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1.
Foods ; 12(21)2023 Oct 29.
Article in English | MEDLINE | ID: mdl-37959067

ABSTRACT

The relationship between fruit position, ripening stage, and variety has not been well studied in pepper plants. To understand the interaction of these factors, a diversity of phytochemical traits as well as antioxidant activity were investigated with agronomic traits in eleven hot pepper varieties collected from the upper and lower parts of the plant and harvested at three maturity stages (green, orange, and red). Capsaicin content (CAP) showed a relatively high genetic effect; on the contrary, total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity were more affected by the ripening stage and fruit position. The CAP values ranged from 0.29 ('FKbM') to 0.77 ('Bka') mg CAP equivalents g-1 DW. The ripening stage was the predominant factor for TPC, TFC, DPPH, and FRAP. There was no significant interaction between A × FP, A × RS, and FP × RS for all agro-morphological fruit traits. Variety, fruit position, and ripening stage effects are more significant than all interactions calculated. Lower fruit positions in all samples showed a maximum fruit size, whereas phytochemical traits and yield per plant were relevant in the upper parts, and Phytochemical traits and yield per plant were significantly correlated. From PCA and cluster analysis, all varieties showed the highest biochemical and antioxidant levels with moderate fruit size, except the 'Bel' variety that showed the smallest fruit traits with high yields, and the 'FKbM' and 'FKbK' varieties that showed the highest fruit size but low yields. This study supplies information to identify interesting cultivars with considerable levels of bioactive and phytochemical metabolites, which is useful for breeding programs of novel varieties.

2.
Heliyon ; 9(11): e21139, 2023 Nov.
Article in English | MEDLINE | ID: mdl-37942157

ABSTRACT

We studied the effect of Ajuga iva leaves extract (AIE) on the intestinal absorption, motricity and its antioxidant capacity against diarrhea. Wistar rats were divided and received either: castor oil (CO), CO and loperamide or CO and different doses of AIE. AIE prevented dose-dependently CO-induced diarrhea. AIE at 800 mg/kg showed inhibition efficiency on defecation and diarrhea. The pro-oxidant effect of the CO in the small intestine was inhibited significantly in presence of AIE: increasing glutathione peroxidase (GPx) activity and lowering oxygen free radicals (OH°, O2°-), carbonyl protein and malondialdehyde (MDA) levels. However, co-administration of AIE in castor oil-exposed groups significantly increased the intestinal contents of calcium and magnesium. AIE exhibits significant anti-diarrheal activity, related in part to its antioxidant properties. Our investigation also provides experimental evidence for the traditional use of this medicinal plant in the treatment of diarrhea.

3.
J Plant Physiol ; 216: 145-151, 2017 Sep.
Article in English | MEDLINE | ID: mdl-28641151

ABSTRACT

Vacuoles have been shown to undergo deep modifications in relation to plant developmental stages and in the maintaining the cellular homeostasis. In this context, we studied the variations of the vacuolar membrane size and α-TIP aquaporin distribution at early and advanced seed stages of maturation, germination and embryo growth in Vicia faba cotyledon storage cells.


Subject(s)
Aquaporins/metabolism , Cotyledon/cytology , Cotyledon/metabolism , Fabaceae/metabolism , Germination , Intracellular Membranes/metabolism , Seeds/metabolism , Vacuoles/metabolism , Cotyledon/ultrastructure , Fabaceae/cytology , Fabaceae/embryology , Fabaceae/ultrastructure , Intracellular Membranes/ultrastructure , Seeds/ultrastructure , Starch/metabolism , Vacuoles/ultrastructure
4.
Bioorg Chem ; 72: 301-307, 2017 06.
Article in English | MEDLINE | ID: mdl-28500956

ABSTRACT

Based on the broad spectrum of biological activities associated with organophosphates, a novel type of this class of compounds was synthesized, bearing a nitrile group, from the sodium alkoxide-catalyzed reaction of dialkylphosphites with γ-ketonitriles at 80°C under solvent-free conditions. A reaction mechanism involving a phospha-Brook type rearrangement is proposed. Eight title compounds were investigated for their in vitro inhibitory potency and selectivity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using Ellman's spectrophotometric method. The synthesized derivatives exhibited mostly a moderate activity against both cholinesterases. The IC50 values for BChE were in a smaller concentration range (5.96-23.35µM) compared to those for AChE inhibition (9.61-53.74µM). The diethyl-3-cyano-1-p-tolylpropylphosphate which displayed the higher dual inhibitory potency towards both cholinesterases could be considered as a potential candidate for developing new drugs to treat Alzheimer's disease.


Subject(s)
Acetylcholinesterase/metabolism , Cholinesterase Inhibitors/pharmacology , Organophosphates/pharmacology , Cholinesterase Inhibitors/chemical synthesis , Cholinesterase Inhibitors/chemistry , Dose-Response Relationship, Drug , Humans , Molecular Docking Simulation , Molecular Structure , Organophosphates/chemical synthesis , Organophosphates/chemistry , Structure-Activity Relationship
5.
Biomed Pharmacother ; 90: 203-215, 2017 Jun.
Article in English | MEDLINE | ID: mdl-28363165

ABSTRACT

The present investigation aimed to study the antioxidant activity and hepatoprotective effects of ethyl acetate extract of R. oxyacantha root cortex (RE) against DDT-induced liver injury in male rats. The RE exhibited high total phenolic, flavonoid and condensed tannins contents. The antioxidant activity in vitro systems showed a significant potent free radical scavenging activity of the extract. The HPLC finger print of R. oxyacantha active extract showed the presence of five phenolic compounds with higher amounts of catechol and gallic acid. The in vivo results showed that a single intraperitoneal administration of DDT enhanced levels of hepatic markers (ALT, AST and LDH) in serum of experimental animals. It also increased the oxidative stress markers resulting in increased levels of the lipid peroxidation with a significant induction of SOD and GPx, metallothioneins (MTs) and a concomitant decrease of non protein thiols (NPSH) in liver. However, pretreatment of rats with RE at a dose of 150 and 300mg/kg body weight significantly lowered serum transaminases and LDH in treated rats. A significant reduction in hepatic thiobarbituric reactive substances and a decrease in antioxidant enzymes activities and hepatic MTs levels by treatment with plant extract against DDT, were observed. These biochemical changes were consistent with histopathological observations, suggesting marked hepatoprotective effect of RE with the two doses used. These results strongly suggest that treatment with ethyl acetate extract normalizes various biochemical parameters and protects the liver against DDT-induced oxidative damage in rats and thus help in evaluation of traditional claim on this plant.


Subject(s)
Chemical and Drug Induced Liver Injury/drug therapy , DDT/pharmacology , Liver/drug effects , Plant Extracts/pharmacology , Plant Roots/chemistry , Protective Agents/pharmacology , Rhus/chemistry , Animals , Antioxidants/metabolism , Aspartate Aminotransferases/metabolism , Chemical and Drug Induced Liver Injury/metabolism , Lipid Peroxidation/drug effects , Liver Function Tests/methods , Male , Oxidation-Reduction/drug effects , Oxidative Stress/drug effects , Phenols/pharmacology , Rats , Rats, Wistar
6.
Asian Pac J Trop Med ; 9(8): 757-62, 2016 Aug.
Article in English | MEDLINE | ID: mdl-27569884

ABSTRACT

OBJECTIVES: To evaluate the contributions of the some quantum dots in different biological uses in order to valorizes such nanomaterials for further applications. METHODS: Zinc sulfide ZnS nanoparticles were synthesized in aqueous medium at pH constant, the obtained nanoparticles has been characterized by X-ray diffraction (XRD), transmission electron microscopy (TEM) and Fourier Transform Infra-red (FTIR) spectroscopies. Zinc sulfide nanoparticles were screened for their antibacterial and antifungal profiling and tested for antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl radical (OH) and hydrogen peroxide (H2O2) scavenging activity, ferric reducing power (FRP) assay and ferrous ion chelating (FIC) methods. RESULTS: The sizes of the crystallites were estimated to 3 nm using the Debye-Scherrer formula based on the XRD data. The shape was identified to be quasi-spherical with agglomerated particles. The obtained ZnS quantum dots present an antioxidant activity especially in oxido-reduction power, and can be used for species profiling either for bacteria and fungus. CONCLUSION: It was found that ZnS nanoparticles showed relatively higher antioxidant activities and antibacterial with an antifungal behavior which proves that this nanomaterials can react at the interface with the life entities.

7.
Biomed Pharmacother ; 83: 186-193, 2016 Oct.
Article in English | MEDLINE | ID: mdl-27470564

ABSTRACT

Obesity is associated with an oxidative stress status, which is defined by an excess of reactive oxygen species (ROS) vs. the antioxidant defense system. We report in this present work, the link between fat deposition and oxidative stress markers using a High Fat Diet-(HFD) induced rat obesity and liver-oxidative stress. We further determined the impact of chronic administration of 3-keto-1, 5-BPs 1 (a & b) (40µg/kg/8 weeks/i.p.) on liver's level. In fact, exposure of rats to HFD during 16 weeks induced body and liver weight gain and metabolic disruption with an increase on liver Alanine amino transférase (ALAT) and Aspartate aminotransférase (ASAT) concentration. HFD increased liver calcium level as well as free iron, whereas, it provoked a decrease on liver lipase activity. HFD also induced liver-oxidative stress status vocalized by an increase in reactive oxygen species (ROS) as superoxide radical (O2), hydroxyl radical (OH) and Hydrogen peroxide (H2O2). Consequently, different deleterious damages as an increase on Malon Dialdehyde MDA, Carbonyl protein PC levels with a decrease in non-protein sulfhydryls NPSH concentrations, have been detected. Interestingly, our results demonstrate a decrease in antioxidant enzymes activities such as superoxide dismutase (SOD), catalase (CAT), glutathione peroxidases (GPx) and peroxidases (POD). Importantly, 3-keto-1,5-bisphosphonates treatment corrected the majority of the deleterious effects caused by HFD, but it failed to correct some liver's disruptions as mineral profile, oxidative damages (PC and NPSH levels) as well as SOD and lipase activities. Our investigation point that 3-keto-1,5-bisphosphonates could be considered as safe antioxidant agents on the hepatic level that should also find other potential biological applications.


Subject(s)
Diphosphonates/pharmacology , Liver/pathology , Obesity/pathology , Animals , Antioxidants/metabolism , Diphosphonates/chemistry , Lipids/blood , Liver/drug effects , Male , Obesity/blood , Rats, Wistar , Reactive Oxygen Species/metabolism
8.
Chem Biol Drug Des ; 86(3): 291-301, 2015 Sep.
Article in English | MEDLINE | ID: mdl-25483977

ABSTRACT

Obesity has become a leading global health problem owing to its strong association with a high incidence of oxidative stress. Many epidemiologic studies showed that an antioxidant supplementation decreases the state of oxidative stress. In the present work, a HFD-induced rat obesity and oxidative stress were used to investigate the link between fat deposition and serum-oxidative stress markers. We also studied the effect of a chronic administration of 3-keto-1,5-bisphosphonates 1 (a & b) (40 µg/kg/8 weeks/i.p.). Exposure of rats to HFD during 16 weeks induced fat deposition, weight gain and metabolic disruption characterized by an increase in cholesterol, triglyceride and glycemia levels, and a decrease in ionizable calcium and free iron concentrations. HFD also induced serum-oxidative stress status vocalized by an increase in ROS (H2 O2 ), MDA and PC levels, with a decrease in antioxidant enzyme activity (CAT, GPx, SOD). Importantly, 3-keto-1,5-bisphosphonates corrected all the deleterious effects of HFD treatment in vivo, but it failed to inhibit lipases in vitro and in vivo. These studies suggest that 3-keto-1,5-bisphosphonates 1 could be considered as safe antioxidant agents that should also find other potential biological applications.


Subject(s)
Diphosphonates/pharmacology , Obesity/blood , Obesity/drug therapy , Oxidative Stress/drug effects , Animals , Antioxidants/pharmacology , Body Weight , Cholesterol/blood , Diet, High-Fat/adverse effects , Diphosphonates/chemical synthesis , Disease Models, Animal , Free Radicals/metabolism , Hydrogen-Ion Concentration , Lipase/antagonists & inhibitors , Male , Rats , Rats, Wistar , Reactive Oxygen Species/metabolism
9.
Med Chem ; 11(2): 206-13, 2015.
Article in English | MEDLINE | ID: mdl-25000984

ABSTRACT

Herein we report an efficient, simple and green synthesis of novel types of α-hydroxyphosphonates bearing a nitrile group, from the reaction of γ-ketonitriles with dialkyl phosphites in the presence of magnesium oxide as solid support, under solvent-free conditions. All the title compounds were screened for their antioxidant activity by 1,1-diphenyl-2- picrylhydrazyl (DPPH), hydroxyl radical, reducing power and ferrous ion chelating (FIC) methods and they showed significant antioxidant activity.


Subject(s)
Antioxidants/chemical synthesis , Drug Design , Green Chemistry Technology , Iron Chelating Agents/chemical synthesis , Organophosphonates/chemical synthesis , Antioxidants/chemistry , Antioxidants/pharmacology , Biphenyl Compounds/chemistry , Free Radicals/chemistry , Iron Chelating Agents/chemistry , Iron Chelating Agents/pharmacology , Molecular Structure , Organophosphonates/chemistry , Organophosphonates/pharmacology , Picrates/chemistry
10.
Toxicol Int ; 20(3): 268-74, 2013 Sep.
Article in English | MEDLINE | ID: mdl-24403737

ABSTRACT

BACKGROUND: Mannich bases are an important class of compounds in medicinal chemistry with a wide spectrum of biological activities, however, knowledge on their toxicity is limited. MATERIALS AND METHODS: Two Mannich base hydrochlorides 1a (2-thienyl-ß-dimethylaminoethyl ketone hydrochloride) and 1b (ß-dimethylaminopropiophenone hydrochloride) were synthesized and characterized on the basis of their infrared and nuclear magnetic resonance spectral data. The potential effects of the synthesized compounds (5 mg/kg, i.p, during 30 days) on relative weight, hematological parameters, biochemical parameters, and neurotoxicity were tested using male Wistar rat. RESULTS: The results showed that compound 1b alters body weight on the first 10 days (182%, P < 0.01) and on the last 10 days (107%, P < 0.01) of treatment. The same treatment decreases food intake (P < 0.01) and increases water intake (P < 0.05). Both compounds induced a deficit on rotarod test manifested by a decrease of grasping time (1a: 65.33%, P < 0.01; 1b: 60.55%, P < 0.01) and fall time (1a: 59.75%, P < 0.01; 1b: 56.81%, P < 0.01) only on the last day of training. Moreover, Mannich base 1b decreases the liver relative weight (22.24%, P < 0.01). It was also observed that both products decrease the total serum cholesterol (Ch) levels (1a: 52.87%, P < 0.01; 1b: 64.70%, P < 0.01). Interestingly, compounds 1a and 1b affect hematological parameters manifested by an increase of the number of white blood cells (1a: 32.29%, P < 0.05; 1b: 20.64%, P < 0.05) and red blood cells (RBCs) (1a: 12.57%, P < 0.05; 1b: 20.11%, P < 0.05), an increase of red cell hemoglobin concentration (1a: 10.48%, P < 0.05; 1b: 16.12%, P < 0.05) and of the volume occupied by RBCs or hematocrit (1a: 18.28%, P < 0.05; 1b: 15.56%, P < 0.05), and an increase of the number of platelets (1a: 16.80%, P < 0.05; 1b: 39.96%, P < 0.05) accompanied by a decrease in hemoglobin level only with the compound 1a (7.41%, P < 0.05). CONCLUSION: These results show that both compounds 1a and 1b induced a hypoxia status associated to low level of Ch and liver toxicity. The deficit observed by rotarod could be explained by the myorelaxant effect of the used products.

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