Neurobehavioral, neurotransmitter and redox modifications in Nauphoeta cinerea under mixed heavy metal (silver and mercury) exposure.

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.

In the quest for the ideal sweetener: Aspartame exacerbates selected biomarkers in the fruit fly (Drosophila melanogaster) model of Alzheimer's disease more than sucrose.

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.

African Jointfir (Gnetum africanum) and Editan (Lasianthera africana) leaf alkaloid extracts exert antioxidant and anticholinesterase activities in fruit fly (Drosophila melanogaster).

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.

Effect of Bitter-leaf (Vernonia amygdalina) Flavored Non-alcoholic Wheat Beer (NAWB) on, Insulin and GLUT-2 expression in Pancreas of High fat diet/Streptozotocin (HFD/STZ) Induced Diabetic Wistar Rats.

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.

Evaluating Water bitter leaf (Struchium sparganophora) and Scent Leaf (Ocimum gratissimum) extracts as sources of nutraceuticals against manganese-induced toxicity in fruit fly model.

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.

Curcumin improves the ability of donepezil to ameliorate memory impairment in Drosophila melanogaster: involvement of cholinergic and cnc/Nrf2-redox systems.

One of the well-established models for examining neurodegeneration and neurotoxicity is the Drosophila melanogaster model of aluminum-induced toxicity. Anti-cholinesterase drugs have been combined with other neuroprotective agents to improve Alzheimer's disease management, but there is not much information on the combination of anti-cholinesterases with dietary polyphenols to combat memory impairment. Here, we assess how curcumin influences some of the critical therapeutic effects of donepezil (a cholinesterase inhibitor) in AlCl3-treated Drosophila melanogaster. Harwich strain flies were exposed to 40 mM AlCl3 - alone or in combination with curcumin (1 mg/g) and/or donepezil (12.5 µg/g and 25 µg/g) - for seven days. The flies' behavioral evaluations (memory index and locomotor performance) were analyzed. Thereafter, the flies were processed into homogenates for the quantification of acetylcholinesterase (AChE), catalase, total thiol, and rate of lipid peroxidation, as well as the mRNA levels of acetylcholinesterase (ACE1) and cnc/NRF2. Results showed that AlCl3-treated flies presented impaired memory and increased activities of acetylcholinesterase and lipid peroxidation, while there were decrease in total thiol levels and catalase activity when compared to the control. Also, the expression of ACE1 was significantly increased while that of cnc/NRF2 was significantly decreased. However, combinations of curcumin and donepezil, especially at lower dose of donepezil, significantly improved the memory index and biochemical parameters compared to donepezil alone. Thus, curcumin plus donepezil offers unique therapeutic effects during memory impairment in the D. melanogaster model of neurotoxicity.

Phytochemicals from African eggplants (Solanum macrocarpon L) and Black nightshade (Solanum nigrum L) leaves as acetylcholinesterase inhibitors: an in-silico study.

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.

Effect of chlorogenic acid plus donepezil on critical neurocortical enzyme activities, inflammatory markers, and synaptophysin immunoreactivity in scopolamine-assaulted rats, supported by multiple ligand simultaneous docking.

The effect of chlorogenic acid (a natural phenolic acid ubiquitous in plant foods) on selected therapeutic properties of donepezil (DON) in a scopolamine (SCOP)-induced rat model of amnesia was the focus of this study. Adult albino (Wister strain) rats were allocated into five groups (n = 11) consisting of control, SCOP, SCOP + chlorogenic acid (CGA), SCOP + DON, and SCOP + CGA + DON for 7 days. Post-treatment, the rat brain cerebral cortex homogenate was assayed for cholinesterase and monoamine oxidase activities. Also, the reactive oxygen species, total thiol and nitric oxide contents, alongside catalase, and superoxide dismutase activities were determined. Routine histology for neuronal and glial cells as well as synaptophysin immunoreactivity was also carried out on the cerebral cortex. Thereafter, multiple ligand simultaneous docking was carried out for DON and CGA at the active sites of AChE and BChE. The results revealed that the biochemical parameters, glial cells, and synaptophysin immunoreactivity were significantly impaired in the cerebral cortex of scopolamine-treated rats. However, impaired butyrylcholinesterase and monoamine oxidase activity, together with antioxidant, glial cells, and synaptophysin levels were significantly ameliorated in scopolamine-treated rats administered DON + CGA compared to donepezil alone. The docking of both DON and CGA at the active sites of AChE or BChE showed higher binding energy to both enzymes compared to individual interactions of either DON or CGA. Hence, this study has been able to show that CGA could improve some of the therapeutic effects of DON, which could broaden the therapeutic spectrum of this drug. PRACTICAL APPLICATIONS: This study showed that chlorogenic acid (a major phenolic acid found in plant foods such as coffee) modulated some of the therapeutic properties of donepezil (an anticholinesterase drug used in the treatment of mild-to-moderate Alzheimer's disease). The combinations elicited better anti-butyrylcholinesterase, antimonoamine oxidase, and antioxidant properties, thus presenting this food-drug interaction as potentially able to offer better therapeutic properties.

Moringa seed-supplemented diets modulate ACE activity but not its gene expression in L-NAME-induced hypertensive rats.

INTRODUCTION: We investigated the effect of dietary inclusions of Moringa seed (5% and 10%) on blood pressure, angiotensin-1 converting enzyme (ACE) activity, and gene expression, as well as redox status in hypertensive rats. MATERIAL AND METHODS: Wistar strain albino rats were fed moringa seed-based diets for two weeks prior L-NAME (40 mg/kg/day, p.o.) administration for another ten days. Subsequently, the blood pressure was monitored. Furthermore, the kidney homogenates were assayed for ACE activity and gene expression, as well as oxidative stress markers. RESULTS: The increased (systolic = 297 ± 59.30 mmHg; diastolic= 242 ± 51.96 mmHg) blood pressure, arginase activity, and reduced nitric oxide level were significantly ameliorated in hypertensive rats treated with the seed. However, the elevated ACE activity was significantly reduced but not the upregulated ACE1 gene. Also, the reduced antioxidant enzyme activities were ameliorated with a significant downregulation in their regulator-Nrf2. Rutin (4.07 ± 0.02 mg/g) and quercitrin (4.06 ± 0.01 mg/g), among others, were found in the seed. DISCUSSION: This study suggests that moringa seed offers its antihypertensive properties by acting as an ACE inhibitor but not its gene modulator, and also modulates the antioxidant system through interaction with Nrf2. CONCLUSION: Moringa seed could act as an ACE inhibitor and not its gene modulator.

Neuroprotective properties of solanum leaves in transgenic Drosophila melanogaster model of Alzheimer's disease.

INTRODUCTION: We investigated the effect of African eggplant (AE) (Solanum macrocarpon L) and Black nightshade (BN) (Solanum nigrum L) leaves; two tropical vegetables consumed by humans on behavioural, biochemical and histological indices in Drosophila melanogaster model of Alzheimer's disease (AD). MATERIALS AND METHOD: Transgenic flies expressing human Amyloid Precursor Protein (hAPP) and ß-secretase (hBACE 1) were exposed to the pulverised leaf samples (0.1 and 1.0%) in their diets for fourteen days. Thereafter, the flies were assessed for their behavioural indices and routine histology of brain cells. Furthermore, fly head homogenates were assayed for ß-amyloid level, activities of acetylcholinesterase (AChE) and ß-secretase (BACE-1), as well as oxidative stress markers. RESULTS: Result showed that the significantly lower (p < 0.05) behavioural parameters (survival, locomotor performance and memory index), higher AChE and BACE-1 activities, ß-amyloid, ROS and lipid peroxidation levels, as well as reduced antioxidant indices observed in the AD flies, were significantly ameliorated (p < 0.05) in AD flies treated with the leaf samples. DISCUSSION: This study has showed that leaves of AE and BN ameliorated behavioural and biochemical indices in AD flies via neural enzyme modulatory, and antioxidant mechanisms. CONCLUSION: Hence, this study further justifies the neuroprotective properties of both AE and BN.

Effect of Solanum vegetables on memory index, redox status, and expressions of critical neural genes in Drosophila melanogaster model of memory impairment.

African eggplant (Solanum macrocarpon L) (AE) and Black Nightshade (Solanum nigrum L) (BN) leaves are green leafy vegetables with nutritional and ethnobotanical values. We have previously characterized the vegetables via HPLC/LC-MS to reveal notable phenolic acids, flavonoids and alkaloids. In this present study, we addressed the efficacy of the two vegetables in mitigating mercuric chloride (HgCl2)-induced neurotoxicity and memory impairment in Drosophila melanogaster. Flies were exposed to HgCl2 (0.30 mg/g) alone or in combination with the vegetables (0.1 and 1.0%) of both samples in their diets for seven days. The results showed that HgCl2 (Hg)-exposed flies had significantly reduced survival rate and memory index, which were ameliorated in the Hg-exposed flies fed AE or BN. This was accompanied by increased reactive oxygen species (ROS) levels, reduced total thiol, as well as catalase, glutathione transferase (GST) and acetylcholine esterase (AChE) activities in Hg-exposed fly heads, but ameliorated in Hg-exposed flies fed dietary inclusions of the vegetables. In addition, the Hg-induced alterations in SOD, NF-ҝB/Relish, Dronc and Reaper mRNA levels were statistically indistinguishable from controls in Hg-treated flies fed diets containing AE or BN. Normalization of cnc/Nrf2 and FOXO were observed only in Hg-treated flies fed BN. These findings suggest that dietary AE or BN leaves offer protection against Hg-induced memory impairment and neurotoxicity in D. melanogaster, and further justify them as functional foods with neuroprotective properties.

Effect of Andrographis paniculata and Phyllanthus amarus leaf extracts on selected biochemical indices in Drosophila melanogaster model of neurotoxicity.

Aluminum (Al)-induced toxicity in fruit fly (Drosophila melanogaster) is one of the established models for studying neurotoxicity and neurodegenerative diseases. Alkaloid phytochemicals have been reported to exhibit neuroprotective effects. Therefore, the aim of this study is to determine the effect of alkaloid extracts of Andrographis paniculata and Phyllanthus amarus leaves on Al-induced toxicity in wild type Drosophila melanogaster. The flies were exposed to diets containing 40 mM AlCl3, and the alkaloid extracts (0.1 and 1 mg/ml). Thereafter, the flies were assessed for learning and memory, as well as locomotor performance 14 days post-treatment. This was followed by homogenizing the flies and the homogenates were assayed for acetylcholinesterase, monoamine oxidase and catalase activities, as well as the malondialdehyde content. The results showed that the alkaloid extracts of both leaves could ameliorate the aluminum-induced behavioral and biochemical impairments in the flies. The HPLC analysis of the alkaloid contents revealed that there is an abundance of Amaryllidaceae alkaloids, caffeine and carpaine. Thus, alkaloid extracts from these leaves could serve as promising therapeutic candidates for the management of neurodegenerative disease.

Can gallic acid potentiate the antihyperglycemic effect of acarbose and metformin? Evidence from streptozotocin-induced diabetic rat model.

This study investigated the influence of dietary phenolic acid- Gallic acid (GA) on the antihyperglycemic properties of acarbose (ACA) and metformin (MET). Streptozotocin-induced diabetic rats were treated (p.o) with ACA, MET, GA and their combinations for 14 days. The effects of the treatments on blood glucose and insulin levels, pancreas α-amylase and intestinal α-glucosidase activities, as well as thiobarbituric acid reactive species (TBARS), thiol and reactive oxygen species (ROS) levels, including antioxidant enzyme activities were investigated. A significant increase in blood glucose, insulin, ROS and TBARS levels, and impaired antioxidant status, as well as elevation in the activities of α-amylase and α-glucosidase observed in diabetic rats were ameliorated in the treatment groups. Hpwever, GA had varying effects on the antidiabetic properties of the drugs. Nevertheless, GA showed more potentiating effects on the antidiabetic effect of MET and these effects were better observed at the lower dose of GA.

Characterization and neuroprotective properties of alkaloid extract of Vernonia amygdalina Delile in experimental models of Alzheimer's disease.

This study emphasized on the neuroprotective properties of bitter leaf alkaloid-rich extract (BLAE) using transgenic fruit fly (Drosophila melanogaster [D. melanogaster]) model and scopolamine-induced amnesia rats. In vitro antioxidant properties and modulatory effects on key neuronal enzymes were carried out. Thereafter, fruit flies expressing human amyloid precursor protein (hAPP) and BACE-1 genes were treated with BLAE for 7 d to determine survival rate, BACE-1, acetylthiocholine (AChE), glutathione-S-transferase (GST), and catalase activities. Also, the aftermath of the BLAE on the neuronal activities of AChE, butyrylcholine (BChE), monoamine oxidase (MAO), angiotensin-I converting enzyme (ACE), ATP diphosphohydrolase (ATPdase), and ADPdase, catalase, superoxide dismutase (SOD), plus TBARS, and nitric oxide (NO) content in rats treated with scopolamine (1 mg/kg. bwt. i.p.) was evaluated. In addition, the alkaloid characterization for constituent BLAE was determined. The outcomes proved that BLAE displayed antioxidant properties and inhibit activities of AChE, BChE, MAO, ACE, ATPdase, and ADPdase in vitro. Furthermore, transgenic flies treated with the BLAE exhibited significant levels of amelioration on survival rate and activities of BACE-1, AChE, GST, and catalase. In scopolamine-treated rats, AChE, BChE, MAO and NTPdases activities, and antioxidant status were upturned in rats pretreated with BLAE. This study disclosed the neuroprotective property of BLAE, which could be related to its alkaloid constituent, thereby making it a good candidate to explore as curative nutraceutical agent for cognitive impairments and affiliated diseases such as AD.

Dietary inclusions of Solanum vegetables mitigate aluminum-induced redox and inflammation-related neurotoxicity in Drosophila melanogaster model.

BACKGROUND: This study investigated the modulatory capacity of two Solanum green leafy vegetables; S. macrocarpon L. (African eggplant AE) and S. nigrum L. (Black nightshade BN) on dysregulation of some antioxidant, pro-apoptotic, pro-inflammatory-like, acetylcholinesterase gene expression and redox status in the Drosophila melanogaster model of aluminum-induced neurotoxicity. METHODS: Flies were exposed to AlCl3 (6.7 mM) alone or in combination with the leaves (0.1 and 1.0%) from both samples in their diet for seven days. Thereafter, the fly heads were rapidly separated, homogenized, and used to assay for reactive oxygen species (ROS), total thiol content, catalase, glutathione-S-transferase (GST), acetylcholinesterase (AChE) activities, and the expression of antioxidant-mediators (Hsp70, catalase, cnc/Nrf2, Jafrac1 and FOXO), acetylcholinesterase (Ace1), pro-apoptotic caspase-like (Dronc) and its regulator (reaper), as well as inflammation-related (NF-kB/Relish) genes. RESULTS: Results showed that AlCl3-exposed flies had significantly reduced survival rate which were ameliorated by AlCl3 also elevated ROS, GST and reduced AChE activities in fly heads while dietary inclusions of AE and BN ameliorated survial rate and oxidative stress in AlCl3-exposed flies. In addition, Hsp70, Jafrac1, reaper and NF-kҝB/Relish were significantly upregulated in AlCl3-exposed fly heads, while cnc/Nrf2 and FOXO were significantly downregulated, but catalase, Dronc and Ace were, not significantly modulated. Nevertheless, these impairments in gene expression levels were ameliorated by dietary inclusions of AE and BN during AlCl3 exposure. CONCLUSION: These findings showed that dietary inclusions of AE and BN leaves offer protection against Al-induced neurotoxicity in D. melanogaster and thus, could serve as functional foods with neuroprotective properties.

Effect of citrus peels-supplemented diet on longevity, memory index, redox status, cholinergic and monoaminergic enzymes in Drosophila melanogaster model.

This study sought to determine the life span promoting effecof orange (Citrus sinensis), tangerine (Citrus maxima) and grapefruit (Citrus paradisi) peels in Drosophila melanogaster model. Flies (both gender, 3 to 5 days old) were divided into seven (7) groups (n = 5) containing 40 flies each; group I (control) flies were fed with basal diet, II-VII were flies were fed with basal diet containing 0.1 and 1.0% of tangerine peel (TP), orange peel (CP), and grapefruit peel (GP) respectively, for 14 days. Locomotor performance and memory index were assessed via negative geotaxis and aversive phototaxis suppression assays, respectively. Thereafter, the fly homogenates were assayed for activities of acetylcholinesterase (AChE), monoamine oxidase (MAO) and antioxidant enzymes as well as other indices of their redox. The results revealed that the citrus peels significantly improved longevity, locomotor performance, memory index, antioxidant status, and modulate cholinesterase and monoamine oxidase enzyme activities in treated flies when compared to the control. The results obtained suggest that the citrus peels offer potentials as dietary supplement with life span promoting properties in D. melanogaster model which could as well serve as a functional food additives. PRACTICAL APPLICATIONS: Citrus peels, although often considered agro-wastes, are used as food supplements and food ingredents especially in production of candies, jams and custards. This study suggests the use of orange (Citrus sinensis), tangerine (Citrus maxima), and grapefruit (Citrus paradisi) peels as dietary supplements which offers potential life span promoting properties.

Anticholinesterase activity and antioxidant properties of Heinsia crinita and Pterocarpus soyauxii in Drosophila melanogaster model.

BACKGROUND: Plant alkaloids have become important sources of nutraceuticals owing to their pharmacological importance especially in the management of neurodegenerative diseases such as Alzheimer's disease. In assessing the therapeutic potentials of plant phytochemicals, the fruit fly (Drosophila melanogaster) has emerged as a very veritable tool and has been largely accepted as an alternative model in biomedical research. OBJECTIVES: In this study, alkaloid extracts from bush apple (Heinsia crinita (Afzel.) G. Taylor and padauk (Pterocarpus soyauxii Taub.) leaves were assessed on D. melanogaster exposed to aluminum toxicity. MATERIALS AND METHODS: Alkaloid extracts were prepared by solvent extraction method. Thereafter, the extracts were evaluated for their in vitro antioxidant properties, Fe2+-chelating abilities and inhibitory effects on drosophila acetylcholinesterase (AChE) activity. The samples were also characterized for their constituent alkaloids via HPLC. Thereafter, effective safe dose of the extracts were determined in D. melanogaster (Harwich strain). Subsequently, flies assaulted with AlCl3 were co-treated with the extracts (8.3 and 16.6 µg/g) for seven days, during which their survival rate was monitored. This was followed by assaying for the activities of AChE, antioxidant enzymes [superoxide dismutase (SOD), catalase and glutathione-S-transferase (GST)]. Also, the flies were assayed for levels of thiobarbituric acid reaction substance (TBARS) and reactive oxygen species (ROS). RESULTS: The results revealed that both extracts showed in vitro antioxidant properties with Padauk showing significantly higher antioxidant properties in vitro. However, there was no significant difference in their in vitro AChE inhibition. In vivo, Al-induced toxicity reduced survival rate, elevated AChE, SOD and GST activities, as well as TBARS and ROS levels which were ameliorated by the extracts. It was also revealed that piperine was predominant in PA, while 1-cyclohexen-1-yl-pyrrolidine was predominant in BA. CONCLUSION: Our data suggest that the protective abilities of these extracts against Al-induced toxicity can be primarily associated with their anticholinesterase and metal chelating abilities. Thus, these vegetables can be potential sources of nutraceuticals against aluminum toxicity and associated diseases.

Solanum vegetable-based diets improve impairments in memory, redox imbalance, and altered critical enzyme activities in Drosophila melanogaster model of neurodegeneration.

The effects of two Solanum vegetables, S. macrocarpon L. (African eggplant), and S. nigrum L. (black nightshade) on aluminum model of neurodegeneration in Drosophila melanogaster was investigated. Flies were treated with AlCl3 alone or in combination with the leaves from both samples in their diets for 7 days. Thereafter, locomotor performance and aversive phototaxic suppression test for learning and memory were carried out. This was followed by assay for reactive oxygen species, antioxidant properties, and enzyme (monoamine oxidase and cholinesterase) activities. Also, the in vitro antioxidant properties and chromatographic phenolic and alkaloid characterization of the samples were determined. Results showed that impaired behavioral physiology, antioxidant status, and enzyme activities observed in Al-treated flies were ameliorated in flies treated with both samples. In addition, both samples exhibited in vitro antioxidant effects. The protective effects from these samples against Al-induced toxicity can be associated with their antioxidant, antimonoaminergic, and anticholinergic properties. PRACTICAL APPLICATIONS: In the quest for a holistic prevention/management approach to neurodegenerative diseases, functional foods are becoming prominent. The use of Drosophila melanogaster to study human diseases is gaining huge recognition due to the high homologue between disease-causing genes between the two organisms. Consequently, this study presents African eggplant and black nightshade leafy vegetables as sources of polyphenols and alkaloids which are able to ameliorate impaired learning and memory, redox status, and enzyme activities in Al-induced D. melanogaster model of neurodegeneration.

Citrus spp. essential oils improve behavioral pattern, repressed cholinesterases and monoamine oxidase activities, and production of reactive species in fruit fly (Drosophila melanogaster) model of Alzheimer's Disease.

Much emphasis has been placed on the biological activities of citrus peel's essential oils (CPEOs) against human ailments. This study investigated the effect of Citrus limon and Citrus reticulata peel's essential oils (EOs) on behavioral and neurochemical imbalance in transgenic and Harwish (Wild) fruit flies. Flies were divided into seven groups comprising of the control and those that were fed with 0.1, 0.5, and 1.0 µg/ml of the dietary inclusions of study CPEOs for 7 days. Thereafter, behavioral profile was examined using lethality response and negative geotaxis assays. Effect of the EOs on cholinesterase and monoamine oxidase (MAO) activities, and antioxidative parameters were determined. The result showed a significant improvement of behavioral pattern and biochemical parameters of the flies fed with studied CPEOs inclusive diets. Conclusively, both EOs exert neuroprotective capability by reducing cholinesterases and monoamine activities, and also prevent oxidative stress, which are implicated in neuronal dysfunction in humans. PRACTICAL APPLICATIONS: With the growing increase in the search for safer alternatives, having no side effects, for the management of neurodegenerative diseases, a large proportion of the populace is beginning to find solace in the use of natural products. Also, the wide array of similarities between the humans and the dipteran insects, fruit flies is a perfect organism for the study of neurodegenerative diseases. Therefore, this study presents the neuroprotective potentials of lemon and tangerine peels-derived EOs, and the possibility of their exploration as neuroactive agents and alternative in the management of Alzheimer's disease (AD).

Involvement of Cholinergic and Redox Impairments in Insecticidal Properties of Essential Oils from Fertility Tree and Horseradish Tree Leaves in Fruit Fly (Drosophila melanogaster).

This study reports the biological activity of essential oils from fertility tree and horseradish tree leaves, and the mechanisms by which these oils promote insecticidal activity using Drosophila melanogaster as a model organism. Adult D. melanogaster were exposed to these essential oils at a final concentration of 10 µL/g for 24 hours. The exposure of flies to the essential oil resulted in significant decrease in their survival and fecundity. In addition, the essential oils produced significant reduction in acetylcholinesterase activity and induced oxidative stress in the flies as evidenced by an increase in reactive oxygen species, thiol and thiobarbituric reactive substance levels, as well as catalase activity. The essential oils were also characterized by gas chromatography coupled with mass spectrometry. Constituents such as terpenoids, Bis (2-ethylhexyl) phthalate, benzeneacetaldehyde, phytol, octadecane, 9,12-octadecadienoic acid (Z,Z)- methyl ester, heneicosane, eicosane and others were characterized. Therefore, our results point out to the potential application of fertility tree and horseradish tree leaf essential oils as natural alternatives to synthetic insecticides in agricultural and pest control practices, especially against dipterans.