Potential Antidiabetic Activity Research Articles

Innovation of 6-sulfonamide-2H-chromene derivatives as antidiabetic agents targeting α-amylase, α-glycosidase, and PPAR-γ inhibitors with in silico molecular docking simulation.

A new series of 2-imino or 2-oxo-2H-chromene-6-sulfonamide derivatives 2-9 with potential anti-diabetic activity were designed and synthesized. The new 6-sulfonamide chromenes were synthesized by reacting 3-formyl-4-hydroxybenzenesulfonyl chloride with activated methylene derivatives in the presence of ammonium acetate as a catalyst. The structure of the products was confirmed by spectroscopic analysis. All the designed derivatives 2-9 were evaluated for their activity against α-amylase and exhibited inhibitory percentage values higher than 93% at 100 μg mL-1. Additionally, the IC50 values represented a variable degree of activity with two derivatives 2 and 9 exhibiting the most promising derivative results with IC50 values of 1.76 ± 0.01 and 1.08 ± 0.02 μM, respectively, compared to Acarbose (IC50 = 0.43 ± 0.01 μM). Additionally, these derivatives showed potency against the α-glucosidase enzyme with IC50 values of 0.548 ± 0.02 and 2.44 ± 0.09 μg mL-1, compared to Acarbose (0.604 ± 0.02 μg mL-1). Moreover, the in vitro PPAR-γ transactivation assay revealed that chromene-6-sulfonamide derivatives 2 and 9 exhibited potential PPAR-γ activity with IC50 values of 3.152 ± 0.03 and 3.706 ± 0.32 μg mL-1, respectively, compared to Pioglitazone (4.884 ± 0.29 μg mL-1). This indicates that these derivatives have insulin sensitivity and glucose metabolism activity. The in silico ADMET prediction showed that these derivatives have an acceptable range of oral bioavailability, drug-likeness, and a safe toxicity profile, including being non-cytotoxic, non-mutagenic, non-immunotoxic, and non-carcinogenic. Finally, computational docking analysis demonstrated the ability of these derivatives to interact with α-amylase, α-glucosidase, and PPAR-γ enzymes, with confirmed successful placement due to good binding energy values and various interactions within the pocket.

Labdanum Resin from Cistus ladanifer L. as a Source of Compounds with Anti-Diabetic, Neuroprotective and Anti-Proliferative Activity

Labdanum resin or “gum” can be obtained from Cistus ladanifer L. by two different extraction methods: the Zamorean and the Andalusian processes. Although its main use is in the fragrance and perfumery sectors, ethnobotanical reports describe its use for medicinal purposes in managing hyperglycemia and mental illnesses. However, data concerning the bioactivities and pharmacological applications are scarce. In this work, it was found that the yield of labdanum resin extracted by the Andalusian process was 25-fold higher than the Zamorean one. Both resins were purified as absolutes, and the Andalusian absolute was purified into diterpenoid and flavonoid fractions. GC-EI-MS analysis confirmed the presence of phenylpropanoids, labdane-type diterpenoids, and methylated flavonoids, which are already described in the literature, but revealed other compounds, and showed that the different extracts presented distinct chemical profile. The potential antidiabetic activity, by inhibition of α-amylase and α-glucosidase, and the potential neuroprotective activity, by inhibition of acetylcholinesterase, were investigated. Diterpenoid fraction produced the higher α-amylase inhibitory effect (~30% and ~40% at 0.5 and 1 mg/mL, respectively). Zamorean absolute showed the highest α-glucosidase inhibitory effect (~14% and ~24%, at 0.5 and 1 mg/mL, respectively). Andalusian absolute showed the highest acetylcholinesterase inhibitory effect (~70% and ~75%, at 0.5 and 1 mg/mL, respectively). Using Caco-2 and HepG2 cell lines, Andalusian absolute and its purified fractions showed moderate cytotoxic/anti-proliferative activity at 24 h exposure (IC50 = 45–70 µg/mL, for Caco-2; IC50 = 60–80 µg/mL, for HepG2), whereas Zamorean absolute did not produce cytotoxicity (IC50 ≥ 200.00 µg/mL). Here we show, for the first time, that labdanum resin obtained by the Andalusian process, and its fractions, are composed of phytochemicals with anti-diabetic, neuroprotective and anti-proliferative potential, which are worth investigating for the pharmaceutical industry. However, toxic side-effects must also be addressed when using these products by ingestion, as done traditionally.

Exploring the pharmacological significance of Murraya koenigii (L.) Spreng: Insights from North-East India

Murraya koenigii (L.) Spreng., is a renowned medicinal and aromatic plant having antimicrobial and broad biological activities. In the present study, the essential oil chemical profile of the leaf and floral part were analysed using GC-FID and GC-MS, and the antimicrobial activities were determined by disk diffusion assay. The scientific analysis revealed α-pinene (40.41%) was the major compound of leaf essential oil (MKL) followed by sabinene (29.66%), β-pinene (7.92%), caryophyllene (4.24%), limonene (3.39%), terpinen-4-ol (3.25%), γ-terpinene (2.63%), terpinolene (1.58%), linalool (1.32%), along with other trace components. The floral part (MKF) contains the compounds α-pinene (74.02%) as the major compound followed by β-pinene (7.17%), sabinene (5.72%), limonene (4.19%), β-myrcene (1.98%), γ-terpinene (1.47%) and terpinen-4-ol (1.41%) along with other trace compounds. The MIC result revealed essential oil showed effectiveness against Escherichia coli (40 μg/mL), Micrococcus luteus (80 μg/mL), Aspergillus fumigatus (60 μg/mL) and Aspergillus brasiliensis (80 μg/mL) for MKL while MKF did not exhibit potent antimicrobial activities. The essential oils revealed potent antioxidant potential as determined by DPPH method with IC50 values of 14.02 μL/mL (MKL) and 5.45 μL/mL (MKF) and the ABTS method with IC50 values of 5.07 μL/mL and 8.38 μL/mL in MKL and MKF respectively as compared to that of the standards. The essential oils revealed potent antidiabetic activity with 6.02 μL/mL (MKL) and 8.18 μL/mL (MKF) as that of the standard. However, both MKL and MKF were not much effective in protease inhibitory activity and anti-tyrosinase activity. The study results exhibited a potent bioactivity profile and revealed many new utilization aspects of this essential oil.

Improvement of phenolic profile and biological activities of wild mustard sprouts

The current study aimed to assess the effect of the germination process of wild mustard seeds on the phenolic profile, antioxidant, antibacterial, and antidiabetic properties, and some relevant enzyme activities. The total phenolic and flavonoid contents increased 5- and 10-fold, respectively, and were maximized on 5-days sprouts. One new phenolic compound was identified on 5-days sprout extract using HPLC. The concentrations of the identified phenolic compounds increased 1.5–4.3 folds on 5-days sprouts compared with dry seeds. The total antioxidant activity multiplied 17- and 21-fold on 5-days sprouts using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assays, respectively. The activity of carbohydrate-cleaving, phenolic-synthesizing and antioxidant enzymes also increased during germination. On 5-days sprouts, there was a substantial correlation between the highest β-glucosidase and peroxidase activities with highest phenolic and flavonoid levels and maximum antioxidant activity. The phenolic extract of 5-days sprouts exhibited antimicrobial activities against Escherichia coli and Staphylococcus aureus and showed potent antidiabetic activity established by its inhibitory effect against α-amylase and α-glucosidase compared to dry seeds.

LC-ESI-MS/MS-Based Comparative Metabolomic Study, Antioxidant and Antidiabetic Activities of Three Lobelia Species: Molecular Modeling and ADMET Study.

The hydroethanol (70%) extracts of three Lobelia species (L. nicotianifolia, L. sessilifolia, and L. chinensis) were analyzed using LC-ESI-MS/MS. Forty-five metabolites were identified, including different flavonoids, coumarin, polyacetylenes, and alkaloids, which were the most abundant class. By applying Principal Component Analysis (PCA) and Hierarchical Cluster Analysis (HCA) based on LC-ESI-MS/MS analysis, the three species were completely segregated from each other. In addition, the three Lobelia extracts were tested for their antioxidant activities using a DPPH assay and as antidiabetic agents against α-glycosidase and α-amylase enzymes. L. chinensis extract demonstrated significant antioxidant activity with an IC50 value of 1.111 mg/mL, while L. nicotianifolia showed mild suppressing activity on the α-glycosidase activity with an IC50 value of 270.8 μg/mL. A molecular simulation study was performed on the main compounds to predict their potential antidiabetic activity and pharmacokinetic properties. The molecular docking results confirmed the α-glycosidase inhibitory activity of the tested compounds, as seen in their binding mode to the key amino acid residues at the binding site compared to that of the standard drug acarbose. Furthermore, the predictive ADMET results revealed good pharmacokinetic properties of almost all of the tested compounds. The biological evaluation results demonstrated the promising activity of the tested compounds, aligned with the in silico results.

Probing benzenesulfonamide–thiazolidinone hybrids as multitarget directed ligands for efficient control of type 2 diabetes mellitus through targeting the enzymes: α-glucosidase and carbonic anhydrase II

Diabetes mellitus is a chronic metabolic disorder characterized by improper expression/function of a number of key enzymes that can be regarded as targets for anti-diabetic drug design. Herein, we report the design, synthesis, and biological assessment of two series of thiazolidinone-based sulfonamides 4a-l and 5a-c as multitarget directed ligands (MTDLs) with potential anti-diabetic activity through targeting the enzymes: α-glucosidase and human carbonic anhydrase (hCA) II. The synthesized sulfonamides were evaluated for their inhibitory activity against α-glucosidase where most of the compounds showed good to potent activities. Compounds 4d and 4e showed potent inhibitory activities (IC50 = 0.440 and 0.3456 μM), comparable with that of the positive control (acarbose; IC50 = 0.420 μM). All the synthesized derivatives were also tested for their inhibitory activities against hCA I, II, IX, and XII. They exhibited different levels of inhibition against these isoforms. Compound 4d outstood as the most potent one against hCA II with Ki equals to 7.0 nM, more potent than the reference standard (acetazolamide; Ki = 12.0 nM). In silico studies for the most active compounds within the active sites of α-glucosidase and hCA II revealed good binding modes that can explain their biological activities. MM-GBSA refinements and molecular dynamic simulations were performed on the top-ranking docking pose of the most potent compound 4d to confirm the formation of stable complex with both targets. Compound 4d was screened for its in vivo antihyperglycemic efficacy by using the oral glucose tolerance test. Compound 4d decreased blood glucose level to 217 mg/dl, better than the standard acarbose (234 mg/dl). Hence, this revealed its synergistic mode of action on post prandial hyperglycemia and hepatic gluconeogenesis. Thus, these benzenesulfonamide thiazolidinone hybrids could be considered as promising multi-target candidates for the treatment of type II diabetes mellitus.

Green Synthesis and Anti-Diabetic Potential of Berberis vulgaris Silver Nanoparticles: A Promising Approach for Natural Therapeutics

This study reports the green synthesis of Berberis vulgaris root water-mediated silver nanoparticles (BvAgNPs) showcasing high purity, size-controlled morphology, and potential anti-diabetic activity. Characterization techniques confirmed the successful synthesis of predominantly spherical BvAgNPs within the 15–70 nm range, coated with organic moieties from the extract. Remarkably, BvAgNPs exhibited significantly enhanced α-amylase and α-glucosidase inhibitory activity compared to the extract alone, with inhibition higher for α-amylase. This superior anti-diabetic activity, even comparable to the standard drug Acarbose for α-amylase inhibition, highlights the potential of BvAgNPs as natural and potentially less-toxic alternatives in diabetes management. Further research on their mechanisms and in vivo efficiency is warranted to pave the way for their future application as promising anti-diabetic therapeutics.

Phytochemical Screening and Antidiabetic Activity of Aqueous Extract of Evolvulus Alsinoides Leaves: An In Vitro and In Silico Study

ABSTRACT Background: Nowadays, diabetes mellitus has become common worldwide due to changes in lifestyle, sedentary life, alterations in food habits, and other genetic and environmental factors. It is necessary to create awareness about the growing pandemic. Aim: To evaluate the antidiabetic potential of Evolvulus alsinoides. Methods: In vitro α-amylase inhibition and α-glucosidase inhibition activity. Molecular docking analysis. Results: The plant is rich in naturally occurring phytocompound. The results of the study showed that E. alsinoides has the potential to inhibit the activity of alpha-amylase and alpha-glucosidase. Moreover, this result was validated using in silico molecular docking studies that showed a good binding affinity of one of the major phytocompound, caffeic acid, with molecules in the insulin signaling cascade. Conclusion: E. alsinoides has a potent antidiabetic activity and can be further employed in animal and human studies.

An Update on Pharmacological and Phytochemical Aspects of Costus pictus D. Don - A Promising Anti-diabetic Plant.

The genus Costus is the largest genus in the family Costaceae and encompasses about 150 known species. Among these, Costus pictus D. Don (Synonym: Costus mexicanus) is a traditional medicinal herb used to treat diabetes and other ailments. Currently, available treatment options in modern medicine have several adverse effects. Herbal medicines are gaining importance as they are cost-effective and display improved therapeutic effects with fewer side effects. Scientists have been seeking therapeutic compounds in plants, and various in vitro and in vivo studies report Costus pictus D. Don as a potential source in treating various diseases. Phytochemicals with various pharmacological properties of Costus pictus D. Don, viz. anticancer, anti-oxidant, diuretic, analgesic, and anti-microbial have been worked out and reported in the literature. The aim of the review is to categorize and summarize the available information on phytochemicals and pharmacological properties of Costus pictus D. Don and suggest outlooks for future research. This review combined scientific data regarding the use of Costus pictus D. Don plant for the management of diabetes and other ailments. A systematic search was performed on Costus pictus plant with anti-diabetic, anti-cancer, anti-microbial, anti-oxidant, and other pharmacological properties using several search engines such as Google Scholar, PubMed, Science Direct, SciFinder, other online journals and books for detailed analysis. Research data compilation and critical review of the information would be beneficial for further exploration of its pharmacological and phytochemical aspects and, consequently, new drug development. Bioactivity-guided fractionation, isolation, and purification of new chemical entities from the plant as well as pharmacological evaluation of the same will lead to the search for safe and effective novel drugs for better healthcare. This review critically summarizes the reports on natural compounds, and different extract of Costus pictus D. Don with their potent anti-diabetic activity along with other pharmacological activity. Since this review has been presented in a very interactive manner showing the geographical region of availability, parts of plant used, mechanism of action and phytoconstituents in different extracts of Costus pictus responsible for particular action, it will be of great importance to the interested readers to focus on the development of the new drug leads for the treatment of diseases.

Evaluation of Antidiabetic Activity and Cytotoxic Effect of Strontium Nanoparticles Synthesized Using Mimosa Pudica

ABSTRACT Nanotechnology is emerging as a promising approach in the development of novel therapeutic strategies. Nanoparticles, due to their unique physicochemical properties and small size, have the potential to improve the delivery of therapeutic agents, enhance their bioavailability, and increase their efficacy. Among various types of nanoparticles, strontium nanoparticles have gained attention due to their potential antidiabetic activity and cytotoxic effects against cancer cells. Mimosa pudica, also known as “Sensitive Plant” or “Touch-Me-Not,” is a medicinal plant known for its diverse pharmacological activities, including antidiabetic and anticancer properties. Recent research has focused on the synthesis of strontium nanoparticles by using Mimosa pudica as a green and sustainable approach. These nanoparticles have shown promising results in terms of their antidiabetic activity and cytotoxic effects against cancer cells. Thus, in this study, the antidiabetic effect was studied using the alpha-amylase inhibitor assay, and the cytotoxic effect was studied using the brine shrimp lethality assay. In these assays, increasing concentration of Mimosa pudica-mediated strontium nanoparticles exhibited increasing antidiabetic and cytotoxic effects, which was similar to the standard used, which is acarbose. Hence, this can be used as a novel antidiabetic and cytotoxic agent in the future.

Efficacy of Quercetin and Kaempferol from Methanolic Extracts of Adiantum lunulatum Burm. F. and Polystichum acrostichoides as Antidiabetic Activity

In present investigation, the aerial parts of two fern species viz. Polystichum acrostichoides (PA) and Adiantum lunulatum (AL) were used to evaluate the potent antidiabetic activity. Methanol solvent was used for extraction by soxhlation method followed by LC-MS analysis to identify the presence of compounds in both the extracts. Further, isolation of the major compounds was carried out and characterized by IR, mass and NMR techniques. Thereafter, in vitro α-amylase inhibitory activity for both the extracts was determined by comparing with acarbose as standard. Thereafter, α-glucosidase inhibition activity followed by glucose uptake was studied using L6 cell line study. Practical yield for both the fern extracts was calculated and observed A. lunulatum extract showed more yield (7 g) than P. acrostichoides (3 g). Based on the analytical data, isolated compound was identified as quercetin and kaempferol from the A. lunulatum and P. acrostichoides extracts, respectively. A. lunulatum extract even showed better dose dependent α-amylase inhibition and α-glucosidase inhibition activity than P. acrostichoides furthermore, L6 cell line study showed increased glucose uptake by A. lunulatum extract than P. acrostichoides extract when compared with standard insulin. Based on the findings, it appears that the both A. lunulatum and P. acrostichoides have the potential to be used as antidiabetic drugs due to presence of major isolated flavonoids i.e. quercetin and kaempferol as among the bioactive compounds. Antidiabetic efficacy was dosage dependent and A. lunulatum extract was more effective in inhibiting glucose uptake than P. acrostichoides extract.

Oral glucose tolerance assay of extract from Mangifera foetida l. and Pandanus amaryllifolius roxb. leaves

This study examines the potential antidiabetic activity of a combination of Mangifera foetida L. and Pandanus amaryllifolius Roxb. leaves. Mangifera leaves contain a compound called mangiferin, which acts as an antidiabetic and antioxidant. On the other hand, Pandanus leaves, are rich in terpenoids and steroids that also possess anti-diabetic effects. An Oral Glucose Tolerance Test (OGTT) was conducted on male mice of the Babl/c strain to assess the antidiabetic effects. The test involved administering a combination of ethanolic leaf extracts from Mangifera foetida L. and Pandanus amaryllifolius Roxb. in a 1:1 ratio. The study followed a pre-test design with a control group, comprising six treatment groups, each consisting of four male mice. The groups were described as follows: Group 1 was served as the normal group without any treatment. Groups II-IV received single extracts or combinations of extracts at doses of 62.5 mg/200g BW, 125 mg/200g BW, and 250 mg/200g BW. Group V acted as the positive control and was given oral glucose and glibenclamide at a dose of 0.09 mg/200g BW. Group VI was served as the negative control, receiving oral glucose and distilled water. The group that exhibited the highest percentage of decreased blood sugar levels was the one given oral glucose at a dose of 0.078g/20g BW of mice, along with the combination of Mangifera foetida L. and Pandanus amaryllifolius Roxb. leaves extract (1:1) at a dose of 35 mg/20g BW. This group demonstrated a decrease of 71.985 ± 4.858 in blood glucose levels. The ANOVA analysis confirmed that the percentage decrease in blood sugar levels was significantly different from the positive control, indicating a higher effectiveness of the combination treatment in reducing blood glucose levels than the positive control.

Potential Antidiabetic Activity of Apis mellifera Propolis Extraction Obtained with Ultrasound.

Recent studies have linked phenolic compounds to the inhibition of digestive enzymes. Propolis extract is consumed or applied as a traditional treatment for some diseases. More than 500 chemical compounds have been identified in propolis composition worldwide. This research aimed to determine Mexican propolis extracts' total phenolic content, total flavonoid content, antioxidant activity, and digestive enzyme inhibitory activity (ɑ-amylase and ɑ-glucosidase). In vitro assays measured the possible effect on bioactive compounds after digestion. Four samples of propolis from different regions of the state of Oaxaca (Mexico) were tested (Eloxochitlán (PE), Teotitlán (PT), San Pedro (PSP), and San Jerónimo (PSJ)). Ethanol extractions were performed using ultrasound. The extract with the highest phenolic content was PE with 15,362.4 ± 225 mg GAE/100 g. Regarding the flavonoid content, the highest amount was found in PT with 8084.6 ± 19 mg QE/100 g. ABTS•+ and DPPH• radicals were evaluated. The extract with the best inhibition concentration was PE with 33,307.1 ± 567 mg ET/100 g. After simulated digestion, phenolics, flavonoids, and antioxidant activity decreased by 96%. In contrast, antidiabetic activity, quantified as inhibition of ɑ-amylase and ɑ-glucosidase, showed a mean decrease in enzyme activity of approximately 50% after the intestinal phase. Therefore, it is concluded that propolis extracts could be a natural alternative for treating diabetes, and it would be necessary to develop a protective mechanism to incorporate them into foods.

Identification and molecular docking of a novel antidiabetic peptide from protamex-camel milk protein hydrolysates against α-amylase and DPP-IV

Antidiabetic peptides were identified from camel milk protein hydrolysates, and their inhibitory activities against α-amylase and dipeptidyl peptidase-IV (DPP-IV) were determined. The possible binding mechanism between the enzymes and the peptide was elucidated through molecular docking. Camel milk proteins were hydrolyzed using protamex, and the hydrolysates were divided into three fractions (>10, 3–10, and <3 kDa) through ultrafiltration. Fraction <3 kDa was more effective at inhibiting α-amylase and DPP-IV and was purified through gel chromatography and identified through LC-MS/MS. In total, 20 peptides were considered as potential bioactive peptides, mainly derived from β-casein. The novel peptide QEPVPDPVRGL exhibited the most potent antidiabetic activity and spontaneously interacted with α-amylase and DPP-IV through hydrogen bonds, salt bridges, and pi–alkyl, thereby occupying their active cavities. This study indicated that camel milk protein hydrolysates are good sources of peptides with antidiabetic potential.

Design, Synthesis, and Molecular Docking Studies of Integrated Benzylidenethiazolidine‐2,4‐Dione and Thieno[2,3‐d]pyrimidine‐6‐Carboxylate Derivatives as Potent Antidiabetic agents

AbstractThe present work describes the synthesis of new series of 5‐arylidene‐thiazolidine‐2,4‐dione, thieno[2,3‐d]pyrimidine‐6‐carboxylate derivatives 9 a–o. A variety of spectroscopic techniques like IR, 13CNMR, 1HNMR and LCMS were used to establish the presence of the every synthesized scaffold. The antioxidant activity of the target compounds has been studied by three different methods indicated the significant DPPH, NO and H2O2. Further, all the derivatives were evaluated for the in vitro antidiabetic potential against human pancreatic α‐amylase (PDB ID: 5NN3) and human lysosomal acid α‐glucosidase (PDB ID: 2QV4) enzymes followed by Molecular docking studies to ascertain the binding interactions of the compounds with the enzymes. The compounds 9 b and 9 g containing methoxy groups were found to exhibit potent antidiabetic and antioxidant activity. Therefore, it was rationalized that two privileged pharmacophores i. e. aryledenethiazolidine‐2,4‐dione and thieno[2,3‐d]pyrimidine‐6‐carboxylate assimilated hybrids, may be beneficial as lead template for the advance of future anti‐diabetic agents. Thus, benzylidenethiazolidine‐2,4‐dione and thieno[2,3‐d], the two preferred pharmacophores, were rationalized. Assimilation of ‐pyrimidine‐6‐carboxylate hybrids could be advantageous as a lead template for the development of new anti‐diabetic drugs.

Dioscorea alata L. Tubers Ethanol Extract Improves Insulin Resistance and Estrogen Defectively in Type 2 Diabetic Ovariectomized Rats

Dioscorea alata L., commonly known as water yam, has attracted the attention of scientific researchers for its potential anti-diabetic and estrogenic properties. However, the existing literature lacks specific studies on the anti-diabetic and estrogenic effects of D. alata in the context of type 2 diabetic ovariectomized rats. Thus, Our research focuses on investigating the influence of D. alata on the antidiabetic and estrogenic properties in rats. These rats have developed diabetes through a high-fat diet and streptozotocin induction and have also undergone ovariectomy, making them type 2 diabetic ovariectomized rats (T2DM OVX). This comprehensive study both in vitro and in vivo methodologies. We conducted a phytochemical analysis, revealing the presence of key bioactive constituents, including flavonoids, alkaloids, terpenoids, tannins, saponins, cardiac glycosides, and steroids. The results of our phytochemical screening confirm the remarkable antidiabetic properties of the D. alata extract, as it effectively inhibits α-glucosidase activity, leading to a significant reduction in fasting blood glucose levels. Additionally, it enhances body weight, serum insulin levels, and pancreatic islet size. The extract also demonstrates notable estrogenic effects by significantly increasing uterine wet weight, endometrial and myometrium thickness, bone calcium, and overall bone density, while reducing bone porosity in the T2DM OVX rats. It is important to note that while the D. alata extract exhibits slightly less potent α-glucosidase inhibition compared to acarbose, it showcases potent antidiabetic activity at a dose of 1,000 mg/kg body weight, comparable to Metformin (250 mg/kg body weight). In terms of estrogenic activity, it is slightly less potent than 17β-estradiol (1 mg/kg body weight). These findings provide robust evidence supporting the traditional use of D. alata and its efficacy in the context of antidiabetic and estrogenic properties within the T2DM OVX model.

Determination of antioxidant, antimicrobial, anticholinesterase, antityrosinase, antidiabetic and antiglaucoma activities of essential oils from three different Thymus species and their chemical characterization by GC-MS analysis

The present study aims to perform a comprehensive chemical characterization of the essential oils of Thymus pubescens var. pubescens (TPEO), Thymus leucotrichus var. leucotrichus (TLEO), and the endemic Thymus canoviridis (TCEO) using GC-MS, besides evaluating the potential antidiabetic, anticholinesterase, antimicrobial, antioxidant, antiglocouma, and antityrosinase activities of these essential oils. The antioxidant activity was assessed using various bioassays including DPPH, ABTS, DMPD, FRAP, CUPRAC, and Fe3+ reducing assays. The IC50 values of TPEO, TLEO, and TCEO for α-glycosidase were 28.32, 28.79, and 57.57 μg/mL, respectively. For tyrosinase, the IC50 values were 359.9, 270.87, and 597.43 μg/mL, respectively. The IC50 values for acetylcholinesterase were calculated as 44.15, 36.75, and 34.99 μg/mL, respectively, while for carbonic anhydrase, the IC50 values were 21.70, 24.75, and 24.45 μg/mL, respectively. The quantitiy of total phenolics present in TPEO, TLEO, and TCEO were determined to be 10.50, 34.50, and 32.50 μg GAE/mg essential oil, respectively. The TPEO, TLEO, and TCEO exhibited distinct antioxidant activities on DPPH, ABTS, and DMPD. TPEO showed antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Acinetobacter baumannii bacterias. TLEO exhibited effective antimicrobial activity against S. aureus; The last of these TCEO demonstrated notable antimicrobial activity towards S. aureus, Enterococcus faecalis, E. coli, K. pneumoniae, Pseudomonas aeruginosa, P. mirabilis, A. baumannii. Additionaly, GC-MS revealed that the major components are TPEO (pulegone 29.01%, piperitenone 17.17%), TLEO (germacrene D 9.59%), and TCEO (carvacrol 52.87%). The essential oils possessed a range of biological activities, including antioxidant, antidiabetic, anticholinesterase, antityrosinase, antiglocouma and antimicrobial activities.

BAAE-AgNPs Improve Symptoms of Diabetes in STZ-induced Diabetic Rats.

Nanoparticles can be employed to improve the therapeutic activity of natural products. Type 2 diabetes mellitus is a serious health condition that has spread like a "modern pandemic" worldwide. In the present study, we developed silver nanoparticles, AgNPs, with an aqueous extract from Balanites aegyptiaca to investigate their antioxidant and anti-inflammatory activity in STZ-induced diabetic rats. Aqueous extracts of Balanites aegyptiaca seeds (BAAE) were used in the synthesis of BAAE-AgNPs, which were characterized using FTIR and TEM. Different doses of BAAE-AgNP (1/50 LD50; 29.4 mg/kg b.w. and 1/20 LD50:73.5 mg/kg b.w.) were administered to STZ-induced diabetic rats to evaluate their potential antidiabetic activity. FTIR spectral data indicated the presence of flavonoids and polyphenols in BAAE-AgNPs. The size of the BAAE-AgNPs, determined by TEM examination, was 49.33 ± 7.59 nm, with a zeta potential of +25.37. BAAE-AgNPs were characterized by an LD50 value of 1470 mg/kg b.w. In diabetic rats, the daily oral administration of both doses of BAAE-AgNPs (29.4 and 73.5 mg/kg b.w.) for 12 weeks resulted in a significant improvement in body weight, insulin homeostasis, HbA1c, HDL-C, MDA, and pancreatic SOD, CAT, and GSH. They reduced plasma glucose, cholesterol, and triglycerides. This treatment also resulted in a significant decrease in pancreatic IL-6, P53, and TNF-α in diabetic rats. Furthermore, BAAE-AgNPs down-regulated pancreatic TGF-β1 and Akt gene expression in diabetic rats and resulted in a significant decrease in the regulation of hepatic GLUT-2, as well as an increase in the regulation of hepatic GK and pancreatic B-cl2 gene expression. The histopathological results obtained indicated that BAAE-AgNPs improved pancreatic tissue metabolism by enhancing antioxidant enzymes, suppressing inflammatory cytokines, and scavenging free radicals. The findings implied that similar to the glibenclamide-treated groups, in the BAAE-AgNPs treated group, the compromised antioxidant status normalized in STZ-induced diabetes. By scavenging free radicals, BAAE-AgNPs protected against lipid peroxidation while reducing the risk of complications from diabetes. Compared to the daily dose of 29.4 mg, the impact was more prominent at 73.5 mg.

Green synthesis and evaluation of anti-microbial, antioxidant, anti-inflammatory, and anti-diabetic activities of silver nanoparticles from Argyreia nervosa leaf extract: An invitro study

The aim of the study is to develop an environmentally friendly development of isolating silver nanoparticles using Argyreia nervosa plant leaves and examine their potential pharmacological properties, including antibacterial, anti-inflammatory, antioxidant, and anti-diabetic activities. Various analytical techniques were employed to examine the isolated silver nanoparticles, encompassing UV spectroscopy, XRD, SEM, EDX, FTIR, zeta potential measurement, and particle size determination. Furthermore, Argyreia nervosa-mediated silver nanoparticles exhibited strong antioxidant, anti-inflammatory activity, and good anti-diabetic activity. Argyreia nervosa-mediated nanoparticles showed a significant antibacterial activity against selected pathogens. The findings indicate that Argyreia nervosa demonstrates encouraging pharmacological properties. However, additional in vivo research focusing on molecular-level investigations is necessary to substantiate these findings and explore the potential of Argyreia nervosa-mediated silver nanoparticles as a viable drug for antioxidant, antibacterial, and anti-diabetic purposes.

Bioactive potential of ripened white cheeses manufactured in different geographical regions of Turkey.

This study investigated the potential bioactive properties of white cheeses produced in different regions of Turkey, including their potential antioxidant, antihypertensive, antidiabetic, antimicrobial, and anticancer activities. The cheese samples were analyzed both before and after in vitro digestion. The study found that all cheese samples exhibited significant angiotensin-converting enzyme inhibition activity both before (45.5%-70.1% for 0.03gcheese/mL) and after in vitro digestion (25.5%-63.5% for 0.0167g cheese/mL), whereas α-amylase inhibition activity was present in all samples (in the range of 5.1%-50.0% for 3.0×10-5 gcheese/mL) but disappeared after digestion, and α-glucosidase inhibition activity was only detected after in vitro digestion (from 20.5% to 60.4% for 5.6×10-5 gcheese/mL), indicating potential antidiabetic properties. However, antimicrobial and anticancer activities were not observed in any of the samples. The results also suggest that the bioactivity potential of white cheese may vary depending on the region of production, as cheeses from the Marmara region exhibited high α-glucosidase inhibition activity after digestion. In conclusion, while white cheese is a valuable addition to the diet due to its high nutritional value and potential health benefits. This study revealed the bioactive potential of ripened white cheese and in vivo investigations of the cheese components would better show their possible benefits. PRACTICAL APPLICATION: Although the bioactivity potentials varied among the ripened white cheese samples produced in different regions of Turkey, a consistent trend was observed in terms of their presence or absence. Our research revealed that all ripened cheese samples demonstrated significant potential antioxidant and antihypertensive activities, as well as potential antidiabetic properties. Moreover, it can be interpreted that ripened white cheese has the potential to reduce the digestion of carbohydrates when consumed with carbohydrate-rich foods. Although the present results provide limited practical findings directly applicable to the industry, if the data and information obtained from this study are further explored and further studies delving into specific mechanisms of bioactive components could emerge.