RESUMEN
Compounds derived from natural sources continue to serve as chemical scaffolds for designing prophylactic/therapeutic options for human healthcare. In this study, we aimed to systematically unravel the chemical profile and antioxidant and anti-inflammatory activities of myrtle methanolic extract (MMEx) using in vitro, in vivo, and in silico approaches. High levels of TPC (415.85 ± 15.52 mg GAE/g) and TFC (285.80 ± 1.64 mg QE/g) were observed. Mass spectrophotometry (GC-MS) analysis revealed the presence of 1,8-cineole (33.80%), α-pinene (10.06%), linalool (4.83%), p-dimethylaminobenzophenone (4.21%), thunbergol (4%), terpineol (3.60%), cis-geranyl acetate (3.25%), and totarol (3.30%) as major compounds. MMEx induced pronounced dose-dependent inhibition in all assays, and the best antioxidant activity was found with H2O2, with an IC50 of 17.81 ± 3.67 µg.mL-1. MMEx showed a good anti-inflammatory effect in vivo by limiting the development of carrageenan-induced paw edema. The pharmacokinetic profiles of the active molecules were determined using the SwissADME website, followed by virtual screening against anti-inflammatory targets including phospholipase A2 (PLA-2), cyclooxygenase-2 (COX-2), tumor necrosis factor alpha (TNF-α), interleukin-1ß (IL-1ß), and NF-κB. A pharmacokinetic study revealed that the molecules have good absorption, distribution, and metabolism profiles, with negative organ toxicity. Among the compounds identified by GC-MS analysis, pinostrobin chalcone, cinnamyl cinnamate, hedycaryol, totarol, and p-dimethylaminobenzophenone were observed to have good binding scores, thus appreciable anti-inflammatory potential. Our study reveals that MMEx from Algerian Myrtus communis L. can be considered to be a promising candidate for alleviating many health complaints associated with oxidative stress and inflammation.
Asunto(s)
Abietanos , Antioxidantes , Myrtus , Humanos , Antioxidantes/farmacología , Myrtus/química , Simulación del Acoplamiento Molecular , Peróxido de Hidrógeno , Antiinflamatorios/farmacología , Extractos Vegetales/farmacologíaRESUMEN
Paw edema volume reduction is a useful marker in determining the anti-inflammatory effect of drugs and plant extracts in carrageenan-induced acute inflammation. In this study, the anti-inflammatory effect of Lobaria pulmonaria (LP) and Parmelia caperata (PC), two lichen species, was examined in carrageenan-induced mouse paw edema test. Compared to the controls in carrageenan-induced inflammation (n = 5/group), our results showed that pretreatment by single oral doses with PC extract (50-500 mg/kg) gives better results than LP extract (50-500 mg/kg) in terms of anti-edematous activity, as after 4 h of carrageenan subplantar injection, paw edema formation was inhibited at 82-99% by PC while at 35-49% by LP. The higher anti-inflammatory effect of PC, at all doses, was also observed on the time-course of carrageenan-induced paw edema, displaying profile closely similar to that obtained with diclofenac (25 mg/kg), an anti-inflammatory drug reference (all p < 0.001). Both LP and PC, at all doses, significantly ameliorated liver catalase (CAT) activity (all p < 0.05). However, superoxide dismutase (SOD) activity, glutathione peroxidase (GPx) activity and glutathione (GSH) levels were found increased in liver of PC- compared to LP-carrageenan-injected mice. Our findings demonstrated on one hand higher preventive effects of PC compared to LP in a mouse carrageenan-induced inflammatory model and suggested, on the other hand, that anti-inflammatory effects elicited by the two lichens were closely associated with the amelioration in the endogenous antioxidant status of liver.
Asunto(s)
Líquenes , Animales , Ascomicetos , Carragenina/metabolismo , Carragenina/toxicidad , Edema/inducido químicamente , Edema/tratamiento farmacológico , Edema/metabolismo , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Hígado/metabolismo , Ratones , Estrés Oxidativo , Extractos Vegetales/farmacologíaRESUMEN
This study aimed to verify whether Olea europaea L. (olive) oil (OEO) exerted a protective effect against oxidative stress induced by deltamethrin (DM) and alterations of pituitary, thyroid and gonadal hormones in adult female rats. DM (0,00256â¯g/kg body weight),OEO (0,6â¯g/kg body weight) and DM with OEO were administered to rats orally for 28 days. Volatile compounds present in olive oil were analysed by GC-MS. Estradiol (E2), Thyroxine (T4),Thyroid Stimulating Hormone (TSH), Triiodothyronine (T3), Follicle Stimulating Hormone (FSH), Luteinizing Hormone (LH), Progesterone (Pg) were measured in serum using Chemiluminescent Microparticle Immunoassay (CMIA). Lipid peroxidation (LPO), protein carbonyls (PCs), reduced glutathione (GSH) levels along with superoxide dismutase (SOD), catalase (CAT), glutathione-S-transferase (GST) and glutathione peroxidase (GPx) activities were determined in thyroid and ovarian tissues. Sesquiterpenes, (E,E)-α-farnesene (16.45%) and α-copaene (9,86%), were analysed as the main volatile compounds of OEO. The relative weight of ovaries and thyroid and body weight significantly decreased in rats treated with DM. DM caused significant alterations in TSH, T4, FSH, Pg and E2 levels while T3 and LH concentrations remained unchanged when compared to control. DM also increased significantly LPO and PCs levels. In addition, GSH reserves as well as CAT, GPx, SOD and GST activities were suppressed in DM-received rats. The presence of OEO with DM returned the levels of oxidative stress markers, thyroid and reproductive hormones at the control values. Our results indicate that OEO is a powerful agent able to protect against DM oxidative stress and endocrine changes.
Asunto(s)
Hormonas/sangre , Insecticidas/toxicidad , Nitrilos/toxicidad , Aceite de Oliva/uso terapéutico , Estrés Oxidativo/efectos de los fármacos , Piretrinas/toxicidad , Animales , Antioxidantes/metabolismo , Catalasa/metabolismo , Estradiol/metabolismo , Femenino , Hormona Folículo Estimulante/metabolismo , Glutatión/metabolismo , Glutatión Peroxidasa/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Hormona Luteinizante/metabolismo , Olea , Aceite de Oliva/farmacología , Ovario/metabolismo , Fitoterapia , Progesterona/metabolismo , Sustancias Protectoras/farmacología , Ratas , Superóxido Dismutasa/metabolismo , Glándula Tiroides/metabolismo , Tirotropina/metabolismo , Tiroxina/metabolismo , Triyodotironina/metabolismo , Vitamina E/farmacologíaRESUMEN
EROD and BFCOD activities were measured in liver and gills of barbel (Barbus callensis, a native North African species) captured at Beni Haroun lake, the most important water reservoir in Algeria. This lake receives wastewater from different origins. Thus, we assessed the level of pollution through the induction of detoxification activities in tissues of barbel, evaluating simultaneously the suitability of this species to be used as a sentinel. Fish were collected between March 2015 and January 2016 at three locations taking into account the pollution sources and accessibility. In liver, EROD and BFCOD showed the highest induction in October specially in the location of the dam that received pollutants. In gills, only EROD, but not BFCOD, activity was detected. Maximal EROD induction was noted in samples from January. Fish cell lines (RTG-2 and PLHC-1) were exposed to sediments extracts collected at Beni Haroun lake and enzyme activities (EROD and BFCOD, respectively) were measured. Sediment extracts did not induce BFCOD activity. The EROD induction observed in RTG-2 cells was in line with the results observed in fish tissues. Our results suggest that the lake is at risk from pollution and that Barbus callensis is a good sentinel species.
Asunto(s)
Cyprinidae/metabolismo , Citocromo P-450 CYP1A1/metabolismo , Branquias/efectos de los fármacos , Lagos/química , Hígado/efectos de los fármacos , Contaminantes Químicos del Agua/análisis , Argelia , Animales , Línea Celular , Monitoreo del Ambiente , Branquias/enzimología , Branquias/metabolismo , Hígado/enzimología , Hígado/metabolismo , Estaciones del Año , Contaminantes Químicos del Agua/toxicidadRESUMEN
Considering the large spectrum of side effects caused by synthetic drugs and the development of natural alternatives utilizing Algerian flora, this study aimed to place a spotlight on the chemical profile and antioxidant and anti-inflammatory activities of Myrtus communis L. essential oils (MCEOs). In this study, essential oils (EOs) were collected via hydro-distillation of the plant's leaves, and a chemical constituent analysis was performed using gas chromatography-mass spectrophotometry (GC-MS). The in vitro antioxidant activity was evaluated using DPPH, ABTS, and hydroxyl radical scavenging tests. The in vitro anti-inflammatory capacity was estimated by studying the antidenaturation effect using bovine serum albumin (BSA) as a protein model. The in vivo anti-inflammatory activity was carried out by utilizing the classical model of carrageenan-induced paw edema in rats, using diclofenac (DCF) as the reference drug. Moreover, the molecular interaction of the compounds obtained from the GC-MS analysis was studied within the binding site of cyclooxygenase-2 (COX-2) using an in silico approach as the confirmatory tool of the in vitro and in vivo experiments. The GC-MS analysis revealed that MCEOs were mainly composed of oxygenated monoterpenes (70.56%), oxygenated sesquiterpenes (3.1%), sesquiterpenes (4.17%), and monoterpenes (8.75%). Furthermore, 1,8-cineole was the major compound (19.05%), followed by cis-geranyl acetate (11.74%), methyl eugenol (5.58%), α-terpineol (4.62%), and ß-myrcene (4.40%). MCEOs exhibited remarkable concentration-dependent free radical scavenging activity, with an IC50 of 15.317 ± 0.340 µg/mL, 18.890 ± 2.190 µg/mL, and 31.877 ± 0.742 µg/mL for DPPH, ABTS, and hydroxyl radical, respectively. The significant in vitro anti-inflammatory activity due to the inhibition of BSA denaturation was proportional to the EO concentration, where the highest value was recorded at 100 µg/mL with an approximately 63.35% percentage inhibition and an IC50 of 60.351 ± 5.832 µg/mL. MCEOs showed a good in vivo anti-inflammatory effect by limiting the development of carrageenan-induced paw thickness. The in silico study indicated that, among the 60 compounds identified by the GC-MS analysis, 9 compounds were observed to have a high binding energy to cyclooxygenase-2 as compared to diclofenac. Our study revealed that EOs from Algerian Myrtus communis L. can be considered to be a promising candidate for alleviating many debilitating health problems and may provide new insights in the fields of drug design, agriculture, and the food industry.
RESUMEN
Concentrations of Cd, Cr, Cu, Pb, and Zn were determined in algae samples collected from the Rabta Bay in the Mediterranean Sea, Algeria. The levels of heavy metals in the macroalgae, Ulva lactuca, Codium fragile (green algae), Jania rubens (red algae), and Dictyota dichotoma (brown algae) recorded high concentrations except for Cd. Moreover, Zn was the most predominant metal in the seaweeds. The obtained HM contents indicate that different species demonstrate various degree of metal accumulation and the obtained higher values in site 1 of the studied zone can be attributed to the discharge influence of two rivers (Mouttas and Larayeche Rivers), entering the Mediterranean Sea and local pollutant emissions. The abundance of heavy metal concentrations in the macroalgae samples was found in the order below: Zn > Cu > Pb > Cr > Cd from the studied zone. The highest amounts of heavy metals in algae samples were Cd, Cu, and Pb in brown algae, and Cr and Zn in green and brown algae from the studied zone (Rabta Bay).
Asunto(s)
Chlorophyta/química , Metales Pesados/análisis , Phaeophyceae/química , Rhodophyta/química , Contaminantes Químicos del Agua/análisis , Argelia , Bahías/química , Cadmio/análisis , Cromo/análisis , Cobre/análisis , Monitoreo del Ambiente , Plomo/análisis , Mar Mediterráneo , Ulva , Contaminación Química del Agua/estadística & datos numéricos , Zinc/análisisRESUMEN
The purpose of this study was to evaluate the protective effect of Pistacia lentiscus oil (PLO), known for its antioxidant properties, on chlorpyrifos (CPF)-induced alterations in the thyroid, reproductive hormone levels, and oxidative damage in the ovaries and thyroid of adult Wistar rats. The animals were treated with orally administered PLO (2 mL/kg), CPF (6.75 mg/kg), and a combination of CPF and PLO for 30 days. Serum levels of luteinizing hormone (LH), follicle-stimulating hormone (FSH), progesterone (Pg), estradiol (E2), triiodothyronine (T3), thyroxine (T4), and thyroid-stimulating hormone (TSH) were assessed using chemiluminescence assay. Malondialdehyde (MDA), protein carbonyl (PC), and reduced glutathione (GSH) levels were examined in the ovaries and thyroid glands. The oil principal volatile compounds detected by gas chromatography analysis were: myrcene, α-pinene and limonene (26.21, 22.66 and 10.33%, respectively). No significant differences were observed between serum concentrations of TSH and FSH in the examined experimental groups. However, serum concentrations of LH, E2, Pg, T3, and T4 decreased significantly in CPF-treated rats in comparison with the controls. The body weight and relative weight of ovaries and thyroids in this group were also significantly reduced. The MDA and PC content increased significantly, while the GSH content was markedly depressed in the thyroid and ovaries of rats treated with CPF. Co-administration of PLO and CPF effectively ameliorated the adverse effects; the oxidative damage was reduced and the levels of thyroid and reproductive hormones restored to a normal range. In conclusion, it appears that PLO substantially alleviates the CPF-induced oxidative damage and hormonal alterations.
Asunto(s)
Cloropirifos/farmacología , Hormonas/metabolismo , Ovario/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Pistacia/química , Sustancias Protectoras/farmacología , Glándula Tiroides/efectos de los fármacos , Animales , Antioxidantes/metabolismo , Femenino , Hormona Folículo Estimulante/metabolismo , Glutatión/metabolismo , Hormona Luteinizante/metabolismo , Malondialdehído/metabolismo , Ovario/metabolismo , Extractos Vegetales/farmacología , Progesterona/metabolismo , Ratas , Ratas Wistar , Glándula Tiroides/metabolismo , Tirotropina/metabolismo , Tiroxina/metabolismo , Triyodotironina/metabolismoRESUMEN
Flavonoids are polyphenols derivatives of plant origin that possesses a broad range of pharmacological properties, including protection of cells and tissues against the deleterious effects of reactive oxygen species. Their antioxidant activity results from scavenging of free radicals and other oxidizing intermediates, from the chelation of iron or copper ions and from inhibition of oxidases. But a number of studies have found both anti and prooxidant effects for many of these compounds. These reasons prompted us to investigate whether flavonoids compounds alone or combined flavonoids had antioxidant, free radical scavenger and antiapoptotic properties. The investigation was carried in vitro using rat hepatic mitochondria. Respiratory control ratio (RCR), oxygen consumption, adenosine tri phosphate (ATP) synthesis, scavenging action, enzymatic activities of involved complexes, superoxide anion and the release of cytochrome C were measured to assess the mechanisms of action of these drugs. Our data showed that the decrease of RCR induced by high concentrations (0.1 mM and 0.01 mM) of all flavonoids tested was due to a common inhibition of oxidative phosphorylation (State 4) and activation of state 3. At the opposite mitochondrial swelling was slightly induced only by low concentrations (10(-8) and 10(-9) M) of the flavonoids. They had no effects on the mitochondrial complexes (I to V) activity. Furthermore the mitochondrial membrane potential was not affected by any flavonoids. The effect of flavonoids on superoxide anion generation was variable. All the flavonoids studied acted between 10(-4) M and 10(-6) M with no effects at lower concentrations. These effects were similar on lipid peroxidation (malondialdehyde [MDA] levels). We remarked a concentration-dependent in the effect of flavonoids since they acted as antioxidant and also as uncoupler at high concentrations, which is a risk for the cells. We conclude that flavonoids extracted from algerian plants have some protecting effects against oxidative stress by protecting the mitochondria.