In order to study the possibility of hydroxytyrosol(HT)as a drug,we used SwissADME system to predict ADME of HT and pkCSM system to predict Tox of HT.The results show that hydroxytyrosol meets the Lipinski’s five pri...In order to study the possibility of hydroxytyrosol(HT)as a drug,we used SwissADME system to predict ADME of HT and pkCSM system to predict Tox of HT.The results show that hydroxytyrosol meets the Lipinski’s five principles of drug-like properties.With strong efficacy and pharmacological activity,HT has high drug-likeness degree.With good bioavailability,it can be easily absorbed by the gastrointestinal tract,though not absorbed by skin.Hydroxytyrosol has not only a strong potency and pharmacological activity,but also no liver toxicity and skin allergy.Tox data predicts that it has mutagenic potential,which may be the result of overreduction.展开更多
Myocardial infarction triggers massive biochemical changes, even cardiac cell death. Endoplasmic reticulum stress is involved in the pathology of myocardial infarction-mediated apoptosis. In the present study, myocard...Myocardial infarction triggers massive biochemical changes, even cardiac cell death. Endoplasmic reticulum stress is involved in the pathology of myocardial infarction-mediated apoptosis. In the present study, myocardial cell line H9c2 cells were treated with cobalt chloride（CoCl_2） to induce hypoxia. Isoproterenol was used for two successive days to induce myocardial infarction in SD rats. The cardioprotective effect of olive leaf extract（OLE） and its main constituent hydroxytyrosol and the underlying mechanisms were evaluated. The results showed that hydroxytyrosol markedly protected H9c2 cells against CoCl2-induced apoptosis. Hydroxytyrosol could reduce the mRNA and protein expression of GRP78 and CHOP induced by CoCl2 in vitro. In vivo, the decreased ejection fraction and fractional shortening, increased heart weight/body ratio, the formation of infarction, disordered cardiac muscle fibers and infiltration of inflammatory cells induced by isoproterenol could be significantly ameliorated by pretreatment with OLE for a month. Similarly, OLE could also reverse the increase of GRP78 and CHOP expression induced by isoproterenol. Therefore, OLE and hydroxytyrosol exert a cardioprotective effect through endoplasmic reticulum stress, which could be a new target for the prevention and treatment of cardiovascular diseases.展开更多
In nature, tyrosol (TY) and hydroxytyrosol (HT) are found in olive leaves which are for medical aims, with immune stimulant and antibiotic properties as well as the ability to be used for the treatment of neurodegener...In nature, tyrosol (TY) and hydroxytyrosol (HT) are found in olive leaves which are for medical aims, with immune stimulant and antibiotic properties as well as the ability to be used for the treatment of neurodegenerative diseases such as Alzheimer. This ability of phytochemical TY and HT compounds are mainly believed to be of higher radical scavenging potential with effective antioxidant properties. In order to establish the possible structure-antioxidant activity relationship of tyrosol, hydroxytyrosol, hydroxytyrosol acetate and two designed hydroxytyrosol derivatives were studied by the help of quantum chemical calculations. The molecular electronic properties such as heat formation of the neutral, radical and orbitals energies were calculated as descriptors to predict the H atom donating abilities of compounds. Considering the results from the calculated descriptors, the derivatives having OH group substitutions in position number four of the aromatic ring can be classified highly active and better antioxidant compound. Therefore, the designed hydroxytyrosol derivatives showed most active feasible H atom donation. This work can be useful to design novel antioxidants.展开更多
The work describes a stability study of hydroxytyrosol (HTyr) in aqueous solutions carried out varying the following parameters: HTyr concentration, temperature and ionic content in the aqueous solution. First, an ana...The work describes a stability study of hydroxytyrosol (HTyr) in aqueous solutions carried out varying the following parameters: HTyr concentration, temperature and ionic content in the aqueous solution. First, an analytical method based on the use of ultra performance liquid chromatography (UPLC-MS) as analytical technique was developed and validated. The equation of the linear model was A/AISTD= –0.0013 + 0.0117. [HTyr], with a very good linearity, since the R-Squared was 99.9% and the P value of the lack of fit test was higher than 5%. Limits of quantification estimated, CCα(α= 0.05%) and CCβ(β= 0.05%), were 0.2 and 0.4 g/L respectively. As well, the relative standard deviation in the intra-day precision was lower than 3%. Therefore, the method is reproducible. We have applied this methodology to study the stability of HTyr and have observed that the most critical aspect turned to be the ionic content of the aqueous solutions. A tap water with high contents of calcium and magnesium (52 and 21 mg/L) degraded HTyr up to 64% in 48 hours whereas a low mineralization water with low contents of calcium and magnesium (4 and 2 mg/L) produced only 19% degradation.展开更多
The aim of this study was to test if previous ingestion of compounds containing resveratrol or hydroxytyrosol, followed by an exhausting hand grip exercise, could induce an acute post-exercise increase in brachial blo...The aim of this study was to test if previous ingestion of compounds containing resveratrol or hydroxytyrosol, followed by an exhausting hand grip exercise, could induce an acute post-exercise increase in brachial blood flow. Six healthy subjects (three males and three females, 35 ± 7 years), 60 minutes after ingestion of a capsule containing 200 mg of resveratrol or 30 ml of extra virgin olive oil enriched with tyrosol, oleuropein and hydroxytyrosol, performed a hand grip exercise equal to half of their maximum strength until they were no longer able to express the same force (2-day interval between tests). The nonparametric Wilcoxon signed rank test was used for statistical evaluations. Brachial artery blood flow (Fba) and both blood velocity (Vba) and artery diameter (Dba) were assessed immediately after exercise cessation by means of colour Doppler ultrasound. After ingestion of the oil mixture the post-exercise value of Fba median was 2.4 times higher than that after ingestion of the resveratrol compound (P = 0.03), and also the Vba median concerning the hydroxytyrosol was 1.9 times higher than that of the resveratrol (P = 0.03). Both functional foods did not lead to a significant difference in the Dba medians. These results indicate that hydroxytyrosol, but not resveratrol, may be an effective adjuvant of recreational or agonistic, long-lasting sports performances, thanks to the powerful blood flow increment which can be obtained as soon as one hour from its oral intake.展开更多
基金This work was supported by China Postdoctoral Science Foundation(2020M670675).
文摘In order to study the possibility of hydroxytyrosol(HT)as a drug,we used SwissADME system to predict ADME of HT and pkCSM system to predict Tox of HT.The results show that hydroxytyrosol meets the Lipinski’s five principles of drug-like properties.With strong efficacy and pharmacological activity,HT has high drug-likeness degree.With good bioavailability,it can be easily absorbed by the gastrointestinal tract,though not absorbed by skin.Hydroxytyrosol has not only a strong potency and pharmacological activity,but also no liver toxicity and skin allergy.Tox data predicts that it has mutagenic potential,which may be the result of overreduction.
基金supported by the National Natural Science Foundation of China (81472977)foundation from the Priority Academic Program Development of Jiangsu Higher Education InstitutionsGraduate Student Practice and Innovation Project of Jiangsu Province Ordinary University (SJZZ 15_0117)
文摘Myocardial infarction triggers massive biochemical changes, even cardiac cell death. Endoplasmic reticulum stress is involved in the pathology of myocardial infarction-mediated apoptosis. In the present study, myocardial cell line H9c2 cells were treated with cobalt chloride（CoCl_2） to induce hypoxia. Isoproterenol was used for two successive days to induce myocardial infarction in SD rats. The cardioprotective effect of olive leaf extract（OLE） and its main constituent hydroxytyrosol and the underlying mechanisms were evaluated. The results showed that hydroxytyrosol markedly protected H9c2 cells against CoCl2-induced apoptosis. Hydroxytyrosol could reduce the mRNA and protein expression of GRP78 and CHOP induced by CoCl2 in vitro. In vivo, the decreased ejection fraction and fractional shortening, increased heart weight/body ratio, the formation of infarction, disordered cardiac muscle fibers and infiltration of inflammatory cells induced by isoproterenol could be significantly ameliorated by pretreatment with OLE for a month. Similarly, OLE could also reverse the increase of GRP78 and CHOP expression induced by isoproterenol. Therefore, OLE and hydroxytyrosol exert a cardioprotective effect through endoplasmic reticulum stress, which could be a new target for the prevention and treatment of cardiovascular diseases.
文摘In nature, tyrosol (TY) and hydroxytyrosol (HT) are found in olive leaves which are for medical aims, with immune stimulant and antibiotic properties as well as the ability to be used for the treatment of neurodegenerative diseases such as Alzheimer. This ability of phytochemical TY and HT compounds are mainly believed to be of higher radical scavenging potential with effective antioxidant properties. In order to establish the possible structure-antioxidant activity relationship of tyrosol, hydroxytyrosol, hydroxytyrosol acetate and two designed hydroxytyrosol derivatives were studied by the help of quantum chemical calculations. The molecular electronic properties such as heat formation of the neutral, radical and orbitals energies were calculated as descriptors to predict the H atom donating abilities of compounds. Considering the results from the calculated descriptors, the derivatives having OH group substitutions in position number four of the aromatic ring can be classified highly active and better antioxidant compound. Therefore, the designed hydroxytyrosol derivatives showed most active feasible H atom donation. This work can be useful to design novel antioxidants.
文摘The work describes a stability study of hydroxytyrosol (HTyr) in aqueous solutions carried out varying the following parameters: HTyr concentration, temperature and ionic content in the aqueous solution. First, an analytical method based on the use of ultra performance liquid chromatography (UPLC-MS) as analytical technique was developed and validated. The equation of the linear model was A/AISTD= –0.0013 + 0.0117. [HTyr], with a very good linearity, since the R-Squared was 99.9% and the P value of the lack of fit test was higher than 5%. Limits of quantification estimated, CCα(α= 0.05%) and CCβ(β= 0.05%), were 0.2 and 0.4 g/L respectively. As well, the relative standard deviation in the intra-day precision was lower than 3%. Therefore, the method is reproducible. We have applied this methodology to study the stability of HTyr and have observed that the most critical aspect turned to be the ionic content of the aqueous solutions. A tap water with high contents of calcium and magnesium (52 and 21 mg/L) degraded HTyr up to 64% in 48 hours whereas a low mineralization water with low contents of calcium and magnesium (4 and 2 mg/L) produced only 19% degradation.
文摘The aim of this study was to test if previous ingestion of compounds containing resveratrol or hydroxytyrosol, followed by an exhausting hand grip exercise, could induce an acute post-exercise increase in brachial blood flow. Six healthy subjects (three males and three females, 35 ± 7 years), 60 minutes after ingestion of a capsule containing 200 mg of resveratrol or 30 ml of extra virgin olive oil enriched with tyrosol, oleuropein and hydroxytyrosol, performed a hand grip exercise equal to half of their maximum strength until they were no longer able to express the same force (2-day interval between tests). The nonparametric Wilcoxon signed rank test was used for statistical evaluations. Brachial artery blood flow (Fba) and both blood velocity (Vba) and artery diameter (Dba) were assessed immediately after exercise cessation by means of colour Doppler ultrasound. After ingestion of the oil mixture the post-exercise value of Fba median was 2.4 times higher than that after ingestion of the resveratrol compound (P = 0.03), and also the Vba median concerning the hydroxytyrosol was 1.9 times higher than that of the resveratrol (P = 0.03). Both functional foods did not lead to a significant difference in the Dba medians. These results indicate that hydroxytyrosol, but not resveratrol, may be an effective adjuvant of recreational or agonistic, long-lasting sports performances, thanks to the powerful blood flow increment which can be obtained as soon as one hour from its oral intake.
