Α-glucosidase Inhibition Assay Research Articles

Gas Chromatography-Mass Spectrometry and Fourier Transform Infrared Spectroscopy Analysis of Potential α-Glucosidase Inhibitors from Terminalia catappa Leaf Extracts

Aims: Postprandial hyperglyceamia is often caused by insulin insufficiency or cellular glucose uptake complications, and conventional treatments often yield undesirable side effects. The aim of the current work was to assess the α-glucosidase inhibitory activities of T. catappa leaf extracts and use spectroscopic techniques to partially characterize possible inhibitors. Study Design: Phytochemical screening, enzyme inhibition assay and spectrometric and spectroscopic characterization of bioactive compounds from leaf extract and fractions of T. catappa. Place and Duration of Study: The entire work was carried out at the Department of Applied Chemistry and Biochemistry, University for Development Studies, Ghana within nine months. Methodology: T. catappa leaf extract and fractions were qualitatively screened for phytochemicals and their biological activity assessed in α-glucosidase inhibition assay. The potential enzyme inhibitors were characterized by Gas Chromatography-Mass Spectrometry (GC-MS) and Fourier Transform Infrared (FT-IR) Spectroscopy. Results: Phytochemical screening of the extract and the various solvent fractions revealed the presence of alkaloids, flavonoids, saponins, flavanol glycosides, phenolics, and terpenoids. The α-glucosidase inhibition potential of the crude leaf extract was concentration-dependent with a half-maximal inhibitory concentration (IC50) of 337.5 µg/ml. Solvent fractions from the crude extract demonstrated α-glucosidase inhibitory activity with IC50 values ranging from 170.40 µg/ml for ethyl acetate (EtOAc) fraction to 71.90 µg/ml for n-hexane (n-Hex) fraction. Acarbose, the control drug, demonstrated significant α-glucosidase inhibition activity in a similar pattern with IC50 of 6.16 µg/ml. The enzyme inhibition kinetics parameters, specifically the Michaelis constant (KM) and Maximum reaction velocity (Vmax) values, suggested that the inhibition of α-glucosidase by T. catappa extract followed a competitive mode. GC-MS and FT-IR analysis of the n-Hexane fraction identified the compounds Eugenol, Urs-12-en-24-oic acid, 3-oxo-, methyl ester (+)-, phytol, trans-isoeugenol, α-amyrin, and squalene as the potential antidiabetic agents that might be responsible for reducing postprandial blood glucose levels. Conclusion: These findings show that T. catappa leaf extract contains α-glucosidase inhibitors and therefore serves as a valuable resource in the discovery of natural anti-diabetic agents.

Synergistic effect of hydrogen bonding and C–H…π interactions to modulate the supramolecular assemblies of isobenzofuranones: X-ray crystallography, DFT analysis and antihyperglycemic potential

This manuscript reports the synthesis, X-ray characterization and antihyperglycemic potential of two isobenzofuranone derivatives. The Suzuki-Miyaura cross-coupling of 5-bromoisobenzofuran-1(3H)-one with phenylboronic acid and p-tolylboronic acid under the action of palladium catalysis afforded the desired compounds in good yields. The structures were fully established using FTIR and NMR spectroscopy and X-ray crystallography. The study further delves into the synergistic effects of hydrogen bonding and C–H…π interactions on the supramolecular assemblies of isobenzofuranones, leveraging a holistic approach that combines X-ray crystallography, Density Functional Theory (DFT) analysis, and evaluation of antihyperglycemic activity. Focusing on two isobenzofuranone derivatives, we meticulously elucidate their structural features and how noncovalent interactions shape their crystal packing. Our exploration extends to assessing the antihyperglycemic potential of these compounds, underpinned by α-glucosidase inhibitory assays and augmented by molecular docking analysis. Compound 3b showed the best potency with an IC50 value of 13 ± 0.01 µM which is 67-folds strong inhibition than acarbose (IC50 = 870.2 ± 1.54 µM). Furthermore, the admetSAR and ProTox-II demonstrated that compound 3b follows the druggable criteria with a safe toxicity profile. Overall, these findings highlight the pivotal role of noncovalent interactions in modulating the supramolecular architectures of isobenzofuranones, thereby offering insights into their therapeutic potential against diabetes mellitus.

Phytochemical Analysis and Evaluation of Antioxidant, Antidiabetic, and Anti-inflammatory Properties of Aegle marmelos and Its Validation in an In-Vitro Cell Model.

Persistent hyperglycemia significantly increases oxidative stress and inflammation resulting in multiple cellular and molecular alterations which further exacerbate the diabetes associated complications.Aegle marmelos (L.) Corrêais a medicinal plant used in the Indian system of medicine for treating various disorders including diabetes. However, studies on phytoconstituents and their pharmacological activity of this plant are limited. Therefore, we aimed to determine the phytochemical components, evaluate the antidiabetic activity, anti-inflammatory activity, and antioxidant activity ofA. marmelosleaf extract, and validate its mechanistic effects in an in vitro cell model. The qualitative and quantitative analysis of the different phytoconstituents in the extract was determined using standardized protocols. The antioxidant activity of the extract was evaluated by 2,2-di-phenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity assay and ferric reducing antioxidant power (FRAP) assay. The antidiabetic activity of the extract was evaluated by α-amylase inhibition and α-glucosidase inhibition assay. The anti-inflammatory activity was studied using an albumin denaturation assay. In addition, the pharmacological effect(s) of leaf extract was checked in the normal rat kidney fibroblast cells (NRK-49F) under high glucose conditions. Intracellular reactive oxygen species (ROS) generation was measured by fluorometry using fluorescence probe 2',7'-dichlorodihydrofluorescin diacetate (DCF-DA). mRNA expression of inflammatory markers including inducible nitric oxide synthase (iNOS) and tumor necrosis factor-alpha (TNF-α) was studied using real-time quantitative polymerase chain reaction (RT-qPCR). Cell migration was studied using cell scratch assay. Statistical analysis was performed using GraphPad Prism version 8.0. The phytochemical analysis ofA. marmelosleaf extract revealed the presence of alkaloids, phenols, flavonoids, and saponins. The extract showed higher antioxidant activity in the DPPH (IC50=258.21 µg/mL) and FRAP assay (IC50=293.83 µg/mL). The extract exhibited prominent antidiabetic activity by inhibiting enzymes α-Amylase (IC50=73.2 µg/mL) and α-glucosidase (IC50=43.9 µg/mL). In addition, the extract showed effective anti-inflammatory activity by significantly inhibiting the denaturation of egg albumin (IC50=102.8 µg/mL). Further, the leaf extract significantly decreased the high glucose-induced ROS generation as well as inflammatory markers in rat fibroblast cell lines in a dose-dependent manner. Additionally, high glucose-induced cell migration as the measure of cell injury was effectively reduced by the extract treatment. A. marmelosleafextract was quantified to possess a substantial amount of important phytoconstituents that have promising pharmacological properties. Besides showing antidiabetic activity, the extract significantly combats the high glucose-induced ROS generation, inflammatory markers expressions, and cell migration. Further, in-depth studies and clinical trials are warranted so as to position these traditional remedies for the treatment of metabolic disorders.

In Vitro Alpha-Glucosidase Inhibitory Effect of Etlingera Elatior Ethanol Extract Growing in Gayo Highland, Aceh Province, Indonesia.

The prevalence of diabetes mellitus (DM) is increasing overtime, potentially leading to various severe health complications and mortality. Despite therapeutic agents have currently been developed, unexpected adverse effects are inevitable. Hence, safe and effective medications such as those of plant origin are critical to prevent unexpected complication in DM sufferers. Etlingera elatior has been widely used as spice and traditional medicine to treat diabetes in Aceh Province, Indonesia. However, study regarding α-glucosidase inhibitory effect of E. elatior growing in Gayo highlands, Aceh, Indonesia, is completely lacking. The aim of this study was to evaluate in vitro α-glucosidase inhibitory effect of E. elatior ethanol extracts (EEEE) growing in Gayo highlands, Aceh Province, Indonesia. Antioxidant activity was determined using DPPH procedure, whereas α-glucosidase inhibition assay was carried out using spectrophotometric method. Data analysis was performed using One-Way Analysis of Variance (ANOVA), followed by Duncan's multiple range test at α=0.05. Phytochemical analysis revealed the presence of total phenolic (TPC), total flavonoid (TFC), and total tannin (TTC) content in all E. elatior plant parts, in which the highest TPC was found in the stem (158.38 GAE/g), whereas the highest TFC and TTC was obtained in the rhizome extracts. The extract of fruit showed the strongest antioxidant activities, followed by the stem and leaf, with IC 50 of 2.381 μg/mL, 6.966 μg/mL, and 19.365 μg/mL, respectively. All E. elatior extracts revealed a significant inhibitory activity against α-glucosidase at the concentration of 500 μg/mL, in which the stem extract showed the most effective α-glucosidase inhibitory effect with IC 50 value of 5.15 μg/mL, suggesting its promising potential as antidiabetic agent. This study highlights E. elatior potency as a novel source of antioxidant and natural antidiabetic compounds that are useful for the prevention and treatment of diabetes.

In vitro and in vivo evaluation of hypoglycemic potential and acute toxicity of microencapsulated turmeric instant powder

BackgroundCurcuma longa L. (turmeric), traditionally used to treat various ailments including diabetes, has demonstrated beneficial health effects. However, its potential in food formulations requires further investigation. PurposeThis study examined the hypoglycemic effects of an instant powder containing microencapsulated turmeric oleoresin both in vitro and in vivo, alongside an acute toxicity assessment in Holtzman rats. MethodsThis study encompassed both in vitro and in vivo evaluations. In vitro, the α-glucosidase (a digestive enzyme) inhibition assay was employed to determine the powder's effectiveness. In vivo assessments included: (1) evaluation of the hypoglycemic effect in mice; (2) conducted safety testing following international guidelines, administering a 2000 mg/kg dose to rats with subsequent monitoring of biochemical parameters; and (3) histological examination of liver, kidney, and spleen tissues for potential harmful effects. ResultsThe instant powder with turmeric oleoresin microencapsulation demonstrated significant α-glucosidase inhibition in vitro and hypoglycemic effects in vivo. The acute toxicity test at 2000 mg/kg showed no mortality but revealed significant alterations in erythrocyte parameters and hemoglobin percentage. Histological examinations of liver, kidney, and spleen tissues did not differ from those of the control group, though pancreatic tissue was not evaluated in this study. ConclusionAccording to this study, the microencapsulated turmeric oleoresin instant powder exhibited antidiabetic effects without signs of overt toxicity at doses up to 2000 mg/kg in rats.

Biological Effects of Green Synthesized Al-ZnO Nanoparticles Using Leaf Extract from Anisomeles indica (L.) Kuntze on Living Organisms.

The synthesis of Al-ZnO nanoparticles (NPs) was achieved using a green synthesis approach, utilizing leaf extract from Anisomeles indica (L.) in a straightforward co-precipitation method. The goal of this study was to investigate the production of Al-ZnO nanoparticles through the reduction and capping method utilizing Anisomeles indica (L.) leaf extract. The powder X-ray diffraction, UV spectroscopy, Fourier transform infrared spectroscopy, and scanning electron microscopy with EDAX analysis were used to analyze the nanoparticles. X-ray diffraction analysis confirmed the presence of spherical structures with an average grain size of 40 nm in diameter, while UV-visible spectroscopy revealed a prominent absorption peak at 360 nm. FTIR spectra demonstrated the presence of stretching vibrations associated with O-H, N-H, C=C, C-N, and C=O as well as C-Cl groups indicating their involvement in the reduction and stabilization of nanoparticles. SEM image revealed the presence of spongy, spherical, porous agglomerated nanoparticles, confirming the chemical composition of Al-ZnO nanoparticles through the use of the EDAX technique. Al-ZnO nanoparticles showed increased bactericidal activity against both Gram-positive and Gram-negative bacteria. The antioxidant property of the green synthesized Al-ZnO nanoparticles was confirmed by DPPH radical scavenging with an IC50 value of 23.52 indicating excellent antioxidant capability. Green synthesized Al-ZnO nanoparticles were shown in in vivo studies on HeLa cell lines to be effective for cancer treatment. Additionally, α-amylase inhibition assay and α-glucosidase inhibition assay demonstrated their potent anti-diabetic activities. Moving forward, the current methodology suggests that the presence of phenolic groups, flavonoids, and amines in Al-ZnO nanoparticles synthesized with Anisomeles indica (L.) extract exhibit significant promise for eliciting biological responses, including antioxidant and anti-diabetic effects, in the realms of biomedical and pharmaceutical applications.

Fabrication and characterization of responsible approach for targeted intestinal releasing and enhancing the effectivity of kidney tea saponin upon porous starch /xanthan gum /sodium alginate-based hydrogel bead

To enhance the intestinal targeted release of kidney tea saponins, a simple delivery system was designed through the use of porous starch (PS), sodium alginate (ALG) and xanthan gum (XG). Porous starch was prepared by hydrolysis with a combination of α-amylase and amyloglucosidase and it was characterized by scanning electron microscopy, which revealed the formation of porous structures in the starch granules. The results of one-way optimisation illustrated that this unique delivery system achieved 79.00 ± 1.22 % of the optimal encapsulation rate. The carrier structure was subjected to analysis using Fourier transform infrared spectroscopy and X-ray diffraction. The α-glucosidase inhibition assay showed better inhibition of kidney tea saponin compared to the positive control acarbose. In addition, the effectiveness of this delivery design was confirmed via an in vitro simulated digestion method. It was showed that only a 15.57 ± 1.27 % release rate of kidney tea saponin was observed in the upper gastrointestinal tract, whereas release rates of 17.51 ± 1.29 % and 41.07 ± 0.76 % were observed for xanthan gum/sodium alginate/kidney tea saponin and sodium alginate/kidney tea saponin beads, respectively. It was concluded that the utilization of PS and a xanthan gum/sodium alginate coating represents an efficacious methodology for the development of an intestinal targeted delivery system.

Volatile profiling of Cinnamomum heyneanum and Cinnamomum Palghatensis and in vitro and in silico antidiabetic activity of essential oil nanoemulsions

Essential oil nanoemulsions (EONs) of two wild cinnamons, Cinnamomum heyneanum (CH) and Cinnamomum Palghatensis (CP), were formulated, characterized and investigated for their antidiabetic activity. Leaf essential oils (EOs) were extracted and characterized by GC-MS and GC-FID. Two sets of EONs were formulated and characterized by zeta analyzer, viscometer and TEM. Antioxidant activity was studied using DPPH, ABTS, superoxide, hydroxyl and hydrogen peroxide assays. Antidiabetic activity was evaluated by α-amylase inhibition, α-glucosidase inhibition, glucose uptake and glucose-stimulated insulin secretion assays. In silico studies were performed to support the efficacy. Methyl eugenol (60.3 %), safrole (27.8 %) in CH EO and bicyclogermacrene (19.5 %), (E)-caryophyllene (14 %) in CP EO were major components. Of two sets of EONs, 1:2 ratio showed better hydrodynamic average diameter [CH 42.9±0.78 nm & CP 27.9±1.70 nm] and better zeta potential [CH −38.4±0.85 mV & CP −38.4±0.45 mV (1st day)]. TEM observation showed that 1:2 ratio EONs were spherical with an average diameter of 85 nm (CH) and 8.98 nm (CP). Both CH and CP showed remarkable antioxidant activity. CP showed better α-glucosidase inhibition (IC50 0.599±0.008 mg/mL), enhanced glucose uptake (0.53±0.08 fold vs. control) and insulin secretion (1.40±0.06 fold vs. control). In silico analysis reveals that all major components of CH and CP interact with key residues of the protein targets associated with diabetes, α-amylase, α-glucosidase, insulin receptor, Glugagon like peptide1 Receptor and Glut 4. In vitro and in silico studies revealed that EON of CH and CP have pharmacological properties due to the presence of various compounds against diabetes mellitus.

Investigation of Anti-Diabetic Properties of Ceylon Cinnamon Bark Extracts by In-Vitro α-Amylase and α-Glucosidase Inhibition, Molecular Modeling, and Postprandial Blood Glucose Regulation for Potential Nutraceuticals

Background: Diabetes Mellitus (DM) can appear due to the absence of insulin (DM1- type 1) or poor response of cells to insulin (DM2-type 2). Even though DM1 cannot be controlled using general treatments, DM2 can be easily controlled or prevented using pharmaceuticals, nutraceuticals, or dietary practices. Ceylon cinnamon (Cinnamomum zeylanicum) is one such natural remedy that has been consumed against elevated blood glucose levels in the past. Cinnamon and different types of cinnamon extracts have been scientifically tested for their activities on the inhibition of α-amylase and α-glucosidase enzymes that are responsible for carbohydrate metabolism and are effective in blood glucose regulation. However, the combined effect of aqueous and ethanol extracts of cinnamon bark on blood glucose regulation is still lacking. In this study, Water Extract of Cinnamon (CWE), Ethanol Extracts of Cinnamon (hot ethanol extract of cinnamon-CHEE, cold ethanol extract of cinnamon-CEE, and 50% ethanol extract of cinnamon- CEE-50) were studied for their sugar-controlling properties. Objectives: This study was performed to identify the efficacy of different cinnamon extracts on the inhibition of α-amylase and α-glucosidase enzymes, followed by animal studies to confirm the use of the extracts in nutraceutical formulations. Methods: Water and ethanol-based extraction method was used to prepare cinnamon extracts. These extracts have been scientifically tested for their activities on the inhibition of α-amylase and α-glucosidase enzymes. Molecular docking studies were used to identify the binding of the active molecules to the substrate binding sites of α-amylase and α-glucosidase. In-vivo time dependence postprandial blood glucose regulation studies have been performed with healthy Wistar male rats. Results: Yields of the CHEE, CEE, and CWE were 14±2%, 12±2%, and 8±1% respectively. According to the LCMS data, the major component in the CEE was cinnamaldehyde. Both CWE and CEE were subjected to the Total Polyphenol assay (TPC) and Total Flavonoids (TFC) assays. The TPC of CWE and CEE were 117±1 mg (Gal)/g and 170±10 mg (Gal)/g, while the TFC of CWE and CEE were 359±1 mg (Qc)/g and 254±4 mg (Qc)/g, respectively. In the α-amylase inhibition assay, Acarbose; a known α-amylase inhibitor, and CEE showed IC50 values of 65.4 ppm and 2.6 ppm, while CWE failed to show inhibition against α-amylase. In the α-glucosidase inhibition assay, Acarbose; a known α-amylase inhibitor, CEE, and CWE showed IC50 values of 312 ppm, 4.5 ppm, and 1.3 ppm, respectively. In-vivo time dependence postprandial blood glucose regulation studies that have been performed with healthy Wistar male rats showed a lowering of blood glucose concentrations by 22%, 11%, and 10% of glucose at 30 min, 60 min, and 90 min compared to the control group. Conclusion: The CEE contains polyphenols and flavonoids and is effective in inhibiting both α- amylase and α-glucosidase. The CWE also contains polyphenols and a comparatively higher level of flavonoids and is effective in inhibiting α-glucosidase while not affecting α-amylase inhibition. Overall, the IC50 data, TPC data, and TFC data proposed that the inhibition of carbohydrate hydrolyzing enzymes by polyphenols may depend on the polarity of particular polyphenols. Based on the rat trials, it can be concluded that the 1:1 combination of CWE and CEE may be useful in formulating postprandial blood glucose level-regulating nutraceuticals.

Curbing Key Digestive Enzymes by Three Plant Extracts for Sustainable Management of Postprandial Hyperglycemia

Background: Diabetes mellitus is a chronic metabolic condition marked by persistently elevated blood sugar levels. Key digestive enzymes viz. α-amylase and α-glucosidase, hydrolyze consumed carbohydrates into glucose which raises the postprandial blood glucose level in a diabetic patient. So, the development of α-amylase and α-glucosidase inhibitors procured from medicinal plants to retard starch digestion is an alternative approach for controlling type 2 diabetes mellitus. Objective: The current study aimed to evaluate the inhibitory potentials of the key digestive enzymes viz. α-amylase and α-glucosidase by the extracts of three medicinal plants; red dragon fruit (Hylocereus polyrhizus) pulp and peel, bamboo (Bambusa vulgaris) shoot, turnip (Brassica rapa L.) shoot and leaf by performing α-amylase and α-glucosidase inhibition assays in vitro. Methods: Inhibition of α-amylase activity was conducted using 3,5-dinitrosalicylic acid method, and 4- Nitrophenyl-α-D-glucopyranoside was used as a substrate to perform α-glucosidase inhibition assay in vitro. Results: Among all the selected sample extracts, red dragon fruit pulp expressed the highest percentage of α-amylase inhibition (59.73 ± 4.33%) at the concentration of 1000 μg/mL which is comparable to standard antidiabetic drug Acarbose (70.59 ± 2.64%), whereas the lowest inhibition was observed in turnip shoot extract (42.48 ± 2.10%) at the same concentration. In terms of α-glucosidase inhibition activity, again, red dragon fruit pulp extract demonstrated the maximum inhibition rate (56.42 ± 2.38%) at 1000 μg/mL concentration. This is respectable in comparison to the reference Acarbose (66.45 ± 1.78%). In contrast, turnip shoot extracts displayed the lowest α-glucosidase inhibition activity (38.27 ± 2.21%) at the same concentration. Conclusion: The current study demonstrated that the red dragon fruit pulp extract possesses substantial antihyperglycemic activity (α-amylase inhibition: 59.73 ± 4.33%, α-glucosidase inhibition: 56.42 ± 2.38%) in vitro, which could be a putative nutraceutical to manage postprandial hyperglycemia.

Multi-target anti-diabetic styrylpyrones from Phellinus igniarius: Inhibition of α-glucosidase, protein glycation, and oxidative stress

Bioactivity screening revealed that the EtOAc extract from the culture broth of Phellinus igniarius SY489 exhibited remarkable α-glucosidase inhibitory activity, with an IC50 value of 1.92 μg/mL. Activity- and ultraviolet (UV) profile-guided isolation led to the discovery of four anti-diabetic styrylpyrones (1–4), including two novel compounds, phelignidins A (1) and B (2). Compounds 1 and 2 represent a rare structural type of styrylpyrone dimer, in which one of the pyrone moieties exists in an open-ring state. The absolute configurations of the new compounds 1 and 2, as well as the previously unresolved compound 3, were established. Compounds 1–4 were effective in α-glucosidase inhibition, anti-glycation, and antioxidant assays, surpassing or being comparable to the positive control drugs, with minimal cytotoxicity. Furthermore, studies on α-glucosidase inhibition mechanisms suggested that these compounds interact with α-glucosidase at a single binding site, causing secondary structure unfolding and exerting inhibitory activity via a mixed-type mechanism. These results provide an important basis for developing novel, low-toxicity, multi-target anti-diabetic drugs from edible and medicinal fungi.

Green Synthesis of Silver Nanoparticles from Syzygium cumini (L.) Skeels Seed Extract and their Potential Medicinal Applications.

Nanotechnology is considered as one of the fastest-developing areas in the biomedicine field. Hence, the green synthesis of silver nanoparticles from Syzygium cumini seed extract was carried out in this study. The synthesized nanoparticles were characterized by UV-Vis spectroscopy, FTIR (Fourier transform infrared), FE-SEM (Field Emission scanning electron microscopic), AFM (Atomic Force Microscope), XRD (X-ray diffraction), and EDX (Energy dispersive X-Ray). Their antioxidant and anti-inflammatory activity were evaluated by DPPH (2,2-diphenyl-1- picrylhydrazyl), PM (Phosphomolybdenum) assay, and albumin denaturation assay. Further, the antibacterial activity of the nanoparticles was studied against Gram-positive and Gram-negative bacteria using the agar well diffusion method. In addition, the antidiabetic activity of nanoparticles was studied by α-amylase and α-glucosidase inhibition assays. The surface plasmon resonance at 430 nm confirmed the formation of silver nanoparticles. They were stable and spherical in shape, with sizes ranging from 30 to 90 nm. The DPPH inhibition % of silver nanoparticles varied from 7.91±0.39% to 68.35±0.76%. The % inhibition of albumin denaturation was comparable to the diclofenac. Further, the results of antibacterial activity revealed that the zone of inhibition for all the test bacteria varied from 14.33±0.58 to 25.33±0.58 mm, where B. cereus was more susceptible. In addition, the % inhibition of α-amylase and α-glucosidase varied from 19.91±0.15% to 61.43±0.31% and 15.26±0.11% to 55.38±0.20%, respectively. This study is the first attempt of utilizing the silver nanoparticles synthesized from S. cumini seed extract for antidiabetic activity. The study suggests that these nanoparticles could be well utilized in pharmaceutical industries as an efficient antioxidant, anti-inflammatory, antibacterial, and antidiabetic drug.

Green synthesis of CuO/TiO2 and ZnO/TiO2 nanocomposites using Parkia timoriana bark extract: Enhanced antioxidant and antidiabetic activities for biomedical applications

The green method provides stable, rapid, and eco-friendly methods for synthesis nanoparticles with plant extract as capping and reducing agents. This method renders biocompatibility, scalability, and potential medical applications of nanoparticles. This study green synthesized CuO/TiO2 and ZnO/TiO2 nanocomposites using Parkia timoriana bark extract. The synthesized nanocomposites were determined utilizing UV–vis DRS FTIR, XRD, TGA, AFM, FE-SEM, E-DAX, HR-TEM, and XPS. Antioxidant assay and antidiabetic studies revealed the biological activity of nanocomposites. The antioxidant property in ZnO/TiO2 (84.07 %) was higher than in CuO/TiO2 nanocomposites (72.76 %). The IC50 value of CuO/TiO2 and ZnO/TiO2 in α-amylase inhibition assay was 72.12 μg/mL and 75.95 μg/mL, respectively and IC50 value of CuO/TiO2 and ZnO/TiO2 in α-glucosidase inhibition assay was 30.80 μg/ml and 25.69 μg/ml. Thus, it concludes ZnO/TiO2 nanocomposites exhibited higher antioxidant and antidiabetic activity than CuO/TiO2 nanocomposites. These results show that biosynthesized nanocomposites can be used for treating diseases.

Potential nanomedicinal applications and physicochemical nature of Hyphaene thebaica-reduced nano-samaria.

Herein we described the biofabrication of samarium oxide nanoparticles (HT-Sm2O3 NPs) by applying the aqueous fruit extract of Hyphaene thebaica was utilized as an eco-friendly chelating agent. The prepared NPs were subjected to various physicochemical properties and potential in biomedical applications. X-ray Diffraction (XRD) pattern revealed sharp peaks that corroborated with the Joint Committee on Powder Diffraction Standards (JCPDS) card no. 00-042-1464. Crystallite size obtained from Debye-Scherrer approximation and Williamson-Hall (W-H) plot was 28.73 and 69.3 nm, respectively. Optical bandgap was calculated by employing Kubelka-Munk (K-M) function and was found to be ~4.58 eV. Raman shift was observed at 121, 351, 424-, and 561 cm-1. Photoluminescence (PL) spectra revealed two major peaks positioned at 360 and 540 nm. The high-resolution transmission electron microscopy (HR-TEM) analysis of HT-Sm2O3 nanoparticles (NPs) showed that they predominantly have spherical to cuboidal shapes. Additionally, the selected area electron diffraction (SAED) pattern presented spotty rings, indicating a high level of crystallinity in these NPs. The potential nanomedicine applications were studied using diverse bioassays using different treatments. The antioxidant activity demonstrated 45.71% ± 1.13% inhibition at 1000 μg/mL. Brine shrimp lethality assay revealed the highest cytotoxicity of 46.67% ± 3.33% at 1000 μg/mL and LC50 value of 1081 μg/mL. HT-Sm2O3 NPs exhibited inhibition of angiogenesis (20.41% ± 1.18%) at of 1000 μg/mL. MTT assay results indicated that HT-Sm2O3 NPs exhibit inhibitory effects on cell lines. Specifically, these NPs showed an IC50 value of 104.6 μg/mL against 3T3 cells. Against MCF-7 cells, the NPs demonstrated an IC50 value of 413.25 μg/mL. Additionally, in the inhibition of acetylcholinesterase (AChE), the newly synthesized NPs showed an IC50 value of 320 μg/mL. The antidiabetic assessment through α-glucosidase and α-amylase inhibition assays revealed, an IC50 value of 380 μg/mL for α-glucosidase and 952 μg/mL for α-amylase was calculated. Overall, our study suggested that the Sm2O3 NPs possess moderate anticancer, cholinesterase inhibition, and antidiabetic potential, however, needs further assessment. RESEARCH HIGHLIGHTS: In this work, nano-samaria is synthesized using an eco-friendly and green approach. The nanoparticles were characterized using techniques such as Raman, HR-TEM, FTIR, DRS, XRD, and so on, and the applications were studied using multiple in vitro bioassays for Diabetes, Alzheimer, and Cancer. The nano-samaria revealed good potential for potential biomedical applications.

Antibacterial, antidiabetic and antioxidant bioevaluation of Calamus leptospadix Griff. and isolation of a flavan type compound

The plant based natural products have always been a rich source of bioactive molecules for drug discovery. The tender shoots of Calamus leptospadix Griff., an edible medicinal plant was extracted using methanol, water and ethanol as three different solvents to study the effect of the extracting solvents and temperature on their antioxidant, antidiabetic and antibacterial properties and total phenolic and flavonoid contents. The antioxidant properties were determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) and ferric reducing antioxidant power (FRAP) assay. The α-glucosidase inhibitory assay was carried out to determine the antidiabetic potential. The antibacterial properties of the extracts were determined against four strains of bacterial species viz. Bacillus subtilis, Streptococcus pneumoniae, Escherichia coli and Citrobacter freundii using Broth macro dilution method.The methanolic extracts of the plant were found to possess the highest total phenolic and total flavonoid contents. In the antioxidant assays, the cold methanolic extract was found to exhibit the highest DDPH radical scavenging activity and ferric-reducing antioxidant power. In the antidiabetic assay, the extract exhibited better α-glucosidase inhibitory potential than that of the positive control acarbose. It was also found to be effective against both gram-positive and gram-negative strains in the antibacterial assay. A flavan-type compound 4-(5,7-dimethoxychroman-2-yl)phenol was isolated from the most bioactive cold methanolic extract of the plant and characterised from its XRD, 1H and 13C NMR, HRMS and IR data.

Assessing anticancer, antidiabetic, and antioxidant capacities in green-synthesized zinc oxide nanoparticles and solvent-based plant extracts

Cancer and diabetes represent significant challenges in the field of biomedicine, with major and global impacts on public health. Acacia nilotica, commonly called 'gum arabic tree,' is recognized for its unique biomedical properties. The current study aimed to investigate the pharmacological potential of A. nilotica-based zinc-oxide nanoparticles (ZnO-NPs) in comparison to the ethanol and methanol-based extracts against cancer, diabetes, and oxidative stress. Green synthesis of ZnO-NPs was performed using barks of Acacia nilotica. Different techniques for the characterization of ZnO-NPs, including UV–Visible spectroscopy, Scanning Electron Microscopy, Fourier Transmission Infrared (FT-IR) spectroscopy, and X-ray Diffraction (XRD), were utilized. The morphological analysis of ZnO-NPs revealed that the fine NPs have mean particle sizes of 15 ± 1.5 nm. For the solvent based-extraction, leaves and barks were utilized and dissolved into ethanol and methanol for further processing. The MTT assay revealed that the optimum concentration of ZnO-NPs to inhibit the proliferation of liver cancer cell line HepG2 was 100 μg/mL where 67.0 % inhibition was observed; and both ethanol- and methanol-based extracts showed optimum inhibition at 100 μg/mL. The DPPH assay further demonstrated that 250 μg/mL of ZnO-NPs and 1000 μg/mL of both ethanol- and methanol-based extracts, as the optimum concentration for antioxidant activity (with 73.1 %, 68.9 % and 68.2 % inhibition respectively). The α-Glucosidase inhibition assay revealed that 250 μg/mL of ZnO-NPs and 10 μg/mL of both ethanol- and methanol-based extracts as the optimum concentration for antidiabetic activity (with 95 %, 93.7 % and 93.4 % inhibition respectively). The study provided interesting insights into the efficacy and reliability of ZnO-NPs for potential pharmacological application. Further research should be focused on examining specific pathways and the safety of ZnO-NPs in comparison to solvent-based extracts.

Anti-diabetic active constituents of pomegranate peel-derived extracellular nanovesicles

Pomegranate peel-derived extracellular nanovesicles(PPENs) were isolated and purified by ultra-high speed centrifugation and sucrose density gradient centrifugation. Their morphology and structure were characterized. In vitro α-glucosidase inhibition assay and model test of insulin resistance(IR) in HepG2 cells showed that PPENs had good anti-diabetic activity. The IC_(50) value of α-glucosidase inhibition was(35.3±1.1) μg·mL~(-1), significantly better than the positive drug acarbose. At a concentration of 100 μg·mL~(-1), PPENs could increase the glucose absorption of IR cells significantly. Lipidome, proteome, and metabolite analysis of PPENs were performed using chromatography-mass spectrometry. MicroRNA(miRNA) sequences were identified, and target genes of miRNA were predicted. The analysis results indicated that PPENs contained abundant lipids and transport proteins, providing a material basis for the transportation and distribution of PPENs in tissue. Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway enrichment analysis suggested that lipids and miRNAs may be the key components of PPENs to exert anti-diabetic activity.

In vitro study of the inhibitory potentials of cold and hot aqueous extract of Vernonia amygdalina, Calotropis procera, and Persea americana on α-glucosidase

Background: The surge in the incidence of diabetes mellitus has spurred heightened interest on alternative and complementary therapies, particularly those derived from medicinal plants. Objective: To assess the α-glucosidase inhibitory activity of cold and hot aqueous extracts of Vernonia amygdalina (bitter leaf), Calotropis procera (locally known as “bomubomu” leaves), and Persea americana (also known as avocado pear) to explore their medicinal applicability. Method: The leaves of V. amygdalina, C. procera, and the seed of P. americana were subjected to cold and hot extraction methods using distilled water. These extracts were specifically targeted for their potential inhibitory effects on α-glucosidase activity, a key enzyme involved in carbohydrate digestion. Results: The α-glucosidase inhibitory assay showed that the extracts from the plants had maximum inhibitory effects at 20 mg/mL. Cold and hot aqueous extracts of V. amygdalina exhibited maximal inhibitory activities of 100% and 86%, respectively, at 20mg/mL. Cold and hot aqueous extracts of C. procera displayed 100% and 91% inhibitory activities, respectively, at 20mg/mL. Similarly, cold and hot extracts of P. americana exhibited the highest inhibitory activities of 77% and 63%, respectively, at 20mg/mL concentration. Conclusions: The findings demonstrated that cold and hot aqueous extracts of Vernonia amygdalina, Calotropis procera, and Persea americana exhibited significant inhibitory activities against α-glucosidase. The observed inhibitory effects suggest the therapeutic potential of these plant extracts as natural remedies for managing post-prandial hyperglycaemia in Type 2 Diabetes mellitus.

α-Glucosidase inhibition assay of galbanic acid and it amide derivatives: New excellent semi-synthetic α-glucosidase inhibitors

α-Glucosidase inhibitory activity of galbanic acid and its new amide derivatives 3a–n were investigated. Galbanic acid and compounds 3a–n showed excellent anti-α-glucosidase activity with IC50 values ranging from 0.3 ± 0.3 μM to 416.0 ± 0.2 μM in comparison to positive control acarbose with IC50 value of = 750.0 ± 5.6. In the kinetic study, the most potent compound 3h demonstrated a competitive mode of inhibition with Ki = 0.57 µM. The interaction of the most potent compound 3h with the α-glucosidase was further elaborated by in vitro Circular dichroism assessment and in silico molecular docking and Molecular dynamics studies. Compound 3h was also non-cytotoxic on human normal cells. In silico study on pharmacokinetics and toxicity profile of the most potent galbanic acid derivatives demonstrated that these compounds are valuable lead compounds for further study in order to achieve new anti-diabetic agents.

In Vitro Analysis of Camellia sinensis Leaf Extract Against Diabetes Mellitus.

Diabetes mellitus (DM) poses a significant global health challenge, with its prevalence steadily increasing. Natural compounds derived from plants have garnered attention for their potential therapeutic effects in managing this metabolic disorder. Camellia sinensis, commonly known as tea, is rich in bioactive compounds exhibiting various pharmacological properties. This study investigates the potential anti-diabetic activity of C. sinensis leaf extract through in vitro analysis. Camella sinensisleaf extract was prepared by grinding the plant's leaf into a powder, mixing it with distilled water, and heating. The antidiabetic activity was assessed through α-Amylase and α-Glucosidase inhibitory assays, employing varying concentrations of the plant extract. Molecular docking analysis utilized Autodock 1.5.6 software (The Scripps Research Institute, California, US)to predict ligand-receptor interactions, guiding subsequent experimental validation. Camella sinensisleaf extract exhibited high phenolic content, suggesting potential in managing hyperglycemia. Tannins may aid glucose absorption and inhibit adipogenesis, making them promising for non-insulin-dependent DM (NIDDM). Terpenoids, with antioxidant activity, inhibit advanced glycation. Saponins and steroids were absent. Molecular docking revealed residues like IR, IRS1, and AS160 with significant impact on α-Amylase and α-Glucosidase, comparable to metformin. The findings of this study highlight the promising potential of C. sinensis leaf extract in managing hyperglycemia associated with DM. The high phenolic content aids in glucose regulation. Specifically, the presence of tannins suggests a potential role in modulating glucose absorption and inhibiting adipogenesis, which could be particularly beneficial for individuals with NIDDM.These findings provide valuable insights into the molecular mechanisms underlying the potential therapeutic efficacy of C. sinensis leaf extract against DM, paving the way for further research and development of novel therapeutic interventions in diabetes management.