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1.
Int J Ophthalmol ; 16(1): 40-46, 2023.
Article in English | MEDLINE | ID: mdl-36659939

ABSTRACT

AIM: To compare the effect of vegetable oils on the uptake of lutein and zeaxanthin by adult retinal pigment epithelial (ARPE)-19 cells in vitro. METHODS: ARPE-19 cells were cultured in Dulbecco's Modified Eagle Medium-F-12 supplemented with 10% foetal bovine serum and 1% penicillin-streptomycin in a humidified 5% CO2 incubator maintained at 37°C. Cells were treated with 247 µmol/L lutein, 49 µmol/L zeaxanthin and 1% (v/v) of either coconut oil, corn oil, peanut oil, olive oil, sunflower oil, soybean oil, castor oil, or linseed oil for 48h. Lutein and zeaxanthin concentration in the cells were quantified by high performance liquid chromatography. RESULTS: Among the oils tested, the highest lutein and zeaxanthin uptake was observed with coconut oil while the lowest was observed with linseed oil. CONCLUSION: ARPE-19 uptake of lutein and zeaxanthin are found to be dependent on the type of oils.

2.
J Food Biochem ; 44(12): e13535, 2020 12.
Article in English | MEDLINE | ID: mdl-33103260

ABSTRACT

Coffee is rich in antioxidant and has been shown to confer various health benefits. Here, we investigated the effect of single-dose coffee consumption in healthy human subjects. About 30 healthy volunteers were recruited and given a serving of sugar free black coffee. Urine and fecal samples were collected and analyzed. Significant changes in urinary metabolites relating to coffee, gut microbial and host energy metabolisms were observed post-coffee consumption. Clear sex differences were also observed in the urinary metabolic profiles pre- and post-coffee consumption. Sex differences in richness and composition of gut microbiota were observed, however, the effect of single-dose coffee consumption on host gut microbiota were unremarkable. These findings indicated that single-dose coffee consumption affects sex-specific host metabolic responses that relates to gut-microbe and energy metabolism. This study demonstrated the utility of systems biology tools to unravel complexity of host-diet biology and gut microbial responses. PRACTICAL APPLICATIONS: This study demonstrated that integrated systems biology approach enabled efficient extractions of host biochemical and microbial information that allows food industry to ascertain the impact of diet and longitudinal assessment of potential functional food in humans.


Subject(s)
Gastrointestinal Microbiome , Adult , Coffee , Diet , Feces , Female , Humans , Male , Sex Characteristics
3.
Bioorg Med Chem Lett ; 30(4): 126910, 2020 02 15.
Article in English | MEDLINE | ID: mdl-31882300

ABSTRACT

Six N-nitroaryl-2-amino-1,3-dichloropropane derivatives have been prepared and evaluated against 18 cancer cell lines and two non-cancerous cell lines. Analysis of cell viability data and IC50 values indicated that the presence of a trifluoromethyl group in the nitroaryl moiety is an important structural feature associated with the compounds' cytotoxicities.


Subject(s)
Antineoplastic Agents/chemical synthesis , Propane/analogs & derivatives , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Line , Cell Survival/drug effects , Drug Screening Assays, Antitumor , Humans , Methylation , Prodrugs/chemical synthesis , Prodrugs/chemistry , Prodrugs/pharmacology , Propane/chemical synthesis , Propane/chemistry , Propane/pharmacology , Structure-Activity Relationship
4.
Cutan Ocul Toxicol ; 37(1): 52-60, 2018 Mar.
Article in English | MEDLINE | ID: mdl-28554225

ABSTRACT

PURPOSE: Dysfunction of the microRNA (miRNA)-processing enzyme DICER1 and Alu RNA accumulation are linked to the pathogenesis of age-related macular degeneration (AMD). This study determined the optimal dose of lutein (LUT) and zeaxanthin (ZEA) to protect human retinal pigment epithelium (RPE) cells against hydrogen peroxide (H2O2). The effect of the optimal dose of LUT and ZEA as DICER1 and Alu RNA modulators in cultured human RPE cells challenged with H2O2 was investigated. MATERIALS AND METHODS: ARPE-19 cells were pre-treated with LUT, ZEA, or both for 24 h before 200 µM H2O2 challenge. Cell viability was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. DICER1 and Alu RNA were quantified by western blotting and real-time polymerase chain reaction, respectively. RESULTS: H2O2 increased cell Alu RNA expression and decreased cell viability of ARPE-19, but had no significant impact on the DICER1 protein level. LUT, alone and in combination with ZEA pre-treatment, prior to H2O2 challenge significantly improved cell viability of ARPE-19 and reduced the level of Alu RNA compared to the negative control. CONCLUSIONS: These results support the use of LUT alone, and in combination with ZEA, in AMD prevention and treatment. This study is also the first to report LUT modulating effects on Alu RNA.


Subject(s)
Alu Elements/genetics , Epithelial Cells/drug effects , Hydrogen Peroxide/toxicity , Lutein/pharmacology , Macular Degeneration/prevention & control , RNA/metabolism , Retinal Pigment Epithelium/cytology , Cell Line , Cell Survival/drug effects , DEAD-box RNA Helicases/metabolism , Drug Therapy, Combination , Epithelial Cells/metabolism , Humans , Ribonuclease III/metabolism , Zeaxanthins/pharmacology
5.
Bioorg Med Chem Lett ; 26(24): 5851-5854, 2016 12 15.
Article in English | MEDLINE | ID: mdl-27876476

ABSTRACT

A series of N-nitroarylated-3-chloromethyl-1,2,3,4-tetrahydroisoquinoline derivatives, several of which also possessed a trifluoromethyl substituent, were prepared and assessed as potential nitroaromatic prodrugs. The enzymatic reduction of these compounds and their cytotoxicities were studied. The compounds were cytotoxic, but this is probably not related to their enzymatic reduction.


Subject(s)
Enzyme Inhibitors/pharmacology , Escherichia coli/enzymology , NAD(P)H Dehydrogenase (Quinone)/antagonists & inhibitors , Nitroreductases/antagonists & inhibitors , Prodrugs/pharmacology , Tetrahydroisoquinolines/pharmacology , Animals , Cell Line , Cell Survival/drug effects , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Humans , Molecular Structure , NAD(P)H Dehydrogenase (Quinone)/metabolism , Nitroreductases/metabolism , Prodrugs/chemical synthesis , Prodrugs/chemistry , Rats , Structure-Activity Relationship , Tetrahydroisoquinolines/chemical synthesis , Tetrahydroisoquinolines/chemistry
6.
Bioorg Med Chem Lett ; 21(24): 7447-50, 2011 Dec 15.
Article in English | MEDLINE | ID: mdl-22074961

ABSTRACT

A series of 2-nitroaryl-1,2,3,4-tetrahydroisoquinolines 10 and nitro-substituted 5,6-dihydrobenzimidazo[2,1-a]isoquinoline N-oxides 11 have been synthesised and evaluated as potential bioreducible substrates for the enzymes NAD(P)H: quinone oxidoreductase 1 (NQO1) and Escherichia coli nitroreductase (NR). Also prepared and evaluated were 2-(3,5-dinitropyridin-2-yl)-1,2,3,4-tetrahydroisoquinoline 12 and 5,6-dihydro-10-nitropyrido[3″,2″:4',5']imidazo[2',1'-a]isoquinoline 12-oxide 13. Both compounds 10b and 13 were reduced faster by human NQO1 than by CB-1954 [5-(aziridin-1-yl)-2,4-dinitrobenzamide].


Subject(s)
Escherichia coli/enzymology , Heterocyclic Compounds/chemistry , Isoquinolines/chemistry , NAD(P)H Dehydrogenase (Quinone)/metabolism , Nitroreductases/metabolism , Oxides/chemistry , Aziridines/chemistry , Aziridines/pharmacology , Heterocyclic Compounds/chemical synthesis , Heterocyclic Compounds/pharmacology , Humans , Isoquinolines/chemical synthesis , Isoquinolines/pharmacology , Oxides/chemical synthesis , Oxides/pharmacology , Structure-Activity Relationship , Substrate Specificity
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