Hydroxytyrosol targets multiple pathways and molecules. It acts as a potent scavenger of reactive oxygen species (ROS), thereby reducing oxidative stress. It inhibits 5-lipoxygenase (5-LO) and 12-lipoxygenase (12-LO), enzymes involved in the production of pro-inflammatory leukotrienes. It also interacts with estrogen receptors (ER) and has been shown to restore ERβ expression in neuronal cells. Additionally, it inhibits LPS-induced TNF-α production and exerts neuroprotective effects by improving mitochondrial function.

When pro-inflammatory cytokines (TNF-α) are exposed to hydroxytyrosol (DOPET), the expression of cyclooxygen synthase 2 and inducible nitric oxide synthase (iNOS) is reduced by about 60% [1]. DOPET (hydroxytyrosol) inhibits DNA oxidation, creates cycle tides, disinfects cells, and arrests cells [1].
Hydroxytyrosol demonstrates potent antioxidant activity in vitro by scavenging free radicals and reducing oxidative stress. It inhibits the proliferation of cancer cells and inhibits LPS-induced TNF-α production. At a concentration of 10 μM for 48 hours, Hydroxytyrosol protects primary rat hippocampal neurons from Aβ25-35-induced cell death and apoptosis by restoring ERβ expression and inhibiting apoptotic signaling pathways. It also inhibits the activity of 5-LO and 12-LO.

Hydroxytyrosol exerts cardioprotective effects in vivo by reducing oxidative stress and inflammation. It contributes to cardiovascular protection, which is a key feature of the Mediterranean diet. Its neuroprotective effects have been demonstrated in models of neurodegeneration, where it alleviates oxidative stress and improves mitochondrial function. The compound also exhibits anticancer, antimicrobial, and anti-aging properties.

Hydroxytyrosol does not have a traditional enzyme/receptor binding assay. Its activity is assessed through various functional assays. Antioxidant activity is measured using DPPH, ABTS, or ORAC assays. Lipoxygenase inhibition is assessed by measuring the production of leukotrienes or by using purified 5-LO and 12-LO enzymes in colorimetric assays. Its effects on ROS levels can be measured using fluorescent probes such as DCFH-DA in cell-based systems.

In vitro cellular experiments for Hydroxytyrosol involve treating various cell types, including neurons, cancer cells, and immune cells. The compound's neuroprotective effects are assessed by measuring cell viability, apoptosis markers (e.g., caspase-3 activation), and ROS levels in neuronal cultures exposed to oxidative stress or amyloid-beta peptides. Its anti-inflammatory effects are evaluated by measuring the production of cytokines such as TNF-α and IL-6 in LPS-stimulated macrophages.

In vivo animal experiments for Hydroxytyrosol involve administering the compound to animal models of cardiovascular disease, neurodegeneration, or cancer. Its effects on oxidative stress markers, inflammatory cytokines, and disease progression are assessed. In models of neurodegeneration, cognitive function and neuronal loss are evaluated. Its cardioprotective effects are assessed by measuring blood pressure, lipid profiles, and markers of endothelial function.

Hydroxytyrosol has a molecular weight of 154.16 g/mol and a molecular formula of C8H10O3. It is a small, water-soluble phenolic compound. It is well absorbed from the gastrointestinal tract and undergoes extensive metabolism, primarily through glucuronidation and sulfation. Its pharmacokinetic properties are characterized by rapid absorption and elimination, with a half-life of approximately 2-3 hours.

Hydroxytyrosol is generally recognized as safe (GRAS) and has low toxicity. It is well-tolerated at doses commonly found in olive oil and dietary supplements. In vitro studies have shown that it has no apoptotic effects at tested concentrations. However, as a research compound, it is not intended for human therapeutic use at high doses. Standard safety precautions should be followed when handling.

[1]. Hydroxytyrosol and potential uses in cardiovascular diseases, cancer, and AIDS. Front Nutr. 2014 Oct 27;1:18.

[2]. Hydroxytyrosol: Health Benefits and Use as Functional Ingredient in Meat. Medicines (Basel). 2018 Jan 23;5(1).

Hydroxytyrosol is a catechol compound with a structure of phenyl-1,2-diol substituted with a 2-hydroxyethyl group at the 4-position. It was isolated from olive (Olea europaea) and possesses antioxidant and antitumor activities. Hydroxytyrosol is both a metabolite and an antioxidant and antitumor agent. It belongs to the catechol class of compounds and is a primary alcohol. Its structure is similar to 2-(4-hydroxyphenyl)ethanol. Hydroxytyrosol has been used in clinical trials for breast cancer prevention. It has been reported to exist in Rehmannia glutinosa, Fraxinus americana, and other organisms with relevant data. Hydroxytyrosol is a phenolic phytochemical naturally found in extra virgin olive oil and has potential antioxidant, anti-inflammatory, and cancer-preventive activities. Although the specific mechanisms by which hydroxytyrosol exerts its effects are not fully elucidated, this substance may affect the expression of various components in the inflammatory response by regulating the nuclear factor-κB (NF-κB) pathway. Its functions include regulating pro-inflammatory cytokines, such as inhibiting interleukin-1α (IL-1α), IL-1β, IL-6, IL-12, and tumor necrosis factor-α (TNF-α); increasing the secretion of the anti-inflammatory cytokine IL-10; and inhibiting the production of certain chemokines, such as CXC motif chemokine ligand 10 (CXCL10/IP-10), CC motif chemokine ligand 2 (CCL2/MCP-1), and macrophage inflammatory protein-1β (CCL4/MIP-1β). Hydroxytyrosol can inhibit the expression of inducible nitric oxide synthase (iNOS/NOS2) and prostaglandin E2 synthase (PGES), thereby preventing the production of nitric oxide (NO) and prostaglandin E2 (PGE2), respectively. In addition, hydroxytyrosol can also regulate the expression of other genes involved in the regulation of tumor cell proliferation, such as extracellular signal-regulated kinases and cyclin-dependent kinases. Simultaneously, hydroxytyrosol can scavenge free radicals and prevent oxidative DNA damage. This can induce apoptosis in susceptible cancer cells and inhibit their proliferation.
Hydroxytyrosol (DOPET) is a naturally occurring phenolic compound found in olive oil and olive leaves. It is a potent antioxidant with cardioprotective, anti-inflammatory, neuroprotective, anticancer, and antimicrobial properties. It is a key component of the Mediterranean diet and is used in nutraceutical, cosmetic, and pharmaceutical formulations. The compound is also known as 3,4-Dihydroxyphenethyl alcohol and is available from various chemical suppliers for research purposes.

C8H10O3

154.1632

154.062

10597-60-1

Hydroxytyrosol-d4;1330260-89-3;Hydroxytyrosol-d5

82755

Light yellow to yellow solid powder

1.3±0.1 g/cm3

355.4±27.0 °C at 760 mmHg

182.6±18.3 °C

0.0±0.8 mmHg at 25°C

1.623

0.02

3

3

2

11

116

0

JUUBCHWRXWPFFH-UHFFFAOYSA-N

InChI=1S/C8H10O3/c9-4-3-6-1-2-7(10)8(11)5-6/h1-2,5,9-11H,3-4H2

4-(2-hydroxyethyl)benzene-1,2-diol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~125 mg/mL (~810.85 mM)
H2O : ~100 mg/mL (~648.68 mM)
Ethanol : ~50 mg/mL (~324.34 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (13.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (13.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (13.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)