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DRUG:

oleandrin (PBI-05204)

i
Other names: PBI 05204, PBI-05204
Associations
Trials
Company:
Phoenix Biotech
Drug class:
AKT inhibitor, FGFR2 inhibitor, NF-κB inhibitor, p70S6K inhibitor
Related drugs:
Associations
Trials
1m
Digoxin and its Na+/K+-ATPase-targeted actions on cardiovascular diseases and cancer. (PubMed, Bioorg Med Chem)
Presented herein are also the antitumor potential of monosaccharide cardiac glycoside analogues of digoxin, including (-)-cryptanoside A, (-)-oleandrin, (-)-ouabain, and (+)-strebloside. It is hoped that this contribution will provide some helpful information for the design and discovery of new cardiac glycoside-type therapeutic agents for the treatment of cardiovascular diseases and cancer.
Review • Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit)
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oleandrin (PBI-05204)
1m
Botanical oleander extract and oleandrin have superior effects on innate immune functions pertaining to dermal allergic reactions in canine cells when compared to oclacitinib. (PubMed, Am J Vet Res)
These results suggest that OE and oleandrin are efficacious agents to treat canine atopic dermatitis. Future studies should evaluate the efficacy of these compounds in dogs affected by atopic dermatitis.
Journal
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IFNG (Interferon, gamma) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • CCL2 (Chemokine (C-C motif) ligand 2) • TGFB1 (Transforming Growth Factor Beta 1)
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oleandrin (PBI-05204)
2ms
Targeting stress induction of GRP78 by cardiac glycoside oleandrin dually suppresses cancer and COVID-19. (PubMed, Cell Biosci)
Our findings validate GRP78 as a target of OLN anti-cancer and anti-viral activities. These proof-of-principle studies support further investigation of OLN as a readily accessible compound to dually combat cancer and COVID-19.
Journal
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HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5)
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HSPA5 overexpression
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oleandrin (PBI-05204)
3ms
Oleandrin enhances radiotherapy sensitivity in lung cancer by inhibiting the ATM/ATR-mediated DNA damage response. (PubMed, Phytother Res)
The combined treatment of Oleandrin and radiotherapy demonstrated superior inhibition of tumor proliferation compared to either treatment alone. Our findings highlight Oleandrin as a novel and effective inhibitor of ATM and ATR kinase, offering new possibilities for the development of clinical radiosensitizing adjuvants.
Journal
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CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1)
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oleandrin (PBI-05204)
4ms
Evaluation of the Activity of Cardiac Glycosides on RORγ and RORγT Nuclear Receptors. (PubMed, Arch Biochem Biophys)
Subsequently, the effects of two endogenous cardiac glycosides (marinobufagenin and ouabain) and the three most potent glycosides (bufalin, oleandrin, and telecinobufagenin) were evaluated in Th17 primary lymphocytes...Thus, we demonstrated that at nontoxic concentrations, cardiac glycosides have agonistic effects on RORγ/RORγT nuclear receptors, augmenting their activity. This potential can be harnessed to modulate the phenotype of IL17-expressing cells (e.g., Th17 or Tc17 lymphocytes) in adoptive therapy for combating various types of cancer.
Journal
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IFNG (Interferon, gamma) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • CCL20 (C-C Motif Chemokine Ligand 20) • GZMB (Granzyme B) • IL17A (Interleukin 17A)
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oleandrin (PBI-05204)
6ms
PBI-05204, a supercritical CO2 extract of Nerium oleander, suppresses glioblastoma stem cells by inhibiting GRP78 and inducing programmed necroptotic cell death. (PubMed, Neoplasia)
Furthermore, oleandrin, a principle active cardiac glycoside component of PBI-05204, showed the ability to inhibit the self-renewal capacity in GSCs. These findings highlight the potential of PBI-05204 as a promising candidate for the development of novel therapies that target GBM stem cells.
Journal
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CD44 (CD44 Molecule) • HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5) • NANOG (Nanog Homeobox) • RIPK1 (Receptor Interacting Serine/Threonine Kinase 1)
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oleandrin (PBI-05204)
over1year
Molecular Modes of Action of an Aqueous Nerium oleander Extract in Cancer Cells In Vitro and In Vivo. (PubMed, Molecules)
The phytochemical characterization by nuclear magnetic resonance spectroscopy (NMR) and low- and high-resolution mass spectrometry revealed several monoglycosidic cardenolides as major constituents (adynerin, neritaloside, odoroside A, odoroside H, oleandrin, and vanderoside). Breastin moderately inhibited breast cancer xenograft tumors in vivo. Remarkably, in contrast to what was observed with paclitaxel monotherapy, the combination of paclitaxel and Breastin prevented tumor relapse, indicating Breastin's potential for drug combination regimens.
Preclinical • Journal
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EGFR (Epidermal growth factor receptor) • TP53 (Tumor protein P53) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • WT1 (WT1 Transcription Factor) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • ABCC1 (ATP Binding Cassette Subfamily C Member 1) • GSTP1 (Glutathione S-transferase pi 1) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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paclitaxel • oleandrin (PBI-05204)
almost2years
The botanical drug PBI-05204, a supercritical CO extract of Nerium oleander, sensitizes alveolar and embryonal rhabdomyosarcoma to radiotherapy in vitro and in vivo. (PubMed, Front Pharmacol)
Notably, both in vitro and in vivo evidence confirmed the higher sensitivity to PBI-05204 of FP-RMS. Thus, PBI-05204 represents a valid radio-sensitizing agent for the treatment of RMS, including the intrinsically radio-resistant FP-RMS.
Preclinical • Journal
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PAX3 (Paired Box 3) • PAX7 (Paired Box 7)
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oleandrin (PBI-05204)
2years
Glycoside oleandrin downregulates toll-like receptor pathway genes and associated miRNAs in human melanoma cells. (PubMed, Gene)
In conclusion, it has been observed that oleandrin has an effect on TLR pathway-related genes and miRNAs in melanoma cells. We show that TLRs pathways and hsa-miR-146a-5p and hsa-miR-21-5p can participate in the oleandrin molecular mechanism of action.
Journal • IO biomarker
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MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • IFNG (Interferon, gamma) • MIR21 (MicroRNA 21) • TLR4 (Toll Like Receptor 4) • TLR7 (Toll Like Receptor 7) • IRAK4 (Interleukin 1 Receptor Associated Kinase 4) • TLR2 (Toll Like Receptor 2)
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oleandrin (PBI-05204)
over2years
The botanical drug PBI-05204, a supercritical CO₂ extract of Nerium oleander, augments the antitumor efficacy of radiotherapy in treatment of human glioblastoma (AACR 2022)
Collectively, these results reveal that PBI-05204 enhances antitumor activity of RT in preclinical/murine models of human GBM. Given the fact that PBI-05204 has already been examined in Phase I and II clinical trials for cancer patients, its efficacy when combined with standard-of-care radiotherapy regimens in GBM should be explored in future clinical trials of this difficult to treat brain cancer.
Clinical
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RAD51 (RAD51 Homolog A) • CASP3 (Caspase 3) • CASP9 (Caspase 9)
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oleandrin (PBI-05204)
over3years
Oleandrin, a cardiac glycoside, induces immunogenic cell death via the PERK/elF2α/ATF4/CHOP pathway in breast cancer. (PubMed, Cell Death Dis)
Taken together, our findings showed that oleandrin triggered ER stress and induced ICD-mediated immune destruction of breast cancer cells. Oleandrin combined with immune checkpoint inhibitors might improve the efficacy of immunotherapy.
Journal • IO biomarker
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CD8 (cluster of differentiation 8) • HMGB1 (High Mobility Group Box 1) • CALR (Calreticulin) • ATF4 (Activating Transcription Factor 4)
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oleandrin (PBI-05204)
4years
Anvirzelregulates cell death through inhibiting GSK-3 activity in human U87 glioma cells. (PubMed, Neurol Res)
Herein, we aimed to study the potential signaling pathways taken role in differential cell-death properties of Anvirzel which is consisted of two toxic cardiac glycosides (oleandrin and oleandrigenin), in U87 human glioblastoma cells. The anti-proliferative and anti-migratory effects of Anvirzel were assessed in U87 cells by WST-1 assay and wound healing assay, respectively...In addition, it was found that Anvirzel™ inhibited GSK-3, NOS and HIF1-α expressions whereas activated ERK in U87 cells compared to vehicle (p < 0.05). The results suggested that Anvirzel regulated cell death distinctly from apoptosis in human glioblastoma cells. Further studies are required for validation of mechanistic insights about the potential signaling pathways taken role in differential cell death properties of Anvirzel.
Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit)
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HIF1A expression
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oleandrin (PBI-05204)
4years
Oleandrin induces apoptosis via activating endoplasmic reticulum stress in breast cancer cells. (PubMed, Biomed Pharmacother)
Taken together, our results suggest that oleandrin induces mitochondrial-mediated apoptosis by activating endoplasmic reticulum stress in breast cancer. Moreover, oleandrin may be an effective strategy for the treatment of breast cancer.
Journal
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BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein)
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BAX expression
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oleandrin (PBI-05204)
4years
The Botanical Drug PBI-05204, a Supercritical CO Extract of Nerium Oleander, Inhibits Growth of Human Glioblastoma, Reduces Akt/mTOR Activities, and Modulates GSC Cell-Renewal Properties. (PubMed, Front Pharmacol)
Both in vitro cell culture and immunohistochemical studies of tumor tissue suggest drug induction of tumor cell apoptosis and inhibition of PI3k/mTOR pathways as well as cancer stemness. Given the fact that PBI-05204 has already been examined in phase I and II clinical trials for cancer patients, its efficacy when combined with standard of care chemotherapy and radiotherapy should be explored in future clinical trials of this difficult to treat brain cancer.
Journal
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CXCR4 (Chemokine (C-X-C motif) receptor 4) • CD44 (CD44 Molecule) • SOX2 • CD31 (Platelet and endothelial cell adhesion molecule 1)
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CD31 expression
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oleandrin (PBI-05204)
almost5years
The effect of 5α-oleandrin on keloid fibroblast activities. (PubMed, BMC Proc)
Antifibrotic activities of 5α-oleandrin in cellular proliferation and collagen deposition were better than mitomycin-C. The 5α-oleandrin has good antifibrotic effect in keloid fibroblast activities.
Journal
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CTNNB1 (Catenin (cadherin-associated protein), beta 1)
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oleandrin (PBI-05204)