| 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 |
| 2964- | PL, | Preformulation Studies on Piperlongumine |
| - | Analysis, | Nor, | NA |
| 2951- | PL, | Aur, | Synergistic Dual Targeting of Thioredoxin and Glutathione Systems Irrespective of p53 in Glioblastoma Stem Cells |
| - | in-vitro, | GBM, | U87MG |
| 2952- | PL, | Piperlongumine suppresses bladder cancer invasion via inhibiting epithelial mesenchymal transition and F-actin reorganization |
| - | in-vitro, | Bladder, | T24 | - | in-vivo, | Bladder, | NA |
| 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, | NA |
| 2954- | PL, | The metabolites from traditional Chinese medicine targeting ferroptosis for cancer therapy |
| - | Review, | Var, | NA |
| 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 |
| 2956- | PL, | Piperlongumine rapidly induces the death of human pancreatic cancer cells mainly through the induction of ferroptosis |
| - | in-vitro, | PC, | NA |
| 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 |
| 2958- | PL, | Natural product piperlongumine inhibits proliferation of oral squamous carcinoma cells by inducing ferroptosis and inhibiting intracellular antioxidant capacity |
| - | in-vitro, | Oral, | HSC3 |
| 2959- | PL, | Piperlongumine mitigates LPS-induced inflammation and lung injury via targeting MD2/TLR4 |
| - | in-vivo, | Nor, | NA |
| 2960- | PL, | Synthesis of Piperlongumine Analogues and Discovery of Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators as Potential Neuroprotective Agents |
| - | Analysis, | Nor, | NA |
| 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 |
| 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 |
| 2963- | PL, | Piperlongumine activates Sirtuin1 and improves cognitive function in a murine model of Alzheimer’s disease |
| - | in-vitro, | AD, | HEK293 |
| 2950- | PL, | Overview of piperlongumine analogues and their therapeutic potential |
| - | Review, | Var, | NA |
| 2965- | PL, | docx, | Piperlongumine for enhancing oral bioavailability and cytotoxicity of docetaxel in triple negative breast cancer |
| - | Analysis, | Var, | NA |
| 2966- | PL, | A strategy to improve the solubility and bioavailability of the insoluble drug piperlongumine through albumin nanoparticles |
| - | in-vitro, | LiverDam, | NA |
| 2967- | PL, | Piperlongumine and its derivatives against cancer: A recent update and future prospective |
| - | Review, | Var, | NA |
| 2968- | PL, | Chit, | Preparation of piperlongumine-loaded chitosan nanoparticles for safe and efficient cancer therapy |
| - | in-vitro, | GC, | AGS |
| 2969- | PL, | Piperlongumine induces autophagy by targeting p38 signaling |
| - | in-vitro, | OS, | U2OS | - | in-vitro, | Cerv, | HeLa |
| 2970- | PL, | Piperlongumine induces apoptosis and autophagy in leukemic cells through targeting the PI3K/Akt/mTOR and p38 signaling pathways |
| - | in-vitro, | AML, | NA |
| 2971- | PL, | Piperlongumine attenuates IL-1β-induced inflammatory response in chondrocytes |
| - | NA, | OS, | NA |
| 2972- | PL, | Piperlongumine Is an NLRP3 Inhibitor With Anti-inflammatory Activity |
| - | in-vitro, | AML, | THP1 |
| 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 |
| 2995- | PL, | Piperlongumine overcomes osimertinib resistance via governing ubiquitination-modulated Sp1 turnover |
| - | in-vitro, | Lung, | H1975 | - | in-vitro, | Lung, | PC9 | - | in-vivo, | NA, | NA |
| 2996- | PL, | Application of longinamide in inhibiting the activation of NLRP3 inflammasome |
| - | NA, | AD, | NA | - | NA, | Park, | NA |
| 2999- | PL, | Piperlongumine alleviates corneal allograft rejection via suppressing angiogenesis and inflammation |
| - | in-vivo, | Nor, | HUVECs |
| 3000- | PL, | Biological and physical approaches on the role of piplartine (piperlongumine) in cancer |
| - | in-vitro, | Nor, | HUVECs | - | in-vitro, | Laryn, | HEp2 |
| 1951- | PL, | Piperlongumine Analogs Promote A549 Cell Apoptosis through Enhancing ROS Generation |
| - | in-vitro, | Lung, | A549 |
| 1938- | PL, | Piperlongumine regulates epigenetic modulation and alleviates psoriasis-like skin inflammation via inhibition of hyperproliferation and inflammation |
| - | Study, | PSA, | NA | - | in-vivo, | NA, | NA |
| 1939- | PL, | Piperlongumine selectively kills hepatocellular carcinoma cells and preferentially inhibits their invasion via ROS-ER-MAPKs-CHOP |
| - | in-vitro, | HCC, | HepG2 | - | in-vitro, | HCC, | HUH7 | - | in-vivo, | NA, | NA |
| 1940- | PL, | Piperlongumine Inhibits Migration of Glioblastoma Cells via Activation of ROS-Dependent p38 and JNK Signaling Pathways |
| - | in-vitro, | GBM, | LN229 | - | in-vitro, | GBM, | U87MG |
| 1941- | PL, | Piperlongumine selectively kills cancer cells and increases cisplatin antitumor activity in head and neck cancer |
| - | in-vitro, | HNSCC, | NA |
| 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 |
| 1943- | PL, | Piperlongumine treatment inactivates peroxiredoxin 4, exacerbates endoplasmic reticulum stress, and preferentially kills high-grade glioma cells |
| - | in-vitro, | GBM, | NA | - | in-vivo, | NA, | NA |
| 1944- | PL, | Piperlongumine, a Novel TrxR1 Inhibitor, Induces Apoptosis in Hepatocellular Carcinoma Cells by ROS-Mediated ER Stress |
| - | in-vitro, | HCC, | HUH7 | - | in-vitro, | HCC, | HepG2 |
| 1945- | PL, | SANG, | The Synergistic Effect of Piperlongumine and Sanguinarine on the Non-Small Lung Cancer |
| - | in-vitro, | Lung, | A549 |
| 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, | NA |
| 1947- | PL, | Piperlongumine as a direct TrxR1 inhibitor with suppressive activity against gastric cancer |
| - | in-vitro, | GC, | SGC-7901 | - | in-vitro, | GC, | NA |
| 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, | NA |
| 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 |
| 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 |
| 992- | PL, | Piperlongumine based nanomedicine impairs glycolytic metabolism in triple negative breast cancer stem cells through modulation of GAPDH & FBP1 |
| - | in-vivo, | BC, | NA |
| 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 |
| 1953- | PL, | Designing piperlongumine-directed anticancer agents by an electrophilicity-based prooxidant strategy: A mechanistic investigation |
| - | in-vitro, | Lung, | A549 | - | in-vitro, | Nor, | WI38 |
| 2649- | PL, | Oxidative Stress Inducers in Cancer Therapy: Preclinical and Clinical Evidence |
| - | Review, | Var, | NA |
| 2940- | PL, | Piperlongumine Induces Reactive Oxygen Species (ROS)-dependent Downregulation of Specificity Protein Transcription Factors |
| - | in-vitro, | PC, | PANC1 | - | in-vitro, | Lung, | A549 | - | in-vitro, | Kidney, | 786-O | - | in-vitro, | BC, | SkBr3 |
| 2941- | PL, | Selective killing of cancer cells by a small molecule targeting the stress response to ROS |
| - | in-vivo, | BC, | MDA-MB-231 | - | in-vitro, | OS, | U2OS | - | in-vitro, | BC, | MDA-MB-453 |
| 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 |
| 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 |
| 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 | - | in-vitro, | Thyroid, | 8505C | - | in-vivo, | NA, | NA |
| 2945- | PL, | Piperlongumine induces ROS mediated cell death and synergizes paclitaxel in human intestinal cancer cells |
| - | in-vitro, | CRC, | HCT116 |
| 2946- | PL, | Piperlongumine, a potent anticancer phytotherapeutic: Perspectives on contemporary status and future possibilities as an anticancer agent |
| - | Review, | Var, | NA |
| 2947- | PL, | Piperlongumine: the amazing amide alkaloid from Piper in the treatment of breast cancer |
| - | Review, | Var, | NA |
| 2948- | PL, | The promising potential of piperlongumine as an emerging therapeutics for cancer |
| - | Review, | Var, | NA |
| 2949- | PL, | Piperlongumine selectively kills glioblastoma multiforme cells via reactive oxygen species accumulation dependent JNK and p38 activation |
| - | in-vitro, | GBM, | LN229 | - | in-vitro, | GBM, | U87MG |
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