| 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 |
| Source: HalifaxProj(inhibit) CGL-CS |
| Type: |
| Phosphatidylinositol 3-kinase (PtdIns3K or PI3K) is a family of enzymes that play a crucial role in cell signaling pathways, particularly in the regulation of cell growth, survival, and metabolism. The PI3K pathway is one of the most frequently altered pathways in human cancer.
Inhibition of the PI3K pathway has been explored as a therapeutic strategy for cancer treatment. Several PI3K inhibitors have been developed and are currently being tested in clinical trials. These inhibitors can target specific components of the pathway, such as PI3K, AKT, or mTOR. Class I phosphoinositide 3-kinase (PI3K) Class III PtdIns3K In contrast to the class III PtdIns3K as a positive regulator of autophagy, class I PI3K-AKT signaling has an opposing effect on the initiation of autophagy. PI3K inhibitors include: -Idelalisib , Copanlisib, Alpelisib -LY294002? -Wortmannin: potent PI3K inhibitor, has some associated toxicity. -Quercetin: -Curcumin -Resveratrol -Epigallocatechin Gallate (EGCG) |
| 2970- | PL, | Piperlongumine induces apoptosis and autophagy in leukemic cells through targeting the PI3K/Akt/mTOR and p38 signaling pathways |
| - | in-vitro, | AML, | NA |
Filter Conditions: Pro/AntiFlg:% IllCat:% CanType:% Cells:% prod#:134 Target#:252 State#:% Dir#:%
wNotes=on sortOrder:rid,rpid