Biochemistry Research International最新文献

Currently, the synthesis of new compounds with potential bioactivities has become a central issue in the drug discovery arena. Among these new compounds, benzimidazole-sulfonyl scaffolds have vital applications in the fields of pharmaceuticals industries. Benzimidazole and sulfonyl compounds have remarkable biological activities, such as antibacterial, antifungal, anti-inflammatory, antiproliferative, carbonic anhydrase inhibitory, and α-amylase inhibitory activities. Furthermore, recent literature mentions the synthesis and bioactivities of some benzimidazole-sulfonyl hybrids. In this review, we focus on reviewing the synthesis of these hybrid scaffolds and their various types of biological activities of the compounds.

Enzyme immobilization is a powerful method to improve the stability, reuse, and enzymatic properties of enzymes. The immobilization of the α-amylase enzyme from Aspergillus fumigatus on a chitin-bentonite (CB) hybrid has been studied to improve its stability. Therefore, this study aims to obtain the higher stability of α-amylase enzyme to reduce industrial costs. The procedures were performed as follows: production, isolation, partial purification, immobilization, and characterization of the free and immobilized enzymes. The CB hybrid was synthesized by bentonite, chitin, and glutaraldehyde as a cross-linker. The free enzyme was immobilized onto CB hybrid using 0.1 M phosphate buffer pH 7.5. The free and immobilized enzymes were characterized by optimum temperature, Michaelis constant (K _M), maximum velocity (V _max), thermal inactivation rate constant (k _i ), half-life (t _1/2), and transformation of free energy because of denaturation (ΔG _i ). The free enzyme has optimum temperature of 55°C, K _M  = 3.04 mg mL^-1 substrate, V _max=10.90 μmolemL^-1min^-1, k _i  = 0.0171 min^-1, t _1/2 = 40.53 min, and ΔG _i  = 104.47 kJ mole^-1. Meanwhile, the immobilized enzyme has optimum temperature of 60°C, K _M  = 11.57 mg mL^-1 substrate, V _max=3.37 μmolemL^-1min^-1, k _i  = 0.0045 min^-1, t _1/2 = 154.00 min, and ΔG _i  = 108.17 kJ mole^-1. After sixth cycle of reuse, the residual activity of the immobilized enzyme was 38%. The improvement in the stability of α-amylase immobilized on the CB hybrid based on the increase in half-life was four times of the free enzyme.

Introduction: In Ethiopia, different medicinal plants have been claimed and used to treat diarrheal diseases. However, these claimed effects for most medicinal plants have not been scientifically verified. One of such plants in Ethiopian folkloric medicine is Moringa stenopetala, which is usually consumed as a vegetable in southern Ethiopia. Thus, this study aimed to evaluate the antidiarrheal and antisecretory effects of 80% methanolic leaf extract of Moringa stenopetala in different mice models.

Method: Using Swiss albino mice, castor oil-induced diarrhea, charcoal meal-based gastrointestinal motility, and castor oil-induced secretion models were employed to assess antidiarrheal activity. In all of the test models, animals were randomly assigned into five groups consisting of six animals in each group. Group I received 0.5 ml of the vehicle (2% tween-80), while group II was treated with standard drug (3 mg/kg loperamide) in the respective models, whereas groups III to V received 150, 300, and 450 mg/kg of the methanolic leaf extracts of Moringa stenopetala. Onset, frequency, consistency, and weight of stool (diarrhea) were recorded, and different parameters and percentage proportions were calculated. Data were analyzed using one-way ANOVA followed by Tukey's test, and p < 0.05 was considered statistically significant at 95% confidence of interval.

Result: In the castor oil-induced diarrheal model, the percentage inhibition of diarrhea was 48.5, 58.6, and 60% for the respective doses of 150, 300, and 450 mg/kg of the extract. And, the extract showed a 36.8, 54.4, and 55.9% reduction of peristalsis in charcoal meal-based gastrointestinal motility test compared to the negative control group. Moreover, in the antisecretory assay, the 150, 300, and 450 mg/kg doses of MEMS inhibited fluid contents of the stool by 11.5, 54.54, and 61.82%, respectively, relative to the vehicle-treated group.

Conclusion: The findings revealed that the 80% methanolic leaf extract of Moringa stenopetala extract has shown antidiarrheal activity.

The stability of the α-amylase enzyme has been improved from Aspergillus fumigatus using the immobilization method on a bentonite matrix. Therefore, this study aims to obtain the higher stability of α-amylase enzyme from A. fumigatus; hence, it is used repeatedly to reduce industrial costs. The procedures involved enzyme production, isolation, partial purification, immobilization, and characterization. Furthermore, the soluble enzyme was immobilized using 0.1 M phosphate buffer of pH 7.5 on a bentonite matrix, after which it was characterized with the following parameters such as optimum temperature, Michaelis constant (K _M ), maximum velocity (V _max), thermal inactivation rate constant (k _i), half-life (t _1/2), and the change of energy due to denaturation (ΔG _i ). The results showed that the soluble enzyme has an optimum temperature of 55°C, K _M of 3.04 mg mL^-1 substrate, V _max of 10.90 μmole mL^-1 min^-1, k _i of 0.0171 min^-1, t_1/2 of 40.53 min, and ΔG _i of 104.47 kJ mole^-1, while the immobilized enzyme has an optimum temperature of 70°C, K _M of 8.31 mg mL^-1 substrate, V _max of 1.44 μmole mL^-1 min^-1, k _i of 0.0060 min^-1, t _1/2 of 115.50 min, and ΔG _i of 107.37 kJ mole^-1. Considering the results, the immobilized enzyme retained 42% of its residual activity after six reuse cycles. Additionally, the stability improvement of the α-amylase enzyme by immobilization on a bentonite matrix, based on the increase in half-life, was three times greater than the soluble enzyme.

Aloe greatheadii var. davyana or spotted aloe is indigenous to South Africa and widely distributed in the northern provinces. The plant has a vast ethnopharmacological application which is mostly attributed to its phytochemical content. The aim of the study was to examine the effect of abiotic stress factors on the plant's phytochemical content. The phytochemical content of A. greatheadii hexane extracts from four different provinces (Limpopo, Mpumalanga, Gauteng, and North West), harvested from the wild at varied altitudes, rainfall patterns, and soil types, was examined using gas chromatography-mass spectra (GC-MS). The phytochemical content of hexane extracts from the four South African provinces was analysed using heat map analysis and hierarchical clustering dendrogram. The phytochemical content of A. greatheadii hexane extracts was composed of fatty acids, alkanes, benzene, carboxylic acids, ketones, phytosterols, and vitamins. Eicosane, henicosane, and [(2S)-2-[(2R)-4-hexadecanoyloxy-3-hydroxy-5-oxo-2H-furan-2-yl]-2-hydroxyethyl] hexadecanoate were the only compounds detected in all samples from the four provinces. The concentration levels of 2-(((2-ethylhexyl)oxy)carbonyl) benzoic acid, beta-sitosterol, tritetracontane, and ethyl 13-methyltetradecanoate were closely related and expressed a low clustering distance amongst the samples. Variations in soil pH, soil type, and rainfall patterns were detected and differed in the four provinces. The different abiotic stress factors affected the biochemical pathways for the different compounds, with conditions in Gauteng being less favourable for many of the compounds detected. Abiotic stress factors have shown to influence phytochemical biochemical pathways and quantity. Aloe greatheadii plants can be selected based on location seemingly due to the variations that persist in their phytochemical content.

Methods: Phytochemical screening, antioxidant activity, α-amylase, and α-lipase inhibitory assessment were carried out on Moringa oleifera extract.

Results: The result of the phytochemical screening revealed the presence of total phenolic, flavonoid, tannin, and alkaloid contents of values 0.070 ± 0.005 mg gallic acid equivalent/g, 0.180 ± 0.020 mg rutin equivalent/g, 0.042 ± 0.001 mg tannic equivalent/g, and 12.17 ± 0.001%, respectively, while the total protein analysis was 0.475 ± 0.001 mg bovine serum albumin equivalent/g. Ferric reducing antioxidant power (FRAP) and total antioxidant capacity (TAC) values were 0.534 ± 0.001 mg gallic acid equivalent/g and 0.022 ± 0.00008 mg rutin equivalent/g, respectively. Diphenyl-2-picrylhydrazyl (DPPH), ABTS (2,2'-azino-bis (ethylbenzothiazoline-6-sulfonic acid)), and nitric oxide (NO) assays showed the extract to have a strong free radical scavenging activity. The 50% inhibitory concentration (IC₅₀) values of the lipase and amylase activities of the extract are 1.0877 mg/mL and 0.1802 mg/mL, respectively.

Conclusion: However, α-lipase and α-amylase inhibiting activity of M. oleifera could be related to the phytochemicals in the extract. This research validates the ethnobotanical use of M. oleifera leaves as an effective plant-based therapeutic agent for diabetes and obesity.

Reservoir water physicochemical characteristics provide important information about water suitability for fish production. Accordingly, the study aimed to characterize the physicochemical characteristics of Dembi reservoir water for sustainable fish production. The study was conducted in Dembi reservoir during the dry season. Water samples were collected in triplicate from selected 10 sampling sites of the reservoir water using manually prepared water sampler made from polyvinyl chloride (PVC) tube. The depth integrated sampling technique was employed to take water samples for all physicochemical characteristics analysis. From the selected 14 physicochemical characteristics, four (temperature, electrical conductivity, pH, and dissolved oxygen) were tested onsite using a multisystem HQ4d electronic meter (probe), whereas the rest 10 water quality characteristics were tested in the laboratory. The result showed that the current average depth of the dam was 5.6 ± 1.61 m. The overall mean values of the water quality characteristics at different sites of the reservoir were as follows: turbidity (26.4 ± 0.44 FTU), total hardness (22.2 ± 0.51 mgL^-1), NO₃ (5.4 ± 0.48 mgL^-1), NO₂ (0.3 ± 0.11 mgL^-1), NH₄ (2.1 ± 0.06 mgL^-1), PO₄ ^-3 (1.7 ± 0.27 mgL^-1), total alkalinity (52.5 ± 0.91 mgL^-1), and BOD₅ (2.7 ± 0.24 mgL^-1). There was a significant difference (p < 0.05) in all physicochemical characteristics among 10 sampling sites of the reservoir water. The recorded values of all physicochemical characteristics, except NO₂, NH₄, and PO₄ ^-3, were found within the recommended standard limit for fish production. The change in reservoir water depth and increase in nutrients shows the presence of sediment siltation and nutrient enrichment. Therefore, proper watershed management practices and waste management should be carried out for sustainable water quality maintenance and fish production.