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.

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.

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.

Solanum leaves extracts exhibit antioxidant properties and inhibit monoamine oxidase and acetylcholinesterase activities (in vitro) in Drosophila melanogaster.

Background This study sought to determine the in vitro antioxidant, anti-monoamine oxidase and anticholinesterase properties of extracts (aqueous and alkaloid) of two tropical vegetables from Solanum spp- African eggplant (Solanum macrocarpon L) and black nightshade (Solanum nigrum L) as indices of their neuroprotective properties. Methods Both aqueous and alkaloid extracts of African eggplant (AE) and black nightshade (BN) were prepared by solvent extraction according to standard methods. Thereafter, the inhibitory effects of the extracts on monoamine oxidase (MAO) and acetylcholinesterase (AChE) activities, as well as their free radical-scavenging and reducing abilities were assessed. Also, phytochemical analysis for phenols, flavonoids, and alkaloids were carried out. Results The results showed that the extracts inhibited MAO and AChE activities dose dependently, with aqueous extracts showing significantly higher MAO inhibition that the alkaloid extracts from both samples, but in all, BN showed higher MAO inhibitory effect compared to AE; the reverse was however, observed for AChE inhibition. Furthermore, the aqueous extracts showed significantly higher antioxidant properties than the alkaloid extracts, while BN had higher antioxidant properties compared to AN. The phytochemical analysis also showed that BN had significantly higher amount of phenols, flavonoids, and alkaloids than AE. Conclusions The anti-monoamine oxidase, anticholinesterase, and antioxidant properties exhibited by extracts from both samples could contribute to their neuroprotective abilities. Thus, these vegetables can be potential sources of functional foods and nutraceuticals in the management of neurodegenerative diseases, especially in the tropics.

Caffeine improves sperm quality, modulates steroidogenic enzyme activities, restore testosterone levels and prevent oxidative damage in testicular and epididymal tissues of scopolamine-induced rat model of amnesia.

OBJECTIVES: This study was designed to assess the role of caffeine on fertility parameters in testicular and epididymal tissues of scopolamine-induced model of amnesia in rats. METHODS: Adult male rats were treated with scopolamine with or without caffeine. The modulatory effects of caffeine or scopolamine on fertility parameters were assessed in rats' testicular and epididymal homogenates. KEY FINDINGS: Scopolamine-induced sperm abnormalities, reduced steroidogenic enzyme 3ß-Hydroxysteroid dehydrogenase (3ß-HSD) and 17ß-Hydroxysteroid dehydrogenase (17ß-HSD) activities and serum testosterone levels in rats' testicular tissues. Treatment with caffeine increased 3ß-HSD and 17ß-HSD as well as testosterone levels. Caffeine also reversed sperm viability, sperm motility and sperm count in testicular tissues of scopolamine-treated rats. Furthermore, scopolamine-induced oxidative damage in rats' epididymal and testicular tissues via reduction of thiol and non-protein thiol content as well as increase in reactive oxygen species (ROS) and malondialdehyde (MDA) levels. Caffeine attenuated oxidative stress in testicular and epididymal tissues of rats treated with scopolamine via increase in non-protein and protein thiol levels with concomitant reduction in ROS and MDA levels. CONCLUSION: This study revealed that caffeine (5 and 25 mg/kg) improved sperm quality, increased steroidogenic enzyme activities and attenuated oxidative damage in testis and epididymis of rats treated with scopolamine.

Phenolic analysis and erectogenic function of African Walnut (Tetracarpidium conophorum) seeds: The impact of the seed shell on biological activity.

This study investigated the erectogenic potential of African walnut seed (AWS). The extract from AWS cooked with/without shell interacted with phosphodiesterase-5 (PDE-5), arginase, angiotensin-I converting enzymes (ACE), and acetylcholinesterase (AChE); enzymes associated with erectile dysfunction (ED) and Fe2+ -induced malonaldehyde (MDA) production in the isolated penile tissue. The results showed that the extracts inhibited the enzymes and MDA production, but Walnut cooked with shell had the highest effect. This agreed with increased phenolic acids and flavonoids, found in the AWS cooked with the shell, compared with that cooked without shell. The inhibition of enzymes and antioxidative potentials could be among the possible mechanisms of actions of AWS in the management/treatment of ED. However, cooking walnut seed with the shell seem to be a contributing factor, as this could prevent possible leaching out of the phytochemicals that could be responsible for these biological effects. PRACTICAL APPLICATIONS: Walnut seed possesses a high content of phenolic compounds and inhibit enzymes relevant to the management of erectile dysfunction. Traditionally, Walnut seed is being cooked with/without the shell and consumed for the purpose of alternative medicine in folklore. Our investigation revealed the possible mechanism underlying the therapeutic effect Walnut seed in the management of ED, but the impact of the shell during cooking contributes to this effect. This result will inform the consumers and food scientist on the importance of cooking Walnut seed with the shell in order to maximize its nutraceutical values.

Modulatory Effects of Alkaloid Extract from Gongronema latifolium (Utazi) and Lasianthera africana (Editan) on Activities of Enzymes Relevant to Neurodegeneration.

Most alkaloids are produced by plants as a defense mechanism against herbivores. Since alkaloids are known to possess pharmacological effects, this study sought to investigate the in vitro modulatory effect of alkaloid obtained from two commonly consumed vegetables in southern Nigeria, Lasianthera africana (editan) and Gongronema latifolium (utazi), on some enzyme activities relevant to neurodegeneration. Effects of the alkaloids on cholinesterases (acetylcholinesterase [AChE] and butyrylcholinesterase [BChE]) and monoamine oxidase (MAO) activities were determined in vitro. In addition, Fe2+ chelating ability as well as radical-scavenging abilities were determined. Alkaloid profile was also determined using gas chromatography coupled with flame ionization detector (GC-FID). The results revealed that the alkaloids inhibited AChE, BChE, and MAO activities in a concentration-dependent manner, such that the alkaloid from G. latifolium showed higher enzyme inhibition (AChE [IC50 = 87.39 µg/ml], BChE [IC50 = 118.65 µg/ml], and MAO [IC50 = 61.37 µg/ml]) than L. africana (AChE = 115.60 µg/ml; BChE = 169.48 µg/ml; MAO = 73.72 µg/ml). In addition, GC-FID analysis revealed abundance of choline in both extracts. Gongronema latifolium and Lasianthera africana alkaloid extracts inhibit enzymes (acetylcholinesterase, butyrylcholinesterase, and monoamine oxidase) implicated in neurodegenerative diseases. Hence, these vegetables could offer dietary supplement in the management of neurodegenerative diseases.

Effect of dietary inclusions of bitter kola seed on geotactic behavior and oxidative stress markers in Drosophila melanogaster.

This study evaluated the effect of dietary inclusions of Garcinia kola (GK) seed on geotactic behavior and some oxidative stress markers in wildߚtype fruit flies (Drosophila melanogaster). Flies were raised on diet supplement with GK seed for 5 days. The negative geotactic behavior of flies which was used to evaluate their locomotor performance was thereafter evaluated. The flies were subsequently homogenized and the reactive oxygen species (ROS) level, acetylcholinesterase (AChE), catalase and glutathioneߚSߚtransferase (GST) activities, as well as nitric oxide (NO) and total thiol contents were assayed. The phytochemical constituents of GK seed were also determined. It was observed that higher dietary inclusions of GK seed reduced the survival rate of D. melanogaster more significantly compared to control flies. Also, higher dietary inclusions of GK seed significantly reduced locomotor performance and AChE activity, while the ROS level was increased compared to the control. Activities of GST and catalase were significantly increased in flies fed diet supplemented with higher GK seed inclusions but their NO content was significantly reduced compared to control. Phytochemical analysis of GK seed revealed abundance of saponin > glycosides > alkaloids > phenols > flavonoids. These results have shown that dietary inclusion of GK seed at higher concentrations reduced survival rate of D. melanogaster and impaired cholinergic system, with elevated activities of some antioxidant enzymes under acute exposure. These observations could be associated with bioactivities of predominant phytochemicals in GK seed such as saponin and glycosides which have been reportedly toxic at high concentration. Therefore, this study suggests that high consumption of GK seed could induce some toxicological effects and moderate consumption is hence recommended.

In vitro anticholinesterase, antimonoamine oxidase and antioxidant properties of alkaloid extracts from kola nuts (Cola acuminata and Cola nitida).

Background The development of cholinesterase (ChE) and monoamine oxidase (MAO) inhibitors for management of neurodegenerative diseases such as Alzheimer's disease (AD) has come with their undesirable side effects. Hence, research for potent but natural ChE and MAO inhibitors with little or no side effects is essential. This study investigated the potentials of alkaloid extracts from two Cola species as nutraceuticals for prevention and management of AD. Methods Alkaloid extracts were obtained from two Cola species (Cola nitida [KN] and Cola acuminata [KA]) by solvent extraction method. The extracts were characterized for their alkaloid contents using gas chromatography (GC). The effects of the extracts on ChE and MAO activities were investigated in vitro. Also, the extracts' ability to inhibit Fe2+-induced lipid peroxidation in rat brain homogenate, scavenge DPPH and OH radicals, as well as chelate Fe2+ were determined. Results GC characterization revealed the presence of augustamine and undulatine as the predominant alkaloids in the extracts. There was no significant (P > 0.05) difference in the inhibitory effects of the extracts on ChE activities. However, KA extract exhibited significantly higher (P < 0.05) MAO inhibitory effect than KN. Also, KA extract inhibited Fe2+- induced malondialdehyde (MDA) production in rat brain homogenate more significantly than KN, while there was no significant difference in DPPH and OH radicals scavenging, as well as Fe2+-chelating abilities of the extracts. Conclusions Our findings revealed that KN and KA alkaloid extracts exhibited significant effect in vitro on biological pathways that may contribute to neuroprotection for the management of neurodegenerative diseases.

Green leafy vegetables from two Solanum spp. (Solanum nigrum L and Solanum macrocarpon L) ameliorate scopolamine-induced cognitive and neurochemical impairments in rats.

This study examined the modulatory effect of Black nightshade (Solanum nigrum L) and African eggplant (Solanum macrocarpon L) leaves on cognitive function, antioxidant status, and activities of critical enzymes of monoaminergic and cholinergic systems of neurotransmission in scopolamine-administered rats. Cognitive impairment was induced in albino rats pretreated with dietary inclusions of Black nightshade (BN) and African eggplant (AE) leaves by single administration (i.p.) of scopolamine (2 mg/kg body weight). Prior to termination of the experiment, the rats were subjected to spontaneous alternation (Y-maze) test to assess their spatial working memory. Thereafter, activities of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), monoamine oxidase (MAO), arginase, and antioxidant enzymes (catalase, SOD, and GST) of rat brain homogenate were determined. Also, the malondialdehyde (MDA), nitrite, and GSH contents of the homogenate were determined. The results showed that pretreatment with dietary inclusions of AE and BN significantly reversed the impairment in the rats' spatial working memory induced by scopolamine. Similarly, elevations in activities of AChE, BChE, and MAO induced by scopolamine were significantly reversed in rats pretreated with dietary inclusions of AE and BN. In addition, impaired antioxidant status induced by scopolamine was reversed by pretreatment with dietary inclusions of AE and BN. This study has shown that dietary inclusions of AE and BN could protect against cognitive and neurochemical impairments induced by scopolamine, and hence, these vegetables could be used as a source of functional foods and nutraceuticals for the prevention and management of cognitive impairments associated diseases such as Alzheimer's disease.

Phenolic constituents and modulatory effects of Raffia palm leaf (Raphia hookeri) extract on carbohydrate hydrolyzing enzymes linked to type-2 diabetes.

This study sought to investigate the effects of Raffia palm (Raphia hookeri) leaf extract on enzymes linked to type-2 diabetes mellitus (T2DM) and pro-oxidant induced oxidative stress in rat pancreas. The extract was prepared and its α-amylase and α-glucosidase inhibitory effects were determined. Radical [2,2-diphenyl-1-picrylhydrazyl (DPPH)] scavenging and Fe2+-chelating abilities, and inhibition of Fe2+-induced lipid peroxidation in rat pancreas homogenate were assessed. Furthermore, total phenol and flavonoid contents, reducing property, and high performance liquid chromatography diode array detector (HPLC-DAD) fingerprint of the extract were also determined. Our results revealed that the extract inhibited α-amylase (IC50 = 110.4 µg/mL) and α-glucosidase (IC50 = 99.96 µg/mL) activities in concentration dependent manners which were lower to the effect of acarbose (amylase: IC50 = 18.30 µg/mL; glucosidase: IC50 = 20.31 µg/mL). The extract also scavenged DPPH radical, chelated Fe2+ and inhibited Fe2+-induced lipid peroxidation in rat pancreas all in concentration dependent manners with IC50 values of 402.9 µg/mL, 108.9 µg/mL and 367.0 µg/mL respectively. The total phenol and flavonoid contents were 39.73 mg GAE/g and 21.88 mg QAE/g respectively, while the reducing property was 25.62 mg AAE/g. The HPLC analysis revealed the presence of chlorogenic acid (4.17 mg/g) and rutin (5.11 mg/g) as the major phenolic compounds in the extract. Therefore, the ability of the extract to inhibit carbohydrate hydrolyzing enzymes and protect against pancreatic oxidative damage may be an important mechanisms supporting its antidiabetic properties and could make Raffia palm leaf useful in complementary/alternative therapy for management of T2DM. However, further studies such as in vivo should be carried out.

Quercetin and Its Role in Chronic Diseases.

Quercetin, a member of the flavonoid class of polyphenol, is one of the most abundantly distributed flavonoids found in various food sources such as fruits, vegetables, nuts, wine and seeds. Quercetin and quercetin-rich foods have been reported to have wide range of health promoting effects, especially in the prevention and management of several diseases; however, the subject of its solubility and bioavailability has limited its use. This section will therefore, consider quercetin as a food-rich flavonoid, the various food sources, the limitations in its use and new approaches at improving its solubility and bioavailability. The therapeutic potentials of quercetin at the prevention/management of some degenerative diseases such as diabetes, hypertension and neurodegenerative diseases, as well as the underlying biochemical mechanisms such as free radical scavenging and enzyme inhibition will also be discussed.

Alkaloid extracts from Jimson weed (Datura stramonium L.) modulate purinergic enzymes in rat brain.

Although some findings have reported the medicinal properties of Jimson weed (Datura stramonium L.), there exist some serious neurological effects such as hallucination, loss of memory and anxiety, which has been reported in folklore. Consequently, the modulatory effect of alkaloid extracts from leaf and fruit of Jimson weed on critical enzymes of the purinergic [ecto-nucleoside triphosphate diphosphohydrolase (E-NTPDase), ecto-5'-nucleotidase (E-NTDase), alkaline phosphatase (ALP) and Na+/K+ ATPase] system of neurotransmission was the focus of this study. Alkaloid extracts were prepared by solvent extraction method and their interaction with the activities of these enzymes were assessed (in vitro) in rat brain tissue homogenate and in vivo in rats administered 100 and 200mg/kg body weight (p.o) of the extracts for thirty days, while administration of single dose (1mg/kg body weight; i.p.) of scopolamine served as the positive control. The extracts were also investigated for their Fe2+ and Cu2+ chelating abilities and GC-MS characterization of the extracts was also carried out. The results revealed that the extracts inhibited activates of E-NTPDase, E-NTDase and ALP in a concentration dependent manner, while stimulating the activity of Na+/K+ ATPase (in vitro). Both extracts also exhibited Fe2+ and Cu2+ chelating abilities. Considering the EC50 values, the fruit extract had significantly higher (P<0.05) modulatory effect on the enzymes' activity as well as metal chelating abilities, compared to the leaf extract; however, there was no significant difference (P>0.05) in both extracts' inhibitory effects on E-NTDase. The in vivo study revealed reduction in the activities of ENTPDase, E-NTDase, and Na+/K+ ATPase in the extract-administered rat groups compared to the control group, while an elevation in ALP activity was observed in the extract-administered rat groups compared to the control group. GC-MS characterization revealed the presence of atropine, scopolamine, amphetamine, 3-methyoxyamphetamine, 3-ethoxyamhetamine cathine, spermine, phenlyephirine and 3-piperidinemethanol, among others in the extracts. Hence, alterations of activities of critical enzymes of purinergic signaling (in vitro and in vivo) by alkaloid extracts from leaf and fruit of Jimson weed suggest one of the mechanisms behind its neurological effects as reported in folklore.