Α-amylase Inhibitory Activity Research Articles

Synthesis of Some Novel 4-bromobenzoic Acid Clubbed Hydrazone Schiff Base Derivatives as Potent α-amylase Inhibitors: In vitro and In silico Studies

Aims: Synthesis of novel 4-bromobenzoic acid-based hydrazone-Schiff base derivatives and to screen them for their α-amylase inhibitory activity. Objective: The biological activities of hydrazone-Schiff base compounds encouraged us to evaluate the synthesized derivatives (4-32) for in-vitro inhibition activity against the α-amylase enzyme. Methods: In current research work twenty-nine Schiff base derivatives (4-32) of 4-bromobenzoic acid were synthesized in worthy yields by treating various replaced aldehydes with 4- bromobenzohydrazide using methanol solvent in catalytic quantity of acetic acid. The products were structurally described through the support of several spectroscopic methods (EI-MS and 1HNMR) and finally evaluated against α-amylase enzyme. Results: All the made derivatives exhibited worthy inhibition potential from IC50 = 0.21 ± 0.01 to 5.50 ± 0.01 μM when equated to the usual acarbose drug having IC50 = 1.34 ± 0.01 μM. Compound 21 (IC50 = 0.21 ± 0.01 μM) was established as the most active inhibitor among the series better than standard. The structure-activity relationship study showed that the alteration in the activity of the produced products might be due to the attached position and nature of the substituents. Furthermore, in-silico study supported the effects of groups attached on the binding interaction with α-amylase enzyme. Conclusion: A series of substituted hydrazone Schiff bases based on 4-bromobenzoic acid were produced, confirmed the structures by EI-MS and 1H-NMR spectroscopic methods and lastly tested for their in-vitro α-amylase inhibitory potential. Among the series, twenty-four products indicated brilliant inhibition potential having IC50 values from 0.21 ± 0.01 to 1.30 ± 0.01 μM. The structure-activity relationship study showed that the alteration in the activity of the synthesized products might be due to the attached position and nature of the substituents. On the other hand, in silico studies advocated that the synthesized Schiff base derivatives have prevalent interactions of binding within the active site of the α-amylase enzyme, and because of their various attached substituent, their conformation is altered in the active site of the enzyme. The current study recognized a number of lead candidates derived from 4-bromobenzoic acid. Additional investigation of the synthesized derivatives for coming research to get novel α-amylase inhibitors.

Polyphenol compounds contributing to the improved bioactivities of fermented Rubus chingii Hu

This research aims to evaluate the phenolic composition, antioxidant and enzyme inhibition activities of fermented Rubus chingii Hu wine, and explore the correlation between them. TPC (Total Phenolic content) and TFC (Total Flavonoid content) increased rapidly from 0 h to 72 h, followed by a slight decrease in TPC and a significant decrease in TFC. Fermentation could significantly increase the antioxidant activity and α-amylase/α-glucosidase enzyme inhibitory activity of Rubus chingii Hu. A total of 39 polyphenols and organic acids in fermented Rubus chingii Hu were identified by UPLC-ESI-Q-TOF-MS/MS and 11 of them were quantitatively analyzed. After fermentation, the contents of all the detected polyphenol compounds, except for quercetin and ellagic acid, significantly increased (p < 0.05). Correlation analysis showed that protocatechuic acid and catechin played an important role in the antioxidant activity of fermented Rubus chingii Hu, while protocatechuic acid and hypericin played an important role in the α-amylase inhibition activity. This study indicated that Rubus chingii Hu could be applided as a potential meterial for the wine production, and has the potential to be a functional food for promoting health.

Green Synthesis of Iron Oxide NPs (IONPs) by Using Aqueous Extract of Parthenium hysterophorus Linnaeus for the In-vitro Antidiabetic and Anti-inflammatory Activities

The Parthenium hysterophorus Linnaeus is one of the anti-inflammatory and antidiabetic ethnomedicine. Therefore the formulation of this plant as nanoparticles will be fruitful anti-inflammatory and antidiabetic as compared to conventional extract. In the current study, the aqueous kernel extract from Parthenium hysterophorus Linnaeus was subjected to synthesize iron oxide nanoparticles (IONPs) and explored their anti-inflammatory and anti-diabetic potentials. The results indicate that the aqueous kernel extract effectively produced IONPs, which were verified using standard analytical methods. UV-visible spectrophotometer analysis was used to check the formation of IONPs. The Fourier-transform infrared spectroscopy (FTIR) was used to check numerous functional groups from the valuable phytochemicals present in the extract. These functional groups play crucial roles as reducing, capping, and stabilizing agents during the synthesis of IONPs. Additionally, scanning electron microscopy (SEM) were utilized to investigate the surface characteristics of the nanoparticles. Notably, the IONPs fabricated from the extract demonstrated promising anti-inflammatory activity, inhibiting Human RBC by 79% and Heat Induced Hemolysis by 72%, as well as showing anti-diabetic potential with 60% inhibition of yeast glucose uptake and 72% inhibition of α-amylase activity, all at a concentration of 100 μg mL-1. These effects were partly comparable to standard drugs with anti-inflammatory activity of 85% inhibition of Human RBC and 78% inhibition of Heat Induced Hemolysis, and anti-diabetic activity of 67% inhibition of yeast glucose uptake and 78% inhibition of alpha amylase.

Phytochemical Compounds, and Antioxidant, Anti-Hyperglycemic, and Anti-Inflammatory Activity of Microencapsulated Garambullo (Myrtillocactus geometrizans) Extract During In Vitro Digestion and Storage

Garambullo fruit (Myrtillocactus geometrizans) is a rich source of phytochemical compounds that exhibit antioxidant, anti-hyperglycemic, and anti-inflammatory activities, helping to prevent diseases associated with oxidative stress. The objective of this study was to evaluate phenolic compound (PC), betalain (BL), betaxanthin (BX), and betacyanin (BC) contents, and in vitro biological activities (antioxidant, anti-hyperglycemic, and anti-inflammatory) in microencapsulated garambullo extract during in vitro gastrointestinal digestion and storage. Microencapsulation was performed using spray drying. Arabic Gum (GA, 10% in feed solution) and soy protein isolate (SPI, 7% in feed solution) were used as wall materials. After in vitro digestion, the microcapsules (GA, SPI) exhibited higher bioaccessibility (p ≤ 0.05) of PC, BL, BX, and BC, and higher antioxidant activity (AA), compared to the non-encapsulated extract. Both microcapsules showed bioaccessibility in anti-hyperglycemic activity: α-amylase (GA: 90.58%, SPI: 84.73%), α-glucosidase (GA: 76.93%, SPI: 68.17%), and Dipeptidyl peptidase-4 (DPP-4) (GA: 52.81%, SPI: 53.03%); and in anti-inflammatory activity: cyclooxygenase-1 (COX-1) (GA: 78.14%, SPI: 77.90%) and cyclooxygenase-2 (COX-2) (GA: 82.77%, SPI: 84.99%). During storage, both microcapsules showed a similar trend with a significant decrease (p ≤ 0.05) in PC (GA: 39.29%, SPI: 39.34%), BL (GA: 21.17%, SPI: 21.62%), BX (GA: 23.89%, SPI: 23.45%), BC (GA: 19.55%, SPI: 19.84%), and AA (GA: 41.59%, SPI: 42.51%) after 60 days at 30 °C. Both microcapsules retained anti-hyperglycemic activity evaluated by the inhibitory activity of α-amylase (GA: 68.84%, SPI: 70.18%), α-glucosidase (GA: 59.93%, SPI: 58.69%), and DPP-4 (GA: 52.81%, SPI: 53.01%), and anti-inflammatory activity evaluated by the inhibitory activity of COX-1 (GA: 82.18%, SPI: 82.81%) and COX-2 (GA: 81.11%, SPI: 81.08%). Microencapsulation protected the phytochemical compounds and in vitro biological activities by allowing controlled release during in vitro digestion compared to the non-encapsulated extract. However, after 60 days storage at 30 °C, 60% of PC and AA, 80% of BL, BX, and BC, and 20–45% of the anti-hyperglycemic and anti-inflammatory activity were lost.

The Heating Under Micro Variable Pressure (HUMVP) Process to Decrease the Level of Saponin in Quinoa: Evidence of the Antioxidation and the Inhibitory Activity of α-Amylase and α-Glucosidase

To reduce the level of saponin while preserving essential nutrients and antioxidative properties in quinoa (Chenopodium quinoa), this study delves into the optimization of the HUMVP process and thoroughly examines its effects on antioxidation as well as its inhibitory influence on α-amylase and α-glucosidase. The optimal HUMVP conditions involved wetting quinoa grains with 6% water (pH = 6.0) and subjecting them to a 4 min treatment under 0.35 MPa pressure. The values of •OH, DPPH, and ABTS•+ scavenging rate of the extracts from the quinoa sample (named Q2HUMVP) treated under the optimum HUMVP process were 70.02, 87.13, and 50.95%, respectively. Furthermore, the treatment preserved 95.20% of polyphenols and 73.06% of flavonoids, while the saponin content was reduced to 23.13% of that in raw quinoa. Notably, Q2HUMVP extracts demonstrated superior inhibitory activity against α-amylase and α-glucosidase compared to dehulled quinoa samples. The inhibition exhibited by the quinoa sample extracts on α-amylase and α-glucosidase was found to be reversible.

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 species screened in the current study were examined for the first time against α-glucosidase, α-amylase, AChE, and BChE.

Isolation, characterization, and analysis of pure compounds from Leea macrophylla leaf extract for antibacterial, antidiabetic, cytotoxicity and phytotoxicity

This research aims to isolate, characterize, and analyze pure compounds from Leea macrophylla leaf extract to investigate its antibacterial, antidiabetic, cytotoxic, and phytotoxic effects. Fresh leaves were collected, dried, and subjected to methanol extraction to obtain a crude extract. From the petroleum ether fraction (PEF) of this extract, three fractions—designated LM1, LM2, and LM3—were prepared using column chromatography. The fractions were tried to be characterized in search for single compound by instrumental technique like ATR-FTIR, 1H NMR and 13C NMR but the 1H NMR and 13C NMR spectra were found complex which were difficult to interpret. To dispel the doubt and get clear idea about the structure, GC-MS analysis of the compounds was carried out whose result showed that all the three extracts were decomposed to several small organic compounds that made the structure elucidation difficult. For this complication, the characterization of the extracts was not possible. Numerous compounds were identified in the methanol extract of L.macrophylla through GC-MS analysis. Among these compounds, Benzene, 1,2,3-trimethyl- and Undecane were found in higher percentages in LM1. LM2 contained Azulene and Bicyclo [4.4.1]undeca-1,3,5,7,9-pentaene, while LM3 was characterized by the presence of 9,9-Dimethoxybicyclo [3.3.1]nona-2,4-dione and 11-(2-Cyclopenten-1-yl)undecanoic acid, among others. The antibacterial activity of these fractions was evaluated against various bacterial strains, demonstrating broad-spectrum effectiveness. LM1 fraction showed the highest antibacterial activity against Proteus sp. With zone of inhibition 25 mm and weak activity against S. sonnei with zone of inhibition 5 mm. LM2 showed the highest activity to both E. cocci and P. aeruginosa with the zone of inhibition of 18 mm and comparatively lower but significant against Proteus sp. LM3 was highly active to S. sonnei with zone of inhibition 20 mm and lower but quite significant against Proteus sp. Moreover, the anti-diabetic potential was assessed, with LM1 showing the strongest α-amylase inhibitory activity, outperforming quercetin (standard). The IC50 values of LM1, LM2, LM3, and quercetin were 57.36 μg/mL, 100.66 μg/mL, 164.92 μg/mL, and 97.45 μg/mL, respectively. In addition, cytotoxicity was assessed using a brine shrimp lethality bioassay, and phytotoxicity was evaluated through seed germination and growth assays. The results suggest that L.macrophylla leaf extracts have potential applications in antimicrobial, antidiabetic, and anti-cancer contexts. This comprehensive study bridges gaps in knowledge surrounding L.macrophylla's multifaceted properties, offering insights into its therapeutic and ecological potential for healthcare and environmental management.

DESIGN, SYNTHESIS, AND BIO PROFILING OF 2, 3-DIHYDROQUINAZOLIN-4(1H)-ONE DERIVATIVE AS TYPE II DIABETES AGENTS: A COMPREHENSIVE IN SILICO, IN VITRO, AND IN VIVO STUDY

Objective: Diabetes mellitus is a significant global health challenge, with Type 2 Diabetes Mellitus (T2DM) being a leading cause of mortality worldwide, demanding the need for effective interventions by developing innovative therapeutic strategies or novel antidiabetic agents. This study explores in silico, in vitro, and in vivo approaches to identify the most potent 2,3-Dihydroquinazolin-4(1H)-One derivative molecule with antidiabetic activity. Methods: Eleven new derivatives were designed, studied in silico to identify the most promising compounds, synthesized, studied spectrally to describe them, and evaluated for both in vitro and in vivo investigations. Alpha amylase and alpha-glucosidase inhibitory activities were investigated in vitro. The endogenous suppression of glucose synthesis in Hepatoblastoma cell line 2(HepG2) cells and the in vitro glucose absorption assay on cultivated L6 cell lines were conducted. To assess the ability of the newly synthesized compounds to prevent diabetes, in vivo investigations were conducted on Streptozotocin (STZ)-induced diabetic rats and the effects on various biochemical parameters were identified.Results: Leveraging computational methods, the QZ9 molecule was identified with stable interactions with key biomolecules associated with T2DM. Subsequent in vitro assays confirmed the inhibitory effects of QZ2, QZ8, and QZ9 on alpha-amylase and alpha-glucosidase activities, suggesting their potential as enzyme inhibitors. Additionally, QZ8 and QZ9 demonstrated enhanced glucose uptake and production inhibition in HepG2 cells, indicating their role in improving glucose homeostasis. In vitro, the top-ranked molecules QZ2, QZ8, and QZ9 were analyzed to validate the in silico findings and assess their potential as therapeutic agents for T2DM. The inhibition of α-amylase activity by QZ2, QZ8, and QZ9 was dose-dependent, with maximum inhibition observed at 1000 µg/ml: 57.33% for QZ2, 52.21% for QZ8, and 87.16% for QZ9. Similarly, α-glucosidase inhibition at 1000 µg/ml was 59.96% for QZ2, 53.50% for QZ8, and 81.51% for QZ9. Both QZ8 and QZ9 significantly increased glucose uptake and inhibited glucose production in HepG2 cells, with maximum glucose production inhibition at 100 µg/ml: 62.22% for QZ8 and 62.35% for QZ9. These findings suggest that QZ8 and QZ9 contribute to glucose homeostasis. QZ9 demonstrated superior enzyme inhibition compared to QZ2 and QZ8, with α-amylase and α-glucosidase inhibition up to 87.16% and 81.51%, respectively, at 1000 µg/ml. In vivo investigations in Diabetic rat models further confirmed the efficacy of these compounds by showing significant reductions in blood glucose levels. These results suggests the potentiality of QZ9 as a promising novel Antidiabetic agent.Conclusion: Combining computational predictions with experimental validations, this integrated approach highlights the promise of 2,3-Dihydroquinazolin-4(1H)-One derivative QZ9 as a novel antidiabetic agent, warranting further investigation for clinical translation.

Development of Mussaenda frondosa sepal infused functional tea with enhanced antioxidant and alpha-amylase inhibitory activities

Mussaenda frondosa (MF) is an edible species of the genus Mussaenda (Rubiaceae) that contains a wide array of medicinal compounds. The present study was conducted to evaluate the physicochemical and functional properties of the MF sepals and to develop a novel herbal tea with improved functional properties. Remarkably high antioxidant and α-amylase inhibitory activities were exhibited by water and ethanol extracts of MF, attributed to their high phenolic and flavonoid contents. None of the extracts showed toxicity, as evaluated by the brine shrimp lethality assay. A tea was formulated by blending different proportions (30, 40 and 50%) of dry sepals of MF with black tea. The sensory analysis showed a significantly high level of acceptance for the formula containing 40% MF (MFT-40) with augmented phenolic contents (138.82 ± 0.21 mg GAE/g), antioxidant (DPPH scavenging activity with IC50 of 12.23 ± 0.45 µg/mL), and hypoglycemic activities (α-amylase inhibition with IC50 of 104.80 ± 0.59 µg/mL) compared to the black tea control (with the values of 128.47 ± 0.13 mg GAE/g, 18.70 ± 0.68 µg/mL and 153.07 ± 0.61 µg/mL respectively). This study revealed the potential use of MF as a source of antioxidants for the development of new functional teas with enhanced health benefits.

Study on the effects of endogenous polyphenols on the structure, physicochemical properties and in vitro digestive characteristics of Euryales Semen starch based on multi-spectroscopies, enzyme kinetics, molecular docking and molecular dynamics simulation

Euryales Semen (ES) is a highly nutritious food with low digestibility, which is closely associated with its endogenous phenolic compounds. In this study, five phenolic compounds (naringenin, isoquercitrin, gallic acid, epicatechin and quercetin) with high concentrations in ES were selected to prepare starch-polyphenol complexes. Subsequently, the effects of endogenous polyphenols on the structure, physicochemical properties and digestion characteristics of ES starch were studied using multiple techniques. The addition of phenolic compounds markedly reduced the in vitro digestibility, swelling power, gelatinization enthalpy, while increased the solubility of ES starch. Fourier-transform infrared spectroscopy and X-ray diffraction analysis showed that phenolic compounds interacted with the starch through non-covalent bonds. Five phenolic compounds inhibited α-amylase activity through a mixed competitive inhibition mechanism, with the inhibition potency ranked as follows: quercetin > epicatechin > gallic acid > isoquercitrin > naringenin. The spectroscopic analysis and molecular dynamics simulations confirmed that five phenolic compounds interacted with the amino acid residues of α-amylase through hydrogen bonding and hydrophobic interactions, caused α-amylase static fluorescence quenching, and altered its conformation and microenvironment. This study provides a better understanding of the interaction mechanisms between ES starch and polyphenols, and supports the development of ES as a food that lowers sugar levels.

Optimization of ultrasound-assisted deep eutectic solvent extraction, characterization, and bioactivities of polysaccharide from Plantaginis Semen

Plantaginis Semen (PS) are the dried mature seeds of Plantago asiatica L. or Plantagodepressa Willd. in the Plantago family. Its polysaccharides are important components of PS. Response surface methodology was used to optimize the ultrasonic-assisted deep eutectic solvent (DES) extraction process of PS polysaccharides (PSP). The results showed that the optimal extraction parameters were a solid-liquid ratio of 1:35 g/mL, an extraction time of 73 min, and a molar ratio of 2:1. The yield of PSP was 0.64% and 1.20% by water immersion and ultrasonic water extraction, respectively, indicating that the DES extraction method (2.21 ± 0.06%) is superior to these two methods, and the optimization effect is good. Through the α-glucosidase and α-amylase inhibition activities experiment, it was found that the IC50 values of PSPs-1 were 1122 and 220.5 μg/mL. DPPH·and ABTS+ scavenging activity experiments showed that the IC50 values of PSPs-1 were 19.2 and 4.3 μg/mL, respectively. Its molar ratio of monosaccharide composition is rhamnose: galactose: galacturonic acid: glucose: glucuronic acid: arabinose: mannose: xylose = 33.6:13.3:6.5:3:2.6:2:1.4:1. Therefore, this study can provide an experimental basis for the establishment of an industrialized production process of polysaccharides and the study of their biological activities.

Untargeted metabolomics profiling for revealing water-soluble bioactive components and biological activities in edible bird’s nest

Edible bird’s nest (EBN) is a functional food renowned for its numerous health benefits. While its nutritional and therapeutic value is well-documented, the metabolites contributing to the bioactivities of EBN remain poorly understood. This study aimed to identify the metabolites present in EBN subjected to different treatments, including double-boiled EBN (EBNdb), EBN hydrolysate (EBNhydro), EBN fermented with Lactobacillus helveticus (EBNLH), Latilactobacillus curvatus (EBNLC), and Latilactobacillus sakei (EBNLS) using liquid chromatography-mass spectrometry (LC-MS) and correlate the identified bioactive metabolites with the bioactivities of EBN. It was found that the fermented EBNs exhibited the highest number of metabolites, with 76 tentatively identified, followed by EBNhydro (45) and EBNdb (37). Citric acid (1.97–4.48 g/kg) was present in all treated EBN samples, while L(+)-lactic acid (3.03–8.07 g/kg) and adipic acid (2.33–3.18 g/kg) were only found in fermented EBNs. Among the treated EBN samples, EBNLC demonstrated the significantly highest (p ≤ 0.05) antioxidative (22.34 ± 0.41 % 1,1-diphenyl-2-picrylhydrazil radical scavenging activity), antihypertensive (5.46 ± 0.26 % angiotensin-converting enzyme inhibitory activity), and antihyperglycemic activities (6.48 ± 0.34 % α-amylase inhibitory activity). A total of 18 metabolites, including citric acid, 4-sphingenin, N-acetylcitrulline, 4-aminophenol, L(+)-lactic acid, 2-oxoadipate, sildenafil, formylglycinamidin-RP, 11β,17α,21-α-5β-pregnane-3,20-dione, 2-ketobutyric acid, homoserine, benzaldehyde, 1-pyrroline4-hydroxy-2-carboxylate, nortriptyline, 1-methylguanine, 3-hydroxy-trimethyllysine, 3-phenylpropionate, and reserphine were predicted as bioactive metabolites using the partial least squares discriminant analysis (PLS-DA). This study provides valuable insights into the metabolites present in EBN and serves as fundamental data for future investigations into the bioactive compounds responsible for its specific health benefits, potentially leading to the development of enhanced EBN-based functional foods.

Identification of new structure of indol-3-acetyl-arylsulfonohydrazide as potent α-glucosidase and α-amylase inhibitors and molecular docking

Herein this work, indole analogs (1-16) were synthesized by treating 2-(1H-indol-3-yl)acetohydrazide with various aryl sulfonyl chloride in pyridine as solvent and screened for α-amylase and α-glucosidase inhibitory activity under positive control of standard drug acarbose (IC50 = 12.80 ± 0.10 μM /12.90 ± 0.10 μM. All analogs of the series appeared with excellent to good inhibitory activity as compared to standard drug. The inhibitory activity range for α-amylase is 0.70 ± 0.01 μM to 19.40 ± 0.40 μM, while for α-glucosidase inhibitory activity is 1.20 ± 0.10 μM to 20.40 ± 0.40 μM respectively. Most of the analogs appeared with excellent inhibitory activity, and some analogs like 5, 6, 7, 8, 9, 10,13 and 14 for both enzymes displayed many folds better inhibitory activity than standard drug acarbose. The influences of substituents on inhibitory activity were superficially resonated via structure activity relationship. Docking studies were established to confirm the binding interaction between analogs and active sites of enzymes.

PHYTOCHEMICAL CONTENTS, GC-MS PROFILE AND ALPHA-AMYLASE INHIBITORY POTENTIAL OF Rauwolfia vomitoria n-HEXANE ROOT EXTRACT

Rauwolfia vomitoria is a tropical medicinal plant that has been used traditionally in the management of several diseases. In this study, the phytocontents and the preliminary alpha-amylase inhibitory activity of the n-hexane extracts of R. vomitoria was investigated. The dried plant material, R. vomitoria root was extracted by macerating in n-hexane for 72 h. The phytochemical screening and quantity of the alkaloids, flavonoid, and saponins in the extract and plant materials was determined using standard methods. The Preliminary alpha amylase inhibitory activity of the extract was carried out using starch iodide reagent assay. The phytochemical contents of the root extract were determined out using Gas Chromatography and Mass spectrophotometry (GC-MS). The extraction of R. vomitoria yielded 2.30% n-Hexane extract. The phytochemical screening of the extract shows the presence of alkaloid, flavonoid, saponins, reducing sugar, de-oxy sugars and steroids while quantitative phytochemical analysis showed the root contain alkaloids: 11.2±0.06, flavonoids: 16.6 ±0.12 and saponins: 14.8 ±0.18. The extract gave a positive alpha-amylase inhibitory activity. The GC-MS indicated the presence of twelve compounds, which are basically long chain fatty acids and esters and the most abundant compound is n-Hexadecanoic acid. Most of the compounds detected have antioxidant, anti-inflammatory, antidiabetic and enzyme inhibitory activities which may explain the various traditional uses of this plant and the observed alpha-amylase inhibitory activity

Assessment of Artemisia Campestris L. Leaf Extract Effects on Polycystic Ovarian Syndrome in Rats, Antioxidant and α-Amylase Inhibition Activities.

Polycystic Ovarian Syndrome (PCOS) is characterized by metabolic and reproductive dysfunction, often associated with elevated oxidative stress markers in the bloodstream. This study examines the potential antioxidant properties and α-amylase inhibitory activity of Artemisia campestris leaves extract (Artemisia campestris L) and its effects on rats with induced PCOS. Estradiol valerate was administered to ten mature Wistar rats to induce PCOS, while a control group consisted of five mature Wistar rats. Following a 16-day induction period, the rats were categorized into three groups: a control group, a PCOS group, and an experimental group receiving 200 mg/kg body weight of A. campestris L. extract orally for 15 days. Serum levels of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were measured using the ELISA technique. The group treated with A. campestris L. extract exhibited significantly reduced LH levels compared to the PCOS group. Histomorphometric analysis indicated notable changes in follicle counts and the thickness of the theca layer. These findings suggest a significant alleviation of PCOS symptoms, potentially linked to the effects of A. campestris L. on oxidative stress pathways. Furthermore, aqueous extracts of A. campestris L. displayed potent in vitro inhibition of α-amylase, with an IC50 value of 2.418 μg/mL.

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.

Phytochemical profiling from Dioscorea bulbifera L. bulbils using LC-MS, proximate analysis and antidiabetic activity: in vitro and in silico approaches

ABSTRACT The nutritional value and medicinal properties of highly edible Bulbils of Dioscorea bulbifera L are still unexplored. This study reported the nutritional and medicinal values by In vitro, and In silico studies along with chemical profiling using LC-MS. The proximate analysis was conducted by the AOAC method. The antioxidant and antidiabetic activities were assessed using DPPH and α- α-glucosidase enzyme inhibition assay. Molecular docking was used to do an In silico examination of the identified molecules, and ADMET analysis of the hit candidate was also performed. The result showed that bulbils of D. bulbifera were found to have a higher percentage of protein (8.83%), fat (0.96%), and fiber (5.40%). It exhibited significant levels of phenolic and flavonoid content 106.93 ± 0.02 mg GAE/g and 11.51 ± 0.02 mg QE/g, respectively. The ethyl acetate fraction of D. bulbifera showed potent antioxidants with an IC 50 = 13.75 ± 0.6 μg/mL. Furthermore, the methanol extract showed more than 50 % inhibition activity with IC 50 values of 26.29 ± 0.6 μg/mL and 191.2 ± 0.7 μg/mL against α-glucosidase and α-amylase, respectively. The ethyl acetate fraction showed higher α-glucosidase and α-amylase inhibitory activity with an IC 50 of 14.42 ± 0.4 μg/mL and 171.5 ± 0.4 μg/mL, respectively, compared to the standard acarbose (p < 0.05). Chemical profiling of most bio-active ethyl acetate fraction was done using LC-MS analysis, where eleven compounds were annotated. In conclusion, bulbils of D. bulbifera demonstrate promising anti-diabetic activity through In vitro and In silico studies.

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.

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