Effect of diet supplemented with African Star Apple Fruit Pulp on purinergic, cholinergic and monoaminergic enzymes, TNF-α expression and redox imbalance in the brain of hypertensive rats.

OBJECTIVE: This study examined whether diet supplemented with African star apple fruit pulp (FP) can mitigate the effect of high blood pressure on brain neurochemicals, histopathology and expression of genes linked with neuroinflammation. METHODS: Rats were administered with cyclosporine (25 mg/kg.bw) to induce hypertension and were fed with or without FP supplemented diet. Purinergic (Nucleoside triphosphate diphosphohydrolases [NTPdase] and adenosine deaminase [ADA]) cholinergic (acetylcholinesterase [AChE]) and monoaminergic (monoamine oxidase-B) enzymes were assessed in treated and untreated hypertensive rats' brains. Oxidative stress biomarkers (catalase, glutathione-S-transferase, thiols, reactive oxygen species [ROS] and malondialdehyde [MDA]), as well as AChE, tumour necrosis factor and receptor (TNF-α and TNF-α-R) expression, were also determined. RESULTS: FP supplemented diet significantly reduced NTPdase and ADA activities and increased Na+/K+-ATPase activities in hypertensive rats' brains compared to the untreated group. Furthermore, FP reduced acetylcholinesterase and monoamine oxidase-B activities compared to the hypertensive group. Redox imbalance was observed in hypertensive rats with inhibition of antioxidant enzymes and high levels of ROS and MDA. However, FP supplemented diet improved antioxidant enzymes, reduced ROS and MDA production in the brain of hypertensive rats. High blood pressure also triggered upregulation of AChE, TNF-α and TNF-α-R while feeding with FP supplemented diet downregulated the genes. CONCLUSION: This study demonstrates the neuroprotective role of FP supplemented diet against alterations in neurochemicals associated with Alzheimer's disease, oxidative stress-induced neuronal damage and expression of genes linked with neuroinflammation. Moreover, studies on animal behaviour and human subjects are required to confirm these beneficial effects.

Glycemic indices and effect of bitter leaf (Vernonia amygdalina) flavored non-alcoholic wheat beer (NAWB) on key carbohydrate metabolizing enzymes in high fat diet fed (HFD)/STZ-induced diabetic Wistar rats.

In a bid to make the use of functional food easier in the management and prevention of diseases, product development and fortification from/with functional foods have become the recent focus of research. This study, therefore, sought to exploit the recent trend in the brewing industry on the production of non-alcoholic beers by investigating the possibility of having a non-alcoholic beer flavored with bitter leaf, a known plant widely reported to have a strong hypoglycemic effect, as against the traditional use of hops, and the effect of the produced beer on the glycemic indices and various diabetic biochemical parameters that serve as biomarkers for type-2 diabetes (T2D). The glycemic indices, as well as the inhibitory potentials of bitter leaf-flavored Non-alcoholic wheat beer (NAWB) in ratios of 100%HP, 100%BL, 75:25BL, 50:50BL, and 25:75BL, on enzymes linked to a high-fat diet/streptozocin (HFD/STZ)-induced T2D albino Wistar rats were investigated. There were no significant difference (p > .05) between the starch (1.72-1.77 mg/100 mL), amylose (0.22-0.24 mg/100 mL), and amylopectin (1.49-1.53 mg/100 mL) contents of the various samples. The Glycemic Index (GI) of the samples ranged from 36 to 73 with 75:25Bl and 50:50BL have the lowest (36) values. The samples reduced blood glucose levels and inhibited pancreatic α-amylase, lipase, and intestinal α-glucosidase activity. The inhibitory potentials of these beer samples on α-amylase and α-glucosidase as well as their ability to reduce blood glucose levels in diabetic rats thus making the bitter leaf flavored NAWB a suitable healthy beverage for better glycemic control in diabetics. PRACTICAL APPLICATIONS: This study revealed the potential of producing non-alcoholic wheat beer flavored with bitter leaves as a possible substitute for hops. The potential inherent in bitter leaf in the management of type 2 diabetes can thus be made available through a far-reaching beverage medium such as non-alcoholic beer to help in the treatment/management of T2D. The results of this research could be an eye-opener to the possible utilization of bitter leaf and by extension other plants that have been reported in the management of T2D. The use of the bitter leaf as a substitute for hops in the production of non-alcoholic beer in the brewing industry could help in a health-oriented campaign for safe drinks that could be helpful in the control of blood glucose levels of diabetic patients.

Synergistic cardioprotective ability of co-administration of Moringa supplemented diets and acarbose in diabetic cardiomyopathy involves attenuation of cholinergic, purinergic, monoaminergic, renin-angiotensin system, and antioxidant pathways.

One of the major complications of diabetes mellitus (DM) is diabetic cardiomyopathy (DCM) due to the multifaceted therapy involved. Here, we evaluated the combinatorial effect of Moringa leaf (ML) and seed (MS) supplemented diets plus acarbose (ACA) on cardiac acetylcholinesterase (AChE), adenosine triphosphatase (ATPase), adenosine deaminase (ADA), monoamine oxidase (MAO), arginase, angiotensin-I converting enzyme (ACE), and lactate dehydrogenase (LDH) activities, thiobarbituric acid reactive species (TBARS), and thiols levels. The diets and ACA (25 mg/kg) were administered for 14 days. The fasting blood glucose level (FBGL), cardiac AChE, ATPase, ADA, MAO, arginase, ACE, LDH activities, and TBARS and thiol levels were determined. Relative to the normal rats, the biomarkers were significantly increased in DM rats but were suppressed significantly in the diets plus ACA-treated rats while improving antioxidant status, with the 4% Moringa plus ACA proving outstanding compared to individual ML/MS and ACA. In addition, ML-supplemented diets with/without ACA had better effects compared to MS with/without ACA, respectively. In conclusion, the combination of ML/MS supplemented diets and ACA synergistically modulates the tested biochemicals. However, the effect on blood vessels and the nerves that control the heart, stiffness of left ventricular (LV) hypertrophy, fibrosis, cell signaling abnormalities, related gene expression, clinical trials, and echocardiology studies should be further investigated to affirm this claim. PRACTICAL APPLICATIONS: Moringa oleifera has been a vocal appetite in mitigating cardiovascular disease induced by diabetes, but the formulation of a medicinal diet as an ameliorative route of attention to the pathology is fairly addressed, not talking of its combination with the synthetic antidiabetic drug, such as ACA. Based on this experiment, it is imperative to explore such an idea. This research shows that co-administration of moringa leaf/seed formulated diets plus ACA exhibits a synergistic effect in DCM management. However, further research is needed in this field of experiment.

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.

Effect of cashew (Anacardium occidentale L.) nut-supplemented diet on steroidogenic enzymes, hormonal and oxidative imbalances, and sperm parameters in cisplatin-induced reproductive toxicity in male rats.

Cisplatin (CP) is a chemotherapeutic/anticancer drug culpable in sperm and testicular damage, but the use of dietary patterns has been reported to averse this effect. To date, no report on the use of roasted cashew nut-supplemented diets (RCNSD) against chemotherapy-induced testicular damage has been presented. In this study, the effect of 10% and 20% RCNSD on reproductive hormones, sperm parameters, testicular and epididymal antioxidant status, and steroidogenic enzymes activities in CP-induced rats were determined. Interestingly, these parameters were boosted, but with a decrement in radical species level in the testes/epididymis of CP-induced rats fed with RCNSD as against the untreated CP-induced rats. The modulatory effect of RCNSD on the tested reproductive parameters in studied tissues could be among the mechanism of action, by which RCNSD mitigates andrological toxicity. Hence, RCNSD could be harnessed as a functional food/nutraceutical agent for alleviating the andrological toxicity of CP-induced male reproduction. PRACTICAL APPLICATIONS: Consumption of cashew nuts has been a great benefit to human health, as a result of its richness in nutritional constituents including biologically active amino acids, tocopherols, fatty acids, polyphenols, and selenium, among others. Cashew nuts are mostly consumed fried/roasted, with yoghurt, as a paste, or used as an ingredient in confectionery products. The folkloric use of cashew nuts in the management of cardiovascular diseases, male reproductive disorders, and diabetes has been reported. In this study, the ability of roasted cashew nut-supplemented diets to modulate reproductive hormones, sperm parameters, testicular and epididymal antioxidant status, and steroidogenic enzymes activities in CP-induced reproductive toxicity in male rats was revealed, thus, indicating its possible use, clinically, in the management of reproductive toxicity induced by cancer drugs.

Beetroot supplemented diet exhibit anti-amnesic effect via modulation of cholinesterases, purinergic enzymes, monoamine oxidase and attenuation of redox imbalance in the brain of scopolamine treated male rats.

OBJECTIVES: Beta vulgaris, commonly known as beetroot, is a vegetable that contains red pigment and rich in betalains, phenolic acids, and flavonoids. This study was designed to assess the effect of beetroot supplemented diet (BRSD) on cognitive function and altered neurochemicals associated with Alzheimer's disease (AD) in the brain of rats treated with scopolamine (SCOP). METHODS: Rats were fed with BRSD (2 and 4%) for 14 days and administered with 2 mg/kg of SCOP intraperitoneally on the last day. Morris water Maze and Y-maze tests were performed to assess cognitive function. Purinergic enzymes [ectonucleotidase (NTPdase) and adenosine deaminase (ADA)], monoamine oxidase (MAO), and angiotensin-I converting enzyme (ACE) activities were determined in rat brain tissues. Furthermore, catalase activity, total thiol (T-SH) and non-protein thiol (NP-SH) levels were also assessed. Beetroot was characterized using liquid chromatography-mass spectrometry, and the structure-activity relationship between the constituents and target enzymes was assessed. RESULTS: BRSD improved cognitive function by increasing memory index in SCOP treated rats. An increase in NTPdase, ADA, MAO, and ACE activities were observed in the brain of rats treated with SCOP. However, the activities of these enzymes were significantly lower after treatment with BRSD. Treatment with BRSD triggered a significant increase in catalase activity, T-SH and NP-SH levels in SCOP-treated rats. Catechin, 6,7-benzocoumarin, gentisin, 5,7-dimethoxyflavone, and vulgaxanthin I was identified in beetroots. DISCUSSION: The result suggests that beetroot could prevent cognitive dysfunction in SCOP-treated rats, and enhance memory function, via modulation of purinergic enzymes, MAO and ACE activities, and neuronal antioxidant status.

Diet Supplemented with Chrysophyllum albidum G. Don (Sapotaceae) Fruit Pulp Improves Reproductive Function in Hypertensive Male Rats.

Hypertension has been implicated as a risk factor of reproductive disorders. High blood pressure may trigger impaired sperm quality and biomarkers of reproductive disorders. This study aims to investigate the effect of diet supplemented with Chrysophyllum albidum fruit pulp (FP) on sperm parameters, reproductive hormones, and antioxidant markers in testes and epididymis of hypertensive rats. Male Wistar rats were divided into seven groups (n = 10): normotensive control rats [NC], cyclosporine (25 mg/kg)-induced hypertensive rats [Hypert], hypertensive rats treated with captopril (10 mg/kg/day) [Hypert + Capt], hypertensive [Hypert + 2%FP and Hypert + 4%FP], and normotensive [2%FP and 4%FP] rats treated with 2% and 4% of diet supplemented with African star apple fruit's pulp [FP]. Hemodynamic parameters (arterial pressure, diastolic, and systolic pressure), sperm count, sperm motility, reproductive hormones, reactive oxygen species, and malondialdehyde levels were assessed. Diet supplemented with FP fed to hypertensive rats reduced mean arterial pressure, diastolic and systolic blood pressure, and heart rate. Furthermore, FP improved sperm quality in hypertensive rats by increasing sperm count, sperm motility with a concomitant reduction in sperm abnormality. FP also increased 3ß and 17ß-hydroxysteroid hydrogenase (3ß-HSD and 17ß -HSD) activities, as well as testosterone, luteinizing hormone, and follicle-stimulating hormone levels. Besides, FP triggered a significant increase in 3ß-HSD, 17ß -HSD, and STAR expression in rats' testicular tissues. Diet supplemented with FP also reduced ROS and malondialdehyde levels and triggered an increase in thiol levels, catalase, and glutathione-S-transferase activities. This study revealed that FP supplemented diet improved sexual function in cyclosporine-induced hypertensive rats by reducing blood pressure and modulation of sperm parameters, steroidogenic enzymes, and reproductive hormones.

Euphorbia-Derived Natural Products with Potential for Use in Health Maintenance.

Euphorbia genus (Euphorbiaceae family), which is the third largest genus of angiosperm plants comprising ca. 2000 recognized species, is used all over the world in traditional medicine, especially in the traditional Chinese medicine. Members of this taxa are promptly recognizable by their specialized inflorescences and latex. In this review, an overview of Euphorbia-derived natural products such as essential oils, extracts, and pure compounds, active in a broad range of biological activities, and with potential usages in health maintenance, is described. The chemical composition of essential oils from Euphorbia species revealed the presence of more than 80 phytochemicals, mainly oxygenated sesquiterpenes and sesquiterpenes hydrocarbons, while Euphorbia extracts contain secondary metabolites such as sesquiterpenes, diterpenes, sterols, flavonoids, and other polyphenols. The extracts and secondary metabolites from Euphorbia plants may act as active principles of medicines for the treatment of many human ailments, mainly inflammation, cancer, and microbial infections. Besides, Euphorbia-derived products have great potential as a source of bioactive extracts and pure compounds, which can be used to promote longevity with more health.

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.

Influence of eugenol on oxidative stress biomarkers in the liver of carrageenan-induced arthritis rats.

Background Eugenol is the foremost constituent of clove oil and widely distributed in many plants. It possesses many pharmaceutical applications, including antioxidant, anti-inflammatory, and anti-tumorigenic properties, among others. This study evaluates the influence of eugenol on oxidative stress biomarkers in the liver of carrageenan-induced arthritis (CIA) rats. Methods Sixty albino rats were randomly divided into 10 (n=6) groups. Group I is the control group that received saline solution orally. Groups II and VII rats received 2.5 mg/kg of eugenol orally (EUG-2.5). Rats in groups III/VIII and IV/IX received 5 and 10 mg/kg of eugenol orally (EUG-5 and EUG-10), respectively. Groups V and X received 0.2 mg/kg of dexamethasone (DEX-0.2) orally. Groups VI to X were injected with 1% carrageenan intra-articularly. Behavioral studies were conducted after 21 days of treatment. Thereafter, the animals were sacrificed, and the livers were isolated and used for biochemical analysis. Results Reduced body weight in arthritic rats was recorded compared to normal controls. Reduced tibiofemoral joint edema and increased spontaneous movement were observed in CIA rats with decreased superoxide dismutase, catalase, reduced glutathione (GSH), glutathione peroxidase, and GSH S-transferase activities compared with the normal control group. Increased endogenous enzyme activities and decreased elevated lipid peroxidation were also observed after eugenol treatment. Conclusion Eugenol ameliorates carrageenan-induced oxidative stress in the liver of arthritic rats.

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.

African crocus (Curculigo pilosa) and wonderful kola (Buchholzia coriacea) seeds modulate critical enzymes relevant to erectile dysfunction and oxidative stress.

Background The seeds of African crocus (AC) (Curculigo pilosa) and wonderful kola (WK) (Buchholzia coriacea) are commonly used in folklore medicine in managing erectile dysfunction (ED) without the full understanding of the possible mechanism of actions. This study investigated and compared the effects of aqueous extracts from the seeds of AC and WK on arginase and acetylcholinesterase (AChE) activities and some pro-oxidant [FeSO4 and sodium nitroprusside (SNP)]-induced lipid peroxidation in rat penile homogenate in vitro. Method Aqueous extracts of AC and WK were prepared, and their effects on arginase and AChE activities as well as FeSO4- and SNP-induced lipid peroxidation in rat penile homogenate were assessed. Furthermore, phenolic constituents of the extract were determined using high-performance liquid chromatography coupled with diode-array detector (HPLC-DAD). Results Both extracts exhibited concentration-dependent inhibition on arginase (AC, IC50=0.05 mg/mL; WK, IC50=0.22 mg/mL) and AChE (AC, IC50=0.68 mg/mL; WK, IC50=0.28 mg/mL) activities. The extracts also inhibited FeSO4- and SNP-induced lipid peroxidation in rat penile homogenate. HPLC-DAD analysis revealed the presence of phenolic acids (gallic, caffeic, ellagic and coumaric acids) and flavonoids (catechin, quercetin and apigenin) in AC and WK. AC had higher arginase inhibitory and antioxidative activities but lower AChE inhibitory properties when compared with WK. Conclusions These effects could explain the possible mechanistic actions of the seeds in the management/treatment of ED and could be as a result of individual and/or synergistic effect of the constituent phenolic compounds of the seeds.

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.

Toxicological Effects of Aqueous Extract From African Walnut ( Tetracarpidium conophorum) Leaves in Rats.

Tetracarpidium conophorum leaves are used in traditional medicine for the treatment of male infertility, without considering its toxicity and side effects. In this study, we investigated the effects of T conophorum leaves on some biochemical parameters such as alanine aminotransferase, aspartate aminotransferase, bilirubin, albumin, creatinine, and uric acid. Histology of the liver and kidney were also assessed. The result revealed that the alanine aminotransferase and aspartate aminotransferase levels of the control group were not significantly different from the experimental groups. There was no significant difference in the albumin and bilirubin levels of the control and experimental groups. Similarly, the uric acid and creatinine levels of the experimental rats were not significantly different from the control. The examination of liver and kidney sections did not show any morphological changes and inflammatory cell infiltrations. These findings suggest that the leaves did not induce any pathological changes at the doses tested.

Comparative Effects of Alkaloid Extracts from Aframomum melegueta (Alligator Pepper) and Aframomum danielli (Bastered Melegueta) on Enzymes Relevant to Erectile Dysfunction.

Aframomum melegueta (alligator pepper (AP)) and Aframomum danielli (bastered melegueta (BM)) seeds have been known to improve sexual function in folkloric medicine. This study investigates the effects of AP and BM seeds' alkaloid extracts on the activities of enzymes (acetylcholinesterase (AChE), angiotensin-1-converting enzyme (ACE), phosphodiesterase-5 (PDE-5), and arginase) relevant to erectile dysfunction (ED). Alkaloids from the seeds were prepared by the solvent extraction method and their interactions with AChE, ACE, PDE-5, and arginase were assessed. Gas chromatographic (GC) analyses of the extracts were also performed. The results revealed that the extracts inhibited the enzymes in a concentration-dependent manner. However, alkaloid extract from AP seed had higher AChE (IC50 = 5.42 µg/mL) and ACE (IC50 = 12.57 µg/mL) but lower PDE-5 (IC50 = 33.80 µg/mL) and arginase (IC50 = 31.36 µg/mL) inhibitory effects when compared to that of BM extract (AChE, IC50 = 42.00; ACE, IC50 = 60.67, PDE-5, IC50 = 7.24; and arginase, IC50 = 2.53 µg/mL). The GC analyses revealed the presence of senkirkine, angustifoline, undulatine, myristicin, safrole, lupanine, powelle, and indicine-N-oxide, among others. The inhibition of these enzymes could be the possible mechanisms by which the studied seeds were being used in managing ED in folklores. Nevertheless, the seed of AP exhibited higher potentials.

Phenolic Extracts from Clerodendrum volubile Leaves Inhibit Cholinergic and Monoaminergic Enzymes Relevant to the Management of Some Neurodegenerative Diseases.

This study investigated the inhibitory effects of phenolic-rich extracts from Clerodendrum volubile leaves on cholinergic [acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)] and monoaminergic [monoamine oxidase (MAO)] enzymes' activities and pro-oxidants [Fe2+ and quinolinic acid-(QA)] induced lipid peroxidation in rats brain homogenates in vitro. Free phenolic extracts (FPE) and bound phenolic extracts (BPE) were obtained via solvent extraction, and the total phenol and flavonoid contents were evaluated. The phenolic constituents of the extracts were also determined using high performance liquid chromatography coupled with diode array detector (HPLC-DAD). Our findings revealed that FPE had higher AChE (2.06 µg/mL), BChE (2.79 µg/mL), and MAO (2.81 µg/mL) inhibitory effects than BPE [AChE, 2.80 µg/mL; BChE, 3.40 µg/mL; MAO, 3.39 µg/mL]. Furthermore, FPE also had significantly (P < 0.05) higher inhibitory effects on Fe2+ and QA-induced lipid peroxidation compared to BPE. FPE (162.61 mg GAE/g) had higher total phenol content than BPE. However, BPE (18.65 mg QE/g) had significantly higher total flavonoid content than FPE (13.32 mg QE/g). Phenolic acids (such as gallic acid, catechin, chlorogenic, caffeic, ellagic, p-Coumaric acids) and flavonoids (catechins, rutin and quercetin) were present in both extracts. This study revealed that the enzymes' inhibitory activities and antioxidant potentials of phenolic-rich extracts from C. volubile could be part of the mechanism of actions behind its use for memory/cognitive function as obtained in folklore. However, FPE exhibited significantly higher enzymes, inhibitory and antioxidant potentials than BPE.

Phenolic Composition and Evaluation of Methanol and Aqueous Extracts of Bitter Gourd (Momordica charantia L) Leaves on Angiotensin-I-Converting Enzyme and Some Pro-oxidant-Induced Lipid Peroxidation In Vitro.

This study sought to assess the effects of bitter gourd leaf extracts (methanol and aqueous) on enzyme linked with hypertension (angiotensin-I-converting enzyme and some pro-oxidants (iron sulfate, sodium nitroprusside, and cisplatin]-induced lipid peroxidation in rat kidney homogenates. Chromatographic analysis of the extract was done using high-performance liquid chromatography-diode array detection. The results revealed that methanol extract (IC50 = 109.63 µg/mL) had significantly (P < .05) higher angiotensin-I converting enzyme inhibitory activity than aqueous extract (IC50 = 182.95 µg/mL). Similarly, methanol extract had significantly (P < .05) higher inhibitory effect on Fe2+- and cisplatin-induced lipid peroxidation than aqueous extract. However, there was no significant (P > .05) difference in the inhibition of sodium nitroprusside-induced lipid peroxidation of both extracts. High-performance liquid chromatography-diode array detection analysis revealed the presence of quercetin, caffeic, gallic, and chlorogenic acids in the leaf. Thus, inhibition of angiotensin-I converting enzyme activity and the antioxidant properties of the extracts could be linked to the presence of phenolic phytochemicals.

Aqueous extracts of avocado pear (Persea americana Mill.) leaves and seeds exhibit anti-cholinesterases and antioxidant activities in vitro.

BACKGROUND: Avocado pear (Persea americana Mill.) leaves and seeds are used in traditional medicine for the treatment/management of Alzheimer disease (AD); however, information on the mechanism of actions is limited. This study sought to investigate the effect of P. americana leaf and seed aqueous extracts on some enzymes linked with AD (acetylcholinesterase [AChE] and butyrylcholinesterase [BChE] activities) and their antioxidant potentials in vitro. METHODS: The inhibitory effects of extracts on AChE and BChE activities and antioxidant potentials (inhibition of Fe2+- and sodium nitroprusside-induced thiobarbiturate reactive species [TBARS] production in rat brain homogenates, radicals [1,1-diphenyl-2-picrylhydrazyl, hydroxyl, and nitric oxide] scavenging and iron [Fe] chelation abilities) were investigated. Phenolic content and phytochemical screening were carried out. Alkaloid profile was also determined using gas chromatography coupled with flame ionization detector (GC-FID). RESULTS: The extracts inhibited AChE and BChE activities and prooxidant-induced TBARS production in a dose-dependent manner, with the seed extract having the highest inhibitory effect and the leaf extract exhibiting higher phenolic content and radical scavenging abilities, but lower Fe chelation ability compared with that of the seed. The phytochemical screening revealed the presence of saponins, alkaloids, and terpenoids in both extracts, whereas the total alkaloid profile was higher in the seed extract than in the leaf extract, as revealed by GC-FID. CONCLUSIONS: The anti-cholinesterase and antioxidant activities of avocado leaf and seed could be linked to their phytoconstituents and might be the possible mechanisms underlying their use as a cheap and natural treatment/management of AD. However, these extracts should be further investigated in vivo.

Essential Oil from Clove Bud (Eugenia aromatica Kuntze) Inhibit Key Enzymes Relevant to the Management of Type-2 Diabetes and Some Pro-oxidant Induced Lipid Peroxidation in Rats Pancreas in vitro.

The inhibition of enzymes involved in the breakdown of carbohydrates is considered a therapeutic approach to the management of type-2 diabetes. This study sought to investigate the effects of essential oil from clove bud on α-amylase and α-glucosidase activities. Essential oil from clove bud was extracted by hydrodistillation, dried with anhydrous Na2SO4 and characterized using gas chromatography-mass spectrometry (GC-MS). The effects of the essential oil on α-amylase and α-glucosidase activities were investigated. The antioxidant properties of the oil and the inhibition of Fe(2+) and sodium nitroprusside-induced malondialdehyde (MDA) production in rats pancreas homogenate were also carried out. The essential oil inhibited α-amylase (EC50=88.9 µl/L) and α-glucosidase (EC50=71.94 µl/L) activities in a dose-dependent manner. Furthermore, the essential oil inhibited Fe(2+) and SNP-induced MDA production and exhibited antioxidant activities through their NO*, OH*, scavenging and Fe(2+)- chelating abilities. The total phenolic and flavonoid contents of the essential oil were 12.95 mg/g and 6.62 mg/g respectively. GC-MS analysis revealed the presence of α-pinene, ß-pinene, neral, geranial, gamma terpinene, cis-ocimene, allo ocimene, 1,8-cineole, linalool, borneol, myrcene and pinene-2-ol in significant amounts. Furthermore, the essential oils exhibited antioxidant activities as typified by hydroxyl (OH) and nitric oxide (NO)] radicals scavenging and Fe(2+)-chelating abilities. The inhibition of α-amylase and α-glucosidase activities, inhibition of pro-oxidant induced lipid peroxidation in rat pancreas and antioxidant activities could be possible mechanisms for the use of the essential oil in the management and prevention of oxidative stress induced type-2 diabetes.

Dietary inclusion of sorghum (Sorghum bicolour) straw dye protects against cisplatin-induced nephrotoxicity and oxidative stress in rats.

CONTEXT: Sorghum straw (dried leaves and stem fiber) extracts and infusion are employed in the management of several ailments in folklore, and it is also a natural dye source used in food preparation. OBJECTIVE: This study sought to investigate the modulatory effect of dietary inclusion of Sorghum straw dye on cisplatin-induced nephrotoxicity and antioxidant status in rats. MATERIALS AND METHODS: Adult male rats were randomly divided into four groups of six animals each. Groups I (normal rats) and II (control rats) were fed with basal diet while Groups III and IV were fed with diets containing 0.5% and 1% sorghum straw dye, respectively. Nephrotoxicity was induced in Groups I-IV on the 20th day by the administration of a single dose of cisplatin solution (7 mg/kg body weight, i.p.) and the experiment was terminated 3 d after. Thereafter, the kidney and plasma of the rats were analyzed for kidney function (creatinine, urea, uric acid, and blood urea nitrogen) and antioxidant indices [superoxide dismutase (SOD), catalase, glutathione-S-transferase (GST), malondialdehyde (MDA), vitamin C, and reduced glutathione (GSH)]. RESULTS: The average feed intake of the rats in all the groups ranged from 9.0 to 9.5 (g/rat/day). Furthermore, the result indicated that administration of cisplatin caused significant (p < 0.05) elevation in plasma creatinine (2.2 mg/dL), uric acid (39.3 mg/dL), urea (81.4 mg/dL), and blood urea nitrogen (38.0 mg/dL) as well as a concomitant decrease in kidney antioxidant indices in control rats as against the normal rats. However, diets supplemented with 0.5 and 1.0% sorghum straw dye significantly reversed the plasma creatinine and the kidney antioxidant indices to near normal levels. DISCUSSION AND CONCLUSION: The study suggests that dietary inclusion of sorghum straw dye as colorants could protect against oxidative stress and cisplatin-induced nephrotoxicity.