Α-glucosidase Inhibition Assay Research Articles

Exploring the inhibitory action of betulinic acid on key digestive enzymes linked to diabetes via in vitro and computational models: approaches to anti-diabetic mechanisms

ABSTRACT Phytochemicals are now increasingly exploited as remedial agents for the management of diabetes due to side effects attributable to commercial antidiabetic agents. This study investigated the structural and molecular mechanisms by which betulinic acid exhibits its antidiabetic effect via in vitro and computational techniques. In vitro antidiabetic potential was analysed via on α-amylase, α-glucosidase, pancreatic lipase and α-chymotrypsin inhibitory assays. Its structural and molecular inhibitory mechanisms were investigated using Density Functional Theory (DFT) analysis, molecular docking and molecular dynamics (MD) simulation. Betulinic acid significantly (p < 0.05) inhibited α-amylase, α-glucosidase, pancreatic lipase and α-chymotrypsin enzymes with IC50 of 70.02 μg/mL, 0.27 μg/mL, 1.70 μg/mL and 8.44 μg/mL, respectively. According to DFT studies, betulinic acid possesses similar reaction in gaseous phase and water due to close values observed for highest occupied molecular orbital (HOMO) and lowest occupied molecular orbital (LUMO) and the chemical descriptors. The dipole moment indicates that betulinic acid has high polarity. Molecular electrostatic potential surface revealed the electrophilic and nucleophilic attack-prone atoms of the molecule. Molecular dynamic studies revealed a stable complex between betulinic acid and α-amylase, α-glucosidase, pancreatic lipase and α-chymotrypsin. The study elucidated the potent antidiabetic properties of betulinic acid by revealing its conformational inhibitory mode of action on enzymes involved in the onset of diabetes.

In vitro cholinesterases, tyrosinase, α-glucosidase inhibitory and anticancer effects of novel silicon phthalocyanines containing geraniol/phytol

The axially silicon phthalocyanines, consisting of different acyclic hydrocarbons, were generated by SiPcCl2 reacting with either geraniol or phytol in toluene in the presence of NaH. FT-IR, UV–Vis, MALDI TOF, and NMR spectroscopy all provided information about the structures of silicon phthalocyanines. The cholinesterase, tyrosinase, and α-glucosidase inhibitory effects of G-SiPc and P-SiPc were tested using spectrophotometric assays. The IC50 values of G-SiPc and P-SiPc were 7.22 ± 0.53 and 11.28 ± 2.73 µM for AChE; 70.05 ± 3.00 and 60.55 ± 3.80 µM for BuChE. In addition, G-SiPc and P-SiPc inhibited the tyrosinase enzyme with IC50 values of 280.36 ± 7.92 µM and 40.51 ± 3.88 µM, respectively. P-SiPc had about seven times stronger inhibitory properties than G-SiPc. The substances exhibited less inhibition than acarbose in the α-glucosidase inhibitory assay. Finally, the cytotoxic effects of G-SiPc and P-SiPc were investigated using the MTT assay on L-929 mouse fibroblast cells as normal cells. G-SiPc and P-SiPc did not reach IC50 values up to 100 μM.

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

Background 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. Methods 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. Results 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 IC50 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 IC50 value of 5.15 μg/mL, suggesting its promising potential as antidiabetic agent. Conclusions 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.

Assessment of anti-diabetic properties of Ziziphus oenopolia (L.) wild edible fruit extract: In vitro and in silico investigations through molecular docking analysis

Abstract Globally, healthcare is concerned about the rising prevalence of type 2 diabetes. Phytochemicals from medicinal plants have shown great promise in improving human health. The present study aimed to determine the secondary metabolites of Ziziphus oenopolia (L.) fruit extract that contribute to its anti-diabetic activity. The anti-diabetic properties were assessed by in vitro and in silico approaches using α-amylase and α-glucosidase inhibitory assays. Gas chromatography and mass spectroscopy analyses were used to profile Z. oenopolia fruit contents, and a total of four bioactive chemicals and eight phytocompounds were tentatively identified, including flavonoids, terpenoids, phenols, steroids, tannins, and saponins. The Z. oenopolia fruit hydroalcoholic extract inhibits α-amylase and α-glucosidase enzymes in a dose-dependent manner (IC50 = 328.76 and 337.28 µg/mL, R 2 = 0.979 and 0.981). Additionally, phytochemicals found in Z. oenopolia fruit exhibit the ability to inhibit anti-diabetic targets, specifically α-amylase and α-glucosidase (2QV4 vs 3A4A; correlation coefficient, r = 0.955), as demonstrated by computational analysis. This establishes the fruit as a promising and environmentally friendly option for treating hyperglycemia, highlighting the positive correlation between anti-diabetic objectives.

Anti-diabetic potential of Chamaerops humilis L. aerial parts: Phenolic compounds with α-amylase and α-glucosidase inhibitory activates in-vitro, in-vivo and in-silico studies

Five compounds were isolated from the aerial parts of Chamaerops humilis L. and characterized as tricin-7-rutinoside (1), tricin (2), dihydrotricin (3) diasteroisomer of tricin 4′-O(erythro-β-guaiacyl glyceryl) ether (salcolin A)(4a), tricin-4′-O-(threo-β-guaiacyl glyceryl) ether (salcolin B) (4b) and (-)-(5s, 6s)-5,6-dihydro-3,8,10-trihydroxy-5-(4-hydroxy-3-methoxyphenyl)-6-hydroxymethyl-2,4-dimethoxy 7H benzo [e] xanthen-7-one (5). Their structures were elucidated by comparing their spectral data with those reported in the literature. To the best of our knowledge, compounds (3-5) were reported here for the first time from Chamaerops humilis. The methanolic extract of Chamaerops humilis (CHME) and the five isolated compounds were studied for its anti-diabetic effect using in vitro α-glucosidase and α-amylase inhibitory assay that showed a significant activity. The toxicological study indicated that CHME was safe up to 5000 mg/kg bw. Two doses were selected for the in vivo study (800 and 1600 mg/kg bw) and orally administered to high fat diet/streptozotocin-induced diabetic rats for 10 consecutive days. The results revealed that the CHME improved the blood glucose levels in a dose dependent manner, the dose 1600 mg/kg showed the best results dependently along the period of the experiment. CHME and the five isolated compounds were evaluated in silico for their anti-diabetic effect. The anti-inflammatory effect of CHME (1600 mg/kg bw) was proved by significant downregulation of expression for interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α) and matrix metalloproteinase-1 (MMP-1) genes. In conclusion, CHME and its constituents may be a potential hypoglycemic agent working through the anti-inflammatory and enzyme inhibitory pathways. The docking studies demonstrated that compounds Tricin7-rutinoside and Salcolin isomers had promising binding energies of -9.10 kcal/mol and -8.70 kcal/mol, respectively, against α-amylase. These binding energies were superior to that of acarbose, which had a binding energy of -7.60 kcal/mol. In addition, docking analysis provided promising results for the inhibition of α-glucosidase by Tricin7-rutinoside and Dihydrotricin with binding affinity -7.9 kcal/mol and -7.9 kcal/mol, respectively while the binding affinity of acarbose is -6.40 kcal/mol. Overall, the methanolic extract from Chamaerops humilis exhibited good in silico of α-amylase and α-glucosidase enzyme inhibition potential. These findings suggest that these compounds may have potential as anti-diabetic agents, with further research needed to verify their efficacy and safety.

Increasing structure diversity of farnesylated chalcones by a fungal aromatic prenyltransferase

Farnesylated chalcones were favored by researchers due to their different biological activities. However, only five naturally occurring farnesylated chalcones were described in the literature until now. Here, the farnesylation of six chalcones by the Aspergillus terreus aromatic prenyltransferase AtaPT was reported. Fourteen monofarnesylated chalcones (1F1−1F5, 2F1−2F3, 3F1, 3F2, 4F1, 4F2, 5F1, 6F1, and 6F2) and a difarnesylated product (2F3) were obtained, enriching the diversity of natural farnesylated chalcones significantly. Ten of them are C-farnesylated products, which complement O-farnesylated chalcones by chemical synthesis. Fourteen products have not been reported prior to this study. Nine of the produced compounds (1F2−1F5, 2F1−2F3, 5F1, and 6F1) exhibited inhibitory effect on α-glucosidase with IC50 values ranging from 24.08 ± 1.44 to 190.0 ± 0.28 μM. Among them, compounds 2F3 with IC50 value at 24.08 ± 1.44 μM and 1F4 with IC50 value at 30.09 ± 0.59 μM showed about 20 times stronger than the positive control acarbose with an IC50 at 536.87 ± 24.25 μM in α-glucosidase inhibitory assays.

Comparative antioxidant, antibacterial, and antidiabetic activities of in vitro-grown callus and wild-grown various parts of Piper longum L

BackgroundPiper longum L. is a tropical and subtropical medicinal plant that has been used as antidiabetic, diarrhea, stomachache, cough, asthma, and bronchitis since ancient times. The in vitro-grown callus from the leaf, however, has not been tested and utilized for any of these conditions. Thus, this research pursues to assess the comparative study of antioxidant, antibacterial, and antidiabetic activities of in vitro-grown callus and various parts of Piper longum-grown in the wild. MethodsThe antioxidant activity of crude extracts and the fractions were determined by DPPH (1,1-diphenyl-2-picrylhydrazyl) free-radical scavenging assay, the antibacterial activity by agar-well diffusion method, and antidiabetic activity by α-amylase and α-glucosidase inhibition assay. In addition, the total phenol content (TPC) and total flavonoid contents (TFC) were calculated using Folin-Ciocalteau reagent and aluminum chloride complex-forming assay respectively. ResultsThe highest antioxidant activity (IC50=134.81±1.16 µg/mL), TPC (41.22±0.50 mg of GAE/g dry weight), and TFC (73.41±0.53 mg of QE/g dry weight) were obtained in the dichloromethane (DCM) fraction of root than other crude extracts and fractions. The DCM fractions of root exhibited the minimum inhibitory concentration (MIC) at 5.0 mg/mL and minimum bactericidal concentration (MBC) of 8.35 mg/mL to the Staphylococcus aureus. Moreover, the DCM fraction of root showed the highest α-amylase and α-glucosidase inhibition (IC50=365.21±31.02 and 489.07±27.96 µg/mL) than other crude extracts and fractions. To the best of our information, comparative antioxidant (IC50=206.61±0.64 µg/mL), antibacterial (suppressed 80 % of tested bacteria), and antidiabetic (IC50=1165.15±15.63 and 1304.76±12.43 µg/mL) properties of the in vitro-grown callus were recorded for the first time in P. longum, and were found to be comparative to those of the wild-grown parts. ConclusionsThese results showed that wild-grown P. longum roots, particularly the DCM fraction, could be an important source of natural antioxidants, antimicrobials, and antidiabetics for better curative uses than other wild-grown parts and in vitro-grown callus. In vitro-grown callus, however, could be used as a natural drug source and used to conserve P. longum in its natural habitats in the future.

Phytochemical profiling, antidiabetic, antiobesity, and antibacterial activities of Cometes abyssinica

This study aims to complete my chemical and biological studies on Cometes abyssinica (CA). The chemical profile was reported by LC-ESI-TOF-MS and GC-MS analyses. Antidiabetic (α-Glucosidase and a-amylase inhibitory activity assay), antiobesity (Lipase inhibitory activity assay), and antibacterial activity (agar well diffusion assay) were determined. The GC-MS analysis led to the identification of 27 hydrocarbons representing 93.4% of the total hydrocarbon content in hexane extract. 11-Octadecenoic acid, methyl ester (28.07%), citronellol (9.31%), hexadecanoic acid, methyl ester (7.64%), phytol (5.93%), and 10-epi-γ-eudesmol (4.91%) were the major components. The LC-ESI-TOF-MS analyses of aqueous-methanolic extract led to the identification of 99 secondary metabolites including phenolics, flavonoids, alkaloids, and vitamins. The percentages of inhibition of the n-hexane, chloroform, ethyl acetate, and methanol extracts of CA were evaluated against α-glucosidase, α-amylase, and pancreatic lipase enzymes at different concentrations. Hexane extract showed the most powerful α-glucosidase and α-amylase inhibitory activity with IC50 value of 0.22 and 0.27 mg/ml comparing with acarbose (IC50 0.43 and 0.38), respectively. Among all CA extracts, only ethyl acetate extract revealed potent antiobesity as a lipase inhibitory activity with IC50 value of 0.079 mg/ml comparing with orlistat (IC50 0.11 mg/ml). CA extracts showed mild-weak antibacterial effect against Pseudomonas aeruginosa and Bacillus cereus. KEY WORDS: Cometes abyssinica, Chemical constituents, α-Amylase inhibitors, α-Glucosidase inhibitors, Lipase inhibitors Bull. Chem. Soc. Ethiop. 2024, 38(4), 1051-1067. DOI: https://dx.doi.org/10.4314/bcse.v38i4.19

The effect of extraction method on biological activity and phytochemical content of Artocarpus heterophyllus (jackfruit) leaves extract concurrent with its principal component analysis

Artocapus heterophyllus (jackfruit) is available in abundance in tropical regions. The present study explored the effect of different extraction method i.e. maceration, ultrasonication and both of ultrasonication and maceration on its biological activity (antioxidant, antidiabetes and antibacterial activities) and phytochemical content of Artocarpus heterophyllus (jackfruit) leaves extract. Jackfruit leaves were extracted using ethanol as solvent. The capability of jackfruit leaves extract to scavenge radicals was evaluated using a DPPH (2,2-diphenyl-1-picryl-hydrazyl) assay, β-carotene bleaching assay and reducing power assay. The total phenolic content (TPC) was assessed using the Folin- Ciocalteau method. Its antibacterial activity was assessed using the disc diffusion and microdilution method against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, Salmonella typhimurim and Escherichia coli. The α-glucosidase inhibitor assay was conducted using α-glucosidase from Saccharomyces cerevisiae. The results revealed that ulrasonication method give the highest antioxidant activity in three metode used, i.e. DPPH assay with IC50 of 42.51 µg/mL, β-carotene bleaching assay of 57.64%, reducing power assay of 919 mg GAE/g. Meanwhile, for α-glucosidase inhibitory assay, ultrasonication method also had the highest value of 83.44% at concentration of 1000 µg/mL. Furthermore, antibacterial assay using disk diffusion method showed ultrasonication had the highest inhibition zone of 7.81 mm at 5 mg/mL against P. aeruginosa, while maceration method had the highest inhibition zone of 8.02 mm at 5 mg/mL against E. coli. These results in accordance with total phenolic content (TPC) of ultrasonication extract which was the highest of 125.06 mg GAE/g. The liquid chromatography-high-resolution mass spectrometry (LC-HRMS) analysis suggested that several bioactive compounds such as phenolic, flavonoid and its derivatives was present in the jackfruit leaves extract. Further analysis using principal component analysis (PCA) revealed that the extraction process affected the metabolite composition of the samples which was confirmed by significant separation of the score plots of extraction methods. The present study revealed that jackfruit leaves is a potent source of natural antibacterial, antioxidants and antidiabetic medicines in functional foods and pharmaceutical industries.

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.

Exploring the multifaceted bioactivities of Lavandula pinnata L. essential oil: promising pharmacological activities.

Introduction: This study investigates the biological activities of Lavandula pinnata essential oil (LPEO), an endemic lavender species from the Canary Islands, traditionally used in treating various ailments. Methods: LPEO was extracted by hydrodistillation and analyzed using GC-MS. Antioxidant activity was assessed by DPPH radical scavenging and total antioxidant capacity assays. Antimicrobial activity was evaluated by disc diffusion, MIC, MBC, and MFC determination against bacterial (Staphylococcus aureus, Micrococcus luteus, Escherichia coli, Pseudomonas aeruginosa) and fungal (Candida glabrata, Rhodotorula glutinis, Aspergillus niger, Penicillium digitatum) strains. Antidiabetic and anti-gout potential were investigated through α-amylase, α-glucosidase, and xanthine oxidase inhibition assays. Antityrosinase activity was determined using a modified dopachrome method. Cytotoxicity was assessed by MTT assay against breast (MCF-7, MDA-MB-468), liver (HepG2), colon (HCT-15) cancer cells, and normal cells (PBMCs). Results and discussion: LPEO exhibits potent antiradical activity (IC50 = 148.33 ± 2.48μg/mL) and significant antioxidant capacity (TAC = 171.56 ± 2.34μg AA/mg of EO). It demonstrates notable antibacterial activity against four strains (Staphylococcus aureus, Micrococcus luteus, Escherichia coli, and Pseudomonas aeruginosa) with inhibition zones ranging from 18.70 ± 0.30mm to 29.20 ± 0.30mm, along with relatively low MIC and MBC values. LPEO displays significant antifungal activity against four strains (Candida glabrata, Rhodotorula glutinis, Aspergillus niger, and Penicillium digitatum) with a fungicidal effect at 1mg/mL, surpassing the positive control (cycloheximide), and MIC and MFC values indicating a fungicidal effect. It exhibits substantial inhibition of xanthine oxidase enzyme (IC50 = 26.48 ± 0.90μg/mL), comparable to allopurinol, and marked inhibitory effects on α-amylase (IC50 = 31.56 ± 0.46μg/mL) and α-glucosidase (IC50 = 58.47 ± 2.35μg/mL) enzymes.The enzyme tyrosinase is inhibited by LPEO (IC50 = 29.11 ± 0.08mg/mL). LPEO displays moderate cytotoxic activity against breast, liver, and colon cancer cells, with low toxicity towards normal cells (PBMC). LPEO exhibits greater selectivity than cisplatin for breast (MCF-7) and colon (HCT-15) cancer cells but lower selectivity for liver (HepG2) and metastatic breast (MDA-MB-468) cancer cells. These findings suggest the potential of LPEO as an antioxidant, antimicrobial, anti-gout, antidiabetic, and anticancer agent.

Formulation and assessment of chickpea pulao using fenugreek seeds and Indian rennet to improve blood glycemic levels.

Diabetes is becoming a significant health concern in Asia, where the prevalence has reached alarming levels. An important contributing factor is the consumption of high-carbohydrate foods, including rice, bread, etc. These high-carbohydrate foods pose a major risk to public health due to their impact on postprandial hyperglycemia. This research aimed to formulate a chickpea pulao (cooked Indian-Pakistani rice dish) and to evaluate its effects on postprandial blood glucose levels in type 2 diabetic individuals. Antioxidant potential and total phenolic contents of herbs at different concentrations (1, 3, 5, 7, and 9%) were measured through DPPH and Folin Ciocalteu assays. The antidiabetic potential was tested by α-amylase and α-glucosidase inhibition assays. After sensory evaluation, the best-chosen concentration was used to formulate the chickpea pulao. The study trial was advertised under "DP trial," and 12 participants were recruited. A single-blind randomized cross-over trial was conducted for 3 weeks with a one-week wash-over time in between. Participants' preprandial and postprandial blood glucose levels were recorded for control and intervention recipes. Results indicated that both fenugreek seeds (FS) and Indian rennet (IR) showed good antioxidant and hypoglycemic activity (p = .000) in raw and boiled extracts. For DPPH, the IC50 values of unboiled and boiled combined (FS + IR) extracts were calculated as 7.4% and 8.02%, respectively. Similarly, for α-amylase, the IC50 values of combined IR and FS unboiled and boiled extracts were 6.58% and 6.83%, and for α-glucosidase inhibition assay, the values were measured as 14.98% and 16.24%. The single-blind randomized cross-over trial showed that consuming the intervention recipe significantly reduced postprandial hyperglycemia (p = .000) in type 2 diabetic participants. The intervention recipe decreased hyperglycemia by approximately 15% daily compared to the control recipe. Incorporation of hypoglycemic herbs into dietary patterns can work as an adjunct therapy for diabetes management, especially in populations with a high prevalence of this disease.

Qualitative chemical compounds analysis and in vitro estimation of antiproliferative, antidiabetic and anti-Alzheimer’s disease effects of Ononis natrix (L.) family Fabaceae

The O. natrix belongs to the family Fabaceae and is distributed in Jordan. Different species of the family Fabaceae contain chemical compounds that may have potential antiproliferative, antidiabetic, and anti-Alzheimer’s disease. High-performance liquid chromatography (HPLC) was applied to analyse the phenolic compounds found in O. natrix methanolic extract. Using the MTT assay, the antiproliferative action was studied. The enzymes α-glucosidase and butyrylcholinesterase inhibition assays were used to study the antidiabetic and anti-Alzheimer’s disease actions, respectively, of methanolic extract of O. natrix. Eleven phenolics and seven flavonoids were identified in the methanolic extract of O. natrix by HPLC. The highest phenolics and flavonoids were gallic acid (1.25 mg/100 g dry weight) and rutin (1.44 mg/100 g dry weight), respectively. The most cancer cell lines influenced by the extract of O. natrix were PC-3 (IC50 = 55 ± 2 µg/mL) and HepG-2 (IC50 = 68 ± 2 µg/mL) compared to positive control cisplatin. However, the cancer cell lines CaCo-2, MCF-7, and HeLa showed IC50 values of 109 ± 2 µg/mL, 123 ± 2 µg/mL, and 79 ± 1 µg/mL, respectively, related to cisplatin. The O. natrix extract inhibited the α-glucosidase enzyme and butyrylcholinesterase enzyme by 84% and 86%, respectively compared to positive controls acarbose and rivastigmine. The O. natrix may possess antiproliferative effects against prostate cancer and hepatocellular carcinoma. It also may have antidiabetic and anti-Alzheimer’s disease effects.

Vitis vinifera L. seed standardized extract; a promising therapeutic against metabolic syndrome induced by high-fat/high-carbohydrate diet and streptozotocin in rats

Metabolic syndrome (MetS) is a group of abnormal disorders; hypertension, glucose intolerance, dyslipidemia, proinflammatory, and prothrombotic states, affecting approximately 14 % of the world's population. The potential of grape seeds extract (GSE) supplementation to improve the metabolic disturbances and their related conditions like obesity, type 2 diabetes, and nonalcoholic fatty liver disease was investigated in this study. In-vitro metabolic syndrome assays were investigated through α-amylase, α-glucosidase, lipase, lipoxygenase (LOX), cyclooxygenases (COX-1 and COX-2), renin and angiotensin converting enzyme (ACE) inhibition assays. Additionally, in-vivo rat model of high-fat-high-carbohydrate diet (HFD)-induced MetS was established, where metformin (MT) (200 mg/kg) was used as a reference drug and GSE was given at 100 and 200 mg/kg by oral gavage. GSE was standardized using HPLC analysis for the major reported compound; catechin which should be ≥ 160.76 ± 5.52 μg/mL. Total phenolic content of GSE was 21.12±0.61 µg gallic acid equivalent/1 mg extract and total flavonoid content was 23.81±0.64 µg rutin equivalent/1 mg extract. In-vitro assays revealed the potential of GSE to manage the metabolic syndrome, besides its strong antioxidant capacity. Treatment with GSE (100 mg/kg and 200 mg/kg) markedly (P < 0.05) controlled the weight gain, improved the metabolic pathways (total glucose, cholesterol, triglycerides, AST, and ALT), oxidative stress parameters (MDA, GSH, and catalase) and inflammatory biomarkers in HFD fed rats. GSE downregulated the expression of insulin resistance gene (IR) and some inflammatory related genes (TNF-α and NF-κB), additionally it improved the pathological features of metabolic conditions and upgraded the expression of Nrf2 compared to HFD group. The superior effects were owned to the high dose of GSE, 200 mg/kg b.wt. (P < 0.05, P < 0.001). All results sustenance the beneficial effects of the standardized GSE in the management of metabolic syndrome.

Liposomal formulations of Oleae europaea L.: analyzing the antioxidant and antidiabetic activities along with toxicity profile in pancreatic beta TC6 cell line

ABSTRACT Olea europaea L. (Oleaceae), is rich in phenolic content and has powerful antioxidant and antidiabetic activity. However, there are no medicinal products prepared due to this feature. Therefore, this study aims to characterize an O. europaea extract with strong antioxidant and antidiabetic properties and to prepare nanoformulations containing this extract. To determine the activities of the extracts prepared from the leaves of the plant, DPPH• and ABTS•+ scavenging, Fe+3 reducing activity, α-amylase, and α-glucosidase inhibition assays were performed. The oleuropein content of the absolute ethanol extract with the highest activity was analysed by HPLC. The characterized extract was loaded into liposomes and chitosan coated liposomes, and the long-term sustainability of their activity was investigated. The encapsulation efficiency was 65.2% for the liposome and 66.8% for the chitosan-coated liposome formulation. The amounts of the extracts released from the formulations were evaluated to exhibit antioxidant and antidiabetic activity.

Exploration of the Molecular Mechanism Underlying the Antidiabetic Activity of a Northeast Indian Plant Zingiber rubens Roxb. through Modulation of PKC Phosphorylation

Background: Zingiber rubens Roxb., a new species of the Zingiberaceae family, is found profoundly in the Northeastern region of India. It is a rhizomatous geophyte and grows primarily in the seasonally dry tropical biome native to Indo-China regimens. Objective: The aim is to research the root part of this plant to discover active constituents and evaluate the molecular mechanism of antidiabetic activity Methods: The hydroalcoholic root extract of this plant (HAZR) was evaluated for in-vitro antioxidant assays α-amylase and α-glucosidase inhibition assay. Further, the antidiabetic activity assay was evaluated, exploring the molecular mechanism for modulating oxidative stress in tissue biochemical parameters and HbA1c. To explore the molecular mechanism, we also investigated the inhibition assay of protein kinase C (PKC) phosphorylation in mouse peritoneal macrophages. Results: The experiments' results helped to conclude that HAZR has potent antioxidant and antidiabetic activity and could have been embedded with potent active molecules. They also revealed the mechanism of action as inhibition of PKC phosphorylation, meriting further studies. Conclusion: The present study revealed that HAZR demonstrated its antidiabetic activity against diabetic animal models through oxidative stress-mediated PKC and TGF-β regulation in diabetic individuals.

Essential Oils of Two Species of Zingiberaceae Family from Vietnam: Chemical Compositions and α-Glucosidase, α-Amylase Inhibitory Effects

The ginger family (Zingiberaceae) is one of the most diverse and abundant families in the plant kingdom in terms of number of species. In terms of chemistry, this is a family of plants containing much essential oil with mainly monoterpene and sesquiterpene derivatives, which has been widely used in medicine, food, and flavor industries. In our series of studies on ginger family plants, the two new species including Wurfbainia schmidtii (K. Schum.) Škorničk. &amp; A.D. Poulsen and Zingiber atroporphyreus Škorničk. &amp; Q.B. Nguyen has been investigated for the first time. This study aimed to identify the chemical compositions of essential oils extracted from the rhizomes and leaves of these two species using gas chromatography-mass spectrometry (GC/MS) analysis and evaluate their hypoglycemic effects through the α-glucosidase and α-amylase inhibitory assays. In terms of chemical composition, in general, the main compounds appearing in the essential oils of both leaves and rhizomes of each species are similar but they are differences in the percentage of the main components, for example, 1,8-cineole is a main component in leaves whereas fenchyl acetate is the main one in rhizomes of W. schmidtii. Several distinctive compounds, in comparison with other members in the genus Zingiber, namely β-pinene, α-pinene, β-elemene, and sabinene, were found in the essential oil of Z. atroporphyreus. Regarding hypoglycemic effects, the essential oils from the two species tested possessed weak α-glucosidase and α-amylase inhibitory effects. For the first time, this study was designed to investigate the chemical composition as well as the hypoglycemic effect of essential oils distilled from the rhizomes and leaves of two species W. schmidtii and Z. atroporphyreus have been reported, serving as a premise for further systematic research on their phytochemistry and pharmacological effects being conducted.

New Garden Rose (Rosa × hybrida) Genotypes with Intensely Colored Flowers as Rich Sources of Bioactive Compounds

Garden roses, known as Rosa × hybrida, hold a prominent position as one of the most important and economically valuable plants in horticulture. Additionally, their products—essential oil, rose water, concrete, and concentrate—find extensive use in the cosmetic, pharmaceutical, and food industries, due to their specific fragrances and potential health benefits. Rose flowers are rich in biologically active compounds, such as phenolics, flavonoids, anthocyanins, and carotenoids. This study aims to investigate the potential of five new garden rose genotypes with intensely colored flowers to serve as sources of biologically active compounds. Phenolic profile was evaluated by determination of total phenolic (TPC), flavonoid (TFC), and monomeric anthocyanins (TAC) contents and LC-MS/MS analysis of selected compounds. Antioxidant activity was evaluated via DPPH and FRAP assays, neuroprotective potential via acethylcholinesterase inhibition assay, and antidiabetic activity viaα-amylase and α-glucosidase inhibition assays. The flowers of investigated genotypes were rich in phenolics (TPC varied from 148 to 260 mg galic acid eq/g de, TFC from 19.9 to 59.7 mg quercetin eq/g de, and TAC from 2.21 to 13.1 mg cyanidin 3-O-glucoside eq/g de). Four out of five genotypes had higher TPC than extract of R. damascene, the most famous rose cultivar. The dominant flavonoids in all investigated genotypes were glycosides of quercetin and kaempferol. The extracts showed high antioxidant activity comparable to synthetic antioxidant BHT, very high α-glucosidase inhibitory potential, moderate neuroprotective activity, and low potential to inhibit α-amylase.

In vitro antioxidant activity, antidiabetic activity and in silico docking studies of 3,3′,4′,5,7-pentahydroxyflavone and stigmasta-5,22-dien-3β-ol isolated from aerial parts of Euphorbia milii. Des moul

This research focused on evaluating the in vitro antioxidant, antidiabetic activities and Insilco docking properties of two phytocompounds 3,3′,4′,5,7-Pentahydroxyflavone (Quercetin) and Stigmasta-5,22-dien-3β-ol (Stigma sterol). These compounds were isolated from the methanol extract of stem and ethanol extract of flower of the E. milii plant. The antioxidant properties of these phytocompounds were studied using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. A comparison was made between the antioxidant activity of quercetin, stigma sterol, and the standard drug ascorbic acid. The results indicated that quercetin showed significant antioxidant activity, suggesting its potential as an effective antioxidant. Additionally, in vitro antidiabetic activity was investigated through α-amylase and α-glucosidase inhibition assays. Screened compounds exhibited significant % of inhibition values against two carbohydrate hydrolysing enzymes, α-amylase and α-glucosidase compared to reference drug (acarbose). Furthermore, molecular docking studies were conducted to analyse the interaction of the compounds with α-d-glucose (PDB ID: 3A4A) and PTP1B I (PDB ID: 1T49) as target molecules. These docking studies provided further insights to support the biological findings of the compounds isolated from E. milii aerial parts.

Debittering of Emblica (Phyllanthus emblica L.) fruit powder: Preparation and biological activity

Emblica, also known as Phyllanthus emblica L., is a drug homologous food that is rich in polyphenols with various biological activities. However, its bitterness and astringency pose a significant challenge to its utilization in food products. In this study, we aimed to identify the optimal conditions for debittering Emblica. Our findings revealed that the best debittering conditions were: temperature = 50 °C, pH = 4, α-l-rhamnosidase concentration 200 U/g, and time = 5 h. High-performance liquid chromatography (HPLC) and molecular docking analysis revealed that enzymatic hydrolysis partially removed bitterness compounds. The results of antioxidant activity, xanthine oxidase, and α-glucosidase inhibitory activity assays confirmed that the Emblica fruit powder still exhibited good biological activity after enzymatic debitterization. Moreover, gastric fluids treatment might contribute to the above enhancing effect of enzymatic hydrolysates of Emblica. This study provided a theoretical basis for promoting the processing and utilization of Emblica fruit powder, as well as understanding its biological activity.