Cyclopeptide alkaloids from the Greek shrub Paliurus spina-christi and their in silico binding affinity to Dipeptidyl Peptidase IV.

A new cyclopeptide alkaloid, spinachristene A (1), along with two previously described, sanjoinenine (2) and oxyphylline C (3), were isolated from the fruits of Paliurus spina-christi Mill. All three metabolites are being isolated for the first time from the genus Paliurus. A model for the in silico binding affinity of compounds 1-3 to Dipeptidyl Peptidase IV (DPP4), which is related to type 2 diabetes (T2D), was developed. According to our model, compounds 1-3 were ranked in positions 9/12, 11/12 and 8/12, respectively and are predicted to exhibit significant affinity to DPP4, in the range of low 2-digit µΜ.

Exploring the potential of semi-synthetic Swertiamarin analogues for GLUT facilitation and insulin secretion in NIT-1 cell lines: a molecular docking and in-vitro study.

Synthesis, characterisation, and anti-diabetic potential of swertiamarin analogues against DPP-4 enzymatic inhibition was done prior to this study. However, swertiamarin and its analogues inhibited DPP-4 enzyme significantly. Semisynthetic swertiamarin analogues have been studied for antidiabetic potential and mechanism of action utilising molecular docking and in-vitro techniques. The mechanism of action for swertiamarin analogues was determined by in-silico molecular docking studies using glucose-transporters, GLUT-1 (PDB ID: 4PYP), GLUT-3 (PDB ID: 7SPS), and GLUT-4 (PDB ID: 7WSM) along with in-vitro glucose uptake and glucose-induced insulin secretion assays. These studies found that synthesised swertiamarin analogues SNIPERSV3, SNIPERSV4, and SNIPERSV7 shown better docking score against different GLUTs and better anti-diabetic effects on glucose uptake and insulin secretion in NIT-1 cell line than standard glibenclamide and swertiamarin. Thus, swertiamarin analogues might be studied for diabetes therapy in the future.

Aloe juvenna Brandham & S.Carter as α-Amylase Inhibitor and Hypoglycaemic Agent with Anti-inflammatory Properties for Diabetes Management.

Despite Aloe's traditional use, Aloe juvenna Brandham & S.Carter is poorly characterized. Other Aloes are known for their antidiabetic activity. This study describes the antidiabetic potentials and phytoconstituents of the A. juvenna leaves methanolic extract (AJME). Twenty-six phytoconstituents of AJME were described using HPLC/MS-MS. Lupeol and vitexin were isolated using column chromatography. The antidiabetic activity of AJME was investigated using an in vivo high-fat diet/streptozotocin-induced diabetic rat model and in vitro α-glucosidase and α-amylase inhibitory activity assays. AJME demonstrated its α-amylase inhibitory activity (IC50=313±39.9 ppm) with no effect on α-glucosidase. In vivo, AJME dose-dependently improved hyperglycaemia in a high-fat diet/streptozotocin-induced diabetic rat model. Notably, the higher dose (1600 mg/kg) of AJME significantly downregulated serum interleukin-6, tumor necrosis factor-α, and matrix metalloproteinase-1 genes, suggesting its anti-inflammatory effect. These findings indicate AJME's potential as a significant antidiabetic agent through its α-amylase inhibition, hypoglycaemic, and anti-inflammatory properties.

Synthesis, Computational Study, and In Vitro α-Glucosidase Inhibitory Action of 1,3,4-Thiadiazole Derivatives of 3-Aminopyridin-2(1H)-ones.

This article reports on the synthesis of nine promising new 1,3,4-thiadiazole derivatives based on 3-aminopyridones, containing various acidic linkers. The synthesis was carried out by cyclizing the corresponding thiohydrazides 4a-c and anhydrides of glutaric, maleic, and phthalic acids upon heating in acetic acid solution. The conducted bio-screening of the synthesized new 1,3,4-thiadiazole derivatives containing different acidic linkers (butanoic, acrylic, and benzoic acids) showed that they have significant inhibitory activity against α-glucosidase (up to 95.0%), which is 1.9 times higher than the value for the reference drug acarbose (49.5%). Moreover, one of the 1,3,4-thiadiazole derivatives with a benzoic acid linker-2-(5-((6-Methyl-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridin-3-yl)carbamoyl)-1,3,4-thiadiazol-2-yl)benzoic acid (9'b)-showed an IC50 value of 3.66 mM, nearly 3.7 times lower than that of acarbose (IC50 = 13.88 mM). High inhibitory activity was also shown by 1,3,4-thiadiazole derivatives with a butanoic acid linker (compounds 7b, 7c)-with IC50 values of 6.70 and 8.42 mM, respectively. A correlation between the structure of the compounds and their activity was also established. The results of molecular docking correlated well with the bioanalytical data. In particular, the presence of a butanoic acid linker and a benzoic fragment in compounds 7b, 7c, and 9b increased their binding affinity with selected target proteins compared to other derivatives 3-6 (a-c). Calculations according to Lipinski's rule of five also showed that the synthesized compounds 7b, 7c, and 9b fully comply with Ro5 and meet all criteria for good permeability and acceptable oral bioavailability of potential drugs. These positive bioanalytical results will stimulate further in-depth studies, including in vivo models.

Phytochemical Profiling and Assessment of Antidiabetic Activity of Curcuma Angustifolia Rhizome Methanolic Extract: an In Vitro and In Silico Analysis.

Curcuma angustifolia Roxb. is a plant with medicinal potential, traditionally used to treat different diseases. The present study aimed to determine the antidiabetic activity of C. angustifolia rhizome in vitro and in silico. The methanolic extract of C. angustifolia rhizome was analyzed by FTIR and GC-MS to determine the phytochemicals present. The antidiabetic potential of the extract was evaluated by different assays in vitro. The extract inhibited both α-amylase and α-glucosidase enzymes and the glucose diffusion through the dialysis membrane in a concentration-dependent manner with IC50 values of 530.39±0.09, 293.75±0.11, and 551.74±0.3 µg/ml respectively. The methanolic extract also improved yeast cell's ability to take up glucose across plasma membranes and the adsorption of glucose. The findings were supported by molecular docking studies. The results showed that the methanol extract of C. angustifolia rhizome has significant antidiabetic activity and thus can be also studied to isolate the potential compound with antidiabetic activities.

Synthesis of Silver Nanoparticles Using Camellia sinensis Leaf Extract: Promising Particles for the Treatment of Cancer and Diabetes.

Both diabetes and cancer pose significant threats to public health. To overcome these challenges, nanobiotechnology offers innovative solutions for the treatment of these diseases. However, the synthesis of nanoparticles can be complex, costly and environmentally toxic. Therefore, in this study, we successfully synthesized Camellia sinensis silver nanoparticles (CS-AgNPs) biologically from methanolic leaf extract of C. sinensis and as confirmed by the visual appearance which exhibited strong absorption at 456 nm in UV-visible spectroscopy. The fourier transform infrared spectroscopy (FTIR) analysis revealed that phytochemicals of C. sinensis were coated with AgNPs. Scanning electron microscopy (SEM) analysis showed the spherical shape of CS-AgNPs, with a size of 15.954 nm, while X-ray diffraction spectrometry (XRD) analysis detected a size of 20.32 nm. Thermogravimetric analysis (TGA) indicated the thermal stability of CS-AgNPs. The synthesized CS-AgNPs significantly inhibited the ehrlich ascites carcinoma (EAC) cell growth with 53.42±1.101 %. The EAC cell line induced mice exhibited increased level of the serum aspartate aminotransferase (AST), alanine transaminase (ALT), and alkaline phosphatase (ALP), however this elevated serum parameter significantly reduced and controlled by the treatment with CS-AgNPs. Moreover, in a streptozotocin-induced diabetic mice model, CS-AgNPs greatly reduced blood glucose, total cholesterol, triglyceride, low-density lipoprotein (LDL) and creatinine levels. These findings highlight that the synthesized CS-AgNPs have significant anticancer and antidiabetic activities that could be used as promising particles for the treatment of these major diseases. However, pre-clinical and clinical trial should be addressed before use this particles as therapeutics agents.

Assessment of antimicrobial, antidiabetic, and anti-inflammatory properties of acetone extract of Aerva lanata (L.) by in-vitro approach and bioactive compounds characterization.

The antimicrobial, antidiabetic, and anti-inflammatory activities efficiency of Aerva lanata plant extracts (aqueous (Aqu-E), acetone (Ace-E), and ethanol (Eth-E)) were investigated in this study. Furthermore, the active molecules exist in the crude extract were characterized by UV-Visible spectrophotometer, Fourier transform infrared (FTIR), High-performance liquid chromatography (HPLC), and Gas Chromatography-Mass Spectrometry (GC-MS) analyses. The preliminary phytochemical study revealed that the Ace-E restrain more phytochemicals like alkaloids, saponins, anthraquinone, tannins, phenolics, flavonoids, glycosides, terpenoids, amino acid, steroids, protein, coumarin, as well as quinine than Aqu-E and Eth-E. Accordingly to this Ace-E showed considerable antimicrobial activity as the follows: for bacteria S. aureus > E. coli > K. pneumoniae > P. aeruginosa > B. subtilis and for fungi T. viride > A.flavus > C. albicans > A.niger at 30 mg ml concentration. Similarly, Ace-E showed considerable antidiabetic (α-amylase: 71.7 % and α-glucosidase: 70.1 %) and moderate anti-inflammatory (59 % and 49.8 %) activities. The spectral and chromatogram studies confirmed that the Ace-E have pharmaceutically valuable bioactive molecules such as (Nbutyl)-octadecane, propynoic acid, neophytadiene, and 5,14-di (N-butyl)-octadecane. These findings suggest that Ace-E from A. lanata can be used to purify additional bioactive substances and conduct individual compound-based biomedical application research.

Secondary metabolites from Scindapsus officinalis (Roxb.) Schott. with in vitro antidiabetic activities.

One new phenolic cyclobutantetraol ester united chromone glycoside (1), one new amide (2), and three new phenyl ethanol glycosides (3-5) were obtained from the water extract of Scindapsus officinalis (Roxb.) Schott, in which compound 1 was the first reported structure incorporating the phenolic cyclobutantetraol ester and chromone via the glucose phenolic metabolites in nature. Structures of the isolated compounds, including absolute configurations, were elucidated according to the analysis of HRESIMS, NMR, ECD and BLYP/6-31G* geometry optimization calculations of 13C NMR data. All isolates (1-5) were evaluated for the antidiabetic activity by the insulin resistance (IR) model and anti-inflammatory activity against NO production in vitro. Compounds 1-3 showed strong antidiabetic activities, greatly promoting the glucose consumption in the insulin resistance HepG2 cells compared with the model group, however, 1-5 showed weak anti-inflammatory activities.

Argan: Phytochemical profiling and evaluation of the antioxidant, hypoglycemic, and antibacterial properties of its fruit pulp extracts.

Herein, we isolated three triterpenoid saponins from the methanol extract of the fruit pulp of argan. The structures of the identified compounds were determined using comprehensive NMR spectroscopy analyses (1H, 13C NMR, COSY, TOCSY, ROESY, and HSQC), combined with mass spectroscopy. Gas chromatography (GC) was utilized to determine the monosaccharide contents after the samples underwent methanolysis and their glycoside configuration was proved via their trimethylsilyl derivatives. Furthermore, the methanol extract of the fruit pulp and its n-butanol fraction were evaluated for their antioxidant properties via DPPH, ABTS, and FRAP assays, antidiabetic activity using α-amylase and α-glucosidase inhibition activities, and antibacterial properties utilizing microdilution and antibiofilm assays. Compared to the crude methanol extract, our results showed that the n-butanol fraction exhibited more potent antioxidant activity and antibacterial potential against Staphylococcus aureus, Escherichia coli, Salmonella typhi, Enterococcus faecalis, and Pseudomonas aeruginosa (MIC = 12.5-50 mg/mL); while no effect on the bacterial biofilm was observed. The methanol extract was more effective in inhibiting α-glucosidase (EC50 = 0.15 mg/mL), however, the n-butanol fraction elicited strong α-amylase inhibition (EC50 = 0.49 mg/mL). These findings suggest that the fruit pulp of argan could serve as a potential source of phytochemicals suitable for the treatment of diabetes and its related complications.

Preparation of bio-synthesized Ag nanoparticles and assessment of their antidiabetic and antioxidant potential against STZ-induced diabetic albino rats.

Bio-synthesized silver nanoparticles (AgNPs) were successfully obtained using the leaf extract from Ventilago maderaspatana. Extensive analysis was conducted to evaluate the physical and chemical characteristics of the bioderived AgNPs. XRD analysis confirmed their cubic structure, and revealed a well-defined size distribution with average crystallite size of 11.7 nm. FE-SEM and TEM images visually supported the observed size range. The presence of plant-mediated phytochemicals on the surface of AgNPs was confirmed through DLS, FTIR, and TGA/DTA studies. To assess their antidiabetic potential, rats were induced with streptozotocin, resulting in elevated levels of biochemical parameters associated with diabetes. Conversely, serum insulin levels (2.50 ± 0.55) and glucokinase activity (64.50 ± 8.66) decreased. However, treatment with AgNPs demonstrated a dose-dependent reduction in blood glucose, total protein, albumin, and HbA1c levels, effectively restoring them to normal ranges. Moreover, the treatment significantly increased insulin levels (7.55 ± 0.63) and glucokinase activity (121.50 ± 4.60), indicating the antidiabetic potential of V. maderaspatana-mediated AgNPs. Notably, the exitance of phytochemicals, like flavonoids and phenols, on the surface of AgNPs facilitated their ability to neutralize reactive oxygen species (ROS) through electron donation. This property enhanced their overall antidiabetic efficiency.

Investigation of Phytochemical, Antioxidant and Antidiabetic Potentials of Scabiosa L. (Caprifoliaceae) Species with Chemometric Methods.

In this research, the total phenolic and flavonoid amounts, phenolic compositions, in vitro antioxidant, antibacterial and antidiabetic properties of the methanol extracts obtained from Scabiosa L. (Caprifoliaceae) species distributed in the flora of Türkiye were investigated using chemometric methods. For this purpose, principal component (PCA) and agglomerative hierarchical clustering analysis were performed as chemometric methods. Chlorogenic acid, quinic acid and cyranoside were determined in the extracts. According to chemometric analysis, S. columbaria subsp. ochroleuca var. ochroleuca and S. triniifolia species were found to be valuable in terms of methanol extract yields, total phenolic and flavonoid contents, antioxidant and antidiabetic activities while S. columbaria subsp. ochroleuca var. webbiana species were found to be valuable in terms of phenolic composition. The methanol extracts of Scabiosa species showed high antioxidant activity, with high phenolic and flavonoid contents. Among the tested 13 bacteria, Scabiosa extracts showed only low activity against Klebsiella pneumoniae, Streptococcus pneumoniae and Pseudomonas aeruginosa. The extracts showed high α-amylase and α-glucosidase inhibitory activity. The results show that Scabiosa methanol extracts may be a source of alternative antioxidants that may be beneficial in slowing or preventing the progression of various oxidative stress-related diseases.

Synthesis and bioactivity assessment of Coccinia grandis L. extract encapsulated alginate nanoparticles as an antidiabetic drug lead.

AIM: This study aimed to prepare, characterise, and evaluate the antidiabetic activity of Coccinia grandis (L.) extracts encapsulated alginate nanoparticles. METHODS: Alginate nanoparticles were prepared using the ionic gelation method and characterised by encapsulation efficiency %w/w, loading capacity %w/w, particle size analysis, zeta potential, Fourier transform infra-red spectroscopy (FTIR), and scanning electron microscopy (SEM). In vitro antidiabetic activity was also evaluated. RESULTS: Encapsulation efficiency %w/w, loading capacity %w/w, mean diameter, zeta potential of C. grandis encapsulated alginate nanoparticles ranged from 10.51 ± 0.51 to 62.01 ± 1.28%w/w, 0.39 ± 0.04 to 3.12 ± 0.11%w/w, 191.9 ± 76.7 to 298.9 ± 89.6 nm, -21.3 ± 3.3 to -28.4 ± 3.4 mV, respectively. SEM and FTIR confirmed that particles were in nano range with spherical shape and successful encapsulation of plant extracts into an alginate matrix. The antidiabetic potential of aqueous extract of C. grandis encapsulated alginate nanoparticles (AqCG-ANP) exhibited inhibition in α-amylase, α-glucosidase and dipeptidyl peptidase IV enzymes of 60.8%c/c, 19.1%c/c, and 30.3%c/c, respectively, compared to the AqCG. CONCLUSION: The AqCG-ANP exerted promising antidiabetic potential as an antidiabetic drug lead.

New Dipterocarpol-Based Molecules with α-Glucosidase Inhibitory and Hypoglycemic Activity.

Dammarane triterpenoids are affordable and bioactive natural metabolites with great structural potential, which makes them attractive sources for drug development. The aim of the study was to investigate the potency of new dipterocarpol derivatives for the treatment of diabetes. Two dammaranes (dipterocarpol and its 20(24)-diene derivative) were modified by a Claisen-Schmidt aldol condensation to afford C2(E)-arylidenes in good yields. The majority of the synthesized compounds exhibited an excellent-to-moderate inhibitory effect toward α-glucosidase (from S. saccharomyces), among them eight compounds showed IC50 values less than 10 µM. 3-Oxo-dammarane-2(E)-benzylidenes (holding p-hydroxy- 3 l and p-carbonyl- 3 m substituents) demonstrated the most potent α-glucosidase inhibition with IC50 0.753 and 0.204 µM, being 232- and 857-times more active than acarbose (IC50 174.90 µM), and a high level of NO inhibition in Raw 264.7 cells with IC50 of 1.75 and 4.57 µM, respectively. An in vivo testing of compound 3 m (in a dose of 20 mg/kg) on a model of streptozotocin-induced T1DM in rats showed a pronounced hypoglycemic activity, the ability to reduce effectively the processes of lipid peroxidation in liver tissue and decrease the excretion of glucose and pyruvic acid in the urine. Compound 3 m reduced the death of diabetic rats and preserved their motor activity.

Synthesis and biological evaluation of indole derivatives containing thiazolidine-2,4-dione as α-glucosidase inhibitors with antidiabetic activity.

In order to develop potential α-glucosidase inhibitors with antidiabetic activity, twenty-six indole derivatives containing thiazolidine-2,4-dione were synthesized. All compounds presented potential α-glucosidase inhibitory activities with IC50 values ranging from 2.35 ± 0.11 to 24.36 ± 0.79 µM, respectively compared to acarbose (IC50 = 575.02 ± 10.11 µM). Especially, compound IT4 displayed the strongest α-glucosidase inhibitory activity (IC50 = 2.35 ± 0.11 µM). The inhibition mechanism of compound IT4 on α-glucosidase was clarified by the investigation of kinetics studies, fluorescence quenching, CD spectra, 3D fluorescence spectra, and molecular docking. In vivo antidiabetic experiments demonstrated that oral administration of compound IT4 would suppress fasting blood glucose level and ameliorate their glucose tolerance and dyslipidemia in diabetic mice.

Identification and characterization of major bioactive compounds from Andrographis paniculata (Burm. f.) extracts showed multi-biomedical applications.

The Andrographis paniculata recognized as most valuable medicinal plant in folk medicine. Hence, this research was designed to evaluate antibacterial potential of petroleum ether (PE) and methanol (ME) extracts of A. paniculata against skin infection causing bacterial pathogens such as Staphylococcus aureus, Streptococcus pyogenes, Klebsiella pneumoniae, Enterobacter aerogenes, Proteus vulgaris, and Propionibacterium acnes. Also assessed the antidiabetic (α-glucosidase and α-amylase inhibition assay), antioxidant, and photoprotective potential of PE and ME extract analyses. The major bioactive compounds were identified and characterized through UV, FTIR, 1H-NMR and 13C-NMR spectra analyses. The ME extract contain more number of phytochemicals (alkaloids, flavonoids, saponins, terpenoids, glycoside, protein, and phytosterol) than PE extract. The antibacterial activity result also revealed that the ME (as dose dependent) extract showed better activity at 250 mg mL-1 as in the following order: P. acnes (6-29 mm) > K. pneumoniae (3-28 mm) > S. aureus (3-27 mm) > P. vulgaris (3-26 mm) > S. pyogenes (2-25 mm) > E. aerogenes (1-23 mm). PE: E. aerogenes (3-20 mm) > P. vulgaris (2-19 mm) > P. acnes (3-18 mm) > K. pneumoniae (3-17 mm) > S. aureus (2-16 mm) > S. pyogenes (0-11 mm). The MIC value of ME extract was found as 100-150 mg mL-1 and it was better than PE extract. Similarly, the ME also possesses dose based α-glucosidase inhibition activity as up to 85% at 250 mg mL-1 concentration. The fluorescence spectra analysis method also stated that the ME extract possess photoprotective bioactive agent. The ME fractions (F01 and F02) obtained from TLC and column chromatogram were identified as 3-O-ß-d-glucosyl-14- deoxyandrographiside and 14-deoxyandrographolide respectively through UV, FTIR, 1H-NMR and 13C-NMR spectra analyses. Such compounds may be responsible for significant antibacterial activity against pathogenic bacteria causing skin infections, excellent antidiabetic activity, as well as photoprotective potential.

Profiling of secondary metabolite and evaluation of anti-diabetic potency of Crotalaria quinquefolia (L): In-vitro, in-vivo, and in-silico approaches.

Traditional medicinal plants have played a promising role in the human health system. In folklore medicine, Crotalaria quinquefolia L. is used to treat fever, pain, eczema, impetigo, lung infections, scabies. The present investigation was executed to identify secondary metabolites responsible for anti-diabetic potential of C. quinquefolia L. leaf extract along with their possible mechanistic pathways. The anti-hyperglycemic activity was assessed by in vitro α-amylase and α-glucosidase inhibitory assays and an in vivo oral glucose tolerance test and diabetogenic effect of streptozotocin in mice, followed by an integrative computational analysis. A total of 23 compounds were identified through GCMS and HPLC. The extract showed potent in-vitro α-amylase and α-glucosidase suppressive activity with IC50 values of 12.8 ± 0.1 µg/mL and 36.3 ± 0.07 µg/mL, respectively. In an in vivo oral glucose tolerance test, the extract (400 mg/kg body weight) prompted blood glucose levels to plummet by 18.9 % after 30 min, compared to the normal control and streptozotocin induced diabetes test, maximum glucose reduction was observed 11.67 % by dose of 200 mg/kg compared to the control; glibenclamide and extract (400 mg/kg) reduced blood glucose levels by 1.3 % and 16.7 %, respectively, compared to diabetic control at the end of the trial. Additionally, among the identified compounds, myricetin, quercetin, rutin, and kaempferol revealed good binding affinity as well as stability with the studied anti-diabetic proteins in docking and molecular dynamics simulation studies. Furthermore, QSAR analysis and network pharmacology studies of the identified compounds divulged enhanced insulin secretion stimulation, insulin receptor kinase activity, PPARγ expression; enzyme inhibition (α-glucosidase, α-amylase) and protection of the pancreas -mediated antidiabetic effects. Besides, they proved strong inhibitory potential against the studied antidiabetic proteins in other computational analysis. Based on the present findings, it can be affirmed that C. quinquefolia extract possesses anti-diabetic activity.

Antidiabetic Effect of a New Original NT-3 Dipeptide Mimetic.

It was previously established that the original dipeptide mimetic of the 4th loop of NT-3, hexamethylenediamide bis-(N-monosuccinyl-L-asparaginyl-L-asparagine) (GTS-301), has a pronounced neuroprotective effect in vitro at concentrations of 10-5-10-12 М. In the present study, experiments on the streptozotocin-induced diabetes model in C57Bl/6 mice showed that GTS-301, when administered intraperitoneally for 32 days at doses of 0.1 and 0.5 mg/kg, has antidiabetic activity manifested in a reduction of hyperglycemia and polydipsia and in an increase in animal survival. The results obtained confirm the concept of the similarity of neurochemical mechanisms underlying the regulation of functions of neurons and ß-cells.

Golden thistle (Scolymus hispanicus L.) hydromethanolic extracts ameliorated glucose absorption and inflammatory markers in vitro.

Golden thistle (GT, Scolymus hispanicus L.) is an edible plant native to the Mediterranean. Several activities have been reported for the GT, as it is used for traditional medicinal purposes in some cultures. In this study, we aimed to investigate the effects of GT crude extract on phenolic bioavailability, antidiabetic, and anti-inflammatory activities by using colonic epithelium (CaCo-2) and murine macrophage (RAW 264.7) cell lines. The CaCo-2 cells were grown on the bicameral membrane system for intestinal bioavailability and glucose efflux. Lipopolysaccharide (LPS, 0.5 µg/mL) was used to induce systemic inflammation on RAW 264.7. The inflammatory medium of RAW 264.7 cells was given to Caco-2 cells to mimic colonic inflammation. Our results showed that 5-o-caffeoylquinic acid had an apparent permeability of (1.82 ± 0.07) × 10-6 cm/s after 6 h. The extract lowered the glucose efflux by 39.4%-42.6%, in addition to the reductions in relative GLUT2 mRNA expressions by 49%-66% in pre- and co-treatments (p < .05). Decreases in systemic inflammation markers of nitric oxide, tumor necrosis factor-alpha, and interleukin-6 (IL-6) were also detected in 30%-45% range after pre-treatments with the GT extract (p < .05). Lastly, colonic inflammation markers of IL-6 and IL-8 were reduced by 8.7%-19.5% as a result of GT pre-treatments (p < .05). Thus, an in vitro investigation of GT extract revealed promising results on antidiabetic and anti-inflammatory activities.

Chemometrics-Driven Variability Evaluation of Phenolic Composition, Antioxidant Capacity, and α-Glucosidase Inhibition of Sorbus aucuparia L. Fruits from Poland: Identification of Variability Markers for Plant Material Valorization.

Sorbus aucuparia L. (rowan tree) is a widely distributed European plant, valued for its nutritional and medicinal qualities. The medicinal application of rowanberries, relying particularly on their antioxidant and antidiabetic effects, is closely connected with the presence of numerous phenolic compounds. However, the broad geographical occurrence of rowan trees may contribute to fluctuations in fruit composition, influencing their biological properties. This study aimed to identify the constituents most involved in this variability to facilitate effective quality control. The investigation encompassed 20 samples collected from diverse locations across Poland, evaluated in terms of the variation in composition and bioactivity. The UHPLC-PDA-ESI-MSn study identified 45 different constituents, including flavonoids, phenolic acid and flavon-3-ols. The detected compounds were quantitatively assessed by HPLC-PDA, alongside spectrophotometric evaluation of total phenolic content and the content of high-molecular-weight proanthocyanidins (TPA). Additionally, •OH scavenging capacity and α-glucosidase inhibition were included as bioactivity parameters. Chemometric analyses, including hierarchical cluster analysis and principal component analysis, revealed geographically dependent variability, with low to moderate variation observed for most factors (variation coefficients 20.44-44.97%), except for flavonoids (variation coefficients 45-76%). They also enabled the selection of seven constituents and TPA as the key markers of variability and biological activity of rowanberries. These markers could be employed for quality control of the fruits, offering a more efficient and cost-effective approach compared to full phytochemical analysis.

Dose-dependent anti-hyperglycemic & anti-dyslipidemic potential of aqueous leaves extract of Typha elephantina in-vivo and in-vitro.

Diabetes mellitus is among the fundamental causes of illness and millions of deaths around the globe are directly attributed to it each year. Current antidiabetic medications often lack sustained glycemic control and carry significant risks of side effects. As a result, the use of plant-based treatments has gained popularity. In this experimental study, we evaluated the aqueous extracts (LQE) of Typha elephantina (also known as Elephant grass) leaves collected from freshwater marshes, for their potential anti-hyperglycemic and anti-hyperlipidemic antioxidant effects in healthy streptozotocin caused diabetic-mice. We employed glucose adsorption tests at different glucose levels and glucose diffusion tests to assess the in-vitro antidiabetic action of plant extract. For the in-vivo trail, we measured fasting blood glucose (FBG), glucose tolerance (GTT), as well as long-term anti-diabetic, anti-hyperlipidemic, and antioxidant activities. Our results from the glucose diffusion test indicated that the extract was highly effective at both low glucose concentrations (5 mmol L) and high glucose concentrations (100 mmol L). However, the glucose-diffusion ability reached its peaked at an excessively high dosage of the aqueous extract, suggesting a dose-related effect. Similarly, we observed that high doses of TEL.AQ extracts (400 mg/kg body weight) significantly reduced blood glucose levels in healthy mice during the glucose tolerance test (GTT) at 3 h and fasting blood glucose studies (FBG) at 6 h. Furthermore, the high-dose TEL.AQ extract effectively reduced liver-related serum markers and blood-glucose concentration (BGC) in severely chronic diabetic rats. The extract dosage also influenced lipid profile, conjugate and unconjugated bilirubin levels, cholesterol, triglycerides, HDL, and total bilirubin levels. Additionally, after administering a high extract dose, we observed considerable improvement in the liver homogenate markers CAT, POD, and SOD. In contrast, the extract at a low dosage (100 mg/kg), showed minimal, while a moderate dose (200 mg/kg), yielded promising results.