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Anti-hyperglycemic and anti-hyperlipidemic effects of hydroethanolic leaf and stem extracts of Vitex doniana on alloxan induced diabetes in rats was evaluated. Thirty (30) male rats were assigned to five (5) groups of six (6) rats each as follows: Group I served as normal control rats and were fed with standard feed and water ad libitum, Group II was induced with diabetes by single intraperitoneal injection of freshly prepared alloxan [150 mg/kg body weight (BW)] to overnight fasted rats but received no treatment, Group III-V were induced with alloxan and treated with 5 mg/kg BW standard drug glibenclamide, 300 mg/kg BW leaf extract and 300 mg/kg BW stem extract of Vitex doniana respectively. The results revealed that the leaf and stem extracts had anti-hyperglycemic activity similar to glibenclamide. Analysis of lipid profile showed that whereas alloxan induced increase in the concentration of total cholesterol, low density lipoprotein and triglycerides, hydroethanolic leaf and stem extracts caused a significant decrease (p

The current work investigated the chemical profile, antimalarial potential and capacity of hydroethanolic

The effects of defattedMoringa oleiferaseed (L) on haemotological indices and body weight was evaluated in rat model of Protein Energy Malnutrition (PEM). Protein Energy Malnutrition is associated with muscle degeneration and anaemia. Protein Energy Malnutrition (PEM) was induced in fifteen (15) rats by feeding them with low protein diet (3% fish meal protein) and water for twenty eight days. Five (5) rats served as positive control (Group A) received commercial feed containing 21% crude protein. The PEM rats were assigned to three groups namely B, C and D. Group B and C were fed with recovery diets ad libitum for another twenty eight days. Group B received feed containing 20% Fishmeal protein and Group C received feed containing 20% defattedM. oleifera seed. Group D were Protein-energy malnourished rats maintained on protein deficient diet (3% fish meal protein). Protein energy malnourished rats had significantly reduced (pM. oleiferain place of 3% fishmeal caused significant (pM. oleiferaseeds ameliorate muscle degeneration and anaemia in PEM rats comparatively similar to 20% fish meal.

Silver nanoparticles are increasingly being used in a wide variety of ways that may lead to frequency of exposure for humans and the environment. Thus, it is necessary to understand the biological effect(s) of these nanoparticles. Previously, we showed that AgNPs activated the kynurenine pathway in rat brain independently of oxidative stress in rats. This present study is aimed at evaluating the effect of AgNPs on some selected cytokines, redox parameters, and on the kynurenine level in rats. Male Wistar rats (130-150 g) were divided into 4 groups. Rats were grouped into control, AgNPs only (50 mg/kg bw), coadministration of AgNPs (50 mg/kg bw), and dexamethasone (100 mg/kg bw) and dexamethasone only (100 mg/kg bw). Results indicated that AgNPs did not significantly elevate MDA levels in rat plasma and brain relative to the control group. AgNPs caused a significant alteration in the level of rat brain and plasma total protein concentration. Meanwhile, AgNPs led to an elevation in the level of reduced glutathione (GSH) in rat plasma but decreased plasma kynurenine level significantly. Furthermore, IFN-γ level was reduced following AgNPs administration, IL-1β decreased across the treatment groups, while NF-κB was reduced in the dexamethasone only and AgNPs + dexamethasone groups when compared with the control. AgNPs led to increased IL-4 levels, while IL-10 levels decreased across the treatment groups. Taken together, our data showed a differential immunomodulatory potential of AgNPs in rats.

Extracts of Alstonia boonei and Carica papaya are used in herbal medicine for the treatment of malaria. This work investigated the phytochemical, antioxidant, and antimalarial effects of hydromethanolic extracts of Alstonia boonei and Carica papaya. A four-day chemosuppressive test was conducted to assess the ability of the extracts to prevent establishment of infection. Three doses of the extracts were administered—100, 200, and 400 mg/kg bw—prior to Plasmodium berghei challenge. Change in body weight, parasitemia, packed cell volume (PCV), and mean survival time was determined. A three-day curative test was also carried out on Plasmodium berghei-infected mice to determine the effects of the plant extracts (200 mg/kg bw) on parasitemia and biochemical indices of liver and kidney functions, lipid metabolism, and oxidative stress. The study revealed that the extracts possessed phenolic compounds (34.13 ± 1.90 mg GAE/g for Alstonia boonei and 27.99 ± 1.46 mg GAE/g for Carica papaya) and flavonoids (19.47 ± 1.89 mg QE/g for Alstonia boonei and 18.24 ± 1.36 mg QE/g for Carica papaya). In vitro antioxidant activity measured as total antioxidant power, total reducing power, and DPPH radical scavenging activity showed that the extracts possessed higher antioxidant activity than the reference compounds. The outcome of the chemosuppressive test revealed that whereas Plasmodium berghei-infected mice had high parasitemia, decreased mean survival time, exhibited loss of weight, and had low PCV, treatment with the extracts reversed the effects in a concentration-dependent manner. Similarly, the curative test revealed that the extracts significantly suppressed parasitemia compared with the malaria negative control group. This was mirrored by reversal of indices of hepatic toxicity (AST, ALT, and ALP levels), nephropathy (urea and creatinine levels), oxidative stress (SOD, CAT, GPx, GSH, and lipid peroxides), and dyslipidemia (TC, HDL, and TG levels and HMG-CoA reductase activity) in infected but treated mice compared with negative control. Put together, the results of this study demonstrate that the extracts of Alstonia boonei and Carica papaya possess antimalarial properties and are able to ameliorate metabolic dysregulations that characterize Plasmodium berghei infection. The phytoconstituents in these extracts are believed to be responsible for the pharmacological activity reported in this study.

Background: Exposure to lead has been linked to biochemical changes similar to those patients suffering from Alzheimer’s disease. Trévo is a phytonutrient-rich product with antiaging and antioxidant properties. Purpose: To investigate the neuroprotective activity of trévo against lead-induced biochemical changes in male Wistar rats. Methods: The study involves 35 animals that were randomly divided into five groups of seven rats each. Group I (Control): Orally administered distilled water; Group II (Induced): Administered 15 mg/kg of lead acetate (PbA) intraperitoneally; Group III (Treatment group): Orally administered 2 mL/kg of trévo for two days before co-administration with PbA for 12 consecutive days; Group IV (Treatment group): Orally administered 5 mL/kg of trévo for two days prior to coadministration with PbA for 12 consecutive days; Group V: Orally administered 5 mL/kg of trévo for 14 consecutive days. Animals were anesthetized with diether and the brain excised and processed for the following biochemical assays: Malonedialdehyde (MDA), glutathione (GSH), catalase (CAT), superoxide dismutase (SOD), glutathione-S-transferase (GT), acetylcholinesterase (AChE), beta-amyloid, glutamate, Na+/K+ ATPase, and glutamate dehydrogenase (GD). Results: PbA caused significant oxidative stress (increased MDA concentration, decreased GSH concentration, suppressed the activity of CAT, SOD), decreased GT activity, increased activity of AChE, increased the concentration of beta-amyloid, and caused glutamate excitotoxicity (increased concentration of glutamate, decreased activity of Na+/K+ ATPase, and GD) in rat brains. Treatment with trévo at the two different doses significantly prevented oxidative damage, beta-amyloid aggregation, glutamate excitotoxicity, and acetylcholine breakdown induced by lead acetate. Conclusion: Our findings added to the reported pharmacological activity of trévo and supported the antiaging potential of trévo.

Postprandial hyperglycemia has orchestrated untimely death among diabetic patients over the decades and regulation of α-amylase activity is now becoming a promising management option for type 2 diabetes. The present study investigated the binding interactions of three structurally diverse dichalcogenoimidodiphosphinate ligands with α-amylase to ascertain the affinity of the ligands for α-amylase using spectroscopic and molecular docking methods. The ligands were characterized using 1H and 31P NMR spectroscopy and CHN analysis. Diselenoimidodiphosphinate ligand (DY300), dithioimidodiphosphinate ligand (DY301), and thioselenoimidodiphosphinate ligand (DY302) quenched the intrinsic fluorescence intensity of α-amylase via a static quenching mechanism with bimolecular quenching constant (Kq) values in the order of x1011 M-1s-1, indicating formation of enzyme-ligand complexes. A binding stoichiometry of n≈1 was observed for α-amylase, with high binding constants (Ka). α-Amylase inhibition was as follow: Acarbose > DY301>DY300>DY302. Values of thermodynamic parameters obtained at temperatures investigated (298, 304 and 310 K) revealed spontaneous complex formation (ΔG, Graphical abstract Synopsis for the Graphical Abstract The present study investigated the binding interaction mechanisms of three structurally diverse dichalcogenoimidodiphosphinate ligands with α-amylase to ascertain the binding affinity of the ligands for α-amylase using spectroscopic techniques and molecular docking. The study provided insights for use of dichalcogenoimidodiphosphinate ligands as novel α-amylase inhibitors for management of postprandial hyperglycemia.Image 1, Highlights • Interaction of α-amylase with dichalcogenoimidodiphosphinate ligands was studied. • Spectroscopy and molecular docking explored the interaction mechanisms. • The main driving forces were hydrophobic interactions with DY300 and DY301. • The ligands quenched α-amylase fluorescence intensity by static mechanism. • Dichalcogenoimidodiphosphinate ligands inhibited α-amylase activity.

Aim: The present study investigated the effects of intensive glucose regulation with combined treatment of Aloe vera gel (a herbal agent) and Metformin in an alloxan-induced diabetic rat model. Methods: Forty rats were assigned to the following groups and treated for 21 days: Group 1 (normal untreated control), Group 2 (untreated diabetic rats, DR), Group 3 (DR + 300 mg/kg PE of Aloe vera ), Group 4 (DR + 2 mg/kg Metformin) and Group 5 (DR + 300 mg/kg PE of Aloe vera + 2 mg/kg Metformin). The effect of the treatments on fasting blood glucose (FBG) level, lipid profile, renal function, atherogenic index, pancreas and kidney histopathologies were assessed. Results: FBG level in Group 5 rats decreased by 28.4, 38.0 and 69.0% at Day 7, 14 and 21, respectively. Hyperlipidaemia, high atherogenic index, increased plasma creatinine and urea levels observed in the diabetic rats were ameliorated by the single and combined treatments with Aloe vera and Metformin. Reduced level of HDL-cholesterol in the untreated diabetic rats significantly improved by 160.0, 89.8 and 178.7% respectively in Group 3, 4 and 5 animals. The pancreas and kidney histopathologies indicated signs of recovery in Group 5 rats unlike those of Group 2 that had evidence of necrotic cells in both the acini and islet in pancreas and total glomeruli erosion in kidney. Conclusion: Aloe vera in combination with Metformin for treatment of diabetic patients could avert diabetes-associated dyslipidaemia, improve cellular integrity and increase, thereby preventing patients from risk of cardiovascular diseases and kidney failure.

Background: Induction of toxicity using nitrosamines provides a reliable animal model for the study of oxidative damage to lipids, cellular membranes, proteins and DNA. In the present report, the effects of partially purified fractions of Senna occidentalis leaves on diethylnitrosamine intoxicated rats were studied.Methods: Fractions obtained from eluting the column with solvents of increasing polarity, n-hexane, chloroform, ethyl acetate, ethanol, methanol and distilled water were subjected to in vitro for their ability to scavenge 1, 1-dipheny l, 2-pycryl hydrazyl (DPPH) radical. Fraction 6a eluted with ethyl acetate:ethanol (50:50) possessed the highest antioxidant activity, this fraction was therefore selected for in vivo studies. Twenty rats, each weighing between 150 to 250 g were randomly allocated into four groups of five rats each. Hepatotoxicity was induced using a single intraperitoneal injection of diethylnitrosamine (DEN) at the 200 mg/kg body weight. Treatment was carried out for 3 weeks by oral gavage as follows: group A, normal control, group B, DEN control, group C, DEN+fraction (10 mg/kg), group D, DEN+silymarin (5 mg/kg).Results: The results showed that DEN toxicity significantly (pConclusions: These results show hepatoprotective potentials of the fraction. Furthermore, GC-MS fingerprinting of fraction 6a revealed the presence of compounds with anticancer, antioxidant and anti-inflammatory properties confirming its high chance for exploration as a medicinal agent.

The interactions between α-amylase, one of the key enzymes linked with postprandial glucose regulation, and Chrysophyllum albidum seed methanolic extract(CSME) and its green-synthesized silver nanoparticles(CSAgNP) were investigated using multiple spectroscopy including Fourier Transform-Infrared(FT-IR), ultraviolet(UV)-visible absorption, fluorescence spectroscopy, and biochemical analysis. FT-IR spectroscopy revealed presence of some functional groups in the samples. CSME and CSAgNP inhibited α-amylase. The intrinsic fluorescence intensity of α-amylase was quenched by CSME and CSAgNP via static mechanisms, indicating formation of complex between the enzyme and inhibitors. α-Amylase-CSAgNP complex had higher binding constants. The binding processes were exothermic, entropy driven, spontaneous, and involved hydrogen bonds and van der Waals force. Synchronous fluorescence quenching indicated alteration in microenvironment of α-amylase catalytic site tyrosine residues.FT-IR spectroscopy revealed shifts in amide I peak position of α-amylase due to interaction with CSME/CSAgNP. Absorption spectroscopy also affirmed changes in enzyme conformation. This study may provide theoretical basis for designing novel α-amylase inhibitors.

In this study, α-amylases from fresh and dried Cyperus esculentus seeds were isolated and characterized for biochemical and thermodynamic properties. The α-amylases (FTNE-α-amylase and DTNE-α-amylase) were optimally active at 60–70 °C, pH 7.0 (FTNE-α-amylase) and pH 6.0 (DTNE-α-amylase) with activation energies (Ea) of 3.56 and 6.81 kJ mol⁻¹, respectively. Both enzymes retained above 70% of their hydrolytic activities after 1 h at pH 6.0–8.0. The enzyme activities were more enhanced in the presence of divalent metal ions (Ca²⁺, Mg²⁺, Zn²⁺, Cu²⁺, Ba²⁺, Co²⁺, Pb²⁺, and Hg²⁺) than monovalent ions. SDS, cyclohexanol, ether and diethylamine inhibited them except EDTA. Using soluble starch as substrate, DTNE-α-amylase had higher Vₘₐₓ, Kcₐₜ and lower Kₘ than FTNE-α-amylase. Both enzymes expressed high substrate preferences for yam flour amidst other substrates with catalytic efficiencies (Kcₐₜ/Kₘ) of 2.71 and 4.44 mL. mg⁻¹sec⁻¹, respectively. The higher catalytic efficiency of DTNE-α-amylase was due to its transition state stabilization (ΔGE₋S = -0.90 kJ mol⁻¹ and ΔGE₋T = -2.22 kJ mol⁻¹). Fourier Transformed-Infrared (FTIR) spectroscopy revealed changes in C–O stretching and -N-H bending in the substrate-bound enzymes. Thermal inactivation of the amylases followed first-order rate kinetics and was non-spontaneous (ΔG#>0). FTNE-α-amylase half-lives and D-values at 70 and 80 °C, and Z-value (256.41 °C), were however higher than in DTNE-α-amylase (Z-value = 63.29 °C; t₁/₂ = 22.43 min at 70 °C) indicating that FTNE-α-amylase is more thermally stable than DTNE-α-amylase and would be more industrially applicable as a thermostable starch-hydrolyzing enzyme.

Medicinal plants are reservoirs of natural products with anti-diabetic potentials. In the present study we screened Costus afer for the presence of plant products and to study the effects of the methanolic leaf extract of the plant on fasting blood glucose of normal rats. Adult male wistar strain albino rats were given graded doses (200-800mg/kg) of the methanolic leaf extract of Costus afer, standard hypoglycaemic drug glibenclamide or a combination of the two in the presence or absence of oral glucose feeding. Fasting blood glucose was monitored for 6 hours post administration of drugs. Phytochemical studies revealed relative amounts of alkaloids, flavanoids, tannins, phenols, glycosides and terpenoids. Costus afer showed significant hypoglycaemic effect (p the standard drug. However, the plant extract did not reduce blood glucose in glucose fed rats. Also, a combination of plant extract and glibenclamide caused a significant reduction in fasting blood sugar of both glucose loaded and unloaded rats. The results validate the use of Costus afer as a hypoglycaemic plant in native medicine. These effects could be attributed to its phytochemical constituents. Costus afer could be a promising plant for the development of anti-diabetic drugs.

Chlamydophila represents a distinct genus of gram negative bacteria associated with a spectrum of both human and animal disease and, as such, is an important health and economic concern. Central to the pathogenicity of Chlamydophila are antigenic proteins among which the Major Outer Membrane Proteins (MOMP) have received significant attention. MOMP from Chlamydophila pneumoniae and Chlamydia trachomatis, the human pathogens, to date, remain the best characterised. In addition, MOMP-derived peptides have been shown to potentiate anti-inflammatory and anti-atherogenecity, by a cell mediated system involving MHC class II proteins [2]. However, despite the importance of this protein as a vaccine target against inflammation driven pathologies attributed to Chlamydia, tremendous challenges in the isolation of this membrane-bound, cysteine-rich protein make it difficult to experimentally isolate the protein for detailed structural and immunological studies. In an effort to reveal a plausible structure and function for Chlamydophila MOMP and aid in the rational design of potential lead candidates for future drug design, computational methods have been employed. Firstly, a knowledge-based approach was used to explore Chlamydia MOMP sequences to identify Asp-ProX (NPX) motifs, commonly found in long chain fatty acid transporters such as aquaporins and some aquaglyceroporins. In Chlamydial MOMPs, a variety of substitutions are found at the third 'X' position; NP-A/S/E/T/K, which may account for its potential to transport a variety of solutes, as a strategy for coping with the absence of essential metabolic enzymes. Earlier findings suggest that MOMP from Chlamydophila pneumoniae is permeable to sugars, amino acids, dicarboxylates and ATP. Subsequent homology modeling of MOMP from C. pneumoniae (using template-based methods) has provided insight into the orientation of these functional motifs in the 3-dimensional structures of MOMPs, from which a plausible novel transport model has been derived [1]. In our model the NPA motif is oriented toward the extracellular side while the two NPS motifs are juxtaposed inside the barrel posed to fulfil a transport role, via solute binding. Secondly, to understand how such MOMP-derived peptides could potentiate an immune response, via binding MHC II alleles, a flexible molecular docking protocol was employed [1]. The reliability of the docking protocol was tested by docking peptides extracted from the PDB coordinates of the MHCs of interest and compared to the original peptide-MHC complex, as seen in the crystal structure of the complex. We used the docking protocol to score four peptides of interest for their candidacy as potential new leads in a rational drug design strategy against chronic inflammation, which characterises Chlamydial involvement in atherosclerosis and respiratory diseases. Our computational work offers new insight into the structure and functional mechanism involved in solute transport via MOMP across Chlamydial cell membranes, which could be used in the design of inhibitors that could obstruct nutrient uptake and halt Chlamydial viability in their host. Also, this work supports the role of MOMP-derived peptides as vaccine candidates for immune-therapy in chronic inflammation that can result in cardiovascular events.

The recent resurgence of interest in the study of mitochondria has been fuelled in large part by the recognition that genetic and/or metabolic alterations in this organelle are causative or contributing factors in a variety of human diseases including cancer. This study hypothesizes that co-administration of artesunate and ferrous sulfate could induce apoptosis which can be targeted on cancerous cells in such a manner, thus providing a novel, viable and perhaps inexpensive way of dealing with the cancer scourge. Artesunate and Ferrous sulfate were co-administered to rats at various doses for seven days. At the end of the treatment, the rats were fasted overnight and sacrificed by cervical dislocation. Low ionic strength mitochondria were isolated from hepatic cells of the rats and assayed for protein content; changes in the absorbance of the liver mitochondria; and mitochondrial swelling. Co-administration of artesunate and ferrous sulfate resulted in a significant increase (P

Major outer membrane proteins (MOMPs) of Gram negative bacteria are one of the most intensively studied membrane proteins. MOMPs are essential for maintaining the structural integrity of bacterial outer membranes and in adaptation of parasites to their hosts. There is evidence to suggest a role for purified MOMP from Chlamydophila pneumoniae and corresponding MOMP-derived peptides in immune-modulation, leading to a reduced atherosclerotic phenotype in apoE(-/-) mice via a characteristic dampening of MHC class II activity. The work reported herein tests this hypothesis by employing a combination of homology modelling and docking to examine the detailed molecular interactions that may be responsible. A three-dimensional homology model of the C. pneumoniae MOMP was constructed based on the 14 transmembrane β-barrel crystal structure of the fatty acid transporter from Escherichia coli, which provides a plausible transport mechanism for MOMP. Ligand docking experiments were used to provide details of the possible molecular interactions driving the binding of MOMP-derived peptides to MHC class II alleles known to be strongly associated with inflammation. The docking experiments were corroborated by predictions from conventional immuno-informatic algorithms. This work supports further the use of MOMP in C. pneumoniae as a possible vaccine target and the role of MOMP-derived peptides as vaccine candidates for immune-therapy in chronic inflammation that can result in cardiovascular events.