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Article Index


OLEOCANTHAL

 

1 . Alzheimer’s-associated Aβ oligomers show altered structure, immunoreactivity and synaptotoxicity with low doses of oleocanthal

This study of Pitt et al. has focused on oleocanthal (OC), as a compound capable of altering the assembly state of soluble oligomers of amyloid-β1-42 peptide (ADDL), which peptide is a neurotoxin that causes Alzheimer’s disease (AD). OC increased the immunoreactivity of soluble Aβ species, indicating changes in oligomer structure. Analysis of oligomers in the presence of OC showed an upward shift in molecular weight and a ladder-like distribution of SDS-stable ADDL subspecies. In comparison with control ADDLs, oligomers formed in the presence of OC (Aβ-OC) showed equivalent co-localization at synapses but exhibited greater immunofluorescence as a result of increased antibody recognition. The enhanced signal at synapses was not due to increased synaptic binding, as direct detection of fluorescently-labeled ADDLs showed an overall reduction in ADDL signal in the presence of OC. Decreased binding to synapses was accompanied by significantly less synaptic deterioration assayed by drebrin loss. Additionally, treatment with OC improved antibody clearance of ADDLs. These results indicate oleocanthal is capable of altering the oligomerization state of ADDLs while protecting neurons from the synaptopathological effects of ADDLs and suggest OC as a lead compound for development in AD therapeutics.

 

SUMMURY

Low dosages of oleocanthal prove to be protective against Alzheimer's disease
This study of Pitt et al indicates that oleocanthal is a substance capable of altering the assembly state of soluble oligomers of amyloid-β1-42 peptide (ADDL), which peptide is a neurotoxin that causes Alzheimer’s disease (AD). The results show that Oleocanthal protects the neurons from the negative effects of Alzheimer's disease even at low doses and as a result in the future it could be used in a potential therapy.

Oleocanthal protects the neurons from the negative effects of Alzheimer's disease even at low doses and as a result in the future it could be used in a potential therapy.

 

1.jpg

Figure. Specific binding of Aβ-OC to synapses shows greatly enhanced immunoreactivity compared to ADDLs PSD-95 (magenta) was used as a synaptic marker to determine if the pattern of binding was similar between ADDLs or Aβ-OC (both in green). Pitt J et al., Toxicol Appl Pharmacol. 2009

 

2. Olive-Oil-Derived Oleocanthal Enhances β-Amyloid Clearance as a Potential Neuroprotective Mechanism against Alzheimer’s Disease:In Vitro and in Vivo Studies

The mechanism by which oleocanthal exerts its neuroprotective effect is still incompletely understood. Abuznait et al. with this study provide in vitro and in vivo evidence for the potential of oleocanthal to enhance Aβ clearance from the brain via up-regulation of P-glycoprotein (P-gp) and LDL lipoprotein receptor related protein-1 (LRP1), major Aβ transport proteins, at the blood-brain barrier (BBB). Results from in vitro and in vivo studies demonstrated similar and consistent pattern of oleocanthal in controlling Aβ levels. In cultured mice brain endothelial cells, oleocanthal treatment increased and LRP1 protein expression and activity. Studies showed that administration of oleocanthal to C57BL/6 wild-type mice resulted in Αβ clearance from the brain and increased the brain efflux index from 62.0 % for control mice to 79.9% for oleocanthal treated mice. Increased P-gp and LRP1 protein expression in the brain microvessels and inhibition studies confirmed the role of up-regulation of these proteins in enhancing Aβ clearance after oleocanthal treatment, which leads to Αβ degradation. In conclusion, these findings provide experimental support that potential reduced risk of AD associated with extra-virgin olive oil could be mediated by enhancement of Aβ clearance from the brain.

 

SUMMURY

Oleocanthal promotes the removal of toxic proteins, called β-Amyloid related to Alzheimer’s disease

In this study, Abuznait and his colleagues study the ability of oleocanthal to promote the removal of toxic proteins, called β-amyloids, related to Alzheimer’s disease, from the brain. Administrating oleocanthal to mouse brain cells led to the increase of proteins that transport substances from and to the brain. The results showed that the increase of these protein levels led to Αβ clearance and brain function enhancement. In conclusion, these findings provide experimental support that potential reduced risk of AD associated with extra-virgin olive oil could be mediated by enhancement of Aβ clearance from the brain.

In cultured micebrain endothelial cells,oleocanthal treatment helpsto purify them from the toxic proteins that causeAlzheimer's disease

 

3. Modulation of tau protein fibrillization by oleocanthal

Oleocanthal is capable of altering the fibrillization of tau protein, which is one of the key factors at the basis of neurodegenerative diseases, and of covalently reacting with lysine amino groups of the tau fragment K18 in an unspecific fashion. In the present study, Monti et al. investigated the recognition process and the reaction profile between oleocanthal and the wild-type tau protein. As a result, oleocanthal has been found to interact with tau441, inducing stable conformational modifications of the protein secondary structure and also interfering with tau aggregation. These findings provide experimental support for the potential reduced risk of AD and related neurodegenerative diseases associated with olive oil consumption and may offer a new chemical scaffold for the development of AD modulating agents.

Monti et al., J. Nat. Prod. 2012

 

SUMMURY

Oleocanthal modulates a selective protein associated with Alzheimer’s disease

Oleocanthal reacts with tau protein, a brain protein related to Alzheimer’s disease. Specifically oleocanthal causes structure alterations, blocking the formation of fibers, which is an important factor in the beginning of neurodegenerative diseases, such as Alzheimer’s.

Οleocanthal modifies a specific protein in the brain associated with the development of Alzheimer's disease

 

4. Inhibition of tau fibrillization by oleocanthal via reaction with the amino groupsof tau

In Alzheimer's disease and related tauopathies, tau fibrillizes and aggregates into neurofibrillary tangles. Unpublished data of Li et al. indicate an inhibitory effect of oleocanthal on Aβ fibrillization, so I was reasoned that oleocanthal might inhibit tau fibrillization as well. Herein it is demonstrated that oleocanthal abrogates fibrillization of tau by locking tau into the naturally unfolded state. Using PHF6 peptide consisting of the amino acid residues VQIVYK, a hexapeptide within the third repeat of tau that is essential for fibrillization, it was shown that oleocanthal forms an adduct with the lysine via initial Schiff base formation. Structure and function studies demonstrate that the two aldehyde groups of oleocanthal are required for the inhibitory activity. These two aldehyde groups show certain specificity when titrated with free lysine and oleocanthal does not significantly affect the normal function of tau. These findings provide a potential scheme for the development of novel therapies for neurodegenerative tauopathies.

2

Figure: Human tau constructs, structure of oleocanthal and Schiff base reaction between oleocanthal and lysine side chain. Li et al., J. Neurochem. 2009

 

SUMMURY

Oleocanthal:a potential future treatment of Alzheimer's disease

Protein Tau alteration is one of the factors causing Alzheimer's disease. This particular study showed that oleocanthal can prevent this alteration, maintaining the original form of the protein. Further studies have shown that oleocanthal, due to its structure, leads to this obstruction without affecting the physiological function of Tau protein. These findings lead to a possible development of new treatments for diseases such as Alzheimer's.

Oleocanthal is a potential future treatment of Alzheimer's disease as it prevents the alteration of a specificprotein associatedwith the developmentof the disease.

 

5. Oleocanthal EnhancesAmyloid-β Clearance from the Brains of TgSwDI Mice and in Vitro acrossa Human Blood-Brain Barrier Model

In the current study, Hisham et al. investigated the effect of oleocanthal on pathological hallmarks of Alzheimer’s disease in TgSwDI, an animal model of AD. Mice treatment for 4 weeks with oleocanthal significantly decreased amyloid load in the hippocampal parenchyma and microvessels. This reduction was associated with enhanced cerebral clearance of Aβ across the blood-brain barrier (BBB). Further mechanistic studies demonstrated oleocanthal to increase the expression of important amyloid clearance proteins at the BBB including Pglycoprotein and LRP1, and to activate the ApoE-dependent amyloid clearance pathway in the mice brains. The anti-inflammatory effect of oleocanthal in the brains of these mice was also obvious where it was able to reduce astrocytes activation and IL-1β levels. Finally, we Hisham et al. could recapitulate the observed protective effect of oleocanthal in an in vitro human-based model, which could argue against species difference in response to oleocanthal. In conclusion, findings from in vivo and in vitro studies provide further support for the protective effect of oleocanthal against the progression of AD.

 

SUMMURY

A potential mechanism of action of oleocanthal against Anzheimer’s disease

Protein Tau alteration is one of the factors causing Alzheimer's disease. This particular study showed that oleocanthal can prevent this alteration, maintaining the original form of the protein. Further studies have shown that oleocanthal, due to its structure, leads to this obstruction without affecting the physiological function of Tau protein. These findings lead to a possible development of new treatments for diseases such as Alzheimer's.

Oleocanthal acts against Alzheimer's disease, preventing the deposition of specific proteins called amyloid in the brain of mice.

 

6. Oleocanthal-rich extra virgin olive oil demonstrates acute anti-platelet effectsin healthy men in a randomized trial

The phenolic profiles of extra virgin olive oils (EVOOs) may influence their cardiovascular benefits. In a randomized crossover of acute EVOO intake on platelet function, participants (n = 9) consumed 40 mL of EVOO weekly. EVOOs were matched for total phenolic content and were either tyrosol-poor with 1:2 oleacein/oleocanthal (D2i0.5), or 2:1 oleacein/oleocanthal (D2i2), or predominantly tyrosol (D2i0). Ibuprofen provided a platelet inhibition control. Blood was collected pre- and 2 h post-EVOO intake. D2i0.5 and D2i2 reduced 1 mg/mL collagenstimulated maximum platelet aggregation (Pmax), with effects best correlated to oleocanthal intake (R = 0.56, P = 0.002). Total phenolic intake was independently correlated to eicosanoid production inhibition, suggesting that cyclooxygenase blockade was not responsible for the Pmax inhibition. Five participants exhibited >25% ΔPmax declines with D2i0.5 and D2i2 intake and plasma metabolomic profiles discriminated subjects by oil responsivity. Platelet responses to acute EVOO intake are associated with oil phenolic composition and may be influenced by diet.

 

SUMMURY

Olive oil rich in oleocanthal effects the cardiovascular system’s function

Olive oil oleocanthal levels, can significantly affect the cardiovascular benefits from its consumption. In this study, participants consumed 40ml of extra virgin olive oil (EVOO), with a known polyphenols concentration, so that they can evaluate the effects on blood platelets function, blood ingredients that are related to blood coagulation. The results were compared with ibuprofen action; a powerful antioxidant factor. This study showed that EVOO samples rich in oleocanthal and oleacein caused a significant decrease in platelet aggregation levels (more than 25% reduction), that is the main cause for blood clotting, indicating that oleocanthal intake holds the bigger part. Finally, seems that the effects of EVOO polyphenols is independent from their antioxidant action and turns out that the chemical profile of olive oil effects directly the cardiovascular system’s function.

According to a randomized crossover of acute EVOO intake, olive oil rich in oleocanthal and oleacein helps to reduce thrombosis, as it causesa decrease in platelet aggregation

 

7. Phytochemistry: ibuprofen like activity in extra virgin olive oil.

Newly pressed extra virgin olive oil contains oleocanthal a compound whose pungency induces a strong stinging sensation in the throat, not unlike that caused by solutions of the nonsteroidal anti-inflammatory drug ibuprofen. In the study of Beauchamp et al.., 2005, this similar perception seems to be an indicator of a shared pharmacological activity, with oleocanthal acting as a natural anti-inflammatory compound that has a potency and profile strikingly similar to that of ibuprofen. Although structurally dissimilar, both these molecules inhibit the same cyclooxygenase enzymes in the prostaglandin biosynthesis pathway. Both enantiomers of oleocanthal, exhibited a dose-dependent inhibition of COX-1 and COX-2 activities, with no effect on lipoxygenase activity, much as observed with ibuprofen.

 

SUMMURY

Oleocanthal:a natural anti-inflammatory compound

Freshly extracted extra virgin olive oil contains oleocanthal, a substance responsible for a strong “pinch” feeling in the throat, similar to the effect of ibuprofen intake, a strong anti-inflammatory drug. According to this study, oleocanthal inhibits some certain enzymes related to inflammation, showing the same action as ibuprofen, although structurally show many differences.

Oleocanthal actsas a natural anti-inflammatory compoundthat hasa potencyand profile strikingly similar to that of ibuprofen, although they are structurally dissimilar

 

8. Oleocanthal as a cMet inhibitor for the control of metastatic breast and prostate cancers

Oleocanthal is a naturally occurring minor secoiridoid isolated from extra virgin olive oil, which showed potent anti-inflammatory activity. In the study of Enagar et al., Computer Assisted Molecular Design (CAMD) identified oleocanthal as a potential virtual cMet inhibitor hit. In this study oleocanthal inhibited the proliferation, migration, and invasion of the epithelial human breast and prostate cancer cell lines with an IC(50) of 4.47μΜ. Moreover, oleocanthal inhibited the phosphorylation of cMet kinase in vitro, with an IC (50) value of 4.8μM. These results show that oleocanthal and EVOO can have potential therapeutic use for the control of cMet-dependent malignancies.


SUMMURY

The role of oleocanthal in breast and prostate cancer

Oleocanthal is a compound found in extra virgin olive oil showing a strong antiinflammatory action. Research of Enagar and his colleagues showed that oleocanthal, at a cellular level, blocks the development and the metastatic action of breast or prostate cancer cells. Even in low dosage, oleocanthal and by extend extra virgin olive oil have a powerful healing role in breast and prostate cancer.

In this studyoleocanthal inhibited the proliferation, migration, and invasionof the epithelial humanbreast and prostate cancercell lines.

 

9. (-)-Oleocanthal inhibits growth and metastasis by blocking activation of STAT3 in human hepatocellular carcinoma

In the present study was explored by Pei et al., the anti-cancer capacity of oleocanthal in human hepatocellular carcinoma (HCC). Oleocanthal inhibited proliferation and cell cycle progression and induced apoptosis in HCC cells in vitro and suppressed tumor growth in an orthotopic HCC model. Oleocanthal also inhibited HCC cell migration and invasion in vitro and impeded HCC metastasis in an in vivo lung metastasis model. Oleocanthal acted by inhibiting epithelialmesenchymal transition (EMT) through downregulation Twist, a protein which is a direct target of the transcription factor STAT3. Oleocanthal also reduced STAT3 nuclear translocation and DNA binding activity, ultimately downregulating its downstream effectors, including the cell cycle protein Cyclin D1, the anti-apoptotic proteins Bcl-2 and survivin, and the invasion-related protein MMP2. Overexpression of constitutively active STAT3 partly reversed the anticancer effects of oleocanthal, which inhibited STAT3 activation by decreasing the activities of JAK1 and JAK2 and increasing the activity of SHP-1. These data suggest that oleocanthal may be a promising candidate for HCC treatment.


SUMMURY

The anticancer activity of oleocanthal

Pei and his colleagues studied the anticancer action of oleocanthal in human liver cancer cells. The results showed that oleocanthal reduced the proliferation of cancer cells, suspended tumor growth and at the same time caused the death of many cancer cells. Also, in an experiment that was held testing the antimetastatic action of the substance, oleocanthal blocked the metastasis on the lungs. These results, give hope for the use of this compound not only on a cellular level, but on the human organism.

Oleocanthal has strong anti-tumor properties in human liver cells, as it reduces tumor cell proliferation, inhibits tumor growth and simultaneously causes the death of many cancercells.

 

10. (-)-Oleocanthal rapidly and selectively induces cancer cell death via lysosomalmembrane permeabilization

LeGendre et al. investigated the effect of oleocanthal (OC) on human cancer cell lines in culture and found that OC induced cell death in all cancer cells examined as rapidly as 30 minutes after treatment. OC treatment of non-transformed cells suppressed their proliferation but did not cause cell death. OC induced both primary necrotic and apoptotic cell death via induction of lysosomal membrane permeabilization (LMP). Here evidence are provided showing that OC promotes LMP by inhibiting acid sphingomyelinase (ASM) activity, which destabilizes the interaction between proteins required for lysosomal membrane stability. The data presented here indicate that cancer cells, which tend to have fragile lysosomal membranes compared to non-cancerous cells, are susceptible to cell death induced by lysosomotropic agents. Therefore, targeting lysosomal membrane stability represents a novel approach for the induction of cancer-specific cell death.


SUMMURY

Oleocanthal promotes only the death of cancer cells and not of normal cells

Ο LeGendre και οι συνεργάτες του μελέτησαν την επίδραση της ελαιοκανθάλης σε ανθρώπινα καρκινικά κύτταρα. Τα πειράματα τους έδειξαν πως η ελαιοκανθάλη προκαλεί στα καρκινικά κύτταρα θάνατο εντός 30 λεπτών, ενώ ταυτόχρονα δεν προκαλεί θάνατο στα φυσιολογικά κύτταρα. Αυτό συμβαίνει διότι η ελαιοκανθάλη δρα σε έναν ειδικό μηχανισμό των κυττάρων όπου τα καρκινικά κύτταρα τυχαίνει να είναι πιο ευαίσθητα απ’ότι τα φυσιολογικά, με αποτέλεσμα να οδηγούνται μόνο αυτα σε θάνατο και όχι τα φυσιολογικά.

Oleocanthal inducescell death in all cancercellsexamined as rapidly as 30 minutes after treatment, with an exclusiveway.

 

11. Cytotoxic Activity of Oleocanthal Isolated from Virgin Olive Oil on Human Melanoma Cells

Oleocanthal’s potential anticancer activity has already been reported but only limited evidence has been provided in cutaneous malignant melanoma. The present study of Fogli S et al. is aimed at investigating the selective in vitro antiproliferative activity of oleocanthal against human malignant melanoma cells. Cell viability experiments demonstrated that oleocanthal had a remarkable and selective activity for human melanoma cells versus normal dermal fibroblasts with IC50s in the low micromolar range of concentrations. Such an effect was paralleled by a significant inhibition of ERK1/2 and AKT protein phosphorylation and downregulation of the gene Bcl2 expression. These findings may suggest that extra virgin olive oil phenolic extract enriched in oleocanthal deserves further investigation in skin cancer.

Fogli S, Nutr Cancer. 2016 Jul;68(5):8737


SUMMURY

Oleocanthal’s anticancer activity in cutaneous malignant melanoma

The aim of this study is to investigate the anticancer activity of oleocanthal against cutaneous malignant melanoma. Oleocanthal had a remarkable and selective activity for human melanoma cells versus normal dermal cells, even at low dosages.

Oleocanthal has a selective in vitro antiproliferative activity against human malignant melanoma cells,even at low doses.

 

12. In Cell Interactome of Oleocanthal, an Extra Virgin Olive Oil Bioactive Component.

Ο Cassiano C και η ομάδα του έδειξαν στην έρευνα τους πως οι πρωτεΐνες HSP70 και HSP90 είναι τα κύρια μόρια αλληλεπίδρασης της ελαιοκανθάλης στα ζωντανά συστήματα. Αυτές οι δύο πρωτεΐνες εμπλέκονται στην ανάπτυξη του καρκίνου και, κατ’ αυτό τον τρόπο, τα αποτελέσματα της μελέτης αυτής μπορεί να έχουν σημαντική ωφέλεια για την φαρμακολογική σημαντικότητα της ελαιοκανθάλης, έναντι του καρκίνου.

Cassiano C et al., Nat Prod Commun. 2015 Jun;10(6):10136.


SUMMURY

The interaction of oleocanthal with mechanismsassociatedwith cancer

Cassiano C et al. revealed in their research via chemical proteomics that heatshock proteins, HSP70 and HSP90, as main oleocanthal interactors in living systems. These two proteins are involved in cancer development and, thus, our findings could have important outcomes for a deep evaluation of the biopharmacological significance of oleocanthal.

The interaction of oleocanthal with mechanisms associated with cancer is indicative of its anti-canceractivity

 

13. Olive Oil-derived Oleocanthal as Potent Inhibitor of Mammalian Target of Rapamycin: Biological Evaluation and Molecular Modeling Studies

Mammalian target of rapamycin (mTOR) is a protein that integrates signals from energy homeostasis, metabolism, stress response, and cell cycle, with reported role in cancer and Alzheimer’s disease development. This function encouraged the team of Mohammad A. Khanfar et al. to examine the possibility that oleocanthal inhibits mTOR. Subsequent experimental validation indicated that oleocanthal indeed inhibited the enzymatic activity of mTOR with an IC50 value of 708 nM. Oleocanthal inhibits the growth of several breast cancer cell lines at low micromolar concentration in a dose-dependent manner. Oleocanthal treatment caused a marked downregulation of phosphorylated mTOR in metastatic breast cancer cell line (MDAMB- 231). These results strongly indicate that mTOR inhibition is at least one of the factors of the reported anticancer and neuroprotective properties of oleocanthal.

Khanfar ΜΑ et al. Phytother Res. 2015 November ; 29(11): 1776–1782


SUMMURY

The effect of oleocanthal on breast cancer

The aim of this study is to investigate the effect of oleocanthal treatment on specific breast cancer cells, even at low dosages. The results have shown that oleocanthal reduces the impact of a protein, that plays an important role in the development of cancer cells and of breast cancer as well.

Oleocanthal inhibits the enzymatic activity of a protein that plays an important role in the development of cancercells,in a dose-dependentmanner.

 

14. Olive Phenolics as c-Met Inhibitors: (-)-Oleocanthal Attenuates Cell Proliferation, Invasiveness, and Tumor Growth in Breast CancerModels

Dysregulation of the Hepatocyte growth factor (HGF)/c-Met signaling axis upregulates diverse tumor cell functions, including cell proliferation, survival, scattering and motility, epithelial-to-mesenchymal transition (EMT), angiogenesis, invasion, and metastasis. The aim of this study was to characterize the intracellular mechanisms involved in mediating the anticancer effects of (-)-oleocanthal treatment and the potential involvement of c-Met receptor signaling components in breast cancer. Results showed that (-)-oleocanthal inhibits the growth of human breast cancer cell lines MDA-MB-231, MCF-7 and BT-474 while similar treatment doses were found to have no effect on normal human MCF10A cell growth. In addition, (-)-oleocanthal treatment caused a dose-dependent inhibition of HGFinduced cell migration, invasion and G1/S cell cycle progression in breast cancer cell lines. Moreover, (-)-oleocanthal treatment effects were found to be mediated via inhibition of HGF-induced c-Met activation and its downstream mitogenic signaling pathways. This growth inhibitory effect is associated with blockade of EMT and reduction in cellular motility. Further results from in vivo studies showed that (-)- oleocanthal treatment suppressed tumor cell growth in an orthotopic model of breast cancer in athymic nude mice. Collectively, the findings of this study suggest that (-)-oleocanthal is a promising dietary supplement lead with potential for therapeutic use to control malignancies with aberrant c-Met activity.


SUMMURY

Intracellular mechanisms of oleocanthal treatment against breast cancer: Oleocanthal reduces tumor proliferation and tumor growth

The aim of this study was to characterize the intracellular mechanisms involved in mediating the anticancer effects of oleocanthal treatment. The results showed that the oleocanthal inhibits the growth of cancer cells, without any effect on normal cells. In particular, oleocanthal modulates the activity of specific proteins associated with the growth, proliferation and migration of cancer cells. In further experiments on mice with cancer of their skin showed remarkable inhibition of tumor growth. In conclusion, the findings of this study suggest that oleocanthal is a promising dietary supplement lead with potential for therapeutic use to control malignancies.

Oleocanthal has a strong anti-cancer effect, by affecting the activity of specific proteins associated with the proliferation and migration of cancer cells, without showingany effect on normal cells.

 

15. Effect of Oleocanthal and Its Derivatives on Inflammatory Response Induced by Lipopolysaccharide in a Murine Chondrocyte Cell Line

In joint diseases, cartilage homeostasis is disrupted by mechanisms that are driven by combinations of biologic factors. Osteoarthritis progression is characterized by increased nitric oxide (NO) production, which has been associated with cartilage degradation. Oleocanthal displays antiinflammatory drug activity similar to that of ibuprofen, a drug widely used in the therapeutic management of joint inflammatory diseases. In this study Iacono et al. evaluated the effect of oleocanthal and its derivatives on the modulation of NO production in chondrocytes. Oleocanthal and its derivatives decreased lipopolysaccharide-induced NOS2 synthesis in chondrocytes without significantly affecting cell viability at lower concentrations. Among the derivatives that were examined, derivative 231 was the most interesting, since its inhibitory effect on NOS2 was devoid of cytotoxicity even at higher concentrations. This class of molecules shows potential as a therapeutic weapon for the treatment of inflammatory degenerative joint diseases.

Iacono et al., ARTHRITIS & RHEUMATISM 2010


SUMMURY

Oleocanthal and its derivates on the treatment of inflammatory degenerative joint diseases

Oleocanthal and its derivatives show potential as a therapeutic weapon for the treatment of inflammatory degenerative joint diseases, such as osteoarthritis. Osteoarthritis is characterized by increased production of nitric oxide (NO) associated with cartilage damage. Oleocanthal and its derivatives reduce the synthesis of NO and inhibit the progression of the disease.

Oleocanthal shows potential as a therapeutic weapon for the treatment of inflammatory degenerative joint diseases,suchas osteoarthritis, by reducing the synthesisof nitrogen monoxide, which isassociatedwith cartilage damage.

 

16. Oleocanthal exerts antitumor effectson human liver and colon cancer cells through ROSgeneration.

Oleocanthal (OC) shows an anti-inflammatory and anticancer activity, which guided Cusimano et al. to study the anticancer effects of OC in hepatocellular (HCC) and colorectal carcinoma (CRC). Several cell lines were used at the study that were treated with OC and estimated the cell viability and apoptosis. OC was more effective comparing with other anti-inflammatory agents like ibuprofen, indomethacin and nimesulide, and induced cell growth inhibition. Moreover, experiments with OC showed inhibition of colony formation and apoptosis induction. Finally, OC showed no toxic effect on normal hepatocytes. All this lead to the conclusion, that OC is a potent agent against in HCC and CRC. These findings provide a strong support of the potential use of extra virgin olive oil as chemotherapeutic.


SUMMURY

Anticancer effects of oleocanthal in hepatocellular (HCC) andcolorectal carcinoma (CRC)
Oleocanthal (OC) shows an anti-inflammatory and anticancer activity in liver and colon cancer cells. OC inhibits the growth of cancer without affecting normal cells, providing a strong support of the potential use of extra virgin olive oil as chemotherapeutic.

Oleocanthal (OC)showsa remarkable anti-inflammatory and anticancer activity in liver and coloncancercellswithout affecting normal cells

Cusimano A1, Balasus D1, Azzolina A1, Augello G1, Emma MR1, Di Sano C1, Gramignoli R2, Strom SC2, McCubrey JA3, Montalto G1, Cervello M1.Int J Oncol. 2017 Aug;51(2):533-544

17. The olive oil phenolic oleocanthal modulates estrogen receptor expression in luminal breast cancer in vitro and synergizeswith tamoxifen treatment

The goal of this study was to explore the effect of oleocanthal treatment on growth of luminal breast cancer cells and to examine the effect of combination of oleocanthal with tamoxifen. Results showed that oleocanthal inhibited growth of various human breast cancer cells in mitogen-free media with IC50 values of 32.7 to 80.93μM. Similarly, oleocanthal suppressed growth of these cells in 17β-estradiolsupplemented media with IC50values of 22.28 to 83.91μM. Combined oleocanthal and tamoxifen treatments resulted in a synergistic growth inhibition of the cells with combination index values of 0.65 to 0.53 for each cell line. Studies indicated high degree of overlapping for the binding of oleocanthal and 17β-estradiol to estrogen receptors, while oleocanthal and tamoxifen have distinguished binding modes. Treatment with 5mg/kg or 10mg/kg (-)-oleocanthal resulted in 97% inhibition of tumor growth in mice. (-)-Oleocanthal treatment reduced total levels of estrogen receptors in cells both in vitro and in vivo. Collectively, (-)-oleocanthal showed a potential beneficial effect in suppressing growth of hormone-dependent breast cancer and improving sensitivity to tamoxifen treatment. These findings provide rational for evaluating the effect of (-)-oleocanthal in combination with endocrine treatments in luminal breast cancer.


SUMMURY


Oleocanthaltreatment on growth of luminal breast cancer cells and the effect of combination of oleocanthal with tamoxifen 
In the present study, oleocanthal seems to prevent the development of breast cancer, but also combined oleocanthal and tamoxifen treatments resulted in a synergistic growth inhibition of the cells. In particular, oleocanthal treatment reduces the total level of estrogen receptors, concerning experiments both on cells and animals, with 97% inhibition of tumor growth in mice. In conclusion, oleocanthal improves the sensitivity to tamoxifen treatment, so it can be used in combination with endocrine therapy for better breast cancer results.

Oleocanthal showed a potential beneficial effect in suppressing growth of hormone-dependent breast cancer and improving sensitivity to tamoxifen treatment.

Ayoub NM1, Siddique AB2, Ebrahim HY2, Mohyeldin MM2, El Sayed KA2. Eur J Pharmacol. 2017 Sep 5;810:100-111. doi: 10.1016/j.ejphar.2017.06.019. Epub 2017 Jun 15.

 

18. Oleocanthal ameliorates amyloid-β oligomers' toxicity on astrocytesand neuronal cells:In vitro studies.

In the current study, Batarseh et al. investigated oleocanthal effect on modulating Aβ oligomers (Aβo) pathological events in neurons and astrocytes. The findings demonstrated oleocanthal prevented Aβo-induced synaptic proteins, SNAP-25 and PSD-95, down-regulation in neurons, and attenuated Aβo-induced inflammation, glutamine transporter (GLT1) and glucose transporter (GLUT1) down-regulation in astrocytes. The inflammation that was induced by Αβο was characterized by interleukin-6 (IL-6) increase and glial fibrillary acidic protein (GFAP) upregulation that were reduced by oleocanthal. In conclusion, this study comes to add more to support the role of oleocanthal against AD pathology.


SUMMURY

Oleocanthal reduces the toxicity of Aβ oligomers in Alzheimer's disease.

Oleocanthal reduces the toxicity of Aβ oligomers associated with the pathogenesis of Alzheimer's disease. The findings showed that oleocanthal prevents the deregulation of specific proteins in the neurons and attenuates the inflammation that is generated. In conclusion, oleocanthal seems to play a very important role in the treatment of the disease.

Neuroscience. 2017 Jun 3;352:204-215. doi: 10.1016/j.neuroscience.2017.03.059. Epub 2017 Apr 7. Batarseh YS1, Mohamed LA1, Al Rihani SB1, Mousa YM1, Siddique AB1, El Sayed KA1, Kaddoumi A2.

Oleocanthal significantly reduces the toxicity of Aβ oligomers associated with Alzheimer'sdiseaseand it canbe a potential future treatment for the disease

 

19. Oleocanthal exerts anti-melanoma activities and inhibits STAT3 signalingpathway.

In this study Gu Y et al. explored the effects of oleocanthal (OC) on the three processes in melanoma and investigated underlying mechanisms. In vitro, OC suppressed proliferation, migration, invasion, in melanoma and human umbilical vascular endothelial cells, and additionally induced apoptosis and suppressed the tube formation, respectively. In vivo studies showed potent activity in suppressing tumor growth. Furthermore, OC suppressed proliferation and angiogenesis. In addition, OC was found to inhibit metastasis of melanoma in a lung metastasis model. Mechanistically, OC significantly suppressed phosphorylation of the protein signal transducer and activator of transcription 3 (STAT3), and, moreover, decreased and inhibited STAT3 nuclear localization and transcriptional activity, respectively. OC also downregulated STAT3 target genes, including Mcl-1, Bcl-xL, MMP-2, MMP-9, VEGF, which are involved in apoptosis, invasion and angiogenesis of melanoma. These results support further investigation of OC as a potential anti-melanoma drug.


SUMMURY

The beneficial effect of oleocanthal on melanoma

In this study Gu Y et. al explored the effects of oleocanthal (OC) on melanoma and investigated the mechanisms. Experiments conducted in cells showed a suppression of tumor growth, migration and penetration of melanoma. Furthermore, animal treatment with oleocanthal led to significant inhibition of tumor growth, through various biochemical pathways. These results support future studies of OC as a drug against melanoma.

Oleocanthal is a potential anti-melanoma drug, as it showed potent activity in suppressingtumor growth and inhibiting metastasis of melanoma, by affecting specificproteinsthat are important for tumor growth and its metastasis.

Oncol Rep. 2017 Jan;37(1):483-491. doi: 10.3892/or.2016.5270. Epub 2016 Nov 23. Gu Y1, Wang J1, Peng L1.

 

 

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