Caffeic acid attenuates memory dysfunction and restores the altered activity of cholinergic, monoaminergic and purinergic in brain of cadmium chloride exposure rats.

Objectives This study aims to evaluate the neuroprotective effect of caffeic acid (CAF) against cadmium chloride (CdCl2) in rats via its effect on memory index as well as on altered enzymatic activity in the brain of CdCl2-induced neurotoxicity. Methods The experimental rats were divided into seven groups (n=6 rats per group) of healthy rats (group 1), CdCl2 -induced (CD) (3 mg/kg BW) rats (group 2), CD rats + Vitamin C (group 3), CD rats + CAF (10 and 20 mg/kg BW respectively) (group 4 & 5), and healthy rat + CAF (10 and 20 mg/kg BW respectively) (group 6 & 7). Thereafter, CdCl2 and CAF were administered orally to the experimental rats in group 2 to group 5 on daily basis for 14 days. Then, the Y-maze test was performed on the experimental rats to ascertain their memory index. Results CdCl2 administration significantly altered cognitive function, the activity of cholinesterase, monoamine oxidase, arginase, purinergic enzymes, nitric oxide (NOx), and antioxidant status of Cd rats (untreated) when compared with healthy rats. Thereafter, CD rats treated with vitamin C and CAF (10 and 20 mg/kg BW) respectively exhibited an improved cognitive function, and the observed altered activity of cholinesterase, monoamine oxidase, arginase, purinergic were restored when compared with untreated CD rats. Also, the level of brain NOx and antioxidant status were significantly (p<0.05) enhanced when compared with untreated CD rats. In the same vein, CAF administration offers neuro-protective effect in healthy rats vis-à-vis improved cognitive function, reduction in the activity of some enzymes linked to the progression of cognitive dysfunction, and improved antioxidant status when compared to healthy rats devoid of CAF. Conclusions This study demonstrated the neuroprotective effect of CAF against CdCl2 exposure and in healthy rats.

Sweet basil (Ocimum basilicum) leaf and seed extracts alleviate neuronal dysfunction in aluminum chloride-induced neurotoxicity in Drosophila melanogaster Meigen model.

Ocimum basilicum is an important medicinal plant and culinary herb generally known as sweet basil (SB). These plants are effective radical scavengers, that have been employed in treatment of nervous system disorders, and thus, could be beneficial for the management of neurodegenerative diseases (NDs). Current clinical treatments for NDs present several side effects, therefore, there is need to develop new treatments that can mitigate these deadly diseases. Hence, this study investigated the neuroprotective activities of SB leaf and seed in aluminum chloride (AlCl3)-induced toxicity in Drosophila melanogaster. HPLC characterization of the leaves and seeds were carried out. AlCl3-diet was used to induce neurodegeneration and treated flies received SB leaf and seed extracts-supplemented diet. Survival and locomotor performance activities/levels of oxidative biomarkers [reactive oxygen species (ROS), thiobarbituric acid reactive species (TBARS), total thiol, catalase, superoxide dismutase (SOD) and glutathione-S-transferase (GST)], enzymes linked with neurodegeneration (acetylcholinesterase (AChE) and monoamine oxidase (MAO)) were investigated. SB leaf had significantly (p < 0.05) higher polyphenol contents; gallic acid and P-coumaric acid were the most abundant polyphenol in the leaf and seed respectively. Percentage survival and locomotor rates, level/activities of total thiol, catalase, SOD and GST were significantly (p < 0.05) reduced while ROS, TBARS, AChE and MAO activities were significantly (p < 0.05) increased in AlCl3-diet-fed flies. Treatment with SB leaf and seed diet lessened these observed impairments. However, SB leaf had better neuroprotective activities that could be related to the observed higher phenolic constituents. Hence, SB leaf diet may offer improved therapeutic effect in NDs.

Modulatory effects of Cannabis sativa co-administration with tramadol and codeine on cognitive function in male rats.

Most teenagers mix up various psychoactive cocktail substances in combinations to get intoxicated. The role of the mixture combination of codeine (CDE), tramadol (TMD), and Cannabis sativa (CNB) on brain cognition, purinergic, cholinergic, and antioxidant enzyme activities remains unknown. This study sought to assess the mechanism of action of combinations of CDE+ TMD+ CNB on the function and activities of the brain of male Wistar rats. Forty-eight male Wistar rats were divided into 8 groups, n = 6. Group 1 served as a control, groups 2, 3, and 4 were exposed to CDE (2 mg/kg bw), TMD (10 mg/kg bw), and CNB (200 mg/kg bw), while groups 5, 6, 7, and 8 were co-administered with CDE+TMD, CNB+ TMD, CNB+CDE, and CNB+TMD+CDE orally for 28 days. This study revealed the effect of prolonged administration of CNB, TMD, and CDE on the suppression of cognitive function, acetyl-cholinesterase (AChE), butyl-cholinesterase (BChE), monoamine oxidase (MAO) enzyme activities, and antioxidant enzyme activities in rats' brains when compared against control rats (P < 0.05). However, the activities of ectonucleosides (NTPdase), adenosine deaminase (ADA), and malondialdehyde levels produced in the brain of rats were significantly elevated (P < 0.05). This study reported the mechanism behind the neurotoxicity of CNB, TMD, and CDE on rats' cognitive, cholinergic, purinergic, and antioxidant enzymes as a consequence of the drastic reduction in cholinesterase enzyme activities leading to neurotransmitter poisoning.

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.

Antioxidant-rich Terminalia catappa fruit exerts antihypertensive effect via modulation of angiotensin-1-converting enzyme activity and H2S/NO/cGMP signalling pathway in Wistar rats.

INTRODUCTION: The present study aimed at investigating the effect of Terminalia catappa fruits on blood pressure, NO/cGMP signalling pathway, angiotensin-1-converting enzyme and arginase activity, and oxidative stress biomarkers in L-NAME-induced hypertensive rats. MATERIALS AND METHODS: Forty-two Wistar rats were divided into seven groups. Hypertension was induced via oral administration of 40 mg/kg of L-NAME for 21 days. Thereafter, the hypertensive rats were treated with Terminalia catappa fruit-supplemented diet and sildenafil citrate for 21 days. The blood pressure was measured and cardiac homogenate was prepared for biochemical analyses. RESULTS: The results showed that L-NAME caused a significant (p < 0.05) increase in systolic and diastolic blood pressure, and heart rate as well as ACE, arginase and PDE-5 activity, with a simultaneous decrease in NO and H2S levels as well as increased oxidative stress biomarkers. However, treatment with Terminalia catappa fruits-supplemented diets and sildenafil citrate lowered blood pressure and modulated ACE, arginase, and PDE-5 activity, improved NO and H2S levels, as well as antioxidant status. CONCLUSION: Findings presented in this study provide useful information on the antihypertensive property of Terminalia catappa fruits, alongside some possible mechanisms. Hence, Terminalia catappa fruits could be considered a dietary regimen and functional food in alleviating hypertension.

Host-parasite relationship modulates the effect of African mistletoe leaves on the cholinergic, monoaminergic and carbohydrate hydrolyzing enzymes in fruit fly.

OBJECTIVES: Mistletoe infests common plant trees of great medicinal values such as Moringa and Almond. According to folklore, mistletoe leaves have been found to have application as food and medicine in the alleviation of various degenerative diseases. Host-parasite relationship may possibly influence the phytochemical and biological activities of mistletoe leaves. Hence, we examined the polyphenol contents, antioxidant properties, α-amylase, α-glucosidase, acetylcholinesterase (AChE) and monoamine oxidase (MAO) inhibitory activities of African mistletoe leaves obtained from Moringa and Almond host plants in fruit fly in vitro. METHODS: The phenolic constituents of the leaves were evaluated using HPLC system. The antioxidant activities were determined through the ABTS, DPPH and OH free radicals scavenging properties, ferric (Fe3+) and malondialdehyde (MDA) reducing abilities and Fe2+ chelation. The inhibitory effects of the leaves aqueous extracts on α-amylase, α-glucosidase, AChE and MAO activities were also assessed. RESULTS: The HPLC characterization of the leaves revealed that host plants caused marked variation in their phenolic composition, however, Almond mistletoe leaves had significantly (p<0.05) greater amounts of phenolic constituents. Both Moringa and Almond mistletoe leaves reduced Fe3+ and MDA levels, scavenged free radicals, chelated Fe2+ and inhibited α-amylase, α-glucosidase, AChE and MAO activities with the Almond mistletoe leaves having significantly (p<0.05) higher antioxidant properties and enzyme inhibitory activities. CONCLUSIONS: This present study indicated that host plants could positively modulate the phenolic profile of mistletoe leaves and this probably brought about the vivid noticeable changes in their antioxidant abilities, cholinergic, monoaminergic and carbohydrate hydrolyzing enzymes inhibitory activities.

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.

Aqueous extract of Massularia acuminata exerts erectogenic effect by modulating critical enzymes and hormones in streptozotocin-induced erectile dysfunction in rats.

Massularia acuminata stem is often used in folkloric medicine in the management of erectile dysfunction (ED), without full scientific basis for its action. Thus, the effects of aqueous extract of M. acuminata stem (MAS) on sexual activity, hormonal action, enzymatic activity and levels of molecules associated with erectile function were assessed. ED was induced by single intraperitoneal injection of 50 mg/kg body weight of streptozotocin in rats and treated with sildenafil citrate or MAS (50 or 100 mg/kg) orally for 2 weeks. The results revealed that there was significant (p < 0.05) reduction in mounting and intromission frequencies, testosterone, luteinizing hormone, and nitric oxide levels, as well as elevation in mounting and intromission latencies, phosphodiesterase 5, arginase, acetylcholinesterase, adenosine triphosphatidase, and adenosine deaminase activities, nitric oxide, thiobarbituric acid reactive species, and glycated haemoglobin levels were observed in ED rats in comparison with the control rats. Treatment with MAS or sildenafil citrate significantly (p < 0.05) modulated the sexual behaviour, biochemical parameters and histological architecture, with 100 mg/kg of MAS having the best erectogenic effects. Furthermore, phenolic characterization revealed that catechin and kaempferol as the main phenolic compounds present in MAS, that can act in synergistically or additively with other phytochemicals to confer erectogenic effect.

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.

Mistletoe infested Moringa oleifera and Terminalia catappa leaves supplemented diet enhances antioxidant and insulin-like peptide mRNA levels in Drosophila melanogaster.

Moringa and Almond are common plants of medicinal and economic value which are often infested with mistletoe. Host plants' infestation could result in major differences in their phytoconstituents and biological activities. Thus, effects of mistletoe infestation on Moringa and Almond host plants supplemented diets on mRNA expression levels of Drosophila insulin-like peptide-2 (Dilp2), heat shock protein-70 (Hsp70) and superoxide dismutase (Sod) in diabetic-like flies were evaluated using quantitative real-time PCR system. Mistletoe infestation on host leaves caused significant upregulation of Sod and significant downregulation of Hsp70 and Dilp2 genes. Hence, we opined that infestation of Moringa and Almond trees with mistletoe resulted in improved expression level of antioxidant and insulin-like peptide genes. This may be the mechanism by which host plants caused enhanced regulation of circulating glucose and oxidative stress. Therefore, consumption of mistletoe infested Moringa and Almond host leaves could possibly offer better antioxidant and hypoglycemic effects.

Black Seed (Nigella sativa): A Favourable Alternative Therapy for Inflammatory and Immune System Disorders.

In the recent years, various food additives, medicinal plants, and their bioactive components have been utilized in anti-inflammatory and immunomodulatory therapy. Nigella sativa is a key dietary supplement and food additive which has a strong traditional background. It is also one of the most broadly studied seeds in the global pharmaceutical and nutraceutical sector. N. sativa seeds are potential sources of natural metabolite such as phenolic compounds and alkaloids. The anti-inflammatory and immunomodulatory abilities of these seeds, most peculiarly with reference to some inflammatory and immune mediators, are reviewed. N. sativa and its bioactive compounds modulate inflammatory and immunomodulatory mediators including tumor necrosis factor-alpha (TNF-α), interferon gamma (IFN-γ), nuclear factor kappa B (NF-kB) cyclooxygenase (COX), lipoxygenase (LOX), transforming growth factor beta (TGF-ß), interleukins, and immunoglobulin levels. This paper comprehensively describes the biomarkers and signaling pathways underlying the anti-inflammatory and immunomodulatory potential of N. sativa. This review also explains the scientific basis and the pharmacological properties of core bioactive ingredients of N. sativa responsible for these biological activities which indicates that their bioactive components could be possibly regarded as favorable therapy for disorders linked to inflammation and immune-dysregulation.

Effects of dietary inclusion of Bambara groundnut and sweet orange peels on streptozotocin/HFD type-2 induced diabetes mellitus complications and related biochemical parameters.

The effects of dietary inclusion of Bambara groundnut and sweet orange peels composite bread on low-dose streptozotocin and high-fat diet (HFD)-induced type-2 diabetes mellitus (T2D) complications was evaluated in the present study. Male experimental rats-induced T2D were administered with acarbose (standard) and fed with Bambara groundnut and sweet orange peels composite bread for a period of 14 days while monitoring their blood glucose levels. More so, the activities of angiotensin-I-converting enzyme (ACE), serum aspartate aminotransferase, alkaline phosphatase, and alanine aminotransferase activities, as well as nitric oxide (NO), reactive oxygen species (ROS), albumin, total bilirubin, creatinine, urea, and uric acid serum concentrations were assayed for. Diabetic untreated rats showed disorders in ACE, AST, ALT, and ALP activities, and NO, ROS, glucose, albumin, bilirubin, creatinine, urea, uric acid levels, as well as lipid profiles. Interestingly, these disorders were significantly ameliorated in composite bread diet-fed rats in comparison to the diabetic untreated rats. Meanwhile, the presence of polyphenols in the Bambara groundnut and sweet orange peels composite bread diet could have aided the amelioration of these metabolic disorders after the 14th day of administration. Finally, it was proposed that the ability of Bambara groundnut-wheat and sweet orange peel composite bread to treat T2D and its complications makes it a more successful therapy than medications that just target one of the diseased states. PRACTICAL APPLICATIONS: Diabetes mellitus is a global and chronic disease that presently affects 536.6 million people alongside 1.5 million deaths directly attributed to it yearly. Several drug and medicinal agents have been employed for the management of diabetes but those drugs are mostly limited to the management of diabetes while the associated complications are most untreated, while drugs that can manage diabetes and its related complications mostly come at high prices. Therefore, there is an urgent need to evaluate legumes, such as Bambara groundnut, with proven therapeutic potential in the management of diabetes and its complications. However, the Bambara groundnut takes a long period to prepare for a meal, therefore including it in a ready-to-eat product will not only improve its acceptability but also add to economic improvement. Furthermore, adding a waste product, sweet orange peels, will both add flavor and source of additional antioxidant attributes.

The prevalence, mechanism of action, and toxicity of Nigerian psychoactive plants.

Cannabis sativa, Datura stramonium, Nicotiana tabacum, and Carica papaya are plants that naturally grow in Nigeria. They are reportedly rich in neuroactive compounds that are capable of reacting with the nervous system to elicit psychoactive and/or toxic effects that deter predators. However, despite the toxicological potential of these plants, their recreational use is on the rise due to the psychoactivity they proffer and prevalence in Nigeria. The aim of the present study is to evaluate the plants' recreational use, mechanism of actions and toxicities. Relevant published documents on psychoactive plants in Nigeria were obtained from Web of Science between 2002 and 2020. Non-English documents, documents not in Science Citation Index Expanded and Google Scholar were removed while 1186 documents were reviewed. Results showed that the plants are recreationally used in Nigeria with a higher prevalence than the global frequency. They are very addictive and lead to dependence. The plants were also observed to elicit different mechanism of action, though the activation of monoaminergic neurotransmission system was common to all. Regrettably, the plants could be toxic when ingested under non-medical conditions. Conclusively, these plants are addictive with potential toxic effects. Therefore, control of the recreational use of these plants should be revamped and overhauled.

Effect of black seeds (Nigella sativa) on inflammatory and immunomodulatory markers in Plasmodium berghei-infected mice.

Nigella sativa, a core dietary supplement and food additive in folklore is one of the most broadly studied seed plants in the global nutraceutical sector. Malaria infection impairs the ability of principal cells of the immune system to trigger an efficient inflammatory and immune response. Ninety-six mice, weighing 20-25 g, were grouped into 12 consisting of 8 animals each. The mice were infected with standard inoculum of the strain NK65 Plasmodium berghei (chloroquine sensitive) and the percentage parasitemia suppression were evaluated. The individual effect of black seed supplemented diet and its combinatory effect with chloroquine (CQ) were investigated on reactive oxygen species (ROS), glutathione peroxidase (GPx), reduced glutathione (GSH), glutathione-S-transferase (GST), serum immunoglobulins (IgG and IgM), and the hematological parameters (hemoglobin, packed cell volume, and red blood cell count) in P. berghei infected mice. The inflammatory cytokines, tumor necrosis factor (TNF-α), interleukin (IL-6 and IL-10), as well as IgG and IgM were assayed in the serum. The mice temperature and behavioral changes were observed. Infected mice treated with the dietary supplementation of black seed with a percentage inclusion (2.5%, 5%, 10%) showed significantly decreased parasitemia and ROS levels (p < 0.05) compared with the untreated mice. The result demonstrated a significant suppression in the pro-inflammatory cytokines (TNF-α, IL-6) levels and a notable elevation in the anti-inflammatory cytokine (IL-10), antioxidant markers as well as the immunoglobulin levels of the P. berghei-infected mice treated with black seed. The study revealed that black seed enhanced host antioxidant status, modulated inflammatory and immune response by regulating some inflammatory cytokines and immunomodulatory mediators. PRACTICAL APPLICATIONS: Black seed (Nigella sativa) has been a dietary supplement and natural remedy for many centuries. Inflammatory and immune diseases are the most notable cause of mortality in the world and more than 50% of deaths have been attributed to it. However, there is paucity of information on the effect of N. sativa on anti-inflammatory and immunomodulatory ability during malaria infection. The result suggests that N. sativa produced antioxidant, anti-inflammatory, and immunomodulatory effect in Plasmodium berghei-infected mice via the participation of glutathione antioxidant system, serum antibodies, and some inflammatory cytokines.

The modulatory effects of alkaloid extracts of Cannabis sativa, Datura stramonium, Nicotiana tabacum and male Carica papaya on neurotransmitter, neurotrophic and neuroinflammatory systems linked to anxiety and depression.

This study investigated the modulatory effects of alkaloid extracts of Cannabis sativa (CSAE), Datura stramonium (DSAE), Nicotiana tabacum (NTAE) and male Carica papaya (CMAE) on neurotransmitter, neurotrophic and neuro-inflammatory systems linked to anxiety and depression. Male Wistar rats were orally administered the alkaloid extracts in doses of 5, 50, 500, and 2000 mg/kg for 90 days. On day 91, neurobehavioural studies were evaluated, rats were sacrificed, brain hippocampus removed and tissue homogenate prepared. Biochemical, cytokine and neurotransmitter metabolisms were estimated in the hippocampus. Expressions of genes linked to anxiety and depression were evaluated by RT-qPCR. Results showed CSAE, NTAE and CMAE act as anxiolytic and antidepressant agents by depleting TNF-α, IL-1ß and reactive oxygen species concentrations, and monoamine oxidase, angiotensin 1-converting enzyme and acetylcholinesterase activities while elevating IL-10 and dopamine concentrations and glutamate dehydrogenase activity at doses of 5, 50 and 500. Same doses of CSAE, NTAE and CMAE also depleted the gene expressions of GSK3ß, JNK, NF-ĸB, and Nesfatin-1 while increasing expressions of CREB, BDNF, serotonin and Nrf2. However, administration of DSAE and 2000 mg/kg CSAE, NTAE and CMAE had adverse modulatory effects on the neurochemical concentrations and activities as well as the gene expressions of the evaluated neurotransmitter, neurotrophic and inflammatory systems. In conclusion, the study established the sub-chronic instrumentalization potential of CSAE, CMAE, and NTAE for anxiolytic and anti-depressive moods, though their use may be associated with dependence and addiction, which may result in more detrimental effects than any therapeutic potential they may proffer.

Almond and date fruits enhance antioxidant status and have erectogenic effect: Evidence from in vitro and in vivo studies.

This study was designed to investigate the efficacies of almond and date fruits on redox imbalance and enzymes relevant to the pathogenesis of erectile dysfunction. The total polyphenol contents, ferric reducing antioxidant power, and vitamin C content were determined spectrophotometrically. Phenolic and amino acid compositions were quantified using HPLC; meanwhile, the antioxidant activities were determined using DPPH, ABTS, FRAP, and metal chelation. Also, the effect of almond and date extract on advanced glycated end-products (AGEs) formation, arginase, and phosphodiesterase-5 activities was evaluated in vitro. Thereafter, the influence of almond and date supplemented diets on copulatory behaviors in normal rats was assessed, followed by arginase and phosphodiesterase-5 activities determination in vivo. The results revealed that date and almond extracts exerted antioxidant properties, prevented AGEs formation in vitro, and inhibited arginase and phosphodiesterase-5 activities in vitro and in vivo. Besides, almond and date supplemented diets significantly enhance sexual behaviors in normal rats when compared with the control. Among the active compounds identified were gallic acid, ellagic acid, quercetin, and rutin. All the 20 basic amino acids were identified. Given the aforementioned, date and almond could represent a reliable source of functional foods highly rich in compounds with antioxidant activity, and arginase and PDE-5 inhibitory properties. PRACTICAL APPLICATIONS: Fruits are essential part of the human diet that furnish the body with important nutrients. Despite the crucial roles of fruits in human diets, some fruits like almond and date are underutilized among Nigerians. However, we characterized the important compounds present in these fruits and how their presence contributes to the biological activities of the fruits. Finally, we relate the chemical composition and the observed biological activities to the overall health and wellness of the consumers.

Plantain peels restore sexual performance, hormonal imbalance, and modulate nitric oxide production and key enzymes of penile function in paroxetine-sexually impaired male rats.

This study focused on the effect of unripe (UPP) and ripe (RPP) plantain peels' extracts (200 and 400 mg/kg) on sexual behavior, hormonal profiles [testosterone, follicle-stimulating hormone (FSH), and luteinizing hormone (LH)], and enzymes [acetylcholinesterase (AChE), phosphodiesterase-5' (PDE-5), arginase, angiotensin-I converting enzyme (ACE), ecto-5'neucleotidase, and adenosine deaminase (ADA)] in paroxetine (PAR)-induced penile dysfunction rats. From the result, arginase, PDE-5', ACE, ecto-5'-nucleotidase ADA, and AChE activities, sexual activities, hormonal profile, and NO level were reduced, while thiobarbituric acid reactive species (TBARS) level increased (p < .05) relative to normal control rats. However, treatment with UPP and URP reduced the activities of these enzymes, decreased TBARS levels, and increased hormones, and penile NO levels in PAR-induced rats. Thus, the use of UPP and RPP could be channeled towards the improvement of sexual performance in erectile dysfunction (ED) disorder. PRACTICAL APPLICATIONS: Plantain fruits are a tropical staple food crop commonly consumed at various stages of ripeness and cooking methods. However, its peels are regarded as a waste product with reported cases of environmental menace. Interestingly, plantain peel is being used as a major raw material for industrial applications in the agro-based industries and in folklore for the treatment of many human ailments due to its rich phytochemicals such as polyphenols, carotenoids, alkaloids, etc., which have been reported. A prelude study has also indicated its usefulness in ED management, but further pharmacological investigations are needed to proffer information on its effect in ED management and its anti-androgenic activity in male Wistar rats. The information from this study could be of pharmaceutical importance in designing natural remedies capable of improving penile rigidity, hormone profiles, and alteration of enzymes linked with ED.

Grapefruit peel extract mitigates paroxetine-induced erectile dysfunction in rats through stimulation of erectile response, antioxidant status, and inhibition of key enzymes related with impaired penile erection.

Despite the antidepressant potency of paroxetine, its side effect of erectile dysfunction is burdensome. Grapefruit peels (GFPs) are underutilized cultivar wastes with wide range of therapeutic potentials which have been attributed to their antioxidant behavior and phenolic contents' abilities to effectively inhibit enzymatic activities and manage endothelial dysfunction in cardiovascular disorders. This study aims to investigate the erectogenic potentials of GFP extract in a rat model of paroxetine-induced ED. Experimental rats were sectioned into five groups: [1: control; 2: paroxetine (10 mg/kg); 3: paroxetine + sildenafil (5 mg/kg); 4: paroxetine + GFP (50 mg/kg); 5: paroxetine + GFP (100 mg/kg)] and treated for 28 days. Sexual behavior of rats was assessed and effect of GFP on ecto-5' nucleotidases, phosphodiesterase-5, and adenosine deaminase (ADA) activities was determined in rats' penile tissues. The levels of malondialdehyde, nitric oxide (NO) as well as superoxide dismutase (SOD) and catalase activities were also determined. HPLC-DAD analysis showed the presence of naringin, rutin, caffeic acid, quercitrin, quercetin, and kaempferol glycoside. Oral administration of paroxetine reduced erectile response as revealed by their low intromission and mounting numbers as well as high intromission and mounting latencies. Paroxetine caused a significant elevation of ADA and phosphodiesterase-5 activities and malondialdehyde levels with drastic reduction in levels of NO, SOD, and catalase activities in rats' penile tissues. However, GFP extract reversed PDE-5, ADA, and antioxidant activities to normal levels, raised the concentration of NO. These results suggest the erectogenic effects and protective potentials of GFP extract against paroxetine-induced erectile dysfunction. PRACTICAL APPLICATION: Grapefruit peels are an environmental menace in many countries and this study showed that the peels can be used in the prevention / management of erectile dysfunction. The therapeutic potentials of the peels are due to the presence of bioactive compounds such as flavonoids and phenolic acids. Therefore, exploring the erectogenic potentials of the peels will translate to conversion of the wastes to therapeutic products.

Functional cereals' anti-diabetic property, phenolic composition, and role on glycemic indices in-vitro.

This study analyzed the effects of functional cereals processed and produced from yellow corn, soybean, acha, orange peels and moringa leaves' polyphenolic content, glycemic index, starch composition and their effects on α-amylase and α-glucosidase enzymes in vitro. Functional cereals were produced as ready-to-eat cereals at different proportion with variations in the amount of measured acha flour, soybean flour, and blends of orange peels and moringa leaves while maintaining a constant amount of yellow corn. The produced orange peels and moringa leaves blends inclusion to functional cereals had significantly increased phenolic constituents, showed inhibitory activity on α-amylase and α-glucosidase enzymes in-vitro and reduced glycemic index, starch content and starch to sugar ratios. Interestingly, amongst the produced functional cereals, the best two cereals were with their composition made up of corn, acha, soybean, orange peel, moringa leaves (30: 5:15: 0.5: 0.5) and corn, acha, soybean, moringa leaves (30: 5: 15: 1) which both had the high inhibitory effects on the activities of α-amylase and α-glucosidase while depleting starch content in-vitro when compared with commercially consumed cereals (golden morn). PRACTICAL APPLICATIONS: Ready-to-eat cereals are highly consumed by children and by adults inclusively. Commercial breakfast cereals are readily available and consumed irrespective of the fact it has high calorie constituent as more emphasis is placed on their nutrients value which includes vitamins A, vitamin C and calcium for boosting immune system and for proper body growth and functioning. However, these commercial breakfast cereals (golden morn) owing to the high maize and millet content present in them are unfavorable to certain consumers or individuals with health challenges such as diabetic patients. This study shows that functional cereals produced in-vitro extensively are not only nutritious but also medicinal in nature, offering benefits in the management of diabetes and related complications.

Effect of aqueous extract from root and leaf of Sphenocentrum jollyanum pierre on wounds of diabetic rats: Influence on wound tissue cytokines, vascular endothelial growth factor and microbes.

ETHNOPHARMACOLOGICAL RELEVANCE: Sphenocentrum jollyanum is a flowering plant of the Menispermaceae family with bright yellow roots and wedged-shaped leaves. The plant is reputed to possess exceptional wound healing properties and used in folkloric medicine to dress chronic wounds. AIM OF THE STUDY: Wound repair in a hyperglycemic state is known to be impaired and delayed making treatment a difficult challenge. This study sought how the aqueous extracts of root and leaf of Sphenocentrum jollyanum facilitated wound healing by modulating pro-inflammatory cytokines, vascular endothelial growth factor and microbial colonization on excision wound created in diabetic rats. METHODS: Diabetes (blood glucose >250 mg/dl) was induced by feeding normal rats with high fat diet for 14 days after which intraperitoneal injection of low dose streptozotocin (35 mg/kg b.w.) was administered. Wounds were subsequently created and treatments administered afterwards for 14 days. RESULTS: Administration of Sphenocentrum jollyanum root and leaf extracts both orally and topically (100 and 200 mg/kg b.w) significantly (p < 0.05) reduced secretion of pro-inflammatory cytokines (TNF-α, IL-6), number of microbial colonies (CFU/ml × 102), activity of myeloperoxidase and significantly increased growth factor secretion on wounds of the diabetic rats. Histological evaluations of wound tissues of treated diabetic rats revealed matured tissue granulation, presence of new blood vessels, collagen and fibroblast with fewer inflammatory cells. CONCLUSION: The use of Sphenocentrum jollyanum effectively enhanced wound healing which may be related to constituents identified by GC-MS analysis and can thus, be suggested as a therapeutic agent for diabetic wound management.