| Features: |
| Artemisinin a compound in a Chinese herb that may inhibit tumor growth and metastasis
Artemisinin (antimalarial drugs) Artesunic acid (Artesunate) , Dihydroartemisinin (DHA), artesunate, arteether, and artemether, SM735, SM905, SM933, SM934, and SM1044 The induction of OS in tumor cells via the production of ROS is the key mechanism of ART against cancer. combination of ART and Nrf2 inhibitors to promote ferroptosis may have more efficient anticancer effects without damaging normal cells. Summary: - Pro-oxidant, mechanism related with iron (hence avoid supplements containing iron? Or perhaps take with iron?) -ROS seems to affect both cancer and normal cells - Delivery of artemisinin in conjugate form with transferrin or holotransferrin (serum iron transport proteins) have been shown to greatly improve its effectiveness. - Potential direct inhibitor of STAT3 - Artemisinin synergized with the glycolysis inhibitor 2DG (2-deoxy- D -glucose) ART Combined Therapy: Allicin, Resveratrol, Curcumin, VitC (but not orally at same time), Butyrate , 2-DG, Aminolevulinic AcidG -possible problems with liver toxicity?? -Artesunate (ART), an artemisinin compound, is known for lysosomal degradation of ferritin, inducing oxidative stress and promoting cancer cell death. Pathways: - Increasing reactive oxygen species (ROS) production. This oxidative stress can cause the loss of mitochondrial membrane potential, leading to cytochrome c release and subsequent activation of caspase cascades. - Downregulate HIF-1α - By impairing glycolysis, artemisinin might force cells to rely on oxidative phosphorylation (OXPHOS) for energy production. - Inhibit GLUT1 (glucose uptake), HK2, PKM2 (slow the glycolytic flux, thereby reducing the energy supply) -Artemisinin has a half-life of about 3-4 hours, Artesunate 40 minutes and Artemether 12 hours. Peak plasma levels occur in 1-2 hour. BioAv 21%, poor-good solubility. Artesunate (ART), a water soluble derivative of artemisinin. concentrations higher in blood, colon, liver, kidney (highly perfused organs) Pathways: - induce ROS production, iron dependent (affect both cancer and normal cells) - ROS↑ related: MMP↓(ΔΨm), ER Stress↑, UPR↑, GRP78↑, Ca+2↑, Cyt‑c↑, Caspases↑, DNA damage↑, cl-PARP↑, HSP↓, - Both Lowers (and raises) AntiOxidant defense in Cancer Cells: NRF2↓(contary), SOD↓, GSH↓ Catalase↓ GPx↓ - Small evidence of Raising AntiOxidant defense in Normal Cells: ROS↓(contary), NRF2↑, SOD↑(contary), GSH↑, Catalase↑, - lowers Inflammation : NF-kB↓, COX2↓, p38↓, Pro-Inflammatory Cytokines : NLRP3↓, TNF-α↓, IL-6↓, IL-8↓ - inhibit Growth/Metastases : TumMeta↓, TumCG↓, EMT↓, MMPs↓, MMP2↓, MMP9↓, TIMP2, IGF-1↓, uPA↓, VEGF↓, ROCK1↓, NF-κB↓, TGF-β↓, ERK↓ - cause Cell cycle arrest : TumCCA↑, cyclin D1↓, cyclin E↓, CDK2↓, CDK4↓, CDK6↓, - inhibits Migration/Invasion : TumCMig↓, TumCI↓, TNF-α↓, ERK↓, EMT↓, TOP1↓, - inhibits glycolysis /Warburg Effect and ATP depletion : HIF-1α↓, PKM2↓, cMyc↓, GLUT1↓, LDH↓, LDHA↓, HK2↓, ECAR↓, GRP78↑, GlucoseCon↓ - inhibits angiogenesis↓ : VEGF↓, HIF-1α↓, EGFR↓, Integrins↓, - some small indication of inhibiting Cancer Stem Cells : CSC↓, Hh↓, β-catenin↓, sox2↓, OCT4↓, - Others: PI3K↓, AKT↓, JAK↓, STAT↓, Wnt↓, β-catenin↓, AMPK, ERK↓, JNK, - Synergies: chemo-sensitization, RadioSensitizer, Others(review target notes), - Selectivity: Cancer Cells vs Normal Cells |
| Source: |
| Type: |
| A radiosensitizer is an agent that makes cancer cells more sensitive to the damaging effects of radiation therapy. By using a radiosensitizer, clinicians aim to enhance the effectiveness of radiation treatment by either increasing the damage incurred by tumor cells or by interfering with the cancer cells’ repair mechanisms. This can potentially allow for lower doses of radiation, reduced side effects, or improved treatment outcomes. Pathways that help Radiosensitivity: downregulating HIF-1α, increase SIRT1, Txr List of Natural Products with radiosensitizing properties: -Curcumin:modulate NF-κB, STAT3 and has been shown in preclinical studies to enhance the effects of radiation by inhibiting cell survival pathways. -Resveratrol: -EGCG: -Quercetin: -Genistein: -Parthenolide: How radiosensitizers inhibit the thioredoxin (Trx) system in cellular contexts. Notable radiosensitizers, including: -gold nanoparticles (GNPs), -gold triethylphosphine cyanide ([Au(SCN) (PEt3)]), -auranofin, ceria nanoparticles (CONPs), -curcumin and its derivatives, -piperlongamide, -indolequinone derivatives, -micheliolide, -motexafin gadolinium, and -ethane selenide selenidazole derivatives (SeDs) |
| 3396- | ART/DHA, | Progress on the study of the anticancer effects of artesunate |
| - | Review, | Var, | NA |
Filter Conditions: Pro/AntiFlg:% IllCat:% CanType:% Cells:% prod#:34 Target#:1107 State#:% Dir#:%
wNotes=on sortOrder:rid,rpid