Inhibition of carbohydrate hydrolyzing enzymes associated with type 2 diabetes and antioxidative properties of some edible seeds in vitro

This study sought to evaluate the antioxidant properties and effects of some edible wild seeds [Afzelia africana Sm. (AFZ), Cyperus esculentus L. (CYP), Eleusine coracana Gaertn. (ELE), Irvingia gabonensis (Aubry-Lecomte ex O’Rorke) Baill. (IRV), Monodora myristica Dunal. (MON) and Parinari curatellifolia Planch. ex Benth. (PAR)] on α-amylase and α-glucosidase activities. The phenolic content and antioxidant activities of aqueous extracts of the seeds as typified by 1,1-diphenyl-2 picrylhydrazyl (DPPH) and hydroxyl (OH) radicals scavenging abilities and inhibition of Fe²⁺-induced malondialdehyde (MDA) production in rat’s pancreas in vitro were also assessed. ELE had significantly (p < 0.05) higher total phenol content than the other seeds; however, AFZ had the highest flavonoid content. The extracts scavenged DPPH· and OH· in a dose-dependent manner with aqueous extracts of PAR having the highest DPPH· scavenging ability, while extracts from IRV had the highest OH· scavenging ability and inhibition of Fe²⁺-induced MDA production in rat’s pancreas. Furthermore, all the extracts inhibited α-amylase and α-glucosidase activities in a dose-dependent manner. The α-amylase inhibitory effect of MON (IC₅₀ = 0.48 mg/mL) was comparable to that of acarbose (IC₅₀ = 0.40 mg/mL), while the α-glucosidase inhibitory effect of AFZ (IC₅₀ = 0.45 mg/mL) was comparable to that of acarbose (IC₅₀ = 0.39 mg/mL). The results suggest the potential use of the seeds in the dietary management of blood glucose levels associated with type 2 diabetes.

     

Berberine modulates crucial erectogenic biomolecules and alters histological architecture in penile tissues of diabetic rats

Berberine is an isoquinoline alkaloid, found in several plants. Diabetes induces erectile dysfunction (ED) via reduction in some hormones and enzymes implicated in sexual function. This study aimed to investigate the role of berberine on crucial biomolecules linked to penile function in diabetic rats. Sixty-three (63) adult male rats were used and distributed into nine groups (each = 7). Group I–IV normal rats administered with citrate buffer (pH 4.5), sildenafil citrate (SD, 5.0 mg/kg), 50 and 100 mg/kg of berberine, respectively, via oral gavage. Rats in groups V–IX were diabetic rat with ED treated with buffer, SD, 50 and 100 mg/kg of berberine, and acarbose (25 mg/kg ACA) respectively. The result revealed that histological architecture in penile tissues were altered in diabetic groups treated with berberine, sildenafil citrate and acarbose when compared to the diabetic control group. Treatment with berberine, increased testosterone, luteinizing hormone and follicle-stimulating hormone in diabetic rat with ED. Also, reduced prolactin level and acetylcholinesterase, angiotensin-1 converting enzyme, adenosine deaminase and arginase activities were observed in berberine treated diabetic rat with ED. Molecular docking analysis revealed that berberine had strong binding affinities for these enzymes. Thus, berberine could represent a potential therapeutic agent for diabetes-induced ED.     

Influence of gallic acid on α-amylase and α-glucosidase inhibitory properties of acarbose

Acarbose is an antidiabetic drug which acts by inhibiting α-amylase and α-glucosidase activities but with deleterious side effects. Gallic acid (GA) is a phenolic acid that is widespread in plant foods. We therefore investigated the influence of GA on α-amylase and α-glucosidase inhibitory properties of acarbose (in vitro). Aqueous solutions of acarbose and GA were prepared to a final concentration of 25μM each. Thereafter, mixtures of the samples (50% acarbose + 50% GA; 75% acarbose + 25% GA; and 25% acarbose + 75% GA) were prepared. The results revealed that the combination of 50% acarbose and 50% GA showed the highest α-glucosidase inhibitory effect, while 75% acarbose + 25% GA showed the highest α-amylase inhibitory effect. Furthermore, all the samples caused the inhibition of Fe²⁺-induced lipid peroxidation (in vitro) in rat pancreatic tissue homogenate, with the combination of 50% acarbose and 50% GA causing the highest inhibition. All the samples also showed antioxidant properties (reducing property, 2,2′-azino-bis (-3-ethylbenzthiazoline-6-sulphonate [ABTS*] and 1,1-diphenyl-2-picrylhydrazyl [DPPH] free radicals scavenging abilities, and Fe²⁺ chelating ability). Therefore, combinations of GA with acarbose could be employed as antidiabetic therapy, with a possible reduction of side effects of acarbose; nevertheless, the combination of 50% acarbose and 50% GA seems the best.     

Hepatoprotective property of ethanolic and aqueous extracts of fluted pumpkin (Telfairia occidentalis) leaves against garlic-induced oxidative stress

Fluted pumpkin (Telfairia occidentalis) leaf is a darkish-green leafy vegetable popularly used in soup and in herbal preparations for the management of many diseases in Nigeria. In this study, the hepatoprotective property of ethanolic and aqueous extracts of T. occidentalis leaf (earlier confirmed to have a high level of antioxidant activity) against garlic induced-oxidative stress in rat hepatocytes was investigated. Oxidative stress was induced in Wistar strain albino rats by overdosing them with raw garlic (4%) for 14 days, and this caused a significant increase (P < .05) in serum alkaline phosphatase (ALP), glutamate oxaloacetate transaminase (GOT), and glutamate pyruvate transaminase (GPT), while there was no significant change (P > .05) in serum bilirubin, albumin, globulin, and total proteins. However, intubation of some of the rats fed raw garlic with 5 mg or 10 mg/0.5 mL of T. occidentalis leaf extract (ethanolic or aqueous) caused a significant decrease (P < .05) in serum ALP, GOT, and GPT when compared with rats fed raw garlic without intubation with the T. occidentalis leaf extract. Moreover, 10 mg/0.5 mL of extract was more effective than 5 mg/0.5 mL of extract, while the aqueous extracts appeared to be more effective than the ethanolic extracts in protecting hepatocytes. It could be inferred that both aqueous and ethanolic extracts of T. occidentalis leaf have hepatoprotective properties, although the aqueous extract is more effective than the ethanolic extract, which could be attributed to the higher antioxidant activity of the aqueous extract than the ethanolic extracts of T. occidentalis leaves.     

Properties of flavonoids influencing the binding to bilitranslocase investigated by neural network modelling

Bilitranslocase is a plasma membrane carrier firstly identified on the sinusoidal (vascular) domain of liver cells and later on also in the gastric epithelium. It transports diverse organic anions, such as bilirubin, some phthaleins and many dietary anthocyanins, suggesting that it could play a role both in the absorption of flavonoids from dietary sources and in their hepatic metabolism. This work was aimed at characterising the interaction of bilitranslocase with flavonols, a flavonoid sub-class. The results obtained show that, contrary to anthocyanins, flavonol glycosides do not interact with the carrier, whereas just some of the corresponding aglycones act as relatively poor ligands to bilitranslocase. These data point to a clear-cut discrimination between anthocyanins and flavonols occurring at the level of the bilitranslocase transport site. A quantitative structure-activity relationship based on counter propagation artificial neural network modelling was undertaken in order to shed light on the nature of flavonoid interaction with bilitranslocase. It was found that binding relies on the ability to establish hydrogen bonds, ruling out the involvement of charge interactions. This requisite might be at the basis of the discrimination between anthocyanins and flavonols by bilitranslocase and could lie behind some aspects of the distinct pharmacokinetic properties of anthocyanins and flavonols in mammals.     

Biochemical changes in micro-fungi fermented cassava flour produced from low- and medium-cyanide variety of cassava tubers

Comparative studies were carried out on the ability of pure strain of Rhizopus oryzae and Saccharomyces cerevisae to alter the nutritional quality of cassava flour produced from low- and medium-cyanide variety of cassava tuber. Low- and medium-cyanide variety of cassava tubers were collected from International Institute of Tropical Agriculture (IITA), Ibadan, Nigeria. These tubers were washed, peeled, grated and aseptically inoculated with pure strains of Rhizopus oryzae and Saccharomyce cerevisae in nutrient solution respectively, before allowing them to ferment aerobically for 3 days. The fermented mash was subsequently dried and milled into cassava flour. Subsequently, the proximate, mineral and the antinutrinet composition of the cassava flour were determined. The results of the study revealed that the unfermented flour from low-cyanide cassava variety had higher protein, fibre, ash, fat, Ca, Na and K; while those produced from medium-cyanide variety, had higher antinutrinet (tannin, cyanide & phytate), Zn, Mg and Fe content. However, solid substrate fermentation of the cassava mash using Rhizopus oryzae and Saccharomyces cerevisae respectively caused a significant (P < 0.05) increase in the protein and fat content. The nutrient enrichment was significantly higher (P < 0.05) in flour produced from low-cyanide cassava variety. In addition, Saccharomyces cerevisae fermentation brought about a higher increase in the nutrient content than Rhizopus oryzae fermentation. Conversely, fermentation of the cassava caused a significant decrease (P < 0.05) in the antinutrient content of the flour; although, the level of decrease was more in the flour produced from low-cyanide variety than medium-cyanide variety. Nevertheless, there was no significant difference (P > 0.05) in the ability of the fungi to decrease the antinutrient (except phytate) of the cassava flour. Furthermore, micro-fungi fermentation did not cause a significant change (P > 0.05) in mineral content (except Mg and K) of the fermented cassava flour. In conclusion, unfermented cassava flour produced from low-cyanide cassava tubers had high nutrient composition and low antinutrient content and more susceptible to micro-fungi nutrient enrichment and detoxification than medium-cyanide variety. Furthermore, Saccharomyces cerevisae was more efficient in the nutrient enrichment of the cassava flour than Rhizopus oryzae.     

Attenuation of oxidative stress and hepatic damage by some fermented tropical legume condiment diets in streptozotocin-induced diabetes in rats

ObjectiveTo investigate the modulatory effect of fermented legume condiments diet on oxidative stress in streptozotocin (STZ) induced diabetic rats.MethodsAdult male Wistar rats were randomly divided into six groups with six animals in each group. Diabetes was induced by intraperitoneal injection of STZ (35 mg/kg b.w.). After being confirmed diabetic, the rats were fed with fermented Bambara groundnut, Locust bean and Soybean diets for 14 days. The plasma was obtained after 14-day treatment and analyzed for hepatic damage marker enzymes (AST, ALT and ALP) and in vivo antioxidant indices.ResultsThe diabetic untreated rats showed elevated (P<0.05) levels of AST, ALT, ALP and malondialdehyde with reduced activities of glutathione^?S^?transferase, catalase as well as plasma reduced glutathione, vitamin C and total protein content. However, treatment of diabetic rats with fermented legume condiments diets for 14 days significantly (P<0.05) reversed the above parameters towards normalcy, suggesting their modulation of oxidative stress, which may be due to their high phenolic content and antioxidant capacity.ConclusionsThe attenuation of oxidative stress and protection of hepatic tissue damage by the legume condiment diets in STZ induced diabetic rats compare favourably with that of metformin, a well known oral hypoglycemic drug.     

Sorghum stem extract modulates Na<Superscript>+</Superscript>/K<Superscript>+</Superscript>-ATPase,ecto-5′-nucleotidase,and acetylcholinesterase activities

Sorghum stem (Sorghum bicolor) has been in use in traditional medicine systems for the management of neurodegenerative conditions. However, there is dearth of information on the scientific basis for its use in the treatment of such conditions. This study sought to assess the antioxidant activity and effects of phenolic extract from sorghum stem (Sorghum bicolor) on some cholinergic (acetylcholinesterase (AChE)) and purinergic (Na⁺/K⁺-ATPase and ecto-5′-nucleotidase) enzymes associated with neurological conditions. Phenolic-rich extract was prepared using methanol: 1 N HCl (1:1, v/v) mixture and characterized using high-performance liquid chromatography-diode array detector (HPLC-DAD). In vitro tests were used to investigate the effects of the phenolic extract on AChE, Na⁺/K⁺-ATPase, and ecto-5′-nucleotidase activities. Furthermore, the hydroxyl (OH) radical scavenging and Fe²⁺-chelating abilities of the extract were investigated. HPLC-DAD analysis revealed the presence of some phenolic acids such as caffeic acid (120.58 mg/g), ferulic acid (76.45 mg/g), gallic acid (17.48 mg/g), chlorogenic acid (16.25 mg/g), and flavonoids such as kaempferol (15.98 mg/g), rutin (51.07 mg/g), quercetin (263.16 mg/g), and quercitrin (89.21 mg/g) in the phenolic extract. The extract significantly inhibited AChE and ecto-5′-nucleotidase activities in a dose dependent manner with IC₅₀?=?24.88 μg/ml and IC₅₀?=?37.49 μg/ml, respectively, and increased Na⁺/K⁺-ATPase activity in a dose dependent manner. Furthermore, the phenolic extract also scavenged OH radicals and was able to chelate Fe²⁺ in a dose dependent manner with IC₅₀?=?54.27 μg/ml and 18.47 μg/ml, respectively. This study revealed the antioxidant and modulatory effects of phenolic extracts from sorghum stem on some cholinergic and purinergic enzymes.