- A new multifunctional hydroxytyrosol-clofibrate with hypolipidemic, antioxidant, and hepatoprotective effects
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Oxidative stress has been regarded as the leading mechanism of the hepatotoxicity of clofibrate (CF). To achieve multifunctional novel hypolipidemic agents with hypolipidemia, antioxidant, and ameliorating liver injury, clofibric acid derivative hydroxytyrosol-clofibrate (CF-HT) was synthesized by molecular hybridization. CF-HT exhibited significant hypolipidemia, reducing serum triglyceride (TG), total cholesterol (TC), and malonaldehyde (MDA) by 30%, 33%, and 29% in hyperlipidemic mice induced by Triton WR 1339. CF-HT also shown hepatoprotective effect, a significant decrease in hepatic indices toxicity was observed, i.e. aspartate and lactate transaminases (AST and ALT) activities, alkalines phosphatases (ALP), and total bilirubin (TBIL) levels. The liver weight and liver coefficient were also ameliorated. Serum superoxide dismutase (SOD) was significantly elevated, and serum catalase (CAT) and malondialdehyde (MDA) content were remarkably restored. The hepatic glutathione (GSH) content was obviously increased and hepatic oxidized glutathione (GSSG) content was reduced dramatically by CF-HT, as compared to the CF treated mice (p 0.05). Moreover, the histopathological damage that hepatocyte hyperplasia and hypertrophy was also significantly ameliorated by treatment with CF-HT. Therefore, the results indicated that CF-HT exerted more potent hypolipidemic activity and definite hepatoprotective effect which may mainly be associated with its antioxidative property in mice.
- Xie, Yun-Dong,Chen, Zi-Zhang,Shao, Li-Hua,Wang, Qiu-Tang,Li, Na,Lu, Wen-Fang,Xu, Yan-Hong,Gao, Yu-Qiong,Guo, Li-Ying,Liu, Hao-Le,Li, Yi-Ping,Yang, Guang-De,Bian, Xiao-Li
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Read Online
- Hydroxytyrosol nicotinate, a new multifunctional hypolipidemic and hypoglycemic agent
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Hydroxytyrosol (HT) is a natural polyphenol antioxidant that exists in olive oil. In the study of multifunctional hypolipidemic of nicotinic derivatives, we found that hydroxytyrosol nicotinate (HT-N) incorporation of niacin with HT displayed α-glucosidase inhibitory activities in vitro, such as yeast α-glucosidase (IC50 = 117.72 μM) and rat intestinal α-glucosidases maltase (IC50 = 31.86 μM) and sucrase (IC50 = 22.99 μM), and had a good control of postprandial blood glucose (PBG). HT-N shown significantly hypoglycemic action by 16.9% and protection of pancreatic tissue in type 2 diabetic mellitus (T2DM) mouse model. HT-N also shown a potent antioxidant activity and property of anti-glycation in vitro, which were benefit for ameliorating diabetic complications. Moreover, HT-N exhibited much significant hypolipidemia, lowering plasma triglyceride (TG), total cholesterol (TC), and malonaldehyde (MDA) by 34.6%, 45.8% and 32.1% respectively, in hyperlipidemic mice induced by Triton WR 1339. The results indicated that HT-N has hypolipidemic, hypoglycemic and antioxidant actions. All these properties could be conducive to amelioration of oxidative stress, hyperlipidemia, and diabetes that HT-N may serve as a multifunctional potential therapeutic strategy in diabetic patients with hyperlipidemia.
- Xie, Yun-Dong,Chen, Zi-Zhang,Li, Na,Lu, Wen-Fang,Xu, Yan-Hong,Lin, Yuan-Yuan,Shao, Li-Hua,Wang, Qiu-Tang,Guo, Li-Ying,Gao, Yu-Qiong,Yang, Guang-De,Li, Yi-Ping,Bian, Xiao-Li
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Read Online
- Straightforward access to novel mitochondriotropics derived from 2-arylethanol as potent and selective antiproliferative agents
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The necessity for developing novel cytostatic agents with improved activities and reduced side-effects to tackle cancer prompted us to investigate mitochondria-targeted compounds, an approach that is gaining attention for the selective transportation of cytotoxic agents. We envisioned the possibility of conjugating a phenethyl alcohol motif, decorated with a series of phenol-based substituents on the aryl moiety, with a triphenyl phosphonium scaffold (a mitochondria-directed vector), through a hydrocarbon chain of different lengths. Thus, such compounds that incorporate the phenethyl skeleton can be considered as masked phenolic compounds derived from relevant natural counterparts found in olive tree (e.g. tyrosol, hydroxytyrosol). Title compounds exhibited very strong in vitro antiproliferative activities against the panel of six human tumor cell lines tested, with GI50 values ranging from the nanomolar (0.026 ± 0.010 μM for 36) to the submicromolar range in most of the cases; this represents an improvement of up to 350-fold compared to classical chemotherapeutic agents, like 5-fluorouracil or cisplatin. Interestingly, decrease in the linker length led to an increase of GI50 values against non-tumor cells, thus allowing a remarkable improvement of selectivity (SI up to 269). The very promising antiproliferative activities prompted us to further investigate their behaviour against multidrug resistant cell lines (MDR). The results indicated a reduced sensitivity of the multidrug resistant cells to compounds, probably due to P-gp-mediated efflux of these antiproliferative agents. Interestingly, activities were completely restored to the same levels by co-administration of tariquidar, a well-known inhibitor of P-gp. Flow cytometry analysis on sensitive cell lines revealed a decrease in the percentage of cells in G1 phase accompanied by increase in S and G2/M phases. In addition, a significant increase in subG1 area, was observed. These results are compatible with the necrotic and apoptotic cell death detected in the Annexin V assay, and with the depolarization of the mitochondria membrane. Thus, the new mitochondriotropic agents reported herein can be considered as promising antiproliferative agents, endowed with remarkable potency and selectivity, including MDR cells, upon co-administration with a pump-efflux inhibitor.
- Hicke, Francisco J.,Puerta, Adrián,Dini?, Jelena,Pe?i?, Milica,Padrón, José M.,López, óscar,Fernández-Bola?os, José G.
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- 2-(3,4-DIHYDROXYPHENYL)ETHYL 3-HYDROXYBUTANOATE, COMPOSITION, AND METHOD FOR IMPROVING FUNCTION OF AORTIC ENDOTHELIAL CELL
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The disclosure relates to a compound, 2-(3,4-dihydroxyphenyl)ethyl 3-hydroxybutanoate, for improving aortic endothelial cell function and use thereof. The compound is capable of inhibiting inflammatory response of the human aortic endothelial cells caused by a saturated fatty acid, and preventing an occurrence and progression of atherosclerosis. The compound is capable of reducing human aortic endothelial inflammation caused by a saturated fatty acid, for example, reducing the mRNA levels of interleukin-6 (IL-6), and is capable of effectively protecting the function of mitochondria in human aortic endothelium from being damaged by a saturated fatty acid, for example, increasing the expression of mitochondrial complex I.
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Paragraph 0039; 0041
(2021/02/19)
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- 3,4-DIHYDROXYPHENETHYL 3-HYDROXYBUTANOATE, PREPARATION AND USE THEREOF
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The present disclosure discloses a novel compound, 3,4-dihydroxyphenethyl 3-hydroxybutanoate, a method for preparing the same and use of the same, and in particular, a compound of formula I, use of the compound of formula I, optically pure isomers of the compound, a mixture of enantiomers in any ratio, or pharmaceutically acceptable salts thereof in preparing health food and drug for relieving brain fatigue, improving learning and memory abilities, and ameliorating mania mood related to brain fatigue.
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Paragraph 0102; 0107
(2021/03/19)
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- Synthesis and antioxidant activity of conjugates of hydroxytyrosol and coumarin
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Antioxidants have been the subject of intense research interest due to their numerous health benefits. In this work, a series of new conjugates of hydroxytyrosol and coumarin were synthesized and evaluated for their free radical scavenging, toxicity and antioxidant mechanism in vitro. The all target compounds 14a–t exhibited better radical scavenging activity than BHT, hydroxytyrosol, and coumarin in both DPPH radical and ABTS+ radical cation scavenging assays. The structure-activity relationships study indicated that the number and position of hydroxyl groups on the coumarin ring were vital to a good antioxidant capacity. Furthermore, the most promising compound 14q showed less toxicity in hemolysis assay and weaker antiproliferative effects than BHT against normal WI-38 and GES cells, and enhanced viability of H2O2-induced HepG2 cells. Additionally, 14q decreased the apoptotic percentage of HepG2 cells, reduced the ROS produce and LDH release, and improved GSH and SOD levels in H2O2-treated HepG2 cells. Lastly, 14q exhibited more stability than hydroxytyrosol in methanol solution. These results revealed that conjugations of hydroxytyrosol and coumarin show better antioxidant capacity, and are the efficacious approach to finding novel potential antioxidant.
- Li, Wen-Bo,Qiao, Xue-Peng,Wang, Zi-Xiao,Wang, Shuai,Chen, Shi-Wu
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- Synthesis and SARs of dopamine derivatives as potential inhibitors of influenza virus PAN endonuclease
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Currently, influenza PAN endonuclease has become an attractive target for development of new drugs to treat influenza infections. Herein we report the discovery of new PAN endonuclease inhibitors derived from a chelating agent dopamine moiety. A series of dopamine amide derivatives and their conformationally constrained 1,2,3,4-tetrahydroisoquinoline-6,7-diol-based analogs were elaborated and assayed against influenza virus A/WSN/33 (H1N1). Most compounds exhibited moderate to excellent antiviral activities, generating a preliminary SARs. Among them, compounds 14 and 19 showed stronger anti-IAV activity compared with the reference Peramivir. Moreover, 14 and 19 demonstrated a concentration-dependent inhibition of PAN endonuclease based on both FRET assay and SPR assay. Docking studies were also performed to elucidate the binding mode of 14 and 19 with the PAN protein and to identify amino acids involved in their mechanism of action, which were well consistent with the biological data. This finding was beneficial to laying the foundation for the rational development of more effective PAN endonuclease inhibitors.
- Liao, Yixian,Ye, Yilu,Li, Sumei,Zhuang, Yilian,Chen, Liye,Chen, Jianxin,Cui, Zining,Huo, Lijian,Liu, Shuwen,Song, Gaopeng
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- Convergent Total Synthesis of Lamellarins and Their Congeners
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A convergent total synthesis of lamellarins S and Z is described. The synthesis features a halogen dance of an easily accessible α,β-dibromopyrrole promoted by an ester moiety. The resultant β,β′-dibromopyrrole undergoes a ligand-controlled Suzuki-Miyaura coupling to provide a range of diarylated pyrrole derivatives. The established synthetic method was also applicable to the synthesis of ningalin B and lukianols A and B.
- Morikawa, Daiki,Morii, Kazuki,Yasuda, Yuto,Mori, Atsunori,Okano, Kentaro
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p. 8603 - 8617
(2020/07/16)
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- A New Series of Salicylic Acid Derivatives as Non-saccharide α-Glucosidase Inhibitors and Antioxidants
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In this study, a series of salicylic acid derivatives were designed and synthesized as novel non-saccharide α-glucosidase inhibitors. Biological evaluation indicated that when compared to acarbose, compounds T9, T10, and T32 exhibited a higher potency of α-glucosidase inhibitory activity with IC50 values of 0.15±0.01, 0.086±0.01 and 0.32±0.02mM, respectively. Evaluation of the inhibition kinetics indicated that T9, T10, T32, and acarbose interacted with α-glucosidase in a mixed non-competitive inhibitory manner. Moreover, T9, T10, and T32 statically quenched the fluorescence of α-glucosidase by formation of an inhibitor-α-glucosidase complex. The docking results showed that hydrogen bonds were generated between the test compounds and α-glucosidase. The antioxidant study revealed that compound T10 exhibited a higher antioxidant activity via scavenging 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH), thereby inhibiting lipid peroxidation and the total reduction capacity. In brief, the salicylic acid derivatives identified in this study were promising candidates for development as novel non-saccharide α-glucosidase inhibitors.
- Chen, Jiangang,Lu, Wenfang,Chen, Hao,Bian, Xiaoli,Yang, Guangde
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p. 231 - 246
(2019/02/19)
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- A new multifunctional hydroxytyrosol-fenofibrate with antidiabetic, antihyperlipidemic, antioxidant and antiinflammatory action
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Dyslipidemia, oxidative stress and inflammation are major risky factors involved in the pathophysiology of type 2 diabetes mellitus and atherosclerosis. Multifunctional intervene is more meaningful. The aim of this study was to evaluate the multifunctional effects of two new compounds, combination of fenofibric acid (FA) with tyrosol (T) or hydroxytyrosol (HT). Compared with fenofibrate (FF), FF-HT exhibited excellent antioxidant capacities in vitro and much improved hypolipidemia, reducing plasma triglyceride (TG), total cholesterol (TC), and malonaldehyde (MDA) by 76%, 54%, and 28%, while FF-T decreased the plasma parameters by 16%, 10%, and 20% in hyperlipidemic mice induced by Triton WR 1339. Furthermore, compound FF-HT exhibited significant antihyperglycemic, antihyperlipidemic, antioxidant and anti-inflammatory activities as well as attenuating hepatotoxicity in a type 2 diabetes experimental mouse model. The histological findings showed that FF-HT suppressed the development of hepatic lipid accumulation and ameliorated the damage in hepatic and pancreatic tissues compared to model mice. This study indicates for the first time that reasonable optimized drug design produce a compound entity which is conducive to the prevention of type 2 diabetes mellitus and its complications.
- Xie, Yundong,Xu, Yanhong,Chen, Zizhang,Lu, Wenfang,Li, Na,Wang, Qiutang,Shao, Lihua,Li, Yiping,Yang, Guangde,Bian, Xiaoli
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p. 1749 - 1758
(2017/09/28)
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- Tyrosol and hydroxytyrosol derivatives as antitrypanosomal and antileishmanial agents
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Trypanosomiasis and leishmaniasis keep being a real challenge for health and development of African countries. Existing treatments have considerable side effects and increase resistance of the parasites. We have measured antitrypanosomal and antileishmanial activity of natural phenols, tyrosol (TYR) and hydroxytyrosol (HT) and several of their esters and metabolites. We found significant IC50 values against Trypanosoma brucei for HT decanoate ester and HT dodecanoate ester (0.6 and 0.36 μM, respectively). This represents a large increase in activity with respect to HT (79 and 132 fold, respectively). Moreover, both compounds displayed a high selectivity index against MRC-5, a non-tumoral human cell line (118 and 106, respectively). Then, we synthesized a focused library of compounds to explore structure-activity. We found the ether and thiourea analogs of HT decanoate ester and HT dodecanoate ester also showed IC50 values against T. brucei in the low micromolar range. In conclusion, the di-ortho phenolic ring and medium size alkyl chain are essential for activity whereas the nature of the chemical bond among them seems less important.
- Belmonte-Reche, Efres,Martínez-García, Marta,Pe?alver, Pablo,Gómez-Pérez, Verónica,Lucas, Ricardo,Gamarro, Francisco,Pérez-Victoria, José María,Morales, Juan Carlos
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p. 132 - 140
(2016/05/24)
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- 3,4-dihydroxyl phenethyl alcohol fibrate carboxylic ester compound and preparation method and application thereof
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The invention discloses a 3,4-dihydroxyl phenethyl alcohol fibrate carboxylic ester compound and a preparation method and application thereof and belongs to the technical field of biological medicine. There is a big difference between the compound and fibrate carboxylic acid, but the compound still has lipid-reducing activity, and TC and TG are reduced at the same time. Besides, the compound has the effect of resisting oxidative stress to protect vascular endothelial injury. The invention further discloses the preparation method of 3,4-dihydroxyl phenethyl alcohol fibrate carboxylic ester compound. 3,4-dihydroxyl phenethyl alcohol, benzyl bromide and potassium carbonate serve as reaction raw materials, 3,4-dibenzyloxy phenethyl alcohol is prepared through a backflow reaction and column chromatographic separation, 3,4-dibenzyloxy phenethyl alcohol, a fibrate carboxylic compound, 1-(3-dimethylamino propyl)-3-ethyl carbodiimide hydrochloride and 4-dimethylamino pyridine are dissolved in N,N-dimethyl formamide to react, finally, palladium on carbon is added for catalysis, and after a cleaning reaction, the hydroxytyrosol fibrate carboxylic ester compound is prepared. Operation of the reaction is easy, the requirement for equipment is low, and the compound is environmentally friendly.
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Paragraph 0051
(2016/10/08)
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- 3,4-dihydroxyphenylethanol fenofibrate acid ester as well as preparation method and application thereof
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The invention discloses 3,4-dihydroxyphenylethanol fenofibrate acid ester as well as a preparation method and an application thereof, and belongs to the technical field of drug preparation. The 3,4-dihydroxyphenylethanol fenofibrate acid ester disclosed by the invention is a novel multi-efficacy active compound, can be used for treating diabetes and hyperlipidaemia, can be used for effectively reducing glucose and lipid (triglyceride and cholesterol), can resist lipid peroxidation, and can improve oxidative stress effect under diabetes and hyperlipidaemia states. The invention further discloses a preparation method for the 3,4-dihydroxyphenylethanol fenofibrate acid ester. The preparation method comprises the following steps: protecting 3,4-dihydroxyl of 3,4-dihydroxyl phenethyl alcohol with benzyl; enabling the 3,4-dihydroxyl phenethyl alcohol to condense with fenofibrate acid to synthesize an ester; then, removing the benzyl under the action of hydrogen and palladium/carbon, thereby preparing the 3,4-dihydroxyphenylethanol fenofibrate acid ester. The preparation method is simple to operate, is low in equipment requirement, and is environmentally friendly.
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Paragraph 0045
(2016/12/01)
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- 3,4-dihydroxyphenylethanol nicotinate and preparation method and application thereof
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The invention discloses 3,4-dihydroxyphenylethanol nicotinate and a preparation method and application thereof, and belongs to the technical field of drug preparation. Derivation is conducted on a chemical structure of Niacin, hydroxytyrosol is introduced into the structure of Niacin, the obtained structure is greatly different from that of Niacin, and the effects of lowering blood sugar, lowering blood lipid, resisting oxidation and the like are achieved. The invention further provides a preparation method of a compound HT-N. The method comprises the steps that Niacin reacts with oxalyl chloride, nicotinoyl chloride is obtained, nicotinoyl chloride reacts with benzyl-protected hydroxytyrosol to generate ester, deprotection is conducted, and the compound HT-N is obtained. The preparation method is easy to operate, low in requirement on equipment and environmentally friendly. The novel compound 3,4-dihydroxyphenylethanol nicotinate is used for treating diabetes and hyperlipidaemia, can lower the blood sugar and the blood lipid and can lower malondialdehyde, improve the oxidative stress effect in the diabetes and hyperlipidaemia state and improve liver damage in the diabetic state.
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Paragraph 0036; 0037
(2016/12/22)
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- Synthesis and antioxidant of activity of alkyl nitroderivatives of hydroxytyrosol
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A series of alkyl nitrohydroxytyrosyl ether derivatives has been synthesized from free hydroxytyrosol (HT), the natural olive oil phenol, in order to increase the assortment of compounds with potential neuroprotective activity in Parkinson's disease. In t
- Gallardo, Elena,Palma-Valdés, Rocío,Sarriá, Beatriz,Gallardo, Irene,De La Cruz, José P.,Bravo, Laura,Mateos, Raquel,Espartero, José L.
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- Selective cytotoxic activity of new lipophilic hydroxytyrosol alkyl ether derivatives
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Recent data suggest that hydroxytyrosol, a phenolic compound of virgin olive oils, has anticancer activity. This communication reports the synthesis of decyl and hexadecyl hydroxytyrosyl ethers, as well as the cytotoxic activity of hydroxytyrosol and a series of seven hydroxytyrosol alkyl ether derivatives against A549 lung cancer cells and MRC5 non-malignant lung fibroblasts. Hydroxytyrosyl dodecyl ether (HTDE) showed the highest selective cytotoxicity, and possible mechanisms of action were investigated; results suggest that HTDE can moderately inhibit glycolysis, induce oxidative stress, and cause DNA damage in A549 cells. The combination of HTDE with the anticancer drug 5-fluorouracil induced a synergistic cytotoxicity in A549 cancer cells but not in non-malignant MRC5 cells. HTDE also displayed selective cytotoxicity against MCF7 breast cancer cells versus MCF10 normal breast epithelial cells in the 1-30 μM range. These results suggest that the cytotoxicity of HTDE is more potent and selective than that of parent compound hydroxytyrosol.
- Calderón-Monta?o, José Manuel,Madrona, Andrés,Burgos-Morón, Estefanía,Orta, Manuel Luis,Mateos, Santiago,Espartero, José Luis,López-Lázaro, Miguel
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p. 5046 - 5053
(2013/07/27)
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- Efficient synthesis of hydroxytyrosol from 3,4-dihydroxybenzaldehyde
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Hydroxytyrosol is a naturally occurred orthodiphenolic component of olive oil. A variety of biological functions for this molecule have been reported. We report herein an efficient and practical method for the chemical synthesis of hydroxytyrosol from 2,3-dihydroxybenzaldehyde. Taylor & Francis Group, LLC.
- Zhang, Zhao-Li,Chen, Jinglei,Xu, Qiongming,Rao, Cui,Qiao, Chunhua
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p. 794 - 798
(2012/01/17)
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- PROCESS FOR PRODUCTION OF HYDROXYTYROSOL USING ORGANOMETALLIC COMPOUNDS
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Disclosed is a process for the production of a 4-(2-hydroxyalkyl)-1,2-benzenediol, comprising the steps of (a) providing protected 1,2-benzenediol having the 1,2-hydroxyl groups protected, (b) halogenating the protected 1,2-benzenediol to obtain a protected 4-halo-1,2-benzenediol having the 1,2-hydroxyl groups protected, (c) reacting, in the presence of a metal or organometallic compound, the protected 4-halo-1,2-benzenediol to protected 4-(2-hydroxyalkyl)-1,2-benzenediol having the 1,2-hydroxyl groups protected, and (d) deprotecting the protected 4-(2-hydroxyalkyl)-1,2-benzenediol to obtain the 4-(2-hydroxyalkyl)-1,2-benzenediol. Also disclosed is the use of 1,2-benzenediol for the production of hydroxytyrosol.
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Page/Page column 16
(2012/02/02)
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- Preparation and antioxidant activity of tyrosyl and homovanillyl ethers
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Preparation of tyrosyl and homovanillyl lipophilic derivatives was carried out as a response to the food industry's increasing demand for new synthetic lipophilic antioxidants. Tyrosyl and homovanillyl ethers were synthesized in high yields by a three-step procedure starting from tyrosol (Ty) and homovanillic alcohol (HMV). The antioxidant activity of these new series of alkyl tyrosyl and homovanillyl ethers was evaluated by the Rancimat test in a lipophilic food matrix and by the FRAP, ABTS and ORAC assays and compared to free Ty and HMV as well as two antioxidants widely used in the food industry, butylhydroxytoluene (BHT) and α-tocopherol. The results pointed out the higher activity of homovanillyl series in comparison with tyrosyl series with all the assayed methods. However, while both synthetic series were less antioxidant than BHT and α-tocopherol in a lipophilic matrix after their Rancimat test evaluation, homovanillyl alkyl ethers showed the best reducing power and radical scavenging activity of all evaluated compounds. This batch of synthetic lipophilic compounds, derived from biologically active compounds such as Ty and HMV, provide interesting and potentially bioactive compounds.
- Madrona,Pereira-Caro,Bravo,Mateos,Espartero
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scheme or table
p. 1169 - 1178
(2012/05/05)
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- Differential inhibition of polymerase and strand-transfer activities of HIV-1 reverse transcriptase
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A new class of inhibitors of HIV-1 reverse transcriptase obtained by the systematic structural simplification of epicatechin and epigallocatechin gallates are also shown here to inhibit DNA-strand-transfer, a process critical to the completion of the HIV-1-RT reproduction and to recombination-associated mutation of the virus. Up to 80-fold selectivity for DNA-strand-transfer inhibition over polymerase inhibition was observed for a defined subset of these agents. Such specific DNA-strand-transfer inhibitors may have important therapeutic potential.
- Tillekeratne,Sherette, Angela,Fulmer, Jennifer A,Hupe, Lynn,Hupe, Donald,Gabbara, Sam,Peliska, James A,Hudson, Richard A
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p. 525 - 528
(2007/10/03)
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- Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase
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Systematic simplification of the molecular structures of epicatechin gallate and epigallocatechin gallate to determine the minimum structural characteristics necessary for HIV-1 reverse transcriptase inhibition in vitro resulted in several compounds that strongly inhibited the native as well as the A17 double mutant (K103N Y181C) enzyme, which is normally insensitive to most known nonnucleoside inhibitors.
- Tillekeratne,Sherette,Grossman,Hupe,Hupe,Hudson
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p. 2763 - 2767
(2007/10/03)
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- Antioxidant activity of hydroxytyrosol acetate compared with that of other olive oil polyphenols
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Hydroxytyrosol acetate was synthesized, and the antioxidant activity of this olive oil component was assessed in comparison with that of other olive oil components, namely hydroxytyrosol, oleuropein, 3,4-DHPEA-EA, and α-tocopherol in bulk oil and oil-in-water emulsions. The activity of the compounds was also assessed by scavenging of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals. Hydroxytyrosol acetate had a weaker DPPH radical scavenging activity than hydroxytyrosol, oleuropein, or 3,4-DHPEA-EA but it had a radical scavenging activity similar to that of α-tocopherol. In oil, the antioxidant activity of hydroxytyrosol acetate was much higher than that of α-tocopherol or oleuropein, but in an emulsion 3,4-DHPEA-EA and α-tocopherol were more effective as antioxidants than hydroxytyrosol acetate. The antioxidant activity of hydroxytyrosol acetate was rather similar to that of hydroxytyrosol in oil and emulsions despite the difference in DPPH radical scavenging activity.
- Gordon, Michael H.,Paiva-Martins, Fatima,Almeida, Miguel
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p. 2480 - 2485
(2007/10/03)
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- Catecholamines in a Semi-Rigid Framework: Synthesis and Biological Activities of N-Substituted 1-Aminomethyl-5,6- and 6,7-Dihydroxyisochromans
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With a view to mapping out the essential structural coordinates of catecholamines required for optimal interaction with catecholamine receptors and also to obtain structural variants of the prototype of specific biological interest, a group of N-substitut
- Kumar, Ashok,Khanna, J. M.,Jain, P. C.,Anand, Nitya,Srimal, R. C.,et al.
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- N-Substituted Imidazolines and Ethylenediamines and Their Action on α- and β-Adrenergic Receptors
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A series of N-substituted imidazolines and ethylenediamines were synthesized and examined for their activity in α- and β-adrenergic systems.The length of the intermediate side chain between the catechol and imidazoline ring or the amine of the ethylenedia
- Hamada, Akihiko,Yaden, Emily L.,Horng, J. S.,Ruffolo, Robert R.,Patil, Popat N.,Miller, Duane D.
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p. 1269 - 1273
(2007/10/02)
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