Highest Antidiabetic Activity Research Articles

Synthesis, Computational Study, and In Vitro α-Glucosidase Inhibitory Action of Thiourea Derivatives Based on 3-Aminopyridin-2(1H)-Ones.

Reactions with allyl-, acetyl-, and phenylisothiocyanate have been studied on the basis of 3-amino-4,6-dimethylpyridine-2(1H)-one, 3-amino-4-phenylpyridine-2-one, and 3-amino-4-(thiophene-2-yl)pyridine-2(1H)-one (benzoyl-)isothiocyanates, and the corresponding thioureide derivatives 8-11a-c were obtained. Twelve thiourea derivatives were obtained and studied for their anti-diabetic activity against the enzyme α-glucosidase in comparison with the standard drug acarbose. The comparison drug acarbose inhibits the activity of α-glucosidase at a concentration of 15 mM by 46.1% (IC50 for acarbose is 11.96 mM). According to the results of the conducted studies, it was shown that alkyl and phenyl thiourea derivatives 8,9a-c, in contrast to their acetyl-(benzoyl) derivatives and 10,11a-c, show high antidiabetic activity. Thus, 1-(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)-3-phenylthiourea 9a has the highest inhibitory activity against the enzyme α-glucosidase, exceeding the activity of the comparison drug acarbose, which inhibits the activity of α-glucosidase by 56.6% at a concentration of 15 mm (IC50 = 9,77 mM). 1-(6-methyl-2-oxo 4-(thiophen-2-yl)-1,2-dihydropyridin-3-yl)-3-phenylthiourea 9c has inhibitory activity against the enzyme α-glucosidase, comparable to the comparison drug acarbose, inhibiting the activity of α-glucosidase at a concentration of 15 mm per 41.2% (IC50 = 12,94 mM). Compounds 8a, 8b, and 9b showed inhibitory activity against the enzyme α-glucosidase, with a lower activity compared to acarbose, inhibiting the activity of α-glucosidase at a concentration of 15 mM by 23.3%, 26.9%, and 35.2%, respectively. The IC50 against α-glucosidase for compounds 8a, 8b, and 9b was found to be 16.64 mM, 19.79 mM, and 21.79 mM, respectively. The other compounds 8c, 10a, 10b, 10c, 11a, 11b, and 11c did not show inhibitory activity against α-glucosidase. Thus, the newly synthesized derivatives of thiourea based on 3-aminopyridine-2(1H)-ones are promising candidates for the further modification and study of their potential anti-diabetic activity. These positive bioanalytical results will stimulate further in-depth studies, including in vivo models.

Shaping the bioactive potential, health-promoting properties, and bioavailability of o/w nanoemulsions by modulating the dose of a carotenoid preparation isolated from Calendula officinalis L.

The use of nanotechnology in food production (in particular protein base nanoemulsion) is a solution that is gaining popularity, which allows to design of smart food with targeted health-promoting properties. This study aimed to assess the impact of the dose of the phytochemical extract (1%; 3%; 5% w/w) comprising isolated lipophilic compounds from Calendula officinalis L. on selected physicochemical properties of the emulsion, antioxidant, antidiabetic and antiaging effects, and its impact on carotenoids content and their in vitro bioavailability.The results showed that the use of a 3% extract dosage appears to be optimal for obtaining a nanoemulsion. This variant was characterized by the highest antidiabetic activity and there was no overloading of the nanostructure. Additionally, the use of a pea protein - lipophilic compounds - sunflower/hemp oil matrix to create nanoforms seems to be a promising solution in the context of pro-health properties and bioavailability of bioactive compounds.

Chemical Profiling and Biological Activities on Nepalese Medicinal Plant Extracts and Isolation of Active Fraction of Nyctanthes arbor-tristis.

The importance of medicinal plants for the treatment of different diseases is high from the aspects of the pharmaceutical industry and traditional healers. The present study involves nine different medicinal plants, namely, Neolamarckia cadamba, Nyctanthes arbor-tristis, Pogostemon benghalensis, Equisetum debile, Litsea monopetala, Spilanthes uliginosa, Desmostachya bipinnata, Mallotus philippensis, and Phoenix humilis, collected from Chitwan district of Nepal for biochemical analysis followed by the isolation of active plant fractions from the bioactive plant extract. The methanolic extracts of roots, barks, seeds, seed cover, and the other aerial parts of plants were used for the phytochemical analysis and biological activities. The DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging assay was adopted to evaluate the antioxidant activity. Antibacterial activity was evaluated using the agar well diffusion method. The antidiabetic activity was studied by the α-amylase enzyme inhibition assay. The highest antioxidant activity was observed in extracts of Nyctanthes arbor-tristis followed by Mallotus philippensis (seed cover), Pogostemon benghalensis, Litsea monopetala, Phoenix humilis, and Neolamarckia cadamba with IC50 values of 27.38 ± 1.35, 32.08 ± 2.81, 32.75 ± 2.13, 33.82 ± 1.07, 40.14 ± 0.93, and 50.44 ± 3.75 µg/mL, respectively. The highest antidiabetic activity was observed in extracts of Phoenix humilis followed by Desmostachya bipinnata and Pogostemon benghalensis with IC50 values of 95.69 ± 6.97, 99.24 ± 12.6, and 106.3 ± 12.89 µg/mL, respectively. The mild α-amylase enzyme inhibition was found in extracts of Nyctanthes arbor-tristis, Spilanthes uliginosa Swartz, Litsea monopetala, and Equisetum debile showing IC50 values of 110.4 ± 7.78, 115.98 ± 10.24, 149.83 ± 8.3, and 196.45 ± 6.04 µg/mL, whereas Mallotus Philippensis (seed cover), Mallotus philippensis (seed), and Desmostachya bipinnata showed weak α-amylase inhibition with IC50 values of 208.87 ± 1.76, 215.41 ± 2.09, and 238.89 ± 9.27 µg/mL, respectively. The extract of Nyctanthes arbor-tristis showed high zones of inhibition against S. aureus (ATCC 25923) and E. coli (ATCC 25922) of ZOI 26 and 22 mm, respectively. The chemical constituents isolated from the active plant Nyctanthes arbor-tristis were subjected to GCMS analysis where the major chemical compounds were 11,14,17-eicosatrienoic acid and methyl ester. These results support the partial scientific validation for the traditional uses of these medicinal plants in the treatment of diabetes and infectious diseases by the people living in different communities of Chitwan, Nepal.

Evaluation of Antioxidants, Antibacterial and Antidiabetic Activities of Aqua-alcoholic Marjoram Extract

Plant extracts possess special significance towards human health and vital activities for a wide range of diseases. The current study aims at verifying the presence of active ingredients in marjoram leaves extract, and determining antioxidants, antibacterial and antifungal activities, LD50 and its antidiabetic activity. The active ingredients were qualitatively analyzed by specific test methods. Antioxidant, LD50, antibacterial and antifungal activities were measured by their standard method. The antidiabetic activity was determined by assessed hyperglycemia, hyperlipidemia and liver functions by spectrophotometric methods. The results confirmed the presence of several active components including flavonoids, alkaloids, terpenoids, tannins, and saponins. Also, the results of antioxidants activity showed that marjoram leaves extract possesses an antioxidant activity similar to ascorbic acid. LD50 results revealed that the allowed dose is 12.5 mg/ml. Biological activity results indicated that marjoram leaves extract possesses antibacterial and antifungal activities against wide range of pathogenic bacteria and fungi, but there is no effect of extract on E. coli and Staphylococcus aureus even at high concentrations. Marjoram extract revealed high antidiabetic activity when treated for two weeks 4mg of the extract daily. Also, lipid profile and liver functions, and testosterone levels were improved after treatment in the diabetic group related to the control group. It can be concluded that marjoram leaves extract has high antioxidant activity with high biological activity and high antidiabetic activity with a significant enhancement of fertility affected in diabetes and a high level of tolerated doses according to the LD50 value.

Evaluation of Antioxidant, Antidiabetic, and Cytotoxic Activities of Lilium nepalense D. Don

Lilium nepalense, a temperate medicinal plant, is used as a diuretic, antipyretic, tonic, flavoring agent, and heart pain treatment. This research aimed to evaluate the in vitro antioxidant and antidiabetic activities of the methanol, dichloromethane (DCM), and hexane fractions, and in vivo cytotoxic activities of the crude extracts of the bulb. The antioxidant activity was assessed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, antidiabetic activity by α-glucosidase inhibitory assay, and cytotoxic activity in terms of LC50 (median lethality concentration) by Brine shrimp assay. The DCM fraction showed the strongest antioxidant activity (IC50=134.99±9.75 µg/mL) and highest antidiabetic activity (IC50=182.01±20.50 µg/mL) than other fractions. Similarly, the DCM fraction had the highest total phenolic contents (243.97±33.78 mg of gallic acid equivalent per gram dry weight) and highest flavonoid contents (7.68±0.85 mg of quercetin equivalent per gram dry weight) than other fractions. Moreover, the crude extract of the bulb was not found to be cytotoxic to the Brine shrimp nauplii (LC50=3.83 mg/mL). It is the first report to date describing the antioxidant, antidiabetic, and cytotoxic properties of L. nepalense. This study concludes that the DCM fraction of the bulb could be used as an antioxidant and antidiabetic agent for therapeutic purposes; however, further identification and characterization of bioactive compounds responsible for the antioxidant, antidiabetic, and cytotoxicity is required for further validation.

Combined Antidiabetic and Antidyslipidemic Activity of Ageratum conyzoides and Gynura procumbens in Alloxan-induced Diabetic Rats

Unhealthy lifestyle habits greatly increase the risks of various degenerative illnesses, for example, diabetes mellitus as well as dyslipidemia. Recent studies have shown that the pharmaceutical drugs used for the treatment of these conditions have undesirable side effects. This indicates that it is necessary to find more effective and safe alternative treatment options, particularly in medicinal plants, such as Ageratum conyzoides and Gynura procumbens. Therefore, this research examined the combined antidiabetic and antidyslipidemic activity of Ageratum conyzoides and Gynura procumbens extracts in alloxan-induced diabetic rats. The insulin sensitivity of the test animals was assessed at the beginning of the experiment using the oral glucose tolerance test (OGTT) through the administration of 3 g/kgBW glucose. Pancreatic destruction was induced with the intraperitoneal injection of a single dose of 150 mg/kgBW alloxan, and the rats were treated with ethanol extract for 14 days. High-density lipoprotein cholesterol (HDL-C), Triglycerides (TG), total cholesterol (TC), and low-density lipoprotein cholesterol (LDL-C) were measured using the enzymatic method. The results showed that the single extracts and their combination exhibited high antidiabetic and antidyslipidemic activity. This was indicated by a substantial reduction in fasting blood sugar, TG, TC, and LDL-C (p<0.05), and an insignificant increase in HDL-C. The activity of the combined extract was similar to the single extracts, but it was not better in decreasing TG levels. Based on these findings, 95% ethanol extract of Ageratum conyzoides, Gynura procumbens, and their combination exhibited high antidiabetic and antidyslipidemic activity in alloxan-induced rats.

Antioxidant, Antimicrobial and Antidiabetic activities of Insulin plant rhizome extracts - A comparative study

retained the name as Insulin plant through traditional practice, further phytochemical and pharmacological evaluation of leaves of the plant has proven record on wider therapeutic potential such as antioxidant, antimicrobial and antidiabetic activity. Our interest of current research is to explore the rhizome by multiple extraction and to screen and find out the specific therapeutic potential of the specific extracts through relevant phytochemical and pharmacological evaluation. DPPH, Disc Diffusion and DNS methods were chosen to evaluate antioxidant and antibacterial and antidiabetic activity on various rhizome extracts (ethyl acetate, methanol, ethanol and aqueous). The anti-oxidant effect is significantly high and almost same for all rhizome extracts. ethyl acetate, ethanol, methanol has moderate antibacterial activity against gram positive ( and) and gram negative organism ( and ) by disc diffusion method as compare to the standard drug (Ceftrioxone sodium). However, aqueous extract lacs antibacterial activity. The α-amylase inhibition activity by DNS method result infers, high antidiabetic activity for ethyl acetate and ethanolic rhizome extracts whereas mild activity for methanolic and aqueous rhizome extracts. Thereby e thonolicrhizome extract might be a good choice for antioxidant, antibacterial and antidiabetic therapeutic segments among the rhizome extracts.

Profiling and In vivo studies of Bromelain Bitter Gourd (Momodica charantia) seed protein hydrolysate with antidiabetic activity

Diabetes mellitus is a multifactorial chronic disease that affects the human population and it is the third most common cause of death worldwide. Momordica charantia is commonly known as Bitter melon, Bitter guard and used as a food and natural medicine. The scientific name, Momordica means "to bite," in Latin which is refers to the jagged edges of the leaves. Including fruits, all parts of the plant, contains a bitter compound, momordicinso and very bitter in taste. It has long been used as a traditional medicine for some ailments. Bromelain bitter guard seed protein hydrolysate was profiled by ultrafiltration and SDS-PAGE analysis revealed that the lower molecular weight peptide ≤ 25 kDa exerted the high antidiabetic activity. Spontaneously diabetic rats showed a decrease in the blood Glucose level (Glu), Glycated haemoglobin (HbA1c) level, Glycogen level and also shows lower level of Lipid profile parameters (Chol, HDL, LDL, and TG) in the serum of the diabetic rats after 21 days of oral administration of bromelain bitter guard seed protein hydrolysate at dosages of 100 mg/kg, 200 mg/kg, and 400 mg/kg. However, the effect was dose-dependent. As a novel protein hydrolysate source with invivo antidiabetic activity, future research should aim to demonstrate the molecular mechanism of action and validate its bioactivity through human intervention trials.

Effect of Lactic Acid Bacteria Fermentation on the Polar Compounds Content with Antioxidant and Antidiabetic Activity of Avocado Seed Extracts

Avocado seeds, a common waste in the avocado processing industry, have been found to have several bioactivities, such as anticancer, antimicrobial, hypocholesterolemic, antioxidant, and antidiabetic activities, among others. Nowadays, this wastage is causing an environmental problem, so the use of new technologies to take advantage of it is a novel field of research. In this study, the submerged fermentation by lactic acid bacteria was used as a novel tool for improving the bioactive compound extraction from avocado seeds. Avocado seeds were fermented by different strains, their polar compounds were identified and quantified by HPLC-ESI-TOF-MS, the antioxidant activity was measured by DPPH and FRAP assays, and the antidiabetic activity was analyzed by the alpha-amylase assay. A total of 32 polar compounds were identified, with 13 of them being described in avocado seeds for the first time. Avocado seeds fermented by Pentosaceus acidilactici showed the highest sum of polar compounds (6279.63 ± 67.74 µg/g d.w.), and by extension, of hydroxytyrosol glucoside (2989.76 ± 3.64 µg/g d.w.). Lactiplantibacillus plantarum CECT 9567 showed the highest antioxidant activity measured by both DPPH and FRAP assays (6294.67 ± 19.44 and 6846.91 ± 2.13 µg TE/g d.w., respectively). Furthermore, Lactiplantibacillus plantarum CECT 748T had the highest antidiabetic activity (52.15% ± 0.67% inhibition of alpha-amylase activity), attributable to the polyphenols. According to the results, submerged fermentation by lactic acid bacteria led to an interesting increase of the polar compounds’ extractability of avocado seeds, consequently improving the bioactivities of the extracts, which could then be used for food nutraceutical or cosmetic purposes.

In vitro antioxidant activity and antidiabetic potential of five spiral ginger (Costus speciosus (J. Koenig) Sm.) populations available in Sri Lanka

Diabetes mellitus has caused millions of deaths worldwide. Costus speciosus leaves are consumed as a green leafy vegetable in Sri Lanka due to their claimed medicinal properties including hypoglycemic effect. This work aimed mainly to evaluate the antioxidant and antidiabetic potential of the five distinct C. speciosus leaves populations (P1, P2, P3, P4, and P5) available in Sri Lanka for future therapeutic food applications. Methanol extracts and hot water infusions of C. speciosus leaves were obtained and the total phenolic content, flavonoid content, total antioxidant capacity, and DPPH radical scavenging activity were determined by colorimetric assays. Moreover, in vitro antidiabetic activity was assessed using alpha-glucosidase and alpha-amylase enzyme inhibition assays. There was a remarkable variation in the functional properties among the five populations of C. speciosus as well as among the five different leaf positions from the apical to the basal part of the twig. The highest total phenolic content, DPPH radical scavenging activity, and total antioxidant capacity were observed in methanol leaf extracts of P3 as 7.49 ± 0.21 mg GAE g-1, 91.57 ± 0.08%, and 10.39 ± 0.50 mg AAE g-1 respectively. Leaf bud contained significantly (p < 0.05) the highest total phenolic content and DPPH radical scavenging activity than the other leaf positions. C. speciosus population 1 exhibited significantly (p < 0.05) the highest antidiabetic activity in terms of alpha-glucosidase enzyme inhibition, with an IC50 value of 2.57 mg mL−1 compared to the standard acarbose (12.85 mg mL−1). In the conclusion of the study, C. specious variety available in Sri Lanka can be considered as a potential candidate for therapeutic food applications.

Synthesis and Characterization of Alpinia calcarata Loaded Nanoparticles to Control Hyperglycemia

Bovine Serum Albumin (BSA) nanoparticles loaded with the bioactive compounds of A. calcarata, which is known to exert its antidiabetic activity through the inhibition of pancreatic enzymes, are a good form of an antidiabetic nutraceutical as they have reduced side effects, protection of active compounds from environmental agents, specific delivery to target sites and prolonged shelf-life. The objective of the present study was to synthesize and characterize A. calcarata loaded nanoparticles (ALNP) to be used as a powder form nutraceutical with higher antidiabetic activity. In this study an aqueous A. calcarata extract (4.00 mL) was added to BSA (20 mg/mL, 4.00 mL, pH 9) in the presence of citric acid as the cross-linking agent. The ALNP gave an IC50 value of 147 µg/mL, a glucose (5 mM) uptake percentage of 73.09% at a 0.5 mg/mL concentration, a solubility value of 64%, A. calcarata loading percentage of 6.66% and A. calcarata entrapment efficiency of 87.71%. They had a spherical morphology and uniform size with a particle size of 1030.70 nm, PDI of 0.199 and a zeta potential of 2.57 mV. The UV-Visible absorbance spectra and FT-IR spectra showed that citric acid had caused conformational changes in the protein structure of BSA and that the active compounds were successfully loaded into the synthesized nanoparticles which interacted with the protein matrix via covalent bonds. Therefore, it can be concluded that the synthesized nanoparticles have an antidiabetic effect and the antidiabetic activity of bioactive compounds of the aqueous A. calcarata extract become enhanced when loaded onto the nanocarriers.

Production and in vitro studies of Bitter Gourd (Momodica charantia) seed protein hydrolysates with antidiabetic activity

Diabetes mellitus is a multifactorial chronic disease that affects the human population and it is the third most common cause of death worldwide. Momordica charantia is commonly known as Bitter melon, Bitter guard and used as a food and natural medicine. The scientific name, Momordica means "to bite," in Latin which is refers to the jagged edges of the leaves. Including fruits, all parts of the plant, contains a bitter compound, momordicinso and very bitter in taste. It has long been used as a traditional medicine for some ailments. Its high protein content (35.18%) makes it a promising candidate as a source of bioactive protein hydrolysates. In this study, the potential of enzymatically hydrolyzed Bitter guard seed protein to generate functional bioactive peptides was evaluated. Bitter guard seed protein concentrate was hydrolyzed using three different proteolytic enzymes (Alcalase, Bromelain, and Papain) at their respective optimum pH and temperature. The choice of enzyme affected the bioactivities to a certain degree as Bitter guard seed were shown to possess high antidiabetic activity. Bromelain Bitter guard seed protein hydrolysate showed the highest DPP-IV inhibitory activity with 79.27% inhibition, α-Glucosidase inhibitory activity with 72.15% inhibition and α-Amylase inhibitory activity with 59.98% compared to other enzymatic hydrolysates, and therefore was chosen for further investigation of its antidiabetic activity.

First report on essential oil composition and biological activities of five Strobilanthes species from Kumaun Region of Uttarakhand, India

In the present investigation the chemical composition and biological activities of essential oils (EOs) of the five Strobilanthes species viz., S. angustifrons C. B. Clarke,S. pentastemonoid M, (Nees) T. Anderson, S. tomentosa (Nees) J.R.I.Wood, S. attenuata (Wall. ex Nees) Jacq. ex Nees and S. glutinosa (Nees) collected from different locations of Kumaon region, Uttarakhand, India were examined and reported for the first time. The essential oils were analysed for their chemical composition by GC-MS. The yield of the hydro distilled essential oils was ranging from 0.2 to 0.3% (v/w). GC-MS results revealed a wide variability in the chemical composition among the studied Strobilanthes species. Among the biological activities, highest anti-inflammatory activity was recorded for S. angustifrons EO (IC50 = 9.6 ± 0.57 μL/mL). Highest antioxidant activity in terms of DPPH and metal chelating activity was shown by S. pentastemonoid EO (IC50 = 15.32 ± 0.48 μL/mL and 23.29 ± 0.13 μL/mL, respectively). Highest antioxidant activity in terms of H2O2 scavenging activity and highest antidiabetic activity was shown by S. attenuate EO (IC50 = 21.82 ± 0.53 μL/mL) and S. tomentosa EO (IC50 = 21.82 ± 0.53 μL/mL), respectively. The biological activity data revealed the significant antioxidant, anti-inflammatory and antidiabetic activities of the studied Strobilanthes species. Therefore, the essential oils of these species can be a good natural product to be used as ecofriendly antioxidant, anti-inflammatory and antidiabetic agents.

Biosynthesis and Characterization of Silver Nanoparticles from the Extremophile Plant Aeonium haworthii and Their Antioxidant, Antimicrobial and Anti-Diabetic Capacities

The present paper described the first green synthesis of silver nanoparticles (AgNPs) from the extremophile plant Aeonium haworthii. The characterization of the biosynthesized silver nanoparticles was carried out by using UV-Vis, FTIR and STM analysis. The antioxidant, antidiabetic and antimicrobial properties were also reported. The newly described AgNPs were spherical in shape and had a size of 35-55 nm. The lowest IC50 values measured by the DPPH assay indicate the superior antioxidant behavior of our AgNPs as opposed to ascorbic acid. The silver nanoparticles show high antidiabetic activity determined by the inhibitory effect of α amylase as compared to the standard Acarbose. Moreover, the AgNPs inhibit bacterial growth owing to a bactericidal effect with the MIC values varying from 0.017 to 1.7 µg/mL. The antifungal action was evaluated against Candida albicans, Candida tropicalis, Candida glabrata, Candida sake and non-dermatophytic onychomycosis fungi. A strong inhibitory effect on Candida factors' virulence was observed as proteinase and phospholipase limitations. In addition, the microscopic observations show that the silver nanoparticles cause the eradication of blastospores and block filamentous morphogenesis. The combination of the antioxidant, antimicrobial and antidiabetic behaviors of the new biosynthesized silver nanoparticles highlights their promising use as natural phytomedicine agents.

An Overview of Herbal-Based Antidiabetic Drug Delivery Systems: Focus on Lipid- and Inorganic-Based Nanoformulations.

Diabetes is a metabolic pathology with chronic high blood glucose levels that occurs when the pancreas does not produce enough insulin or the body does not properly use the insulin it produces. Diabetes management is a puzzle and focuses on a healthy lifestyle, physical exercise, and medication. Thus far, the condition remains incurable; management just helps to control it. Its medical treatment is expensive and is to be followed for the long term, which is why people, especially from low-income countries, resort to herbal medicines. However, many active compounds isolated from plants (phytocompounds) are poorly bioavailable due to their low solubility, low permeability, or rapid elimination. To overcome these impediments and to alleviate the cost burden on disadvantaged populations, plant nanomedicines are being studied. Nanoparticulate formulations containing antidiabetic plant extracts or phytocompounds have shown promising results. We herein aimed to provide an overview of the use of lipid- and inorganic-based nanoparticulate delivery systems with plant extracts or phytocompounds for the treatment of diabetes while highlighting their advantages and limitations for clinical application. The findings from the reviewed works showed that these nanoparticulate formulations resulted in high antidiabetic activity at low doses compared to the corresponding plant extracts or phytocompounds alone. Moreover, it was shown that nanoparticulate systems address the poor bioavailability of herbal medicines, but the lack of enough preclinical and clinical pharmacokinetic and/or pharmacodynamic trials still delays their use in diabetic patients.

In Vitro, Molecular Docking, and Meta-analysis Studies of Screening Antidiabetic Bioactive Compounds from Roselle (Hibiscus sabdariffa Linn.)

Diabetes mellitus is a chronic metabolic disorder due to insulin function insufficiency. This study aimed to test the effectiveness of flower extract of roselle (Hibiscus sabdariffa L.) extract in producing antidiabetic compounds. The inhibition of roselle flower extract on the alpha- glucosidase enzyme was carried out in vitro. Molecular docking was also carried out to bind ligands derived from roselle flower extract's secondary metabolites to the alpha-glucosidase and alpha-amylase enzymes. Based on molecular docking, models have negative binding energies suggesting those ligands make a complex to the site receptor. Kaemferol-3-O-rutinoside and tiliroside become the most stable complex based on the lowest energy score of –9.5 and –8.1 kcal/mol for alpha-amylase and alpha-glucosidase, respectively. The highest antidiabetic activity was obtained at a 100 ppm roselle flower ethanol extract and distilled water with an inhibition value of 100.00 and 99.25%, respectively. The alpha-amylase inhibiting test, using a concentration of 2.5 mg/mL, had an inhibitory activity of 41.77%. The in vitro assessment was conducted using the meta-analysis. The meta-analysis study showed that roselle flower extract could reduce glucose levels in fasting rats better than negative controls (diabetic rats) by 61% than those not given the roselle flower extract.

Characterization and analysis of the antidiabetic activities of sulphated polysaccharide extract from Caulerpa lentillifera

Caulerpa lentillifera is a type of green seaweed that is cultivated in tropical and subtropical areas. The objectives of this study were to determine the characteristics of the sulfated polysaccharides from C. lentillifera and evaluate its antidiabetic activity. In the initial process of this study, samples were macerated with ethanol (1:10). Then, the maceration residue was extracted with an accumulator at 75 °C for three hours. The crude extract yield was 4.16% based on weight seaweed. Ion chromatography purification with DEAE-Sepharose resin provided a yield of 14.8% of crude extract. The monomer analysis of C. lentillifera from the crude extract and purified extract revealed that galactose monomers were dominant and glucose was a minor component. The total carbohydrate and sulfate contents of purified C. lentillifera were higher than those of crude C. lentillifera. Bioactivity tests revealed that purified polysaccharides had higher antidiabetic activity against α-glucosidase enzyme than crude ones with IC50 values of 134.81± 2.0 µg/mL. Purified sulfated polysaccharides of C. lentillifera could potentially be used as an antidiabetic medication.

Light Tailoring: Impact of UV-C Irradiation on Biosynthesis, Physiognomies, and Clinical Activities of Morus macroura-Mediated Monometallic (Ag and ZnO) and Bimetallic (Ag-ZnO) Nanoparticles.

A nano-revolution based on the green synthesis of nanomaterials could affect all areas of human life, and nanotechnology represents a propitious platform for various biomedical applications. During the synthesis of nanoparticles, various factors can control their physiognomies and clinical activities. Light is one of the major physical factors that can play an important role in tuning/refining the properties of nanoparticles. In this study, biocompatible monometallic (AgNPs and ZnONPs) and bimetallic Ag–ZnONPs (0.1/0.1 and 0.1/0.5) were synthesized under UV-C light irradiation from the leaf extract of Morus macroura, which possesses enriched TPC (4.238 ± 0.26 mg GAE/g DW) and TFC (1.073 ± 0.18 mg QE/g DW), as well as strong FRSA (82.39%). These green synthesized NPs were evaluated for their anti-diabetic, anti-glycation, and biocompatibility activities. Furthermore, their anti-cancerous activity against HepG2 cell lines was assessed in terms of cell viability, production of reactive oxygen/nitrogen species, mitochondrial membrane potential, and apoptotic caspase-3/7 expression and activity. Synthesized NPs were characterized by techniques including ultraviolet-visible spectroscopy, SEM, EDX, FTIR, and XRD. UV-C mediated monometallic and bimetallic NPs showed well-defined characteristic shapes with a more disperse particle distribution, definite crystalline structures, and reduced sizes as compared to their respective controls. In the case of clinical activities, the highest anti-diabetic activity (67.77 ± 3.29% against α-amylase and 35.83 ± 2.40% against α-glucosidase) and anti-glycation activity (37.68 ± 3.34% against pentosidine-like AGEs and 67.87 ± 2.99% against vesperlysine-like AGEs) was shown by UV-C mediated AgNPs. The highest biocompatibility (IC50 = 14.23 ± 1.68 µg/mL against brine shrimp and 2.48 ± 0.32% hemolysis of human red blood cells) was shown by UV-C mediated ZnONPs. In the case of anti-cancerous activities, the lowest viability (23.45 ± 1.40%) with enhanced ROS/NOS production led to a significant disruption of mitochondrial membrane potential and greater caspase-3/7 gene expression and activity by UV-C mediated bimetallic Ag–ZnONPs (0.1/0.5). The present work highlights the positive effects of UV-C light on physico-chemical physiognomies as well as the clinical activities of NPs.

EVALUATION OF DIFFERENT BIOLOGICAL ACTIVITIES OF LEAVES OF EHRETIA ACUMINATA R. BR.

Ehretia acuminata R. Br. is a plant with alternative medicinal properties, commonly found in Asian, African and North American countries. The present study was undertaken to prepare crude extracts of E. acuminata leaves with different polarity solvents (petroleum ether (PE), chloroform (CH), ethyl acetate (EA), ethanol (EOL) and aqua (AQ)) by using successive Soxhelet extraction method and assessing antidiabetic, antiinflammatory and antihemolytic activities by the spectrophotometric method and antimicrobial activity by the zone inhibition method. The highest antidiabetic activity was found in the chloroform extract (IC50 260-265 µg/mL) and the lowest was in the aqueous extract (IC50 1560-1550 µg/mL). In anti-inflammatory assay, highest potential was shown by ethyl acetate (IC50 290 µg/mL) extract and lowest in petroleum ether (IC50 750µg/mL) extract. The zone of inhibition is highest in ethanol extract (12-18mm) by different food poisoning microbes, similarly, ethyl acetate extract showed the highest potential in antihemolytic activity with IC50 90 µg/mL. Many extracts of E. acuminata leaves showed a high biological potential that could be attributed to the high amount of phytoconstituents and thus could be utilized as value added functional food.

Whey protein based electrosprayed nanospheres for encapsulation and controlled release of bioactive compounds from Tinospora cordifolia extract

The synergistic effects of bioactive compounds of Tinospora cordifolia have insulin mimicking and hypoglycemic activity, however, low bioavailability and poor stability limits its potential. In the present study, an appropriate delivery system was developed for the controlled release of its anti-diabetic activity. The bioactive compounds such as palmatine, berberine and palmatoside had better binding energy as observed in docking studies compared to that of the commercial active compounds. However, as these biocompounds from Tinospora cordifolia are associated with low stability and poor bioavailability, these compounds were encapsulated in a core-shell matrix of whey protein isolate. The bioactive compounds had highest antidiabetic activity in chloroform extract with an IC50 concentration of 11.34 mg/ml. An increase in 28.12% activity was observed in nanoemulsion form with an average size of 82.68 ± 4.37 nm. The bioactive compounds were further encapsulated by electrospray technique for increased stability. The particles had an encapsulation efficiency of 91.2 ± 3.27% with an average particle size of 187 ± 2.71 nm. The kinetic study revealed the complete release of bioactive compounds after 24 h of incubation in buffer solution. This formulation can be further explored as novel nutraceutical delivery system with minimal side effects as compared to their synthetic counterparts. Considering the potential application of this developed technology, further upscaling as well as in-vivo experimentation on small as well as large animals should be performed.