akt/mTOR and p38 signaling pathways

in-vitro,

AML,

"highlight2" >AntiAg↑, "highlight2" >TumCG↓, "highlight2" >Apoptosis↑, "highlight2" >PI3K↓, "highlight2" >Akt↓, "highlight2" >mTOR↓, "highlight2" >p38↑, "highlight2" >Casp3↑,

2971-

PL,

Piperlongumine attenuates IL-1β-induced inflammatory response in chondrocytes

NA,

OS,

"highlight2" >*NO↓, "highlight2" >*PGE2↓, "highlight2" >*iNOS↓, "highlight2" >*COX2↓, "highlight2" >*MMP3↑, "highlight2" >*MMP13↓, "highlight2" >*Inflam↓,

2972-

PL,

Piperlongumine Is an NLRP3 Inhibitor With Anti-inflammatory Activity

in-vitro,

AML,

THP1

"highlight2" >NLRP3↓, "highlight2" >IL1β↓, "highlight2" >LDH↓, "highlight2" >cl‑Casp1↓, "highlight2" >Inflam↓,

2973-

PL,

The Natural Alkaloid Piperlongumine Inhibits Metastatic Activity and Epithelial-to-Mesenchymal Transition of Triple-Negative Mammary Carcinoma Cells

in-vitro,

BC,

MDA-MB-231

in-vitro,

BC,

4T1

"highlight2" >MMP2↓, "highlight2" >MMP9↓, "highlight2" >IL6↓, "highlight2" >E-cadherin↑, "highlight2" >ROS↑, "highlight2" >EMT↓, "highlight2" >Zeb1↓, "highlight2" >Slug↓, "highlight2" >TumMeta↓, "highlight2" >selectivity↑, "highlight2" >MMP2↓, "highlight2" >GSH↓,

2995-

PL,

Piperlongumine overcomes osimertinib resistance via governing ubiquitination-modulated Sp1 turnover

in-vitro,

Lung,

H1975

in-vitro,

Lung,

PC9

in-vivo,

NA,

"highlight2" >Sp1/3/4↓, "highlight2" >cMET↓, "highlight2" >Apoptosis↑, "highlight2" >Cyt‑c↑, "highlight2" >p‑ERK↓, "highlight2" >p‑Akt↓, "highlight2" >TumCG↓,

2996-

PL,

Application of longinamide in inhibiting the activation of NLRP3 inflammasome

NA,

AD,

NA,

Park,

"highlight2" >*NLRP3↓,

2999-

PL,

Piperlongumine alleviates corneal allograft rejection via suppressing angiogenesis and inflammation

in-vivo,

Nor,

HUVECs

"highlight2" >*Inflam↓, "highlight2" >*angioG↓, "highlight2" >*Hif1a↓, "highlight2" >*VEGF↓, "highlight2" >*ICAM-1↓, "highlight2" >*VCAM-1↓, "highlight2" >*neuroP↑,

3000-

PL,

Biological and physical approaches on the role of piplartine (piperlongumine) in cancer

in-vitro,

Nor,

HUVECs

in-vitro,

Laryn,

HEp2

"highlight2" >Inflam↓, "highlight2" >AntiTum↑, "highlight2" >*α-tubulin↓, "highlight2" >selectivity↑, "highlight2" >HIF2a↓, "highlight2" >MCP1↓,

1951-

PL,

Piperlongumine Analogs Promote A549 Cell Apoptosis through Enhancing ROS Generation

in-vitro,

Lung,

A549

"highlight2" >ROS↑, "highlight2" >lipid-P↑, "highlight2" >MMP↓, "highlight2" >TumCCA↑, "highlight2" >TrxR↓, "highlight2" >eff↑,

1938-

PL,

Piperlongumine regulates epigenetic modulation and alleviates psoriasis-like skin inflammation via inhibition of hyperproliferation and inflammation

Study,

PSA,

in-vivo,

NA,

Mice: 10 (PL = PPL low dose) and 30 (PH = PPL high dose) mg/kg dose of PPL was fixed for topical intervention

"highlight2" >ROS↑, "highlight2" >Apoptosis↑, "highlight2" >MMP↓, "highlight2" >TumCCA↑, "highlight2" >DNAdam↑, "highlight2" >STAT3↓, "highlight2" >Akt↓, "highlight2" >PCNA↓, "highlight2" >Ki-67↓, "highlight2" >cycD1/CCND1↓, "highlight2" >Bcl-2↓, "highlight2" >K17↓, "highlight2" >HDAC↓, "highlight2" >ROS↑, "highlight2" >*IL1β↓, "highlight2" >*IL6↓, "highlight2" >*TNF-α↓, "highlight2" >*IL17↓, "highlight2" >*IL22↓,

1939-

PL,

Piperlongumine selectively kills hepatocellular carcinoma cells and preferentially inhibits their invasion via ROS-ER-MAPKs-CHOP

in-vitro,

HCC,

HepG2

5-20 μM

in-vitro,

HCC,

HUH7

in-vivo,

NA,

(1.5 mg/kg

mice

"highlight2" >TumCMig↓, "highlight2" >TumCI↓, "highlight2" >ER Stress↑, "highlight2" >selectivity↑, "highlight2" >tumCV↓, "highlight2" >ROS↑, "highlight2" >GSH↓, "highlight2" >eff↓, "highlight2" >Ca+2↑, "highlight2" >MAPK↑, "highlight2" >CHOP↑, "highlight2" >Dose↝,

1940-

PL,

Piperlongumine Inhibits Migration of Glioblastoma Cells via Activation of ROS-Dependent p38 and JNK Signaling Pathways

in-vitro,

GBM,

LN229

1, 2, or 5 μM, 10uM

in-vitro,

GBM,

U87MG

"highlight2" >ROS↑, "highlight2" >GSH↓, "highlight2" >p38↑, "highlight2" >JNK↑, "highlight2" >IKKα↑, "highlight2" >NF-kB↓, "highlight2" >eff↓,

1941-

PL,

Piperlongumine selectively kills cancer cells and increases cisplatin antitumor activity in head and neck cancer

in-vitro,

HNSCC,

"highlight2" >selectivity↑, "highlight2" >eff↑, "highlight2" >ROS↑, "highlight2" >toxicity↑, "highlight2" >GSH↓, "highlight2" >GSSG↑, "highlight2" >*GSSG∅, "highlight2" >cl‑PARP↑, "highlight2" >PUMA↑, "highlight2" >GSTP1/GSTπ↓, "highlight2" >ChemoSen↑,

1942-

PL,

Piperlongumine inhibits antioxidant enzymes, increases ROS levels, induces DNA damage and G2/M cell cycle arrest in breast cell lines

in-vitro,

BC,

MCF-7

"highlight2" >ROS↑, "highlight2" >SOD1↑, "highlight2" >Trx1↓, "highlight2" >Catalase↓, "highlight2" >PrxII↓, "highlight2" >ROS↑, "highlight2" >GADD45A↑, "highlight2" >P21↑, "highlight2" >DNAdam↑, "highlight2" >TumCCA↑,

1943-

PL,

Piperlongumine treatment inactivates peroxiredoxin 4, exacerbates endoplasmic reticulum stress, and preferentially kills high-grade glioma cells

in-vitro,

GBM,

0-10 μM

in-vivo,

NA,

mice

"highlight2" >selectivity↑, "highlight2" >ROS↑, "highlight2" >selectivity↑, "highlight2" >Prx4↓, "highlight2" >*Prx4∅, "highlight2" >ER Stress↑, "highlight2" >CHOP↑, "highlight2" >UPR↑,

1944-

PL,

Piperlongumine, a Novel TrxR1 Inhibitor, Induces Apoptosis in Hepatocellular Carcinoma Cells by ROS-Mediated ER Stress

in-vitro,

HCC,

HUH7

0.625, 2.5, 5, 10, 15, 20, 30, 40, and 50 µM

in-vitro,

HCC,

HepG2

"highlight2" >ER Stress↑, "highlight2" >TrxR1↓, "highlight2" >ROS↑, "highlight2" >eff↓, "highlight2" >Bcl-2↓, "highlight2" >proCasp3↓, "highlight2" >BAX↓, "highlight2" >cl‑Casp3↑, "highlight2" >TumCCA↑, "highlight2" >p‑PERK↑, "highlight2" >ATF4↑, "highlight2" >TumCG↓, "highlight2" >lipid-P↑, "highlight2" >selectivity↑,

1945-

PL,

SANG,

The Synergistic Effect of Piperlongumine and Sanguinarine on the Non-Small Lung Cancer

in-vitro,

Lung,

A549

1-8uM(PL), 0-2uM(SAN)

ic50, 8.03µM for PL and 2.19 µM for SAN

"highlight2" >toxicity∅, "highlight2" >Apoptosis↑, "highlight2" >TumMeta↓, "highlight2" >ROS↑, "highlight2" >TumCCA↑,

1946-

PL,

PI,

Piperlonguminine and Piperine Analogues as TrxR Inhibitors that Promote ROS and Autophagy and Regulate p38 and Akt/mTOR Signaling

in-vitro,

Liver,

"highlight2" >eff↑, "highlight2" >toxicity↓, "highlight2" >TrxR↓, "highlight2" >ROS↑, "highlight2" >MMP↓, "highlight2" >p38↑, "highlight2" >Akt↓, "highlight2" >mTOR↓,

1947-

PL,

Piperlongumine as a direct TrxR1 inhibitor with suppressive activity against gastric cancer

in-vitro,

GC,

SGC-7901

in-vitro,

GC,

"highlight2" >TrxR1↓, "highlight2" >ROS↑, "highlight2" >ER Stress↑, "highlight2" >mtDam↑, "highlight2" >selectivity↑, "highlight2" >NO↑, "highlight2" >TumCCA↑, "highlight2" >mt-ROS↑, "highlight2" >Casp9↑, "highlight2" >Bcl-2↓, "highlight2" >Bcl-xL↓, "highlight2" >cl‑PARP↑, "highlight2" >eff↓, "highlight2" >lipid-P↑,

1948-

PL,

born,

Natural borneol serves as an adjuvant agent to promote the cellular uptake of piperlongumine for improving its antiglioma efficacy

in-vitro,

GBM,

"highlight2" >selectivity↑, "highlight2" >ROS↑, "highlight2" >BioAv↓, "highlight2" >BioAv↑, "highlight2" >Apoptosis↑, "highlight2" >TumCCA↑, "highlight2" >eff↑,

1949-

PL,

Design, synthesis, and biological evaluation of a novel indoleamine 2,3-dioxigenase 1 (IDO1) and thioredoxin reductase (TrxR) dual inhibitor

in-vitro,

CRC,

HCT116

in-vitro,

Cerv,

HeLa

"highlight2" >TrxR↓, "highlight2" >selectivity↑, "highlight2" >ROS↑, "highlight2" >IDO1↓,

1950-

PL,

Increased Expression of FosB through Reactive Oxygen Species Accumulation Functions as Pro-Apoptotic Protein in Piperlongumine Treated MCF7 Breast Cancer Cells

in-vitro,

BC,

MCF-7

in-vitro,

Lung,

A549

"highlight2" >selectivity↑, "highlight2" >ROS↑, "highlight2" >SETBP1↓, "highlight2" >cl‑Casp9↑, "highlight2" >eff↓, "highlight2" >FOSB↑,

992-

PL,

Piperlongumine based nanomedicine impairs glycolytic metabolism in triple negative breast cancer stem cells through modulation of GAPDH & FBP1

in-vivo,

BC,

zebrafish and nude mice

"highlight2" >EPR↓, "highlight2" >Glycolysis↓, "highlight2" >GAPDH↓, "highlight2" >GSTP1/GSTπ↝, "highlight2" >FBPase↑,

1952-

PL,

5-FU,

Piperlongumine induces ROS accumulation to reverse resistance of 5-FU in human colorectal cancer via targeting TrxR

in-vivo,

CRC,

HCT8

10uM

mice

"highlight2" >ROS↑, "highlight2" >TrxR↓, "highlight2" >eff↑, "highlight2" >p‑Akt↓,

1953-

PL,

Designing piperlongumine-directed anticancer agents by an electrophilicity-based prooxidant strategy: A mechanistic investigation

in-vitro,

Lung,

A549

in-vitro,

Nor,

WI38

"highlight2" >ROS↑, "highlight2" >selectivity↑, "highlight2" >TrxR↓, "highlight2" >TumCCA↑, "highlight2" >GSH?, "highlight2" >H2O2↑,

2649-

PL,

Oxidative Stress Inducers in Cancer Therapy: Preclinical and Clinical Evidence

Review,

Var,

"highlight2" >AntiCan↑, "highlight2" >ROS↑, "highlight2" >GSH↓, "highlight2" >TrxR↓, "highlight2" >Trx↓, "highlight2" >Apoptosis↑, "highlight2" >TumCCA↑, "highlight2" >ER Stress↑, "highlight2" >DNAdam↑, "highlight2" >ChemoSen↑, "highlight2" >BioAv↓,

2940-

PL,

Piperlongumine Induces Reactive Oxygen Species (ROS)-dependent Downregulation of Specificity Protein Transcription Factors

in-vitro,

PC,

PANC1

 5-15 μM

in-vitro,

Lung,

A549

in-vitro,

Kidney,

786-O

in-vitro,

BC,

SkBr3

"highlight2" >ROS↑, "highlight2" >TumCP↓, "highlight2" >Apoptosis↑, "highlight2" >eff↓, "highlight2" >Sp1/3/4↓, "highlight2" >cycD1/CCND1↓, "highlight2" >survivin↓, "highlight2" >cMyc↓, "highlight2" >EGFR↓, "highlight2" >cMET↓,

2941-

PL,

Selective killing of cancer cells by a small molecule targeting the stress response to ROS

in-vivo,

BC,

MDA-MB-231

mice

in-vitro,

OS,

U2OS

in-vitro,

BC,

MDA-MB-453

"highlight2" >ROS↑, "highlight2" >Apoptosis↑, "highlight2" >selectivity↑, "highlight2" >*ROS∅, "highlight2" >GSH↓, "highlight2" >GSSG↑, "highlight2" >H2O2↑, "highlight2" >NO↑, "highlight2" >Half-Life?,

2942-

PL,

Piperlongumine increases sensitivity of colorectal cancer cells to radiation: Involvement of ROS production via dual inhibition of glutathione and thioredoxin systems

in-vitro,

CRC,

CT26

in-vitro,

CRC,

DLD1

in-vivo,

CRC,

CT26

CT26 tumor-bearing mice

"highlight2" >ROS↑, "highlight2" >GSH↓, "highlight2" >TrxR↓, "highlight2" >RadioS↑, "highlight2" >DNAdam↑, "highlight2" >TumCCA↑, "highlight2" >mitResp↓, "highlight2" >GSTs↓, "highlight2" >OS↑,

2943-

PL,

Piperlongumine Inhibits Thioredoxin Reductase 1 by Targeting Selenocysteine Residues and Sensitizes Cancer Cells to Erastin

in-vitro,

CRC,

HCT116

in-vitro,

Lung,

A549

in-vitro,

BC,

MCF-7

"highlight2" >TrxR1?, "highlight2" >TumCD↑, "highlight2" >ROS↑, "highlight2" >GSH↓, "highlight2" >eff↑,

2944-

PL,

Piperlongumine, a Potent Anticancer Phytotherapeutic, Induces Cell Cycle Arrest and Apoptosis In Vitro and In Vivo through the ROS/Akt Pathway in Human Thyroid Cancer Cells

in-vitro,

Thyroid,

IHH4

 2 and 3 μM

in-vitro,

Thyroid,

8505C

in-vivo,

NA,

10 mg/kg

Nude mice

"highlight2" >ROS↑, "highlight2" >selectivity↑, "highlight2" >tumCV↓, "highlight2" >TumCCA↑, "highlight2" >Apoptosis↑, "highlight2" >ERK↑, "highlight2" >Akt↓, "highlight2" >mTOR↓,

* indicates research on normal cells as opposed to diseased cells
Total Research Paper Matches: 56

Pathway results for Effect on Cancer / Diseased Cells:

Pathway results for Effect on Normal Cells:

Redox & Oxidative Stress ⓘ

GSH↑, 2, GSSG∅, 1, GSTA1↓, 1, HO-1↑, 1, lipid-P↓, 1, NQO1↑, 1, NRF2↑, 1, NRF2⇅, 1, Prx4∅, 1, ROS↓, 1, ROS↑, 1, ROS∅, 2, Trx↑, 1, TrxR↑, 1,

Core Metabolism/Glycolysis ⓘ

SIRT1↑, 1,

Cell Death ⓘ

iNOS↓, 1,

Transcription & Epigenetics ⓘ

other↝, 1,

Migration ⓘ

MMP13↓, 1, MMP3↑, 1, VCAM-1↓, 1, α-tubulin↓, 1,

Angiogenesis & Vasculature ⓘ

angioG↓, 1, Hif1a↓, 2, NO↓, 1, VEGF↓, 1,

Immune & Inflammatory Signaling ⓘ

COX2↓, 1, ICAM-1↓, 1, IL17↓, 1, IL1β↓, 1, IL22↓, 1, IL6↓, 1, Inflam↓, 4, PGE2↓, 1, TNF-α↓, 1,

Protein Aggregation ⓘ

Aβ↓, 1, NLRP3↓, 1,

Drug Metabolism & Resistance ⓘ

BioAv↓, 1, BioAv↑, 3, eff↓, 1, eff↑, 1, Half-Life↑, 1,

Clinical Biomarkers ⓘ

IL6↓, 1,

Functional Outcomes ⓘ

cognitive↑, 1, hepatoP↑, 1, neuroP↑, 2, toxicity↓, 2,
Total Targets: 46

Query results interpretion may depend on "conditions" listed in the research papers.
Such Conditions may include : 
  -low or high Dose
  -format for product, such as nano of lipid formations
  -different cell line effects
  -synergies with other products 
  -if effect was for normal or cancerous cells

Filter Conditions: Pro/AntiFlg:%  IllCat:%  CanType:%  Cells:%  prod#:134  Target#:%  State#:%  Dir#:%
  wNotes=0  sortOrder:rid,rpid

Database Query Results : Piperlongumine, ,

Pathway results for Effect on Cancer / Diseased Cells:

Redox & Oxidative Stress ⓘ

Metal & Cofactor Biology ⓘ

Mitochondria & Bioenergetics ⓘ

Core Metabolism/Glycolysis ⓘ

Cell Death ⓘ

Kinase & Signal Transduction ⓘ

Transcription & Epigenetics ⓘ

Protein Folding & ER Stress ⓘ

DNA Damage & Repair ⓘ

Cell Cycle & Senescence ⓘ

Proliferation, Differentiation & Cell State ⓘ

Migration ⓘ

Angiogenesis & Vasculature ⓘ

Barriers & Transport ⓘ

Immune & Inflammatory Signaling ⓘ

Protein Aggregation ⓘ

Hormonal & Nuclear Receptors ⓘ

Drug Metabolism & Resistance ⓘ

Clinical Biomarkers ⓘ

Functional Outcomes ⓘ

Pathway results for Effect on Normal Cells:

Redox & Oxidative Stress ⓘ

Core Metabolism/Glycolysis ⓘ

Cell Death ⓘ

Transcription & Epigenetics ⓘ

Migration ⓘ

Angiogenesis & Vasculature ⓘ

Immune & Inflammatory Signaling ⓘ

Protein Aggregation ⓘ

Drug Metabolism & Resistance ⓘ

Clinical Biomarkers ⓘ

Functional Outcomes ⓘ

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