Α-amylase Activity Research Articles

Phytochemical analysis, antibacterial and anti-diabetic activity of three different seaweed extracts

Aim: Marine seaweed contains potential phytochemical compounds that could able to cure different health issues in humans naturally. Hence the research was aimed to investigate the antibacterial and in vitro anti-diabetic activity of three different seaweed extracts. Methods: Phytochemical compounds like phenol, flavonoids, tannins and alkaloids were quantitatively identified. Antibacterial activity of the seaweed extracts were determined against five different test bacteria. In vitro anti-diabetic activity of the extracts were investigated based on its inhibition effect on the alpha-amylase and alpha-glucosidase activity. Findings: Phytochemical analysis showed more phenolic and flavonoid content in green and brown seaweed extracts and lesser content in red seaweed extract. Antibacterial activity of green and brown seaweed extracts showed good inhibitory zones against all test bacteria ranging from 22.9 ± 0.57 mm to 24.9 ± 0.57 mm (green seaweed extract) and 17.9 ± 0.57 mm to 21.6 ± 0.75 mm (brown seaweed extract) respectively. In vitro anti-diabetic activity of seaweed on the inhibition of enzymes showed promising results. Among the three types, green seaweed extracts showed maximum inhibition of α-Amylase and α-glucosidase activity of 86.6 ± 0.76 % and 82.9 ± 0.57 % respectively. Conclusion: Findings showed that the phytochemicals present in the methanolic extract of seaweeds attribute positively for different pharmacological properties like antibacterial, anti-oxidant and anti-diabetic activity. Optimizing the production factors would able to commercialize the seaweeds in drug forms and could be used for the treatment of various diseases in humans.

Biological Potential of Asphodelus microcarpus Extracts: α-Glucosidase and Antibiofilm Activities In Vitro

Type 2 diabetes (T2D), characterized by insulin resistance and β-cell dysfunction, requires continuous advancements in management strategies, particularly in controlling postprandial hyperglycemia to prevent complications. Current antidiabetics, which have α-amylase and α-glucosidase inhibitory activities, have side effects, prompting the search for better alternatives. In addition, diabetes patients are particularly vulnerable to yeast infections because an unusual sugar concentration promotes the growth of Candida spp. in areas like the mouth and genitalia. Asphodelus microcarpus contains bioactive flavonoids with potential enzyme inhibitory properties. This study investigates α-amylase and α-glucosidase inhibitory activities and antioxidant and antimycotic capacity of ethanolic extracts from different parts of A. microcarpus. Results show that extracts significantly inhibit α-glucosidase, with the IC50 value being up to 25 times higher than for acarbose, while exerting low α-amylase activity. The extracts also demonstrated strong antioxidant properties and low cytotoxicity. The presence of phenolic compounds is likely responsible for the observed biological activities. Molecular docking analysis of 11 selected compounds identified emodin and luteolin as significant inhibitors of α-glucosidase. Additionally, the extracts demonstrated significant antibiofilm action against an MDR strain of Candida albicans. These findings suggest that A. microcarpus is a promising source of natural compounds for T2D management.

Proximate, Mineral, Amino Acid Composition, and Bioactive Properties of Dough Meals Supplemented with African Walnut Flour

This study investigated the impact of African walnut flour supplementation on the nutritional and bioactive properties of dough meals formulated with varying proportions of plantain flour. The proximate composition, mineral content, amino acid profile, color characteristics, antioxidant and anti-diabetic properties were analyzed for five different formulations: 100% plantain flour (P100), 95% plantain flour with 5% African walnut flour (PAW95), 90% plantain flour with 10% African walnut flour (PAW90), 85% plantain flour with 15% African walnut flour (PAW85), and 80% plantain flour with 20% African walnut flour (PAW80). The proximate analysis revealed significant variations, with moisture content ranging from 53.71% to 71.89%, ash content from 0.77% to 1.28%, and protein content from 3.38% to 11.14%. Notably, PAW80 showed the highest protein content. Mineral analysis showed that calcium, potassium, and magnesium levels varied significantly across the samples, with the highest calcium content observed in PAW80 (32.55 mg/kg) and the highest potassium content in PAW95 (47.80 mg/kg). Amino acid analysis indicated that essential amino acids, particularly leucine, valine, and lysine, were present in higher concentrations in the supplemented samples compared to P100. Antioxidant assays indicated that PAW80 had the highest 2,2-diphenyl-1-picrylhydrazyl (DPPH) (67.22%) and hydroxyl (73.66%) free radical scavenging activities. The in vitro anti-diabetic assays revealed that α-amylase and α-glucosidase inhibitory activities were enhanced with higher walnut flour supplementation. These findings suggest that African walnut flour can significantly enhance the nutritional quality and bioactive properties of plantain-based dough meals, and thus make it a functional food with potential health benefits.

Effects of dietary fish meal replacement by Periplaneta americana meal on growth, metabolism, intestinal health and resistance against Aeromonas hydrophila of Micropterus salmoides

An 8-week culture experiment was conducted to investigate the effects of partial replacement of fish meal (FM) with Periplaneta americana meal (PAM) on growth performance, body composition, serum biochemical parameters, intestinal health and resistance against Aeromonas hydrophila of largemouth bass, Micropterus salmoides. A total of 450 healthy largemouth bass with an initial body weight (IBW) of 14.55±0.09 g were randomly divided into five groups. Five experimental diets were prepared by replacing 0 % (P0), 15 % (P15), 30 % (P30), 45 % (P45) and 60 % (P60) of the FM in the basal diet with PAM, respectively. The results showed that final body weight (FBW), weight gain rate (WGR), and specific growth rate (SGR) were no significant difference in P15 and P30 compared with the control group (P > 0.05). Crude protein of whole fish body was significantly increased and crude lipid was significantly decreased in all PAM groups (P < 0.05). In the P30, the antioxidant enzyme activities were significantly higher than those in the control and other experimental groups, and malondialdehyde (MDA) was significantly decreased (P < 0.05). The activities of α-amylase and pepsin increased significantly in P15 and P30 and decreased significantly in P45 and P60 (P < 0.05). Lipase was significantly increased in all groups except P15 than in the control group (P < 0.05). There were no significant differences in villus height (VH), crypt depth (CD), and muscle thickness (MT) among all groups (P > 0.05), but villus width (VW) was significantly decreased in P45 and P60 (P < 0.05). The relative expression of IL-10 and TGF-β1 were first up-regulated and then down-regulated, while IL-8 was opposite (P < 0.05). The relative expression of Casp3, Casp9 and IFN-γ were significantly up-regulated in P45 and P60 (P < 0.05). After injecting A. hydrophila, all groups of largemouth bass experienced mortality, but cumulative mortality was lowest in the P30. In conclusion, PAM can partially replace FM in the diet of juvenile largemouth bass. The replacement of no more than 30 % is unlikely to adversely affect growth performance, and can increase the crude protein content of the whole fish body, and is beneficial to intestinal health.

Effects of freshness of poultry by-product meal on the growth performance, immune response, and hepatopancreatic health of Macrobrachium rosenbergii

A 73-day feeding trial was conducted to determine the effects of the freshness of poultry by-product meal on the growth performance, immune response and hepatopancreatic health of giant freshwater prawn, Macrobrachium rosenbergii. Three semi-purified diets were formulated containing 2.5 % poultry by-product meal with different TVB-N value, designated as L group (untreated poultry by-product meal, TVB-N 10 mg/100 g, i.e., dietary TVB-N 55 mg/100 g), M group (TVB-N 300 mg/100 g, i.e., dietary TVB-N 60 mg/100 g), and H group (TVB-N 450 mg/100 g, i.e., dietary TVB-N 68 mg/100 g), and fed to three groups of prawns (initial weight: 0.82 ± 0.01 g), respectively. Results showed that the weight gain rate (WGR) and specific growth rate (SGR) of prawns significantly decreased with the TVB-N value increased (P < 0.05). The survival rate (SR) and hepatosomatic index (HSI) of prawns in group M and group H were significantly decreased (P < 0.05), while the feed conversion ratio (FCR) was significantly increased (P < 0.05). In addition, the lipase (LPS) and α-amylase (α-AMS) activity of prawns in group L was significantly higher than that in group H (P < 0.05). With the poultry by-product meal TVB-N value increased, the activity of total superoxide dismutase (T-SOD) and glutathione S-transferase (GST) was significantly decreased. RT-qPCR results showed that the expression of bok in group H was significantly higher than that in group L and group M (P < 0.05), the expressions of caspase3, caspase9, bax, and nf-κb in group H were significantly higher than that in group L (P < 0.05). High temperature stress and ammonia nitrogen stress significantly decreased the cumulative survival rate of prawns in group M and group H. Conclusively, it is necessary to guarantee the freshness of the ingredients in prawn formulated diets, and the TVB-N value of diets is recommended not to exceed 60 mg/100 g.

Combination of maleic hydrazide and coumarin inhibits rice seed germination involving reactive oxygen species accumulation, ABA metabolism and starch degradation

Pre-harvest sprouting (PHS) in cereal crops is a prevalent phenomenon that impacts grain yield and quality. Several PHS inhibitory compounds were screened and identified in previous studies, such as eugenol (EUG), maleic hydrazide (MH), coumarin (COU), etc. However, few studies have focused on the combination of PHS inhibitors, and the inhibitory mechanism remains unclear. Here, through combination tests of EUG, MH, and COU, the optimal combination of PHS inhibitors was selected as MH 20 mg L−1 + COU 100 mg L−1, which presented the lowest germination percentages. The optimal combination treatment significantly decreased the germination rate, α-amylase activity, content of soluble sugar and soluble protein, enhanced ABA content and the activity of superoxide dismutase (SOD) and peroxidase (POD), inhibited the production of superoxide anion (O2−) and hydrogen peroxide, and reduced the content of malondialdehyde (MDA); conversely, this trend is precisely the opposite in normal germination. Furthermore, gene expression analysis revealed that the optimal combination of MH and COU significantly decreased the expression level of OsAmy1A and OsAmy3D at 12 and 48 h after imbibition (HAI); and promoted the expression of OsRbohs (OsRbohA, OsRbohC, OsRbohD, OsRbohE, OsRbohH) and ABA biosynthetic genes OsNCED1, OsNCED2, and OsNCED5, especially OsNCED2 at 12 HAI, but down-regulated expression of OsRbohs and ABA catabolic genes OsABA8ox1-3 at 48 HAI. These results demonstrated that the delay in seed germination induced by MH and COU involved in ROS, ABA, and sugars; the optimal combination of MH and COU inhibited the germination process by promoting ABA biosynthesis and reducing ABA catabolism, and restraining the α-amylase activity to lower soluble sugar content. Intriguingly, although the expression of OsRbohs, which play a crucial role in generating ROS, increased in early imbibition (12h), the activity of the antioxidant enzymes SOD and POD also increased with the optimal combination treatment of MH and COU, which lead to the delay in ROS accumulation and inhibition of germination. These results have deepened our understanding of the regulatory mechanism of PHS inhibitors and provided theoretical support for the application of MH and COU in preventing sprouting before crop harvesting.

Synthesis of newly designed hydrazones, in vitro and in silico studies, and structure-activity relationship

Herein, new N'-(substituted benzylidene)-3,5-dihydroxybenzohydrazide (1–13) series were synthesized, and their antioxidant, anticholinesterase, anti-tyrosinase, anti-urease, and antidiabetic activities were investigated together with in silico studies. The synthesized derivates were characterized using molecular spectroscopy, and the structure-activity relationships (SAR) were discussed for all tested biological assays. According to activity results, compound 3 exhibited excellent antioxidant activity in all tests, while compound 1 demonstrated the best acetylcholinesterase (AChE) inhibitory and butyrylcholinesterase (BChE) inhibitory activities. On the other hand, compound 11 showed excellent tyrosinase inhibitory (IC50:3.02±0.10 mM) and urease inhibitory (IC50:9.21±0.27 µM) activity. Moreover, among the synthesized compounds, compound 6 was detected as the best antidiabetic compound by inhibiting α-amylase (IC50:30.68±0.94 µM) and α-glycosidase (IC50:41.35±0.03 µM) enzymes, which were related with the antidiabetic activity. Molecular docking analysis confirmed AChE, BChE, tyrosinase, urease, α-amylase, and α-glucosidase inhibitory activities. In line with the findings obtained from in vitro bioactivity results and molecular docking analysis, hydrazone compounds are a suitable class of organic compounds for developing acetylcholinesterase, butyrylcholinesterase, urease, α-amylase, and α-glucosidase inhibitors.

Bioaccessibility and Antidiabetic Potential of xique-xique and mandacaru Fruits in a Simulated Gastrointestinal Tract Model.

This study evaluated the influence of gastrointestinal digestion on the bioaccessibility and antidiabetic potential of xique-xique (Pilosocereus gounellei) and mandacaru (Cereus jamacaru) fruits. After digestion, the content of total phenolics and flavonoids reduced by 58.3 and 73.51% in xique-xique and 48.33 and 88.43% in mandacaru. In addition, compounds such as rutin, ρ-coumaric acid, catechin and epicatechin reduced during digestion for both fruits. The antioxidant potential by the ABTS assay increased by 153.3% for xique-xique and 273.46% for mandacaru in the intestinal phase. However, using the ORAC assay, the antioxidant potential of xique-xique reduced from 255.42 to 112.17 μmol TE g-1. The capacity of xique-xique fruit to reduce α-amylase activity reduced 23.71-fold after digestion, but the potential to inhibit α-glucosidase increased 17.8-fold. The antiglycation potential reduced in both fruits after the in vitro gastrointestinal digestion. Thus, the bioaccessibility of the phenolic compounds from the fruits, as well as their functional potential, were influenced by the digestive process, as well as by the sample evaluated.

Phytochemical Extract from Syzygium cumini Leaf: Maximization of Compound Extraction, Chemical Characterization, Antidiabetic and Antibacterial Activity, and Cell Viability

This work aimed to obtain a phytochemical extract from jambolan leaf using a hydroethanolic solvent and ultrasound-assisted extraction. For this purpose, an experimental design was applied to analyze the effect of process variables related to temperature (30–60 °C), time (10–30 min), and solvent to leaf ratio (5–15 mL g−1), on the extraction mass yield (EMY) and on the yield of phenolic compounds (PCY). The effect of extractor solvent, AE (absolute ethanol), 75E (75% v·v−1 ethanol) and 50E (50% v·v−1), on the chemical characterization of the extracts, antidiabetic and antimicrobial activity, and cell viability, were also evaluated. The application of the highest values of process variables resulted in obtaining the maximum of the response variables (EMY = 9.94 wt% and PCY = 13.01 mg GAE g−1 leaf). A higher content of phenolic compounds and flavonoids was obtained with 50E, which is mainly composed of sinapic, vanillic, trans-caffeic, and quinic acids, which were responsible for the greatest antioxidant potential, antibacterial activity (against Staphylococcus aureus and Pseudomonas aeruginosa), and inhibition of α-amylase. On the other hand, the use of AE allowed us to obtain extracts with higher concentrations of squalene, α-tocopherol, β-sitosterol, and friedelin. From cell viability tests, the extracts are not considered toxic at the concentration tested (100 µg mg−1).

LC-MS/MS Profiling, Biological Activities and Molecular Docking Studiesof Simmondsia Chinensis Leaves.

This study aimed to assess the biological activities of Tunisian Simmondsia chinensis and characterize their potential bioactive compounds. Different extracts of S. chinensis were tested for their antioxidant, antibacterial, anti α-amylase, and anti-acetylcholinesterase activities through in vitro assays. The methanolic extract exhibited the highest levels of antioxidant activity and total phenolic content (976.03 GAE/g extract) compared to the other extracts. Additionally, it demonstrated a substantial anti-acetylcholinesterase activity (PI= 75%) and potent antibacterial property, particularly against Enterococcus faecalis, Listeria monocytogenes, Bacillus cereus, Bacillus subtilis, and Salmonella enterica. The IC50 values of ethyl acetate and methanolic extracts against α-amylase were 42 μg/mL and 40 μg/mL, respectively, indicating potent anti-diabetic effects. HPLC-ESI-MS/MS analyses identified flavonoids and lignans as the major phenolic compounds in the methanolic extract. To better comprehend the mechanisms behind inhibitory effects on α-amylase and acetylcholinesterase enzymes, a molecular docking study was conducted. Consequently, these findings indicate that S. chinensis is a highly valuable natural resource with potential industrial applications.

Chemical profiling and bioactivity analysis of shoots and roots essential oil of Indian Blumea mollis D. Don (Merr.)

Aromatic plants contain essential oils, potent extracts renowned for therapeutic benefits. Essential oils are commonly utilized due to their diverse range of phytochemicals that possess therapeutic properties. The present study analyses the chemical composition of the essential oil obtained from shoots and roots of Blumea mollis (Family: Asteraceae), using GC-FID and GC-MS techniques. A total of 49 and 46 compounds were identified from shoots and roots accounting for 95.6 % and 88.4 % respectively. β-caryophyllene is reported as major compound 36.2 ± 0.50 % in essential oil of the shoots and 33.8 ± 0.55 % in essential oil of the roots. Both essential oils of shoots and roots were dominated by sesquiterpene hydrocarbons (59.2–76.4%), followed by oxygenated sesquiterpene (14.9–20.3%). The in vitro antioxidant activity was determined using DPPH radical scavenging activity, H2O2 radical scavenging activity, and Iron(II) complexing activity. The highest antioxidant activity was observed in root essential oil of B. mollis. The oils also inhibited the activity of α-amylase with IC50 of 3.53 ± 0.04 μg/ml (shoot), 3.45 ± 0.04 μg/ml (root). Root oil also showed good activity for protein denaturation with IC50 of 3.02 ± 0.03 g/ml as compared to shoot essential oil. This is first time that essential oil constituent and biological activity of B. mollis roots and shoots have been characterized from India.

Mitigation of microplastic toxicity in soybean by synthetic bacterial community and arbuscular mycorrhizal fungi interaction: Altering carbohydrate metabolism, hormonal transduction, and genes associated with lipid and protein metabolism

Microplastics (MPs) have become ubiquitous environmental pollutants, eliciting concerns about their negative impacts on terrestrial and agroecosystems. However, employing sustainable remediation approaches holds the potential to mitigate these negative impacts and bolster MPs tolerance in both the seeds and vegetative structures of plants. The current investigation explores the impact of arbuscular mycorrhizal fungi (AMF) and synthetic bacterial community (SynCom) as potential alleviators of MP-induced stress. Results exhibited that co-applied SynCom and AMF, resulted in the highest plant biomass, leaf area, pod per plant, and 100-seed weight under control (no MPs) and MPs stress. The combined application of SynCom and AMF enhanced colonization, association, and arbuscule abundance in the non-stressed plants (no MPs) as compared to stressed plants. The sole or co-application of SynCom and AMF enhanced the primary metabolites content and mitigated the MPs-induced reduction in soluble sugars, lipids, protein, and oil contents. Soybean inoculation stimulated the genes expression involved in lipid and protein biosynthesis, while a contradictory drift was noted for genes associated with lipid and protein degradation, underpinning the observed increment in protein and lipid content. Soybean inoculated with AMF exhibited the utmost α-amylase and β-amylase activities, demonstrating enhanced osmolyte (soluble sugar) production, mainly under MPs stress. Remarkably, sole or co-application further reinforces the positive effect of MPs stress on the osmoprotectants and antioxidant levels, for instance, phenol, flavonoid, glycine betaine contents, and glutathione-S-transferase (GST) activities. Subsequent to the stress release, a stress hormones known as abscisic acid (ABA) reduced in the seeds of inoculated soybean while gibberellin (GA), trans-zeatin riboside (ZR), and indole acetic acid (IAA) were increased. Therefore, it is concluded that the combined application of SynCom and AMF protected the soybean plants from MPs-induced oxidative damage by upregulating osmoprotectants and antioxidant levels. This study provides insights into the potential of sustainable remediation approaches in alleviating the complex impact of MPs on soybean, contributing to future strategies for environmental sustainability. Future studies could explore the optimization of SynCom and AMF formulations for different crops and environmental conditions, potentially leading to practical applications in sustainable agriculture and pollution management.

Synthesis, C-N/N-N bond conformational analysis and evaluation of naphtho[2,3-d][1,2,3]triazole-4,9-dione tethered N-acyl hydrazones as α-amylase inhibitors: Insights from molecular modeling and ADMET analysis

In an effort to expand the repertoire of potent α-amylase inhibitors, we sought to develop novel inhibitors by combining 1,4-naphthoquinone, 1,2,3-triazole, and N-acyl hydrazone scaffolds in a single matrix. To achieve this, twelve novel naphtho[2,3-d][1,2,3]triazole-4,9‑dione tethered N-acyl hydrazones were synthesized through condensation reaction of 2-(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)acetohydrazide with various substituted aryl aldehydes. Structural elucidation for all the compounds was performed using 1D, 2D-NMR, FTIR, and mass spectral analyses. The synthesized molecules were evaluated for their ability to inhibit α-amylase activity using acarbose as the standard drug. All the derivatives exhibited potent inhibition of α-amylase, with IC50 values ranging between 17.26 ± 0.07 to 25.62 ± 0.03 μg/mL. Notably, compound 9c possessing –meta substituted –NO2 group displayed the highest activity (IC50 = 17.26 ± 0.07 μg/mL) among the series. Structure-activity relationship (SAR) revealed the pivotal role of aryl ring substitutions in determining inhibitory efficacy. To validate these findings and to assess the binding stability of 9c within the catalytic site α-amylase dervied for A. oryzae (PDB ID:7TAA), in silico studies were performed. The compound 9c effectively occupies the enzyme's active pocket, with minimal RMSD fluctuations observed over 100 ns simulation, indicating stable protein-ligand complex. ADMET predictions suggested favorable drug-like properties, underscoring the potential of these compounds as novel α-amylase inhibitors for managing type 2 diabetes mellitus

Allelochemicals Released from Rice Straw Inhibit Wheat Seed Germination and Seedling Growth

Recently, returning rice straw to soil has become a common problem in wheat production because it causes decreased wheat seedling emergence. Allelopathy is an important factor affecting seed germination. However, the effects of rice straw extracts on wheat seed germination and seedling growth remain unclear. Wheat seeds and seedlings were treated with 30 g L−1 of rice leaf extracts (L1), 60 g L−1 of rice leaf extracts (L2), 30 g L−1 of rice stem extracts (S1), 60 g L−1 of rice stem extracts (S2) and sterile water (CK) to study the allelopathic effects of rice straw extracts on wheat seed germination and seedling growth. The α-amylase and antioxidant enzyme activities in wheat seeds; the agronomic traits, photosynthetic indicators, and nutrient contents of wheat seedlings; and the phenolic acids in rice stem extracts were determined. Common allelochemicals, including 4-hydroxybenzoic acid, hydrocinnamic acid, trans-cinnamic acid, vanillic acid, benzoic acid, protocatechualdehyde, caffeic acid, syringic acid, sinapic acid, and salicylic acid, were detected in rice stem extracts. Low-concentration rice leaf and stem extracts (30 g L−1) had no effect on the germination rate of wheat seeds. High-concentration (60 g L−1) rice stem and leaf extracts decreased the seed germination rate by 11.00% and 12.02%. Rice stem extract (60 g L−1) decreased the α-amylase activity, and gibberellin content of wheat seeds but increased superoxide dismutase, peroxidase, and catalase activities and malondialdehyde content in wheat seeds. Allelochemicals entered the internal tissues of wheat seeds, where they decreased the gibberellin content and α-amylase activity and increased the antioxidant enzyme activity, ultimately leading to an inhibitory effect on seed germination. Rice stem and leaf extracts decreased the SPAD value and photosynthetic indicators of wheat seedlings. Rice stem extract (60 g L−1) decreased the fresh weight and root length of wheat seedlings by 31.37% and 45.46%. Low-concentration rice leaf and stem extract (30 g L−1) had no effect on the nutrient contents of wheat seedlings. Rice leaf and stem extracts (60 g L−1) decreased the nitrogen and potassium contents of wheat seedlings. These results indicated that low-concentration rice leaf and stem extract (30 g L−1) had no effect on wheat seed germination and the high-concentration rice stem extract (60 g L−1) released allelochemicals and inhibited wheat seed germination and seedling growth. These findings provide a basis for the improvement of straw return techniques.

Synthesis, α-Glucosidase, α-Amylase, and Aldol Reductase Inhibitory Activity with Molecular Docking Study of Novel Imidazo[1,2-a]pyridine Derivatives.

Inhibition ofaldose reductase (AR), α-glycosidase (α-GLY), and α-amylase (α-AMY) are some of the essential targets in diabetes mellitus (DM). Here, a series of imidazo[1,2-a]pyridine-based 1,3,4-thiadiazole derivatives (8a-k) were successfully synthesized and characterized using 1H NMR, 13C NMR, and HRMS spectroscopic techniques. The inhibition effects of the synthesized derivatives against AR, α-GLY, and α-AMY were evaluated using both in vitro and in silico methods. In vitro studies revealed that the derivatives (8a-k) showed significant inhibition activity. The results showed that the novel derivatives (8a-k) demonstrated potential inhibitory activity, with K I values covering the following ranges: 23.47 ± 2.40 to 139.60 ± 13.33 nM for AR and 6.09 ± 0.37 to 119.80 ± 12.31 μM for α-GLY, with IC50 values 81.14 to 153.51 μM for α-AMY. Furthermore, many of these compounds exhibited high inhibition activity, while some of them showed higher potency than the reference compounds. Molecular docking of the target compounds was carried out in the active sites of AR (PDB ID: 4JIR) and α-GLY (PDB ID: 5NN8).

Chemical Profiling, Enzyme Inhibitory Activity and Antioxidant Capacity of South African Herbal Teas: Buddleja saligna, Lippia javanica, L. scaberrima and Phyla dulcis.

Herbal teas are used in South Africa as digestives to lower glycaemia and for other indications. However, the chemical composition of the infusions and their effect on enzymes related to metabolic syndrome is poorly known. The composition of infusions and methanol extracts of B. saligna (Scrophulariaceae), Lippia javanica, L. scaberrima, and Phyla dulcis (Verbenaceae) was assessed and the effect of the infusions and extract was determined towards α-glucosidase, α-amylase, and pancreatic lipase. The commercial herbal products were extracted separately with MeOH or hot water to obtain the extract/infusion for comparative studies. Total phenolic, total flavonoid and antioxidant capacity were assessed. The fingerprints of the MeOH extracts and infusions were compared by HPLD-DAD. The extract constituents were tentatively identified by HPLC-MS/MS and NMR analyses. From the extracts/infusions, 57 compounds were identified, including iridoids, phenylpropanoid glycosides, flavonoids, and caffeic acid derivatives, among others. The MeOH extracts and infusions showed strong inhibition towards α-glucosidase with IC50 in the range of 0.13-0.84 µg/mL for the phenolic-enriched infusion extract (PEI) and 0.47-0.50 µg/mL for the MeOH extracts, respectively. The P. dulcis PEI showed higher inhibition towards α-glucosidase, and the MeOH extract of L. scaberrima was better than the PEI. At 100 µg/mL, the PEI from the four herbal teas reduces the activity of α-amylase by 23.03-28.61%, with L. javanica as the most active tea. Three of the species are high in phenylpropanoid glycosides, while P. dulcis contains rosmarinic acid. Some 26 compounds were identified in the infusion from B. saligna, 28 from L. scaberrima, and 21 from P. dulcis. Four of them are common in all the teas, namely decaffeoylverbascoside, verbascoside, isoverbascoside, and tuberonic acid hexoside. Ten compounds occur in two of the teas and seventeen, fifteen, and eleven compounds were detected only in B. saligna, L. scaberrima, and P. dulcis, respectively. Most of the compounds are reported for the first time from the crude drug infusions. The results give some support for the traditional use of herbal teas as digestives and/or indications for diabetes. The chemical fingerprints set the basis for quality control of the crude drugs, based on the main constituents and differential compounds occurring in the samples.

Enzyme Inhibitory Activities and RP-HPLC Analysis of Geranium And Erodium Species.

The genera Geranium and Erodium (Geraniaceae) have been documented to possess diverse ethnopharmacological uses, including diabetes mellitus. Relevant to their ethnopharmacological use, the current study aimed to evaluate the α-glucosidase, α-amylase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activity of ethanol extracts from 46 samples belonging to thirty-one species of Geranium (20) and Erodium (11) collected throughout Türkiye. The majority of the extracts displayed a marked α-glucosidase and α-amylase inhibitory activity. Besides, 23 extracts out of 46 exhibited a concentration-dependent inhibitory effect over 50% towards AChE. The highest AChE inhibition was found in G. subcaulescens collected from Konya with an IC50 value of 4.73 ± 2.96 µg/mL. E. somanum, E. leucanthum, and E. sipthorpianum exhibited the most potent α-glucosidase inhibitory activity, while E. birandianum and E. pelargoniiflorum were the most active extracts against AChE and BChE, respectively. Three extracts that had inhibitory activity over 50% against four of the enzymes were selected and proceeded to RP-HPLC analysis. Geraniin and ellagic acid were identified as major compounds in the active extracts. Most of the species screened in the current study were examined for the first time against α-glucosidase, α-amylase, AChE, and BChE.

In vitro Anti-Diabetic and Antioxidant Potential of the Siddha formulation Mega Sanjeevi Chooranam

Background: The increasing prevalence of type 2 diabetes mellitus (T2DM) presents a significant public health challenge due to its long-term complications and its role as a primary risk factor for cardiovascular diseases, which have both economic and social implications. Plant-derived antidiabetic drugs are being extensively studied due to their safety and efficacy. The main objective of the present study is to evaluate the anti-diabetic and anti-oxidant potential of the formulation Mega Sanjeevi Chooranam (MSC) through in-vitro investigation. Materials and Methods: The in vitro investigation of traditional siddha formulation MSC were performed to ascertain its inhibitory potential against α-amylase and α-glucosidase enzymes along with antioxidant analysis. Results: The MSC displayed the highest activity against α-amylase enzyme, with a percentage inhibition of 73.44 ± 6.87% (IC50, 299.4 ± 27.27 μg/ml), followed by a moderate level of α-glucosidase inhibition at 48.89 ± 13.38% (IC50, 402.2 ± 86 μg/ml). Furthermore, the MSC exhibited the strongest antioxidant activity in quenching ABTS● radicals (IC50, 110.1 ± 18.6 μg/ml), followed by DPPH● (IC50, 144.4 ± 36.8 μg/ml), H2O2● (IC50, 172.7 ± 39.3 μg/ml), and NO● radicals (IC50, 238.4 ± 58.56 μg/ml). Conclusion: In conclusion the formulation MSC demonstrated the significant antioxidant activity and effectively inhibited α-amylase and α-glucosidase enzyme activities. Further study is needed to isolate bioactive phytoconstituents and determine the molecular mechanism behind their antidiabetic effect.

Biogenic Silver Nanoparticles (AgNPs) Ameliorates Oxidative Biomarkers in Type-2 Diabetic Rats: In vitro and In vivo Report

Objective: Nanoparticles (NPs) are reliable biological tools for curative purposes through their application in nanomedicine. The present study synthesized and characterized silver nanoparticles (AgNPs) from Tetrapetra tetrapleura fruit. The investigation aims to examine the antidiabetic effect of the AgNPs using in vitro and in vivo models. Methods: Briefly, the synthesized AgNPs were confirmed by the application of ultraviolet-visible (UV-Vis) spectroscopy, and five other techniques, viz; transmission electron microscopy (TEM) techniques, Fourier transform infrared (FTIR) spectroscopy, energy dispersive X-ray spectroscopy (EDX), X-ray diffraction analysis (XRD) and scanning electron microscope (SEM). The in vitro model assay investigated the scavenging effect of AgNPS on 2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide anion (O2ˉ), hydroxyl anion (-OH), ferric reducing antioxidant power (FRAP), and α-amylase/α-glucosidase inhibitory activity. The in vivo model involving rats-induced type-2 diabetes with streptozotocin (STZ) was divided into six (6) groups of seven (7) rats each to assess antioxidative parameters. Results: The AgNPs scavenged free radicals (DPPH) and moderately inhibited (O2ˉ), hydroxyl anion (-OH), reduced ferric to ferrous ions, and inhibited both α-amylase and α-glucosidase activity with increasing concentrations. Similarly, AgNPs ameliorated oxidative stress imposed by type 2 diabetes on the rats’ tissues significantly (p &lt; 0.05), depleting total cholesterol, low-density lipoprotein (LDL), and increased total protein composite and high-density lipoprotein (HDL) contents. The AgNPs enhanced catalase and superoxide dismutase, reduced glutathione (GSH), and, concomitantly, decreased malondialdehyde (MDA) levels in the tissue homogenate. Conclusion: These findings provide scientific evidence for the first time, finding the application of a biogenic compound synthesized from T. tetrapleura fruit in the treatment of type 2 diabetes.

Effects of preservatives on the activities of salivary enzymes

ObjectivesTo investigate the effects of common preservatives used in oral health care products on the enzymatic activities of lysozyme, peroxidase, and α-amylase in-solution and on-hydroxyapatite surface phases. DesignThe preservatives used in this study were sodium benzoate, methylparaben, propylparaben, and benzalkonium chloride. Hen egg-white lysozyme, bovine lactoperoxidase, and α-amylase from Bacillus sp. served as sources of purified enzymes. Human unstimulated whole saliva was used as a source of salivary enzymes. Hydroxyapatite beads were used as the surface phase. The preservatives were incubated with purified enzymes or saliva samples in-solution or on-hydroxyapatite surface phases, respectively. Enzymatic activities of lysozyme, peroxidase, and α-amylase were measured by hydrolysis of fluorescein-labelled Micrococcus lysodeikticus, oxidation of fluorogenic 2′,7′-dichlorofluorescin, and hydrolysis of fluorogenic starch, respectively. ResultsThe effects of the preservatives on the enzymatic activities of lysozyme and peroxidase were more distinct in the saliva samples than purified substances, and in the in-solution phase than on-hydroxyapatite surface phase, and the opposite was true for α-amylase. The most significant result was apparent decrease in peroxidase activities caused by the parabens in the in-solution phase (P<0.05). Sodium benzoate and parabens inhibited lysozyme activity in the in-solution phase, but differently for the purified and salivary lysozymes. Parabens and benzalkonium chloride inhibited the enzymatic activity of α-amylase from Bacillus sp., not saliva samples, only on-hydroxyapatite surface (P<0.05). ConclusionsEach preservative affected the enzymatic activities of lysozyme, peroxidase, and α-amylase differently. Based on the effects on salivary enzymes, sodium benzoate or benzalkonium chloride was recommended as preservatives rather than parabens.