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DRUG:

piceatannol

Associations
Trials
Company:
Kyushu University, New York Medical College
Drug class:
Apoptosis stimulant, SYK inhibitor, NF-κB inhibitor, MMP-9 inhibitor
Related drugs:
Associations
Trials
1year
An Open-label Study of the Safety and Pharmacokinetics of the TGKP (clinicaltrials.gov)
P1, N=25, Not yet recruiting, Gamaleya Research Institute of Epidemiology and Microbiology, Health Ministry of the Russian Federation
New P1 trial
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piceatannol
1year
Cytotoxic and Apoptotic Effects of Pinostilbene and Bortezomib Combination Treatment on Human Multiple Myeloma Cells. (PubMed, Int J Mol Sci)
BTZ as well as RES and its derivatives pinostilbene (PIN) and piceatannol (PIC) decreased MM cell viability in a dose- and time-dependent manner and increased expression of cleaved proapoptotic proteins poly(ADP-ribose) polymerase 1 (PARP1) and caspase-3 in a dose-dependent manner. Expression of oxidative stress defense proteins (catalase, thioredoxin, and superoxide dismutase) in RPMI 8226 cells were reduced after 24 h treatment, and cytotoxic effects of the treatment were ameliorated by antioxidant N-acetylcysteine (NAC), suggesting the treatment impacts antioxidant levels in RPMI 8226 cells. Our results suggest that this combination of BTZ and PIN decreases MM cell viability synergistically by inducing apoptosis and oxidative stress in MM cells.
Journal • PARP Biomarker
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CASP3 (Caspase 3) • CAT (Catalase)
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PARP1 expression
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bortezomib • piceatannol
over1year
The Mechanisms of Piceatannol in Inhibiting the Malignant Biological Characteristics of Acute Myeloid Leukemia Cells (PubMed, Zhongguo Shi Yan Xue Ye Xue Za Zhi)
Piceatannol can inhibit the proliferation of AML cells and induce programmed death, which may be related to the inhibition of Akt/NF-κB signaling pathway, the hydrolysis of caspase-3 and the down-regulation of Bcl-2 protein expression, and the suppression of the expression of some drug resistance genes.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • CASP3 (Caspase 3) • ANXA5 (Annexin A5)
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BCL2 expression
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piceatannol
over1year
The Antiproliferative Activity of Adiantum pedatum Extract and/or Piceatannol in Phenylhydrazine-Induced Colon Cancer in Male Albino Rats: The miR-145 Expression of the PI-3K/Akt/p53 and Oct4/Sox2/Nanog Pathways. (PubMed, Molecules)
However, the administration of AP or P or AP + P as therapy or prophylaxis significantly ameliorated these changes and upregulated the colonic mir-145 and mRNA expression of P53 and PDCD-4 while downregulating the colonic mRNA expression of PI3K, AKT, c-Myc, CK-20, SOX-2, OCT-4, and NanoG compared to the PHZ group. These findings suggest that the candidate drugs may exert their anti-cancer effects through multiple mechanisms, including antioxidant and apoptotic activities.
Preclinical • Journal
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TP53 (Tumor protein P53) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • SOX2 • POU5F1 (POU Class 5 Homeobox 1) • NANOG (Nanog Homeobox) • MIR145 (MicroRNA 145) • PI3K (Phosphoinositide 3-kinases)
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MYC expression • TP53 expression • POU5F1 expression
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piceatannol
over1year
The cancer preventive activity and mechanisms of prenylated resveratrol and derivatives. (PubMed, Curr Res Toxicol)
The expression of Caspase-3 and Caspase-9 were upregulated by 4-C-prenyl piceatannol and the expression of CDK2 and Cyclin A2 in HepG cells were downregulated, which contributed to apoptosis. The above results eludicated the possible antiproliferative mechanisms of prenylated stilbenoids.
Journal
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CASP3 (Caspase 3) • CCNA2 (Cyclin A2) • CDK2 (Cyclin-dependent kinase 2) • CASP9 (Caspase 9)
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CDK2 expression
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piceatannol
over1year
Piceatannol Protects PC-12 Cells against Oxidative Damage and Mitochondrial Dysfunction by Inhibiting Autophagy via SIRT3 Pathway. (PubMed, Nutrients)
In addition, the autophagy activator (rapamycin) abrogated the protective effects of piceatannol on PC-12 cell death. These findings demonstrated that piceatannol could alleviate PC-12 cell oxidative damage and mitochondrial dysfunction by inhibiting autophagy via the SIRT3 pathway.
Journal
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SIRT3 (Sirtuin 3) • ATG5 (Autophagy Related 5) • TFAM (Transcription Factor A, Mitochondrial)
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ATG5 expression
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sirolimus • piceatannol
over1year
Protective Effects of Piceatannol on DNA Damage in Benzo[a]pyrene-Induced Human Colon Epithelial Cells. (PubMed, J Agric Food Chem)
The upregulation of phase II detoxification enzymes, such as nicotinamide adenine dinucleotide phosphate (NADPH) and quinone oxidoreductase 1 (NQO1), and the antioxidative enzyme, heme oxygenase 1 (HO-1), via the activation of the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway was observed in the PIC-treated group. Our results suggest that PIC is a potential CRC-blocking agent due to its ability to alleviate DNA damage, decrease intracellular ROS production, modulate the metabolism and detoxification of B[a]P, and activate the Nrf2 signaling pathway in B[a]P-induced NCM460 cells.
Journal
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CHEK1 (Checkpoint kinase 1) • HMOX1 (Heme Oxygenase 1) • NQO1 (NAD(P)H dehydrogenase, quinone 1) • MIR27B (MicroRNA 27b) • CYP1B1 (Cytochrome P450 Family 1 Subfamily B Member 1)
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piceatannol
almost2years
Inhibition of Colorectal Cancer Cell Proliferation by Treatment with Itadori Leaf Extract. (PubMed, J Oleo Sci)
Itadori extracts are rich in neochlorogenic acid and rutin and also contain quercetin and piceatannol. These polyphenols are thought to be involved in the observed DNA fragmentation and caspase 3/7 activation in colon cancer cells and may thus have anticancer effects. There is hence scope for development of the leaf of itadori, which currently has only a few known uses, as a novel anti-tumor therapeutic.
Journal
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CASP3 (Caspase 3) • CASP7 (Caspase 7)
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piceatannol
almost2years
Main Determinants Affecting the Antiproliferative Activity of Stilbenes and Their Gut Microbiota Metabolites in Colon Cancer Cells: A Structure-Activity Relationship Study. (PubMed, Int J Mol Sci)
The antiproliferative IC values of pterostilbene, oxy-resveratrol, piceatannol, resveratrol, dihydroresveratrol, lunularin, 3,4'-dihydroxy-trans-stilbene, pinosylvin, dihydropinosylvin, 4-hydroxy-trans-stilbene, 4-hydroxydibenzyl, 3-hydroxydibenzyl, and 4-trans-stilbenemethanol were calculated...These results (i) suggest that gut microbiota metabolism determines the antiproliferative effects of dietary stilbenes. Therefore, RSV consumption might exert different effects in individuals depending on their gut microbiota metabotypes associated with RSV metabolism, and (ii) could help design customized drugs with a stilbenoid and (or) dibenzyl core against colorectal cancer.
Journal
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ITGB2 (Integrin Subunit Beta 2)
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piceatannol
almost2years
Attenuation of N-Nitrosodiethylamine -Induced Hepatocellular Carcinoma by Piceatannol and/or Cisplatin: The Interplay between Nuclear Factor (Erythroid Derived 2)-like 2 and Redox Status. (PubMed, Asian Pac J Cancer Prev)
PIC in combination with cisplatin has been shown to have a synergistic anticancer impact through modulating Nrf2 and redox state. In addition, adding PIC to an HCC therapy plan that includes chemotherapeutic medicines may boost the efficacy of cisplatin while reducing its negative effects.
Journal
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TNFA (Tumor Necrosis Factor-Alpha) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2) • NFKB1 (Nuclear factor of kappa light polypeptide gene enhancer in B-cells 1) • CASP3 (Caspase 3) • NQO1 (NAD(P)H dehydrogenase, quinone 1)
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cisplatin • piceatannol
2years
Piceatannol enhances Beclin-1 activity to suppress tumor progression and its combination therapy strategy with everolimus in gastric cancer. (PubMed, Sci China Life Sci)
Xenograft models confirmed that piceatannol inhibits tumor development and elicits a potent synergistic effect with everolimus in vivo. Taken together, the findings of this study strongly support the application of combinatorial piceatannol and everolimus therapy in future clinical trials for gastric cancer patients.
Journal • Combination therapy • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • BECN1 (Beclin 1)
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everolimus • piceatannol
2years
Piceatannol induces apoptotic cell death through activation of caspase-dependent pathway and upregulation of ROS-mediated mitochondrial dysfunction in pancreatic cancer cells. (PubMed, Mol Biol Rep)
Our results show that piceatannol has an anti-cancerogenic effect on PANC-1 and MIA PaCa-2 cells, and exerts this effect by suppressing proliferation and inducing apoptosis. Therefore, piceatannol could be considered to be a potential chemotherapeutic agent candidate for the treatment and prevention of PC.
Journal
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CASP3 (Caspase 3) • CASP9 (Caspase 9) • ANXA5 (Annexin A5)
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piceatannol
over2years
Piceatannol prevents colon cancer progression via dual-targeting to M2-polarized tumor-associated macrophages and the TGF-β1 positive feedback signaling pathway. (PubMed, Mol Nutr Food Res)
These novel findings demonstrate that PIC is a potent TGF-β1/TGF-βR1 pathway inhibitor and TME modulator for preventing tumor progression and metastasis in CRC by reeducating TAMs.
Journal
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TGFB1 (Transforming Growth Factor Beta 1)
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piceatannol
over2years
Piceatannol, a Dietary Polyphenol, Alleviates Adipose Tissue Loss in Pre-Clinical Model of Cancer-Associated Cachexia via Lipolysis Inhibition. (PubMed, Nutrients)
Moreover, piceatannol protected tumor-bearing mice against weight-loss in early stages of CAC largely through preserving adipose tissue, with no effect on survival. This study demonstrates the use of a dietary compound to preserve adipose in models of early stage CAC and provides groundwork for further investigation of piceatannol or piceatannol-rich foods as alternative medicine in the preservation of body fat mass and future CAC therapy.
Preclinical • Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha)
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piceatannol
over2years
Piceatannol SNEDDS Attenuates Estradiol-Induced Endometrial Hyperplasia in Rats by Modulation of NF-κB and Nrf2/HO-1 Axes. (PubMed, Nutrients)
This anti-inflammatory effect was further confirmed by a significant increase in Nrf2 and heme oxygenase-1 (HO-1) expression. These results indicate that SNEDDS nanoformulation of PIC possesses protective effects against experimentally induced EH.
Preclinical • Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • HMOX1 (Heme Oxygenase 1) • NFKB1 (Nuclear factor of kappa light polypeptide gene enhancer in B-cells 1)
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HMOX1 expression
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piceatannol
over2years
Passion fruit seed extract protects beta-amyloid-induced neuronal cell death in a differentiated human neuroblastoma SH-SY5Y cell model. (PubMed, Food Sci Nutr)
Our study is the first to report that piceatannol-rich PFSE can repress Aβ-induced neuronal cell death by protecting against neurite fragmentation in the AD human cell model. These findings suggest that piceatannol-rich PFSE can be considered a potentially neuroprotective functional food for both prevention and treatment of AD.
Journal
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BDNF (Brain Derived Neurotrophic Factor)
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piceatannol
over2years
Synergistic Effects of Resveratrol Derivatives with Bortezomib on Reducing Viability and Inducing Apoptosis in Multiple Myeloma Cells. (PubMed, FASEB J)
We found that BTZ as well as RES and its derivatives pinostilbene (PIN) and piceatannol (PIC) decreased MM cell viability in a dose- and time-dependent manner and increased expression of cleaved proapoptotic proteins PARP1 and caspase-3 in a dose-dependent manner. We screened different combinations of RES derivatives with BTZ for synergistic effects on MM viability using CompuSyn and selected the combination of 5 nM BTZ and 5 μM PIN for further assessment as a synergistic treatment. In conclusion, a combination of low doses of BTZ and PIN synergistically decreases MM cell viability, possibly through inducing apoptosis.
Journal • PARP Biomarker
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CASP3 (Caspase 3)
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bortezomib • piceatannol
3years
Piceatannol, a Structural Analog of Resveratrol, Is an Apoptosis Inducer and a Multidrug Resistance Modulator in HL-60 Human Acute Myeloid Leukemia Cells. (PubMed, Int J Mol Sci)
Our findings also imply that HL-60 cells are able to acquire resistance to piceatannol toxicity via mechanisms related to MRP1 activity. Our results suggest that the use of piceatannol as a potential chemotherapeutic agent may be associated with the risk of multidrug resistance, warranting its use in combination with other chemotherapeutic agents.
Journal
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CASP3 (Caspase 3)
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piceatannol
3years
Long-Term Oral Administration of Piceatannol (3,5,3',4'-Tetrahydroxystilbene) Attenuates Colon Tumor Growth Induced by Azoxymethane Plus Dextran Sulfate Sodium in C57BL/6J Mice. (PubMed, Nutr Cancer)
In mice administered piceatannol (12.5 mg/kg), the tumor number, tumor area, and Ki-67-positive cell numbers decreased by 30.1%, 57.2%, and 89.1%, respectively, colon MCP-1 and PD-1 levels showed reductions of 43.8% and 70.9%, respectively, and COX-2-positive cell numbers declined by 60.2%. The inhibitory effects of piceatannol on AOM/DSS-induced colon tumor growth appear to be associated with reductions in colon MCP-1 and PD-1 levels through the downregulated expression of COX-2 in the tumor microenvironment.
Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker
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PD-1 (Programmed cell death 1) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • PTGS2 (Prostaglandin-Endoperoxide Synthase 2) • IL1B (Interleukin 1, beta)
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PTGS2 expression
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piceatannol
3years
Comparison of the Effects of Resveratrol and Its Derivatives on the Radiation Response of MCF-7 Breast Cancer Cells. (PubMed, Int J Mol Sci)
The aim of this study was to investigate whether the stilbene derivatives piceid, resveratrol, and piceatannol have a radiosensitising effect on breast cancer cells (MCF-7)...This was due to a significant decrease in the activity of antioxidant enzymes, which resulted in the accumulation of formed reactive oxygen species (ROS). The effect of resveratrol and IR enhanced the expression of apoptotic genes, such as Bax, p53, and caspase 8, leading to apoptosis.
Journal
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BAX (BCL2-associated X protein) • CASP8 (Caspase 8)
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TP53 expression • BAX expression
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piceatannol
over3years
Effect of piceatannol against malignant melanoma in vivo and in vitro. (PubMed, Hua Xi Kou Qiang Yi Xue Za Zhi)
PIC might block the progression of malignant melanoma by inhibiting spleen tyrosine kinase.
Preclinical • Journal
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MMP2 (Matrix metallopeptidase 2) • SYK (Spleen tyrosine kinase) • MMP9 (Matrix metallopeptidase 9)
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piceatannol
over3years
Systemic antioxidant and anti-inflammatory effects of yellow passion fruit bagasse extract during prostate cancer progression. (PubMed, J Food Biochem)
Piceatannol, scirpusin-B, dicaffeoylquinic acid, citric acid, and (+)-catechin were identified in PFBE, and the extract showed high in vitro antioxidant capacity...However, in vivo studies are scarce. Our results provided information about in vivo impacts of PFBE oral consumption on antioxidant defense and inflammation, indicating its potential as an adjuvant during the initial steps of prostate cancer.
Journal
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TNFA (Tumor Necrosis Factor-Alpha) • NFKB1 (Nuclear factor of kappa light polypeptide gene enhancer in B-cells 1) • CAT (Catalase)
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piceatannol
over3years
Piceatannol-Loaded Bilosome-Stabilized Zein Protein Exhibits Enhanced Cytostatic and Apoptotic Activities in Lung Cancer Cells. (PubMed, Pharmaceutics)
In addition, the wound healing experiment confirmed the results. To conclude, compared to pure PIC, PIC-BZ demonstrated a higher cell death-inducing activity against A549 cells.
Journal
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CASP3 (Caspase 3)
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piceatannol
over3years
Real-Time Analysis of Polyphenol-Protein Interactions by Surface Plasmon Resonance Using Surface-Bound Polyphenols. (PubMed, Chemistry)
A selection of bioactive polyphenols of different structural classes, such as the ellagitannins vescalagin and vescalin, the flavanoids catechin, epicatechin, epigallocatechin gallate (EGCG), and procyanidin B2, and the stilbenoids resveratrol and piceatannol, were chemically modified to bear a biotin unit for enabling their immobilization on streptavidin-coated sensor chips. The types and levels of SPR responses unveiled major differences in the association, or lack thereof, and dissociation between a given protein analyte and different polyphenolic ligands. Thus, this multi-analysis SPR technique constitutes a valuable methodology to rapidly screen and qualitatively compare various polyphenol-protein interactions.
Journal
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BCL2 (B-cell CLL/lymphoma 2)
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piceatannol
over3years
Augmentation of anti-proliferative, pro-apoptotic and oxidant profiles induced by piceatannol in human breast carcinoma MCF-7 cells using zein nanostructures. (PubMed, Biomed Pharmacother)
Conclusively, ZN nanostructures of PCT revealed superior cell death-inducing activities against MCF-7 cells in comparison with free PCT. This is mediated, at least partly, by enhanced cellular uptake, pro-apoptotic activity, and oxidative stress potential.
Journal • IO biomarker
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TP53 (Tumor protein P53) • BCL2 (B-cell CLL/lymphoma 2) • CASP3 (Caspase 3)
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BCL2 expression • TP53 expression • BAX expression
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piceatannol
4years
Piceatannol attenuates fat accumulation and oxidative stress in steatosis-induced HepG2 cells. (PubMed, Curr Res Food Sci)
Moreover, piceatannol significantly suppressed FA-induced oxidative stress and inhibited phosphorylation of c-Jun N-terminal kinase (JNK) and extracellular signal-regulated kinases 1/2 (ERK1/2). Overall, it is suggested that piceatannol reduced fat accumulation in steatosis-induced HepG2 cells by suppressing lipogenesis (SREBP1 and ACC) and FA uptake (CD36), and promoting FAs oxidation (FXR, PPARα and CPT1α).
Journal
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CD36 (thrombospondin receptor)
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piceatannol
4years
Piceatannol suppresses proliferation and induces apoptosis by regulation of the microRNA‑21/phosphatase and tensin homolog/protein kinase B signaling pathway in osteosarcoma cells. (PubMed, Mol Med Rep)
In addition, we further verified that phosphatase and tensin homolog (PTEN), a tumor suppressor gene, is the functional target of miR‑21 and Pice blocks the PTEN/AKT signaling pathway through inhibiting miR‑21 expression in OS cells. Our findings suggested that Pice may exert anticancer effects on OS cells via mediating the miR‑21/PTEN/AKT signaling pathway and could be considered to be a potential anticancer agent for treating OS.
Journal
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PTEN (Phosphatase and tensin homolog) • MIR21 (MicroRNA 21)
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piceatannol
4years
Piceatannol, a Natural Analog of Resveratrol, Exerts Anti-angiogenic Efficiencies by Blockage of Vascular Endothelial Growth Factor Binding to Its Receptor. (PubMed, Molecules)
Thus, these lines of evidence supported the conclusion that piceatannol could down regulate the VEGF-mediated angiogenic functions with no cytotoxicity via decreasing the amount of VEGF binding to its receptors, thus affecting the related downstream signaling. Piceatannol may be developed into therapeutic agents or health products to reduce the high incidence of angiogenesis-related diseases.
Journal
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NOS3 (Nitric oxide synthase 3)
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piceatannol