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Heavy metals are encountered in nature, and are used in several human endeavors, including in dental fillings. It is well known that the safety of metals depends on their chemical form, as well as the dose and route through which biological systems are exposed to them. Here, we used the Nauphoeta cinerea model to examine the mechanism by which salts of the heavy metals used in dental fillings - silver and mercury - exert their neurotoxicity. Nymphs exposed to heavy metals presented with reduced motor and exploratory abilities as they spent more time immobile, especially in the periphery of a novel object, and covered less distance compared with control nymphs. Exposure to AgNO3 and HgCl2 also exacerbated levels of oxidative stress markers (MDA & ROS) and the neurotransmitter regulators - AChE and MAO, while reducing antioxidant activity markers, both in biochemical (thiol & GST) and RT-qPCR (TRX, GST, SOD, Catalase) examinations, in neural tissues of the cockroach. The observed disruptions in neurolocomotor control, synaptic transmission and redox balance explain how heavy metal salts may predispose organisms to neurological disorders.
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Oxidación-Reducción , Estrés Oxidativo , Animales , Oxidación-Reducción/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Mercurio/toxicidad , Plata/farmacología , Plata/toxicidad , Neurotransmisores/metabolismo , Acetilcolinesterasa/metabolismo , Ninfa/efectos de los fármacos , Ninfa/metabolismo , Monoaminooxidasa/metabolismo , Conducta Animal/efectos de los fármacos , Especies Reactivas de Oxígeno/metabolismo , Nitrato de Plata/farmacología , Cloruro de Mercurio/toxicidadRESUMEN
BACKGROUND: The study investigated the effect of co-administration of curcumin and donepezil on several markers of cognitive function (such as spatial memory, astrocyte activation, cholinesterase expressions) in the brain cortex and hippocampus of scopolamine-treated rats. METHOD AND RESULTS: For seven consecutive days, a pre-treatment of curcumin (50 mg/kg) and/or donepezil (2.5 mg/kg) was administered. On the seventh day, scopolamine (1 mg/kg) was administered to elicit cognitive impairment, 30 min before memory test was conducted. This was followed by evaluating changes in spatial memory, cholinesterase, and adenosine deaminase (ADA) activities, as well as nitric oxide (NO) level were determined. Additionally, RT-qPCR for glial fibrillary acidic protein (GFAP) and cholinesterase gene expressions was performed in the brain cortex and hippocampus. Also, GFAP immunohistochemistry of the brain tissues for neuronal injury were performed in the brain cortex and hippocampus. In comparison to the control group, rats given scopolamine had impaired memory, higher levels of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and ADA activities, as well as elevated markers of oxidative stress. In addition to enhanced GFAP immunoreactivity, there was also overexpression of the GFAP and BChE genes in the brain tissues. The combination of curcumin and donepezil was, however, observed to better ameliorate these impairments in comparison to the donepezil-administered rat group. CONCLUSION: Hence, this evidence provides more mechanisms to support the hypothesis that the concurrent administration of curcumin and donepezil mitigates markers of cognitive dysfunction in scopolamine-treated rat model.
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Acetilcolinesterasa , Astrocitos , Curcumina , Donepezilo , Proteína Ácida Fibrilar de la Glía , Hipocampo , Escopolamina , Memoria Espacial , Animales , Donepezilo/farmacología , Curcumina/farmacología , Curcumina/administración & dosificación , Escopolamina/farmacología , Astrocitos/efectos de los fármacos , Astrocitos/metabolismo , Ratas , Masculino , Memoria Espacial/efectos de los fármacos , Acetilcolinesterasa/metabolismo , Acetilcolinesterasa/genética , Hipocampo/efectos de los fármacos , Hipocampo/metabolismo , Proteína Ácida Fibrilar de la Glía/metabolismo , Proteína Ácida Fibrilar de la Glía/genética , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Ratas Wistar , Estrés Oxidativo/efectos de los fármacos , Colinesterasas/metabolismo , Adenosina Desaminasa/metabolismo , Adenosina Desaminasa/genética , Butirilcolinesterasa/metabolismo , Butirilcolinesterasa/genética , Óxido Nítrico/metabolismo , Inhibidores de la Colinesterasa/farmacología , Inhibidores de la Colinesterasa/administración & dosificaciónRESUMEN
Malaria impedes the ability of primary cells of the immune system to generate an efficacious inflammatory and immune response. Black seed (Nigella sativa) is a core dietary supplement and food additive in folklore. This study investigated the antioxidant, immunomodulatory, and anti-inflammatory effects of N. sativa cookies in Plasmodium berghei-infected mice. Aqueous extract of black seed was prepared, and the total phenol and flavonoid contents were determined. The mice were infected with standard inoculum of the strain NK65 P. berghei. The mice weight and behavioral changes were observed. The mice were fed with the N. sativa cookies (2.5%, 5%, and 10%) and 10 mg/kg chloroquine for 5 consecutive days after the infection was established. The reactive oxygen species (ROS), malondialdehyde (MDA), superoxide dismutase, catalase, and hematological parameters (red cell indices, leukocytes, and its differentials) in the infected mice were determined. The inflammatory mediators, C-reactive protein (CRP), and myeloperoxidase (MPO) were also assayed. The result revealed that black seed had a total phenol content of 18.73 mgGAE/g and total flavonoid content of 0.36 mgQUE/g. The infected mice treated with N. sativa cookies showed significantly decreased parasitaemia, MDA, and ROS levels. Furthermore, the results showed significant suppression in proinflammatory mediators (CRP and MPO) levels and enhanced antioxidant status of infected mice treated with N. sativa. The study suggests that N. sativa could function as nutraceuticals in the management of Plasmodium infection associated with inflammatory and immunomodulatory disorders.
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Malaria , Nigella sativa , Estrés Oxidativo , Extractos Vegetales , Plasmodium berghei , Semillas , Animales , Plasmodium berghei/efectos de los fármacos , Malaria/tratamiento farmacológico , Malaria/inmunología , Estrés Oxidativo/efectos de los fármacos , Ratones , Nigella sativa/química , Semillas/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Masculino , Antioxidantes/farmacología , Modelos Animales de Enfermedad , Especies Reactivas de Oxígeno/metabolismo , Malondialdehído/metabolismo , Inflamación/tratamiento farmacológico , Antiinflamatorios/farmacología , Alimentos Fortificados , Proteína C-Reactiva/metabolismo , Proteína C-Reactiva/análisis , Superóxido Dismutasa/metabolismo , Humanos , Flavonoides/farmacología , Flavonoides/uso terapéutico , Peroxidasa/metabolismoRESUMEN
OBJECTIVES: This study aims to evaluate the neuroprotective effect of caffeic acid (CAF) against cadmium chloride (CdCl2) in rats via its effect on memory index as well as on altered enzymatic activity in the brain of CdCl2-induced neurotoxicity. METHODS: The experimental rats were divided into seven groups (n=6 rats per group) of healthy rats (group 1), CdCl2 -induced (CD) (3â¯mg/kg BW) rats (group 2), CD rats + Vitamin C (group 3), CD rats + CAF (10 and 20â¯mg/kg BW respectively) (group 4 & 5), and healthy rat + CAF (10 and 20â¯mg/kg BW respectively) (group 6 & 7). Thereafter, CdCl2 and CAF were administered orally to the experimental rats in group 2 to group 5 on daily basis for 14 days. Then, the Y-maze test was performed on the experimental rats to ascertain their memory index. RESULTS: CdCl2 administration significantly altered cognitive function, the activity of cholinesterase, monoamine oxidase, arginase, purinergic enzymes, nitric oxide (NOx), and antioxidant status of Cd rats (untreated) when compared with healthy rats. Thereafter, CD rats treated with vitamin C and CAF (10 and 20â¯mg/kg BW) respectively exhibited an improved cognitive function, and the observed altered activity of cholinesterase, monoamine oxidase, arginase, purinergic were restored when compared with untreated CD rats. Also, the level of brain NOx and antioxidant status were significantly (p<0.05) enhanced when compared with untreated CD rats. In the same vein, CAF administration offers neuro-protective effect in healthy rats vis-à-vis improved cognitive function, reduction in the activity of some enzymes linked to the progression of cognitive dysfunction, and improved antioxidant status when compared to healthy rats devoid of CAF. CONCLUSIONS: This study demonstrated the neuroprotective effect of CAF against CdCl2 exposure and in healthy rats.
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Encéfalo , Cloruro de Cadmio , Ácidos Cafeicos , Trastornos de la Memoria , Fármacos Neuroprotectores , Ratas Wistar , Animales , Ratas , Trastornos de la Memoria/inducido químicamente , Trastornos de la Memoria/tratamiento farmacológico , Trastornos de la Memoria/metabolismo , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Ácidos Cafeicos/farmacología , Masculino , Fármacos Neuroprotectores/farmacología , Aprendizaje por Laberinto/efectos de los fármacos , Antioxidantes/farmacología , Antioxidantes/metabolismo , Monoaminooxidasa/metabolismo , Memoria/efectos de los fármacos , Colinesterasas/metabolismo , Óxido Nítrico/metabolismo , Arginasa/metabolismoRESUMEN
INTRODUCTION: The present study aimed at investigating the effect of dietary supplementation of Phoenix dactylifera, an important component of aphrodisiac supplements, on sexual performance, oxido-inflammatory mediators and purinergic signaling system in hypertensive rats. MATERIAL AND METHODS: Hypertension was induced via oral administration of 40 mg/kg L-NAME. Thereafter, the sexual performance of the experimental animals was determined and the hypertensive rats with impaired sexual activities were placed on P. dactylifera-supplemented diet for 21 days, and the effects of the treatment on the overall sexual behavior, antioxidant status, oxido-inflammatory biomarkers, and enzyme activity of the purinergic system were assessed. RESULTS: Hypertensive rats showed a significant (p < 0.05) decrease in sexual performance, elevated level of oxido-inflammatory mediators, and altered purinergic enzymes activity when compared with the control. However, sub-chronic feeding with P. dactylifera-supplemented diet improved sexual performance, significantly lowered oxido-inflammatory biomarkers, and enhanced the activity of purinergic enzymes in hypertensive rats. CONCLUSION: Findings presented in this study suggest that dietary inclusion of P. dactylifera could be useful in managing erectile dysfunction (ED) commonly observed in subjects with hypertension. Findings highlighted in this study thus provide the scientific basis supporting the folkloric use of P. dactylifera as a key ingredient in aphrodisiac supplements.
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Afrodisíacos , Hipertensión , Phoeniceae , Humanos , Ratas , Masculino , Animales , Frutas , Afrodisíacos/efectos adversos , Hipertensión/inducido químicamente , BiomarcadoresRESUMEN
Ocimum basilicum is an important medicinal plant and culinary herb generally known as sweet basil (SB). These plants are effective radical scavengers, that have been employed in treatment of nervous system disorders, and thus, could be beneficial for the management of neurodegenerative diseases (NDs). Current clinical treatments for NDs present several side effects, therefore, there is need to develop new treatments that can mitigate these deadly diseases. Hence, this study investigated the neuroprotective activities of SB leaf and seed in aluminum chloride (AlCl3)-induced toxicity in Drosophila melanogaster. HPLC characterization of the leaves and seeds were carried out. AlCl3-diet was used to induce neurodegeneration and treated flies received SB leaf and seed extracts-supplemented diet. Survival and locomotor performance activities/levels of oxidative biomarkers [reactive oxygen species (ROS), thiobarbituric acid reactive species (TBARS), total thiol, catalase, superoxide dismutase (SOD) and glutathione-S-transferase (GST)], enzymes linked with neurodegeneration (acetylcholinesterase (AChE) and monoamine oxidase (MAO)) were investigated. SB leaf had significantly (p < 0.05) higher polyphenol contents; gallic acid and P-coumaric acid were the most abundant polyphenol in the leaf and seed respectively. Percentage survival and locomotor rates, level/activities of total thiol, catalase, SOD and GST were significantly (p < 0.05) reduced while ROS, TBARS, AChE and MAO activities were significantly (p < 0.05) increased in AlCl3-diet-fed flies. Treatment with SB leaf and seed diet lessened these observed impairments. However, SB leaf had better neuroprotective activities that could be related to the observed higher phenolic constituents. Hence, SB leaf diet may offer improved therapeutic effect in NDs.
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Introduction: Africa faces immense food and health insecurity challenges, a problem partly attributed to food loss and waste during postharvest handling and distribution. In the context of research to meet the sustainable development goals, this project specifically addressed the postharvest loss of the ripe indigenous eggplant (Solanum anguivi lam) fruit called "Igba Yinrin" by Yoruba in South-West Nigeria, which is usually discarded in farms. The study was carried out on ripe and unripe fruits to better understand their value by comparing their effects in diabetes treatment. Methods: The study sought to assess the effects of a diet including ripe or unripe mature eggplant fruits in the sucrose-induced diabetic-like fruit fly. Bioactive compounds were identified and quantified with HPLC-UV, while the antioxidant vitamin (A, C, E), carotenoid, and mineral (Na, K, Ca, Mg, Fe, P, and Zn) content was analyzed in the fruits. Extracts were used to investigate their in vitro anti-inflammatory properties on cyclooxygenases (COX 1 and 2), 5-lipoxygenase (5-LOX), and anti-diabetes enzymes [α-amylase and α-glucosidase], while extract-supplemented diets (0.25-1% concentration) were fed to the fruit flies for 14 days. Results: Interestingly, the results showed that the ripe fruits had a significantly (p < 0.05) higher total phenol and flavonoid content, as well as a higher content of vitamins, carotenoids, and minerals, than the unripe fruits. The in vivo activities of antioxidant enzymes [superoxide dismutase (SOD), catalase (CAT), and glutathione transferase (GST)] and the total thiol level increased, while the blood glucose, reactive oxygen species (ROS), and malondialdehyde (MDA) levels decreased in Drosophila melanogaster (fruit fly). An in silico docking analysis showed strong binding affinity of the above-mentioned enzymes under investigation with the ligands hesperidin, naringin, and myricetin, which are bioactive compounds contained in the examined extracts. Conclusions: There was no significant difference in the biological effects of the ripe and unripe fruit extracts on inflammatory and anti-diabetes enzyme activities, which means that the ripe fruit, usually discarded, could serve as a sustainable alternative source of food nutrients.
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OBJECTIVES: This research work studied the phenolic composition of Pentaclethra macrophylla (PM), the inclusion of dietary supplementation of PM leaves on sexual functions and its connection to inhibit enzymes (arginase and phosphodiesterase-5) and nitric oxide level, linked to type 2 diabetes-induced erectile dysfunction in rats. METHODS: Gallic acid, chlorogenic and ellagic acids, Kaempferol, and epicatechin etc. was spotted with High performance liquid chromatography-diode array detector from PM extract. Twenty-five (25) rats were used for the study. Five rats were placed with basal diet; diets not supplemented with PM leaves (normal rat group) while twenty rats were made diabetic by feeding them with high fat diet for two weeks, prior to single injection with 35â¯mg/kg of streptozotocin (STZ). After checking with glucometer, experimental animals with blood glucose level >250â¯mg/dL were accepted as diabetic. The diabetic rats were subsequently divided into four groups of five rats each (n=5). The diabetic rats were placed on basal diet, or diets supplemented with PM leaves (10â¯% or 5â¯% inclusion) or sildenafil citrate (SC). RESULTS: The result revealed that PM supplemented diets caused significant (p<0.05) reduction in blood glucose level, and augmented erectile function by inhibiting arginase and PDE5 activities as well as enhancing nitric oxide level. CONCLUSIONS: In conclusion, dietary inclusion of PM leaves could serve as a potent nutraceutical source in hyperglycemia induced erectile dysfunction management.
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Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Disfunción Eréctil , Masculino , Humanos , Ratas , Animales , Disfunción Eréctil/tratamiento farmacológico , Disfunción Eréctil/etiología , Glucemia , Diabetes Mellitus Experimental/complicaciones , Óxido Nítrico , Arginasa , Piperazinas/farmacología , Óxido Nítrico Sintasa de Tipo IIIRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: The King of Bitters (Andrographis paniculata) is a plant used to cure a wide range of infectious diseases which includes malaria, fever and others. However, there is a paucity of scientific evidence of its effect on male reproductive indices during malaria treatment. AIM OF THE STUDY: The aim of this study is to evaluate the effect of supplemented diet on antiplasmodial, hematological and male reproductive indices in mice infected with Plasmodium berghei. MATERIALS AND METHODS: Aqueous extract of A. paniculata (King of Bitters, KGB) was prepared and the total phenol and flavonoid contents were determined. Forty-two mice, weighing 20-25 g, were distributed into 7 groups consisting of 6 mice each. The mice were innoculated with strain NK65 Plasmodium berghei (Chloroquine, CQ sensitive) and the parasitemia suppression was assessed. The mice were fed with the dietary supplementation of KGB at varying inclusions (2.5%, 5%, 7.5%, and 10%) and administered 10 mg/kg CQ (which served as the positive control) for 5 consecutive days after infection was established. The reactive malondialdeahyde (MDA), antioxidant [superoxide dismutase (SOD), catalase (CAT), reduced glutathione (GSH)] and the hematological (hemoglobin, packed cell volume and red blood cell) parameters in the infected mice were determined. The reproductive indices (serum testosterone, luteinizing hormone (LH), follicle-stimulating hormone (FSH), sperm count, sperm motility, and sperm viability) and testis histopathology were also assessed. RESULT: The result revealed that KGB had a total phenol content of 32.55 mgGAE/g and total flavonoid content of 19.71 mgQUE/g. The infected mice treated with the dietary supplementation of KGB showed significantly decreased (p < 0.05) parasitaemia and MDA levels. Furthermore, the 7.5% dietary inclusion showed significant improvement in the antioxidant, hematological and reproductive indices as well as the restoration of testis morphology as seen in the histopathology plate of the infected mice treated with KGB. Hence, this study suggests that the KGB- supplemented diet (7.5%) may be a potential alternative and complementary therapy in the treatment of malaria infection and reproductive disorders.
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Antimaláricos , Malaria , Masculino , Animales , Ratones , Antimaláricos/farmacología , Antimaláricos/uso terapéutico , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Plasmodium berghei , Andrographis paniculata , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Motilidad Espermática , Semillas , Malaria/tratamiento farmacológico , Suplementos Dietéticos , Dieta , Flavonoides/farmacología , Fenoles/farmacologíaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: West African Albizia (Albizia zygia DC J. F. Macbr) leaves are a tropical plant that are frequently used in folkloric medicine to treat a number of illnesses, including type 2 diabetes (TY2D) and erectile dysfunction (ED), without having a complete scientific foundation. AIM OF THE STUDY: This investigation examined the effect of action of dietary augmentation of Albizia zygia leaves (AZL) on rat sexual functioning and important enzymes related to TY2D and ED. MATERIALS AND METHODS: Thirty matured adult Wistar rats of the weight 180-200 g were acclimatized in a lab environmental condition for two weeks prior to experiment given food and water to acclimate. Twenty-four of the rats got high fat diet (HFD) for periods of two weeks before receiving streptozotocin (STZ) intraperitoneally (i.p.), 35 mg/kg body weight single dose. Six rats got basal diets. Type 2 diabetes was identified in rats 72 h after STZ treatment. Rats were then used to evaluate the mounting number, mount delay, intromission number, and intromission latency. RESULTS: Following that, meals supplemented with AZL (5% or 10% inclusion) were given to diabetic-ED rats for 14 days. AZL was added. Therefore, in diabetic-ED rats, AZL supplementation could significantly (p0.05) lower blood glucose levels and the activities of alpha amylase, alpha glucosidase, phosphodiesterase-5, and arginase. In the case of diabetic-ED treated rats in consideration with diabetic-ED control group, nitric oxide levels were increased along with sexual function. CONCLUSION: Thus, experimental results of this study demonstrated rats that consumed AZL in their diets had less erectile dysfunction. In order to address ED caused by diabetes, AZL could be suggested as functional meals.
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Albizzia , Afrodisíacos , Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Disfunción Eréctil , Masculino , Humanos , Ratas , Animales , Disfunción Eréctil/tratamiento farmacológico , Disfunción Eréctil/etiología , Afrodisíacos/farmacología , Erección Peniana , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Diabetes Mellitus Tipo 2/complicaciones , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Ratas Wistar , Diabetes Mellitus Experimental/complicaciones , DietaRESUMEN
In folk medicine, the almond nut (Terminalia catappa) and orange peel (Citrus sinensis) are cost-effective sources of nutraceutical utilized in the treatment of degenerative diseases. Hyperlipidemia and hypertension are two pathological conditions implicated in cardiovascular disorders. This study sought to evaluate the cardiomodulatory effect of almond-citrus peel fortified shortbread in hyperlipidemic-hypertensive rats induced by high fat diet and Nω-nitro-l-arginine methyl ester. The experimental animals were divided into eight groups. The experimental rats were fed with shortbread supplemented with almond and citrus peel at varying inclusions of 0.2% citrus, 50% almond, and almond (50%)- citrus (0.2%) for 21 days. The mean arterial blood pressure (MABP), systolic blood pressure (SBP), and lipid profile of the experimental rats were measured. Thereafter, the activities of angiotensin-1-converting enzyme (ACE), arginase, malondialdehyde (MDA), phosphodiesterase-5, nitric oxide (NO), and antioxidant indices were evaluated. The result showed significant elevation in SBP, MABP, blood cholesterol, triglyceride, ACE, arginase, activities, and MDA levels in the heart tissue of the untreated rats. In contrast, the antioxidant status and NO level were significantly decreased in the untreated groups. Remarkably, the treatment with almond-citrus peel fortified shortbread and the individual effect of almond (50%) and citrus peel (0.2%) all reversed these trends in the hyperlipidemic-hypertensive rats. Intriguingly, the blend of almond (50%)-citrus peel (0.2%) fortified shortbread showed the best antioxidative and cardioprotective effect. The results suggest that almond and citrus peel offer potentials as therapeutic agent in the prevention and management of hyperlipidemia and hypertension.
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Citrus , Cardiopatías , Prunus dulcis , Masculino , Animales , Ratas , Ratas Wistar , Antioxidantes/farmacología , Prunus dulcis/química , Citrus/química , Hipertensión , Cardiopatías/prevención & control , Hiperlipidemias , NG-Nitroarginina Metil Éster/farmacología , Dieta Alta en GrasaRESUMEN
This study evaluated the effect of dietary inclusions of aspartame and sucrose on some selected behavioral and biochemical indices linked with Alzheimer's disease in a transgenic fruit fly (Drosophila melanogaster) model expressing human amyloid precursor protein and secretase. Flies were raised on a diet supplemented with sucrose and aspartame for 14 days. Thereafter, the flies were assessed for their survival rate, learning and memory, as well as locomotor performance, 14 days post-treatment. This was followed by homogenising the fly heads, and the homogenates were assayed for acetylcholinesterase and monoamine oxidase activities, as well as levels of lipid peroxidation, reactive oxygen species, and total thiol. The results showed aspartame at all levels of dietary intake and a high proportion of sucrose significantly aggravated the mortality rate, locomotor deficiency, and impaired biomarkers of oxidative stress and antioxidant status in the transgenic flies, while no significant effect was found on acetylcholinesterase activity or memory function. These findings therefore suggest that while low dietary inclusions of sucrose are tolerable under AD-like phenotypes in the flies, high inclusions of sucrose and all proportions of aspartame tested aggravated mortality rate, locomotion and oxidative stress in the flies.
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Most teenagers mix up various psychoactive cocktail substances in combinations to get intoxicated. The role of the mixture combination of codeine (CDE), tramadol (TMD), and Cannabis sativa (CNB) on brain cognition, purinergic, cholinergic, and antioxidant enzyme activities remains unknown. This study sought to assess the mechanism of action of combinations of CDE+ TMD+ CNB on the function and activities of the brain of male Wistar rats. Forty-eight male Wistar rats were divided into 8 groups, n = 6. Group 1 served as a control, groups 2, 3, and 4 were exposed to CDE (2 mg/kg bw), TMD (10 mg/kg bw), and CNB (200 mg/kg bw), while groups 5, 6, 7, and 8 were co-administered with CDE+TMD, CNB+ TMD, CNB+CDE, and CNB+TMD+CDE orally for 28 days. This study revealed the effect of prolonged administration of CNB, TMD, and CDE on the suppression of cognitive function, acetyl-cholinesterase (AChE), butyl-cholinesterase (BChE), monoamine oxidase (MAO) enzyme activities, and antioxidant enzyme activities in rats' brains when compared against control rats (P < 0.05). However, the activities of ectonucleosides (NTPdase), adenosine deaminase (ADA), and malondialdehyde levels produced in the brain of rats were significantly elevated (P < 0.05). This study reported the mechanism behind the neurotoxicity of CNB, TMD, and CDE on rats' cognitive, cholinergic, purinergic, and antioxidant enzymes as a consequence of the drastic reduction in cholinesterase enzyme activities leading to neurotransmitter poisoning.
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Cannabis , Tramadol , Ratas , Masculino , Animales , Ratas Wistar , Antioxidantes , Tramadol/toxicidad , Codeína , Colinesterasas , Colinérgicos , CogniciónRESUMEN
African Jointfir (Gnetum africanum) and Editan (Lasianthera africana) leaves are two leafy green veggies with several nutritional and medicinal properties. Alzheimer's disease (AD) is a form of neurodegeneration that is believed to cause dementia in affected individuals. The quest for alternative treatments has necessitated the exploitation of plants' secondary metabolites. Plant alkaloids have recently demonstrated relevance in the management of a variety of neurodegenerative disorders; although there is limited information on the neuroprotective properties of alkaloids from various tropical green leafy vegetables with neuroprotective potentials. As a result, this study examined the cholinesterase inhibitory activity and antioxidant potential of alkaloid extracts from the leaves of African Jointfir (G. africanum) and Editan (L. africana). Standard solvent extraction techniques were used to prepare alkaloid extracts. After that, these extracts were characterized using high-performance liquid chromatography. In vitro acetylcholinesterase inhibition assay for the extracts was also carried out. Subsequently, the alkaloid extracts were included in the diets of these flies (2 and 10 µg/g) for 7 days. Thereafter, treated fly homogenates were assayed for cholinesterase, monoamine oxidase, and antioxidant enzymes (specifically, glutathione-S-transferase catalase, and superoxide dismutase) activities, in addition, thiobarbituric acid reactive substance, reactive oxygen species, and total thiol contents. The extracts showed considerable anticholinesterase, antioxidant, and antimonoamine oxidase capabilities, according to the study's findings. Also, HPLC characterization revealed that desulphosinigrin (597,000 ng/100 g) and atropine (44,200 ng/100 g) are the predominating phytochemicals in Editan and African Jointfir respectively. These extracts could serve as potential sources of nutraceuticals with neuroprotective properties which can be used in the treatment/management of Alzheimer's disease.
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OBJECTIVES: Rauwolfia vomitoria is one ethno-botanicals in Nigeria used by traditional health practitioners in managing several human diseases. However, necessary information regarding its effect on enzymes implicated in the development and progression of erectile dysfunction is missing in the literature. Thus, this study investigated the antioxidant property and impact of Rauwolfia vomitoria extract on erectile dysfunction-related enzymes in vitro. METHODS: High performance liquid chromatography was used to identify and quantify Rauwolfia vomitoria's phenolic components. Then, utilizing common antioxidant assays, the extract's antioxidant properties were evaluated and finally the effect of the extract on some enzymes (AChE, arginase and ACE) implicated in erectile dysfunction was investigated in vitro. RESULTS: The results showed that the extract inhibited AChE (IC50=388.72⯵g/mL), arginase (IC50=40.06⯵g/mL) and ACE (IC50=108.64⯵g/mL) activities. In addition, phenolic rich extract of Rauvolfia vomitoria scavenged radicals and chelated Fe2+ in concentration dependent manner. Furthermore, rutin, chlorogenic acid, gallic acid, and kaempferol were found in large quantities by HPLC analysis. CONCLUSIONS: Therefore, one of the potential reasons driving Rauwolfia vomitoria's use in folk medicine for the treatment of erectile dysfunction could be its antioxidant and inhibitory activities on several enzymes linked to erectile dysfunction in vitro.
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Disfunción Eréctil , Rauwolfia , Masculino , Humanos , Antioxidantes/farmacología , Arginasa , Antihipertensivos , Fenoles/farmacología , Extractos Vegetales/farmacologíaRESUMEN
Purpose: In the management of type 2 diabetes (T2D), dietary intervention has been proposed to be highly effective. This study, therefore, investigated the effect of bitter leaf-flavored non-alcoholic wheat beer (NAWB) on insulin secretion and GLUT-2 expression in the pancreas of STZ-induced diabetic rats. Methods: In this study, the rats received a single intraperitoneal injection (i.p.) of STZ (35 mg/kg) after being fed a high-fat diet for 14 days to induce T2D. The rats were treated with bitter leaf flavored NAWB samples (100%HP- Hops only, 100%BL-Bitter leaf only, 75,25BL- 75% Hops, 25% Bitter Leaf, 50:50BL- 50% Hops:50% Bitter Leaf, and 25:75BL-25%Hops:75% Bitter Leaf) and Acarbose for 14 days. The superoxide dismutase, catalase, and glutathione peroxidase activity were also determined. Results: The results from this study showed a correlation between GLUT-2 and Insulin expression. There was an upregulation of Insulin as GLUT-2 expression was upregulated. Furthermore, the treated groups showed better antioxidant activity when compared with the diabetic control. Conclusion: Bitter leaf-flavored NAWB might thus be a good dietary intervention for type 2 diabetics.
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INTRODUCTION: The present study aimed at investigating the effect of Terminalia catappa fruits on blood pressure, NO/cGMP signalling pathway, angiotensin-1-converting enzyme and arginase activity, and oxidative stress biomarkers in L-NAME-induced hypertensive rats. MATERIALS AND METHODS: Forty-two Wistar rats were divided into seven groups. Hypertension was induced via oral administration of 40 mg/kg of L-NAME for 21 days. Thereafter, the hypertensive rats were treated with Terminalia catappa fruit-supplemented diet and sildenafil citrate for 21 days. The blood pressure was measured and cardiac homogenate was prepared for biochemical analyses. RESULTS: The results showed that L-NAME caused a significant (p < 0.05) increase in systolic and diastolic blood pressure, and heart rate as well as ACE, arginase and PDE-5 activity, with a simultaneous decrease in NO and H2S levels as well as increased oxidative stress biomarkers. However, treatment with Terminalia catappa fruits-supplemented diets and sildenafil citrate lowered blood pressure and modulated ACE, arginase, and PDE-5 activity, improved NO and H2S levels, as well as antioxidant status. CONCLUSION: Findings presented in this study provide useful information on the antihypertensive property of Terminalia catappa fruits, alongside some possible mechanisms. Hence, Terminalia catappa fruits could be considered a dietary regimen and functional food in alleviating hypertension.
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Hipertensión , Terminalia , Ratas , Animales , Ratas Wistar , Antioxidantes/farmacología , Antihipertensivos/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/química , Frutas , Terminalia/química , Citrato de Sildenafil/farmacología , NG-Nitroarginina Metil Éster , Arginasa , Hipertensión/tratamiento farmacológico , AngiotensinasRESUMEN
Memory deficit has been reported as one of the complications of diabetes. Fermented seeds of Pentaclethra Macrophylla (P. macrophylla) have been used in folklore for the management of metabolic diseases. The research aims to evaluate the impact of diets with the inclusion of the fermented seed of P. macrophylla on memory deficit in diabetic rats and its underlying mechanisms. Before the induction, the rats were subjected to training sessions. Thereafter, streptozotocin (50 mg/kg body weight) was administered to the trained rats via intraperitoneal (i.p). 72 hours after, the rats blood glucose level was checked, rats with blood glucose level greater than 250 mg/dl were selected for the memory index evaluation study. The induced rats were randomly distributed into groups: Normal rats (group 1), untreated diabetic rat (Group 2), acarbose treated diabetic rats (group 3); diabetic rats placed on diet supplemented with fermented seed of P. macrophylla (10 & 20% inclusion) were allotted to group 4 & 5. Then, evaluation of memory retention capacity was performed on the day 14 of the experiment. Thereafter, experimental rats were sacrificed, tissue of interest (brain) was excised, homogenized and homogenates were used for biochemical analysis. The cholinergic, angiotensin-1-converting enzyme (ACE), arginase activity and biomarkers for oxidative stress were significantly altered in untreated diabetic rats when compared with non-diabetes rats. Also, the memory capacity of the diabetic rats was significantly reduced when compared with the non-diabetes rats. Meanwhile, diabetic rats placed on diet with fermented seeds of P. macrophylla (10 & 20% inclusion) exhibited significantly higher memory capacity, lower activity of cholinergic, ACE, arginase activity in relation to untreated diabetic rats while the antioxidant status of the brain was enhanced. Nevertheless, fermented seeds of P. macrophylla ameliorated memory deficit in STZ induced diabetes rats. This gave credence to P. macrophylla nutraceutical potential as claimed in folk medicine.
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Diabetes Mellitus Experimental , Ratas , Animales , Ratas Wistar , Estreptozocina , Diabetes Mellitus Experimental/complicaciones , Glucemia/metabolismo , Arginasa , Encéfalo/metabolismo , Trastornos de la Memoria/etiología , Trastornos de la Memoria/complicaciones , ColinérgicosRESUMEN
Tropical vegetables remain one of the major sources of functional foods and nutraceuticals, while their constituent phytochemicals, especially alkaloids, have been reported to exhibit neuroprotective properties. Here, the protective effect of alkaloid extracts from Scent leaf (Ocimum gratissimum) and Water bitter leaf (Struchium sparganophora) on manganese (Mn)- induced toxicity in wild type fruit fly (Drosophila melanogaster) model was investigated. Flies were exposed to 30 mM of Mn, the alkaloid extracts (20 and 200 µg/g) and co-treatment of Mn plus extracts, respectively. The survival rate and locomotor performance of the flies were assessed 7 days post-treatment, after which the flies were homogenized and assayed for activities of acetylcholinesterase (AChE), monoamine oxidase (MAO), glutathione-S transferase (GST), catalase, superoxide dismutase SOD), as well as total thiol, reactive oxygen species (ROS) and neural L-DOPA levels. Results showed that the extract significantly reversed Mn-induced reduction in the survival rate and locomotor performance of the flies. Furthermore, both extracts counteracted the Mn-induced elevation in AChE and MAO activities, as well as reduced antioxidant enzyme activities, with a concomitant mitigation of Mn-induced elevated ROS and neural L-DOPA level. The HPLC characterization of the extracts revealed the presence of N-propylamine, Vernomine and Piperidine as predominant in Water bitter leaf extract, while 2, 6-dimethylpyrazine and sesbanimide were found in scent leaf extract. Therefore, the alkaloid extract of these leaves may thus be sources of useful nutraceuticals for the management of pathological conditions associated with manganese toxicity.
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Alcaloides , Ocimum , Animales , Ocimum/química , Manganeso/toxicidad , Extractos Vegetales/farmacología , Extractos Vegetales/química , Drosophila melanogaster , Especies Reactivas de Oxígeno , Agua , Acetilcolinesterasa , Levodopa/farmacología , Odorantes , Antioxidantes/farmacología , Alcaloides/farmacología , Suplementos Dietéticos , Monoaminooxidasa , Hojas de la PlantaRESUMEN
Acetylcholinesterase inhibitors (AChEIs) like donepezil are commonly used to treat Alzheimer's disease. AChEIs have also been considered for other therapeutic uses, such as anti-inflammatory neuroprotective agents. Consequently, the use of natural plant products as potential AChEIs can have therapeutic benefits. We previously reported the anticholinesterase properties of the phenolics and alkaloids found in the leaf extracts of two tropical plants with nutritional and ethnobotanical importance-African eggplant (Solanum macrocarpon L) and Black nightshade (Solanum nigrum L). Here, we tested the ability of both extracts to inhibit human erythrocyte AChE (an indirect mediator of pro-inflammatory cytokines production via acetylcholine degradation). We further used molecular docking and MD simulation to identify the potential molecular mechanism(s) of phenolic and alkaloid compounds as human AChEIs. Special focus was given to compounds containing the benzyl group that can establish stacking interactions similar to donepezil (a standard AChEI). Flavone-luteolin rutinosides (LR) were identified as single-binding or dual-binding AChEIs; specifically, we attributed the dual-binding LR4 and LR5 to their linked hexose moiety. This characteristic allows the dual binders to occupy the catalytic triads and the peripheral anionic subsite, while exploring the catalytic gorge. We further delineated the inhibition of human erythrocyte AChE, as the flavone common to both plant extracts-luteolin rutinosides-had positive in silico interactions with AChE. These findings suggest that phytochemicals from S. macrocarpon and S. nigrum with dual binding properties can be potential AChE inhibitors. In fact, compounds such as LR4 and LR5 should be further investigated as potential inhibitors of human AChE and may represent important natural alternatives to donepezil.Communicated by Ramaswamy H. Sarma.