Amylase Inhibitor Research Articles

An Insight into Biochemical Characterization and Explorations of Antioxidant, Antibacterial, Cytotoxic, and Antidiabetic Activities by Trachyspermum ammi Nanosuspensions.

Trachyspermum ammi is a frequently utilized traditional medicinal plant renowned for its pharmacological attributes, particularly in the realm of treating infectious diseases. This current study aims to comprehensively assess the in vitro properties of freshly prepared nanosuspensions derived from Trachyspermum ammi extracts, with a focus on their cost-effective potential in various areas, including antioxidant, antibacterial, cytotoxic, and antidiabetic activities. Biochemical characterization of T. ammi nanosuspensions by high-performance liquid chromatography (HPLC) and Fourier-transform infrared spectroscopy (FTIR) analyses. HPLC analysis revealed the presence of kaempferol and sinapic acid in various amounts at 11.5 ppm and 12.3 ppm, respectively. FTIR analysis of T. ammi powder revealed the presence of alcohols and amines. The assessment of antioxidant activity was conducted using a DPPH scavenging assay, indicating that the nanosuspensions exhibited their highest free radical scavenging activity, reaching 14.9%. Nanosuspensions showed 3.75 ± 3.529.5% biofilm inhibition activity against Escherichia coli. The antidiabetic activity was accessed through antiglycation and α- amylase inhibition assays, while nanosuspension showed the maximum inhibition activity at 25.35 ± 0.912133% and 34.6 ± 1.3675%. Hemolytic activity was also evaluated, and T. ammi nanosuspension showed 22.73 ± 1.539% hemolysis. This nanotechnology approach has established a foundation to produce plant-based nanosuspensions, offering a promising avenue for the biopharmaceutical production of herbal nanomedicines. These nanosuspensions have the potential to enhance bioavailability and can serve as a viable alternative to synthetic formulations.

In‐Vitro Investigation of the α‐Amylase Inhibition Activity of Bare Bis‐Benzylidene‐Cyclohexanone Synthesized by a Highly Selective Solvent‐Free Route

AbstractCurrent work reports the highly selective, solvent‐free synthesis of an endorsed bioactive compound, Bis benzylidine cyclohexanone (BBC) through solid acid catalysed cross aldol condensation route and checks its in‐vitro bio activity. The catalytic support (Multiwalled carbon nanotube) employed was synthesized through the highly sophisticated catalytic chemical vapor deposition (CVD) method and simple mechanical grinding strategy was adopted to decorate sulfonic acid on the support. The C1s X‐ray photoelectron peak of at 290.3 eV confirms the effective interaction of sulfonic acid with MWCNT. The sharp and intense desorption peaks observed at approximately 528.7 °C and 655.15 °C in the TPD analysis unmistakably substantiate the strong acidity of the synthesized system. The alpha amylase inhibition activity of the synthesized compound was calculated to be around 88.5 %, which is in par with the commercial drug as it could inhibit only 96 %. Further, the in‐silico (Docking and Molecular Dynamic Simulation) investigations unveiled a new target site for the compound and this can further be studied in detail to advance the applications in drug design. Detailed scrutiny of various parameters was conducted to validate the bioactivity and pharmaceutical potential of the synthesized compound.

The secretion of the pancreas upon intraduodenal administration of trypsin and trypsin with its specific synthetic substrate

Earlier in our laboratory, conclusions were drawn regarding the specific substrates alleviating the selective inhibitory effects of enzymes by interacting at the catalytic center of the enzyme with the substrate. This was evidenced by data using a specific trypsin inhibitor that blocked the inhibitory effect of intraduodenally and intravenously administered trypsin (1), along with our laboratory's findings of alleviating the selective inhibition of amylase secretion by intraduodenal administration of a specific pancreatic amylase inhibitor (2). However, both protein and lipid emulsion, as substrates, exhibited elements of nonspecific enzyme sorption in their alleviating action

Insect α-Amylases and Their Application in Pest Management.

Amylase is an indispensable hydrolase in insect growth and development. Its varied enzymatic parameters cause insects to have strong stress resistance. Amylase gene replication is a very common phenomenon in insects, and different copies of amylase genes enable changes in its location and function. In addition, the classification, structure, and interaction between insect amylase inhibitors and amylases have also invoked the attention of researchers. Some plant-derived amylase inhibitors have inhibitory activities against insect amylases and even mammalian amylases. In recent years, an increasing number of studies have clarified the effects of pesticides on the amylase activity of target and non-target pests, which provides a theoretical basis for exploring safe and efficient pesticides, while the exact lethal mechanisms and safety in field applications remain unclear. Here, we summarize the most recent advances in insect amylase studies, including its sequence and characteristics and the regulation of amylase inhibitors (α-AIs). Importantly, the application of amylases as the nanocide trigger, RNAi, or other kinds of pesticide targets will be discussed. A comprehensive foundation will be provided for applying insect amylases to the development of new-generation insect management tools and improving the specificity, stability, and safety of pesticides.

GC/MS Profiling, In Vitro Antidiabetic Efficacy of Origanum compactum Benth. Essential Oil and In Silico Molecular Docking of Its Major Bioactive Compounds

Diabetes is a global health concern with significant implications for individuals and healthcare systems. Finding effective and safe antidiabetic agents is crucial for the management of this chronic disease. Natural products have emerged as potential alternatives to allopathic drugs, offering a vast source of bioactive compounds. In this study, we conducted an assessment of the antidiabetic potential of Origanum compactum essential oil, employing a two-pronged approach, i.e., experimental investigation and computational docking analysis. The results of gas chromatography–mass spectrometry (GC-MS) showed that thymol (54.6%), carvacrol (23.18%), and p-cymene (7.12%) were the major compounds. Experimental assessments revealed higher IC50 values (150 µg/mL for α-amylase; 120 µg/mL for α-glucosidase) of O. compactum oil, compared to the control drug acarbose. In silico analysis revealed the best binding affinity of the oil components (carvacrol and thymol) with human NADPH oxidase, while the lysosomal acid-α-glucosidase and salivary amylase also demonstrated good binding affinity towards carvacrol and thymol. Our findings highlight the translational potential of O. compactum oil-based treatment for diabetes mellitus and provide a basis for further studies on the modulation of NADPH oxidase, amylase inhibition, and α-glucosidase by antidiabetic natural products. However, further in vivo investigations are strongly required to confirm the results of in vitro antidiabetic effect of O. compactum EO.

Wound healing and antidiabetic properties of green synthesized silver nanoparticles in 3T3-L1 mouse embryo fibroblast cells through 2-NBDG expression

The antibacterial and antifungal properties of silver and silver-based compounds have been recognized for quite some time. This study employed an extracellular method to produce silver nanoparticles (AgNPs) using the leaves of Barringtonia racemosa (B. racemosa). B. racemosa's aqueous leaf extract underwent a color change from grey to dark brown, which revealed the formation of AgNPs. UV spectrophotometry analysis confirmed the presence of silver with the maximum absorbance of 427 nm. FTIR analysis supported the existence of alcohols with the OH stretch and alkenes with the CC stretch. The existence of AgNPs with an average hydrodynamic diameter of 36.58 nm was confirmed using dynamic light scattering (DLS). Energy dispersive X-ray spectroscopy (EDX) confirmed the presence of silver. Additionally, the AgNPs showed spherical structure particles with the size distribution ranging from 10 to 17 nm with polydispersity, under transmission electron microscopy (TEM). Thermogravimetric analysis (TGA) findings revealed that AgNPs maintain good thermal stability even at high temperatures. A variety of bacterial and fungal pathogens were successfully inhibited by the AgNPs, with S. epidermidis (27 mm) showing the strongest antibacterial activity and a 20 mm inhibitory zone was against Candida albicans for its antifungal activity. Furthermore, AgNPs also showed a positive synergistic impact with the tested antibiotic and antifungal agents. In addition, the AgNPs demonstrated strong antioxidant activity. The considerable inhibition of alpha amylase and alpha glucosidase by the AgNPs were noted by their respective IC50 values of 16.65 μg/ml and 18.97 μg/ml. Flow cytometry analysis revealed a significant increase in glucose uptake by 3T3-L1 cells after exposure to AgNPs, as indicated by the upregulation of 2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl) amino)-2-deoxyglucose (2-NBDG) expression. In 3T3/L cells, the AgNPs also demonstrated remarkable potential in accelerating wound healing achieving 92% closure of wounds after 48 h of incubation. As a result, it can be concluded that the AgNPs exhibit positive antidiabetic properties, suggesting their potential applications in the pharmaceutical industry including in the management of diabetic foot ulcers.

Influences of Household Processing Methods on Nutritional Composition, Anti-nutritional Factors and Antioxidant Activities of Foxtail Millet

The present investigation aims to study the influence of household processing methods, such as soaking, germination, and steam cooking, on nutritional composition (proximates, amino acids, minerals, and vitamins), antinutrient factors (phytochemicals: tannins, total phenols, phytic acid; enzyme inhibitors: trypsin and α-amylase inhibitors) and antioxidant properties of whole grains of foxtail millet. The contents of total ash (1.42%), fat (3.02 g/100 g), and mineral chromium (12.83 mg/100 g) were found to be high upon soaking. Trypsin inhibitors were reduced from 26.84% (steam cooking) to 12.45% upon soaking. Germination enhanced the contents of protein (11.57 g/100 g), minerals, i.e., Ca (32.48 mg/100 g), P (5.82 mg/100 g), Fe (5.81 mg/100 g), amino acid tyrosine and vitamin B<sub>1</sub>. A significant decrease in the contents of tannins from 218.93 mg GAE/g (soaking) to 93.93 mg GAE/g), phytic acid from 307.5 mg/g (soaking) to 97.63 mg GAE/g) and α-amylase inhibitors from 35.20% (steam cooking) to 5.61% were recorded upon germination. The TPCs were reduced from 13.63 mg GAE/g (soaking) to 6.81 mg GAE/g upon steam cooking. Germinated grains recorded the highest antioxidant properties based on the scavenging capacity of DPPH (0.59 mg AScE/g), ABTS<sup>+</sup> (10.77 mg TE/g) radicals and RPA (0.89 mg AScE/g). Overall, different household processing methods altered the composition of nutrients, antinutrients, and antioxidant properties. Germination has enriched the bioavailability of protein, carbohydrates, minerals, amino acids, and antioxidant properties and reduced the anti-nutritional factors, especially phytic acid, tannins, and α- amylase inhibitors.

Effects of ultrasonic-enzymatic-assisted ethanol precipitation method on the physicochemical characteristics, antioxidant and hypoglycemic activities of Tremella fuciformis polysaccharides

This investigation involved the extraction of a novel polysaccharide from the spore fermentation broth of Tremella fuciformis using a method that combined ultrasonic and enzymatic assistance with ethanol precipitation. It was then compared with enzymatic and ultrasonic extraction methods. The objective of this research is to offer a reference point for expanding the application of ultrasonic-assisted enzymatic extraction technology in T. fuciformis polysaccharides (TFPs). Based on single-factor experiments, Box-Behnken was used to optimize the extraction conditions of TFPs by ultrasonic-enzymatic-assisted ethanol precipitation extraction. The results revealed an optimal combination of enzymes, with a cellulase-to-papain ratio of 2:1, an enzyme addition of 4000U/100 mL, an enzymolysis temperature of 49 °C, ultrasonicpower at 3 W/mL and an ultrasonictime of 20 min. The extraction rate of TFPs and α- amylase inhibition rates were 23.94 % and 61.44 %, respectively. Comparing the physicochemical properties, structural characterization and in vitro activity of TFPs extracted through different methods, the results showed that ultrasonic treatment significantly influences the apparent morphology of polysaccharide and could enhance its in vitro biological activity. However, different extraction techniques exhibit insubstantial impact on the chemical composition, glycosidic bonds or glycosidic ring configurations within the polysaccharides. Among them, ultrasonic-enzymatic-assisted ethanol precipitation extraction of polysaccharide has the highest extraction rate and the lowest viscosity. It has significant effects on ABTS+ scavenging activity, α- amylase inhibition rate and glucose dialysis retardation index, polysaccharide treated with ultrasonic-enzymatic showed the best performance. These findings suggest that ultrasonic-enzymatic-assisted ethanol precipitation extraction can enhance the activities of TFPs, thereby providing a valuable insight for their future development and application.

Antioxidant Capacity, Alpha Amylase Inhibition, and Calorie Value of Dark Chocolate Substituted with Honey Powder

The antioxidant and antidiabetic properties of honey have led to studies exploring using honey powder as a sugar substitute in chocolate innovation for its health benefits. In this study, sugar was substituted with 70% honey powder to evaluate the effect on the antioxidant, alpha-amylase inhibition, and calorie value of dark chocolate. The honey powder was produced by adding 70% of either dextrose (honey/dextrose, H/D), maltodextrin (honey/maltodextrin, H/M), or sucrose (honey/sucrose, H/S) and vacuum dried at 40°C for 6 hr. The substitution of honey powder into chocolate at a 70% level was based on the preliminary study, which showed the most acceptable particle size value. The addition of honey powder into dark chocolate showed a significant increase (p < 0.05) in antioxidant capacity, assessed by 2,2-diphenyl-1-picrylhydrazyl and ferric reducing antioxidant power. Chocolate containing H/M showed the highest antioxidant capacity for both assays, followed by chocolate with H/D, H/S, and the control. Alpha amylase inhibition was also significantly higher (p < 0.05) for H/M chocolate relative to other samples. The calorie values of dark chocolate were not affected by the honey powder substitution, which remained at 600 kcal/100 g. Therefore, chocolate containing H/M showed the best properties due to its highest antioxidant capacities and alpha-amylase inhibition effect. Hence, it can be recommended for further application in chocolate.

Activity-based investigation of the possible anti-diabetic potentials of some Nigerian medicinal plants

A major therapeutic approach presently used in managing Type 2 Diabetes mellitus is the use of a-glucosidase and a -amylase inhibitors. Hence the growing attention in the quest for medicinal plants of natural sources with inhibitory potentials on these enzymes. This study was done, therefore, to determine the inhibitory potentials of the different parts of three medicinal plants; Nigella sativum (seeds), Spondias mombin (leaves and stem bark), and Picralima nitida (seeds and mesocarp) on a-amylase and a- glucosidase as well as to determine inhibition kinetics. The in vitro a-amylase and a-glucosidase inhibitory activities of the plant extract were assessed using 3,5-dinitrosalicylic acid (DNS) and p-nitro-phenyl-a-D glucopyranoside (p-NPG) respectively. The results indicated that all plant extracts assayed exhibited better a- glucosidase inhibitory effects than the reference drug(acarbose), as indicated by the higher IC50 (76.10 μg/mL) value of the reference drug, whereas the n-hexane extract of N. sativum seeds gave the best a-amylase effect (IC50 = 35.83 μg/mL). All the extracts exhibited an “uncompetitive” type of inhibition pattern. Our findings hence support the use of these plants in the management of diabetic conditions.

ISOLATION, CHARACTERIZATION OF Β-SITOSTEROL FROM THE HERBAL EXTRACTS AND EVALUATION OF IN VITRO ANTI-OXIDANT AND ANTI-DIABETIC ACTIVITIES

Plants naturally produce phytochemicals, physiologically active chemical compounds that serve as a natural defence mechanism and have considerable potential for treating a wide range of ailments. Cyperus rotundus and Tinospora cordifolia are the potent traditional herbs used in Ayurveda medicine, especially for diabetes. The current study aimed to isolate and characterize the bioactive compound β-sitosterol from the combined ethanolic extracts of the rhizome of Cyperus rotundus (C. rotundus) and the stem of Tinospora cordifolia (T. cordifolia). Furthermore, the in vitro antioxidant and anti-diabetic activities of isolated compounds are tested by DPPH assay, alpha amylase inhibition assay, alpha glucosidase inhibition assay and glucose uptake activity in 3T3L1 cells. The combined ethanolic extract of both medicinal plants was initially subjected to column and preparative thin layer chromatography for the isolation of bioactive compounds, followed by their characterization by spectral methods like UV, FT-IR, 1H and 13C NMR. The structure of the isolated compound is identified as β-sitosterol and further confirmed by structural elucidation. Similarly, the isolated compound β-sitosterol exhibited higher antioxidant scavenging activity of 64.54±1.38 µg/ml against DPPH at a concentration 100µg/ml. The study also confirmed that β-sitosterol showed good inhibitory activities towards alpha-amylase (62.21±1.25 µg/ml) and alpha-glucosidase (65.48±1.47 µg/ml). β-sitosterol showed significantly increased glucose uptake (28% at 100μg/ml). Based on the conclusion that the organic compound β-sitosterol exhibited good antioxidant and anti-diabetic efficacy, it could have been used in the treatment of free radical disease and can be utilized in the management of diabetes mellitus.

In vitro study of antioxidant, antigylycation, sugar hydrolysis enzyme inhibitory effect and molecular in silico docking study of angularly condensed diquinothiazines

BackgroundAngularly condensed diquinothiazines (MY1, MY2, and MY3) a phenothiazine derivative was evaluated for antioxidant, antiglycation, sugar hydrolysis enzyme inhibitory effect and molecular in silico docking. MethodAntioxidants were evaluated using DPPH, chelating ion, FRAP and lipid peroxidation. Alpha glucosidase and alpha amylase inhibition was used for sugar hydrolysis enzyme inhibitory activity and antiglycation with BSA-Glucose and BSA-MGO. In silco docking was done with AutoDock Vina and ADMET properties with pkCSM software. ResultAngularly condensed diquinothiazines (MY1, MY2, and MY3) showed free radical scavenging, antiglycation and alpha-glucosidase and alpha-amylase inhibition. Insilco docking and pkCSM ADME shows interaction with aldose reductase, glyoxalase 1, receptor AGE, alpha-glucosidase, and alpha-amylase. ConclusionAntiglycation, alpha-glucosidase, and alpha-amylase inhibition activity of Angularly condensed diquinothiazines maybe through deactivation of aldose reductase enzyme activity, activation of glyoxalase 1 pathway, reduction of dicarbonyl stress and oxidative stress.

Exploring the hypoglycaemic efficacy of bio-accessed antioxidative polyphenolics in thermally processed Cucumis dipsaceus fruits – An in vitro and in silico study

Inhibition of breakdown of dietary carbohydrates, by controlling the postprandial activity of diabetic enzymes through fruit polyphenolics can help downregulate the effects of Type 2 Diabetes Mellitus (T2DM). The study focuses on deciphering the induction of hyperglycaemic control by bio-accessed anti-oxidative polyphenols of Cucumic dipsaceus fruits. Chiefly, we examined the antioxidant activity of bio-accessed polyphenols of C. dipsaceus fruits (DPPH: ME (GDE)-66.26 %; ABTS: FE (IDE)-1963.83 µM TEAC/mg extract; Phosphomolybdenum reduction: FE (IDE)- 64.95 mg AAEAC/g extract). To add more significance, the anti-diabetic activity was predetermined by in silico docking analyses (Pseudojervine - −5.43; Squalene- −10.41) and was concurrently confirmed by in vitro studies (α amylase inhibition: ME (GDE) – 69.58 %; α glucosidase inhibition: FE (UDE)- 88.67 %). A higher bio-accessibility of rutin (37.92 mg/g ODE) and gallic acid (8.36 mg/g ODE) was observed after quantification by HPLC, which confirmed the correlation between anti-diabetic activity and C. dipsaceus fruit phenolic compounds.

Aconitum lycoctonum L. (Ranunculaceae) mediated biogenic synthesis of silver nanoparticles as potential antioxidant, anti-inflammatory, antimicrobial and antidiabetic agents

In this study, a polar extract of Aconitum lycoctonum L. was used for the synthesis of silver nanoparticles (AgNPs), followed by their characterization using different techniques and evaluation of their potential as antioxidants, amylase inhibitors, anti-inflammatory and antibacterial agents. The formation of AgNPs was detected by a color change, from transparent to dark brown, within 15 min and a surface resonance peak at 460 nm in the UV–visible spectrum. The FTIR spectra confirmed the involvement of various biomolecules in the synthesis of AgNPs. The average diameter of these spherical AgNPs was 67 nm, as shown by the scanning electron micrograph. The inhibition zones showed that the synthesized nanoparticles inhibited the growth of Gram-positive and negative bacteria. FRAP and DPPH assays were used to demonstrate the antioxidant potential of AgNPs. The highest value of FRAP (50.47% AAE/mL) was detected at a concentration of 90 ppm and a DPPH scavenging activity of 69.63% GAE was detected at a concentration of 20 µg/mL of the synthesized AgNPs. 500 µg/mL of the synthesized AgNPs were quite efficient in causing 91.78% denaturation of ovalbumin. The AgNPs mediated by A. lycoctonum also showed an inhibitory effect on α-amylase. Therefore, AgNPs synthesized from A. lycoctonum may serve as potential candidates for antibacterial, antioxidant, anti-inflammatory, and antidiabetic agents.

Phytochemical composition, anti-amylase and anti-acetylcholinesterase activities of leaf extracts and herbal tea of Dolichandrone serrulata (DC.) seem

The number of elderly population is continually growing in Thailand. Major health problems mostly occurred in the elder are non-communicable diseases namely Alzheimer's disease and type 2 diabetes mellitus. In current study, phytochemical composition, anti-amylase and anti-acetylcholinesterase activities of leaf extracts and herbal tea from Dolichandrone serrulata (DC.) Seem were determined. The result showed that extracts and herbal tea samples of D. serrulata leaves had effective in inhibition of amylase (an effective concentration at half maximum (EC50) = 1.21 to 23.80 mg/ml) and acetylcholinesterase activities (EC50 = 2.63 to 49.55 mg/ml). The effect of infusion time on the inhibition of amylase indicated that the best infusion time for preparing herbal tea beverage was 3 min, while the inhibition of acetylcholinesterase was 5 min. The fourier transform infrared spectroscopy (FTIR) and gas chromatograph - mass spectrometer (GC–MS) data indicated the presence of phytochemicals in the extracts and herbal tea samples related to phenolic compounds and flavonoids. The principal component analysis (PCA) result from FTIR data could discriminate herbal tea samples from the ethanol and aqueous extracts better than the PCA biplot of anti-amylase activity and anti-acetylcholinesterase activity.

LC-MS/MS and GC-MS profiling, antioxidant, enzyme inhibition, and antiproliferative activities of Thymus leucostomus H ausskn. & V elen. extracts.

The chemical composition as well asantioxidant, antiproliferative, and enzyme inhibition activities of extracts from aerial parts of Thymus leucostomus H ausskn. & V elen. obtained with hexane, methanol, and water were evaluated. Results showed that the methanol extract had significantly (p < 0.05) the highest total phenolic content (TPC; 107.80 mgGAE/g) and total flavonoids content (TFC; 25.21 mg RE/g) followed by the aqueous extract (102.72 mg GAE/g and 20.88 mg RE/g, respectively). LC-MS/MS-guided profiling of the three extracts revealed that rosmarinic acid (34.8%), hesperetin (42.9%), and linoleic acid (18%) were the dominant compounds in the methanol, aqueous and hexane extracts, respectively. GC-MS analysis of the hexane extract showed that ɣ-sitosterol (29.9%) was the major constituent. The methanol extract displayed significantly (p < 0.05) the highest Cu++ , Fe+++ , and Mo(VI) ions scavenging and reducing properties while the aqueous extract exerted significantly (p < 0.05) the highest metal chelating power (42.51 mg EDTAE/g). Both the hexane and methanol extracts effectively inhibited the acetylcholinesterase enzyme (2.63 and 2.65 mg GALAE/g, respectively) while the former extract exerted significantly (p < 0.05) the highest butyrylcholinesterase (2.32 mg GALAE/g), tyrosinase (19.73 mg KAE/g), and amylase (1.16 mmol ACAE/g) inhibition capacity. The aqueous extract exhibited the best glucosidase inhibition property (0.49 mmol ACAE/g). The methanol and hexane extracts exerted a higher cytotoxic effect on HT-29 (IC50 : 8.12 µg/mL) and HeLa (IC50 = 8.08 µg/mL) cells, respectively. In conclusion, these results provide valuable insight into the potential use of T. leucostomus bioactive extracts in different pharmaceutical applications.

Pharmacognostical and Pharmacological Evaluation of leaves of Citrullus lanatus L.

Citrullus lanatus (Watermelon) is commonly available throughout India and traditionally used in treatment of various ailments. This plant is well-explored for its fruit but the potential of its leaves is still unexplored. Thus, the present study focuses on pharmacognostical and pharmacological evaluation of leaves of Citrullus lanatus. In pharmacognostical evaluation, all macroscopic, microscopic, qualitative, quantitative and microbiological analysis were performed. In pharmacological evaluation, the study mainly focuses on the potential of leaves for antioxidant and antidiabetic activities. The antioxidant activity has been performed by various methods such as DPPH and phospho-molybdenum method. The antidiabetic activity has been performed by non-enzymatic glycosylation of hemoglobin assay method, glucose uptake in yeast cells method, alpha amylase inhibition assay method and alpha glucosidase inhibition assay method. The results of antioxidant activity shows that the plant extract possess good free radical scavenging properties due to the presence of vitamin C, polyphenol and flavonoid content. The results of antidiabetic activity by non-enzymatic glycosylation method shows that the plant extract of C. lanatus exhibit significant inhibition of glycosylation as compared with standard drug alpha tocopherol. In glucose uptake by yeast cells method, the extract showed greater efficiency in increasing the glucose uptake by yeast cells as compared to standard drug acarbose. In alpha amylase inhibition method, Alpha amylase inhibitors bind to alpha bond of polysaccharide and prevent breakdown of polysaccharide in mono and disaccharide which shows significant activity of plant extract as compared to an acarbose standard drug. Thus from the above findings, it can be concluded that C. lanatus leaves possess a great potential for antioxidant and antidiabetic activity and this plant should be more researched and formulation should be marketed in the recent future.&#x0D; Keywords: Citrullus lanatus (Cucurbitaceous), Watermelon, Anti-oxidant Activity, Anti-diabetic Activity

A comprehensive assessment of phytochemicals from Phyla nodiflora (L.) Greene as a potential enzyme inhibitor, and their biological potential: An in-silico, in-vivo, and in-vitro approach

This work explored Phyla nodiflora (L.) Greene as a potential source of the bioactive medicinal agent. In this aspect, methanol (PN-M) and dichloromethane (PN-D) extracts were prepared from the whole plant and evaluated for phytochemical composition (total bioactive contents, UHPLC-MS analysis, and HPLC-PDA polyphenolic quantification), biological (antioxidant and enzyme inhibition) potential and in-vivo toxicity. The PN-M was found to contain higher phenolic (26.08 mg GAE/g extract) and flavonoid (50.25 mg QE/g extract) contents which might correlate to the higher radical scavenging (DPPH: 52.94 mg TE/g extract; ABTS: 72.11 mg TE/g extract) and reducing power (FRAP: 71.96 mg TE/g extract; CUPRAC: 142.65 mg TE/g extract) antioxidant potential, as well as AChE (4.33 mg GALAE/g extract), tyrosinase (125.36 mg KAE/g extract), and amylase (1.86 mmol ACAE/g extract) inhibition activity of this extract. In contrast, the PN-D extract was found to be most active for phosphomolybdenum (1.30 mg TE/ g extract) and metal chelation (54.84 mg EDTAE/g extract) assays in addition to BChE (4.70 mg GALAE/g extract) and glucosidase (0.62 mmol ACAE/g extract) enzyme inhibition activity. The PN-M extract on UHPLC-MS analysis revealed the tentative identification of 24 different secondary metabolites, most of which belonged to the flavonoid, glycoside, and terpenoid classes of phytochemicals. The polyphenolic composition of the extracts was appraised by HPLC-PDA. Seven phenolic compounds were identified in the extracts. PN-M was found to be rich in catechin (0.25 µg/extract) and 3-OH benzoic acid (0.64 µg/extract), while PN-D contained epicatechin (0.30 µg/extract), 3-OH-4-MeO benzaldehyde (0.21 µg/extract), and 2,3-Di-Meo benzoic acid (0.97 µg/extract) in higher amounts. The methanol extract was found to be non-toxic even at higher doses. Furthermore, the relationship between the phytochemicals and the tested enzymes was highlighted by molecular docking studies. In sum, this research showed that the studied extracts were effective as enzyme inhibitors and antioxidants, suggesting it would be worth investigating in more depth for further advanced studies to explore its pharmacological properties.

A Comparative In Vitro Study on Potential of Anti-Diabetic and Anti-Oxidant Properties in Extracts of Allium Hypsistum, Allium Przewalskanium and Allium Wallichii

Allium hypsistum, Allium przewalskanium, and Allium wallichii are among the plants which are found at high altitude of Himalayan region. This in-vitro study has been focused on anti-diabetic and antioxidant properties of selected plants taken from Nepal region. Antidiabetic property was determined by in-vitro α- amylase inhibition method. Alcoholic extract of Allium hypsistum showed greatest α-amylase inhibitory action about 80% with an IC50 worth of 1.10 milligram/ ml followed by Allium przewalskanium which showed about 66% inhibition with an IC50 worth of 1.48 milligram/ ml. The antioxidant activities were evaluated using total phenolic content (TPC) and 2, 2-diphenyl -1-picrylhydrazyl (DPPH) radical scavenging assay method. Ethanolic extract of A. hypsistum showed the highest DPPH free radical scavenging property 67% as compared to reference ascorbic acid (75%). Among selected three plants, both TPC and %RSA revealing the antioxidant activities were found to be higher in A. hypsistum followed by A. prsewalskanium and A. wallichii.

Synthesis, characterization, DFT studies and biological assessment of palladium(II) complexes with imidazole derivatives

Six palladium(II) complexes (1–6) with 2-phenylimidazole (L1) and 1,2-dimethylimidazole (L2), were synthesized and characterized by elemental analyses, IR and NMR spectroscopy. The crystal structure of one of them ([Pd(2-phenylimidazole)2Br2], 1) was determined by X-ray crystallography. The palladium(II) ion in complex 1 is coordinated by two nitrogen atoms of 2-phenylimidazole and two bromide ions at trans positions, adopting a nearly regular square planar geometry. The structures of PdBr2 complexes {[Pd(2-phenylimidazole)2Br2] (1) and [Pd(1,2-dimethylimidazole)2Br2] (4)} as well as their chloride analogues, {[Pd(2-phenylimidazole)2Cl2] (1a) and [Pd(1,2-dimethylimidazole)2Cl2] (4a)} were predicted by DFT calculations. Complexes 1 and 1a appeared to be stabilized by a weak agostic interaction between palladium and hydrogen atoms. The energy of Pd⋯H bond was estimated to be 1.6 kcal/mol for both complexes that was comparable to the strength of Cl⋯H hydrogen bond in 1a (1.7 kcal/mol). The complexes were examined for various biological activities including; antimicrobial, antioxidant and anti-diabetic assays. The complexes exhibited moderate antimicrobial activities but they were not good as antioxidants. However, the alpha amylase inhibition assay showed the excellent anti-diabetic effect of the complexes.