Enzyme Inhibitory Activity Research Articles

Compositional changes and physiological activities of fresh ginseng extracts prepared at various temperatures in subcritical water

BackgroundSubcritical water (SW) is regarded as an effective conversion technology for lignocellulosic biomass. The effect of SW on ginseng are limited to evaluate the ginsenoside composition of red ginseng, and there is little information on the effects of SW on fresh ginseng. MethodsThe general characteristics of ginseng extracts (GE) prepared with SW were evaluated in terms of brix, reducing sugar and residual solid content, and compositions of GE was estimated using chromatography. For utilization of GE as a bioactive food, the ginsenoside composition, antioxidative activity, angiotensin-converting enzyme (ACE) inhibitory activity, prebiotic potential and taste attributes were measured. ResultsIncreasing SW temperature decreased residual solid content of ginseng and the soluble compounds of GE were yielded by SW at 250 °C. Despite that ginsenoside content decreased with SW temperature, a steep increase in Rg5 was observed at 200 °C. The SW at 200–250 °C manifested the highest antioxidant activities and ACE inhibitory activity of GE. However, the GE prepared at greater than 250 °C completely lost prebiotic potentials. Based on electronic-tongue, umami taste was enhanced by SW at 200 °C, but sweetness and bitterness were dominated at 250–300 °C. ConclusionThe results demonstrated that SW has a potential application to convert lignocellulosic wastes generated from ginseng roots into bioactive food resource, and SW at ∼200 °C can be potentially used to enhance the physiological activities of GE.

Cytotoxic, antioxidant, and enzyme inhibitory activities of Centaurea stapfiana extracts and their HPLC-ESI-QTOF-MS profiles: Insights into an unexplored Centaurea species

The members of the genus Centaurea have a great interest in pharmaceutical and nutraceutical fields due to their biological potential. Based on this information, we aimed to evaluate the biological properties (antioxidant, enzyme inhibition and cytotoxicity) and chemical profile of the extract of Centaurea stapfiana, an unstudied species. The highest total phenolic content was found in the ethanol/water extract with 32.17 mg GAE/g. A total of 102 of them were identified by HPLC-ESI-QTOF-MS analysis. These compounds were mainly hydroxybenzoic acid and hydroxycinnamic acid as well as flavonoids. In the antioxidant tests, the ethanol/water extract had the best free radical scavenging and reducing ability. However, in the enzyme inhibition test, the ethanol extract was the most active. The extracts were also tested on two tumour cell lines (RAW 264.7 and HepG2) and one non-tumour cell line (S17). The ethanol extract showed the promising effect on HepG2 (cell viability: 28.6 % at 50 g/ml). Furthermore, we examined the interactions between the compounds and enzymatic and cellular targets. A good interaction was found between quercetin-3-xylosyl-(1- > 6)-glucoside and iNOS. In summary, our results suggest that C. stapfiana can be considered as a versatile raw material for the development of health-promoting applications in the pharmaceutical and cosmeceutical fields.

Synthesis, Characterization, DPPH Radical Scavenging, Urease Enzyme Inhibition, Molecular Docking Simulation, and DFT Analysis of Imine Derivatives of 4-formylpyridine with Selective Detection of Cu+2 Ions.

This study aimed to prepare three imine derivatives (1, 2, and 3) via a condensation reaction of phenyl hydrazine, 2-hydrazino pyridine, and 4-methoxy aniline with 4-formyl pyridine. Electron impact mass spectrometry (EIMS), proton nuclear magnetic resonance (1H-NMR), ultraviolet-visible (UV-Vis) and Fourier transform infrared (FTIR) spectroscopy were utilized for the characterization. The chemosensing properties of [4((2-phenyl hydrazono)methyl) pyridine] (1), [2-(2-(pyridin-4-ylmethylene)hydrazinyl) pyridine] (2), and [4-methoxy-N-yl methylene) aniline] (3) imino bases have been explored for the first time in aqueous media. The photophysical properties of chemosensors (1, 2, and 3) were examined by various cations (Na+, NH4+, Ba+2, Ni+2, Ca+2, Hg+2, Cu+2, Mg+2, Mn+2, and Pd+2). The chemosensor (1) showed very selective binding capability with copper ions at low concentrations (20 μM) without the influence of any other mentioned ions. The maximum complexation was noted with Cu+2 and 1 at pH between 7 to 7.5. The stoichiometry binding ratio between chemosensor (1) and Cu+2 was determined by Job's plot and it was found to be 1:2. The current study explored the use of these Schiff bases for the first time as heterocyclic chemosensors. DPPH radical scavenging, urease enzyme inhibition activities, molecular docking simulation, and density functional theory (DFT) analysis of compounds 1, 2, and 3 were also conducted.

Combining chemical profiles and biological abilities of different extracts from Tanacetum nitens(Boiss. & Noë)Grierson using network pharmacology.

Tanacetum nitens(Boiss. & Noë)Grierson is an aromatic perennial herb used in Turkish traditional medicine to treat headache, fever, and skin diseases. This study aimed to investigate the chemical composition, antioxidant, enzyme inhibition, and cytotoxic properties of T. nitens aerial parts. Organic solvent extracts were prepared by sequential maceration in hexane, dichloromethane, ethyl acetate, and methanol while aqueous extracts were obtained by maceration or infusion. Nuclear magnetic resonance (NMR) and LC-DAD-MS analysis allowed the identification and quantification of different phytoconstituents including parthenolide, tanacetol B, tatridin B, quinic acid derivatives, β-sitosterol, and glycoside derivatives of quercetin and luteolin. The type and amount of these phytochemicals recovered by each solvent were variable and significant enough to impact the biological activities of the plant. Methanolic and aqueous extracts displayed the highest scavenging and ions-reducing properties while the dichloromethane and ethyl acetate extracts exerted the best total antioxidant activity and metal chelating power. Results of enzyme inhibition activity showed that the hexane, ethyl acetate, and dichloromethane extracts had comparable anti-acetylcholinesterase activity and the latter extract revealed the highest anti-butyrylcholinesterase activity. The best α-amylase and α-glucosidase inhibition activities were obtained from the hexane extract. The dichloromethane and ethyl acetate extracts exhibited the highest cytotoxic effect against the prostate carcinoma DU-145 cells. In conclusion, these findings indicated that T. nitens can be a promising source of biomolecules with potential therapeutic applications.

Design and synthesis of novel tetrahydronephthalene-1-amine based analogues as cholinesterase inhibitors

Inhibiting cholinesterase (ChE) such as AChE and BChE is thought to be one of the most effective treatments for Alzheimer’s disease (AD) and dementia. In the present work, a new facile method for (1S,4S)-4-(3,4-dichlorophenyl)-n-methyl-1,2,3,4-tetrahydronaphthalen-1-amine based analogues 4 (a–p) in good yield (66–93 %) were synthesized by refluxing demethylsertraline (2) with different aldehydes and ketones 3 (a–p). The newly synthesized analogues 4 (a–p) were characterized by physical and spectroscopic techniques for instance FTIR, LR-MS and HR-MS. The synthesized demethylsertraline based analogues 4 (a–p) were examined for their biological activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). In case of AChE activity, electron donating substituents have shown more inhibition as 4–hydroxyphenyl– (4b, IC50, 0.98 ± 0.99 µM) and 3,4–dimethoxyyphenyl– (4c, IC50, 1.0 ± 0.98 µM) and exhibited excellent binding affinity. In case of BChE activity, 4e consisting of electron withdrawing substituent has shown potent inhibition (1.26 ± 0.34 µM). Similarly, 4i and 4n depicted good inhibition with IC50 values 1.66 ± 0.78 µM and 1.66 ± 0.98 µM respectively as they possess weakly donating substituents. The structure activity relationship of BChE inhibition has shown opposite trend than AChE inhibition. It has been scrutinized that strong electron donating substituent decrease the BChE inhibitory activities whereas electron withdrawing groups greatly enhance the enzyme inhibition activity. In silico study of the synthesized compounds 4 (a–p) of the series was carried out. Compound 4b demonstrated excellent interaction with AChE compare with Eserine (standard) with a score of 6228 and an ACE value of –101.33 kcal/mol. Compound 4e demonstrated potent interaction with BChE compare with Eserine (standard) with a score of 6028 and ACE value of –258.53 kcal/mol. Compound 4b has the potential to serve as a lead molecule in medication development for Alzheimer’s disease treatment.

Algerian Prickly Pear Seed By-Products: Fatty Acids Composition, Antioxidant, Enzyme Inhibitory Activities towards Tyrosinase, Urease, α-Amylase, and Cholinesterase, along with the Ability to Protect from Thermal Protein Denaturation.

Prickly pear seed is a source of the most expensive oil in the world, which is rich in vitamins and polyunsaturated fatty acids. Its extraction generates a large quantity of press cake. These two by-products need to be valued. The current study aimed to assess the fatty acid composition of oil and the phytochemical composition of press cake. In addition, the antioxidant and the inhibition of thermal protein denaturation effects of both Algerian seed by-products were evaluated with their inhibitory action against the activities of urease, tyrosinase, α-amylase, and cholinesterase enzymes. The GC MS analysis result revealed the richness of our oil in linoleic (74%) and palmitic (13%) acids methyl esters, respectively. The chemical composition of press cake was characterized by a high value of dry matter (94.94 ± 0.05%), especially the carbohydrates (85.13 ± 0.94%). The results of antioxidant activity presented by IC50 and A0.5 ranged from 7.51 ± 0.03 to 88.10 ± 0.92 µg/mL. Furthermore, the IC50 values were 40.19 ± 1.21 and 61.18 ± 0.03 µg/mL in thermal protein denaturation assay, and ranging from 22.97 ± 0.72 to 385.99 ± 0.27 µg/mL for the inhibition of enzymatic activities. These results indicate that the studied oil can be one of the strongest oils for its impressive effects and also encourage us to reuse its press cake in feed livestock.

Peptidomics profiling and biological activities of grape pomace protein hydrolysates

Grape pomace protein isolate was hydrolysed by Alcalase, Flavourzyme and Protease either individually or in combination to produce hydrolysates with antihypertensive and antimicrobial properties. The degree of hydrolysis (DH) ranged between 22 and 52 % for Protease and Flavourzyme, respectively. Among all treatments, hydrolysates prepared using Flavourzyme exhibited the highest angiotensin-converting enzyme inhibitory (ACEi) activity, with an IC50 value of 91 μg/mL. The peptidomics analysis revealed that the peptides identified in Flavourzyme hydrolysate presented molecular features compatible with its bioactivity, like a high density of ACEi sequences per peptide. The hydrolysates were also able to inhibit the growth of Escherichia coli in a range between 9 and 54 % for Alcalase and Alcalase + Flavourzyme, respectively. Peptides in the most active hydrolysate evidenced a high occurrence of proline residues, which is a structural feature of some antimicrobial peptides.

Total Phenolics, Flavonoids, and ɑ-Glucosidase Inhibitory Activity of Red Betel (Piper crocatum) Extract in Various Solvents

Alpha-glucosidase enzyme activity needs to be inhibited to avoid increasing blood sugar levels in diabetics. Red betel leaf extract is reported to have active compounds such as phenolics and flavonoids that have alpha-glucosidase enzyme inhibition activity. Previous research showed that 70% betel leaf extract has an ɑ-glucosidase enzyme inhibition activity of 69.84%, but it is not yet known how the effect of extracts with different levels of polarity on the inhibition activity of alpha-glucosidase enzyme. This study aimed to determine extracts that have optimal levels of phenolic and flavonoid content and the highest suppression of α-glucosidase activity. The multistage maceration method was used to extract red betel leaf simplicia using solvents with different levels of polarity (n-hexane, ethyl acetate, methanol). Tests were conducted on overall phenolic concentration, flavonoids, and ɑ-glucosidase inhibition ability. Data were analyzed using one-way ANOVA test with Tukey's further test (p<0.05). The results of the assessment of phenolic concentration, flavonoids, and α-glucosidase inhibitory activity as a whole showed statistically significant differences (p<0.05) in all extracts with the highest total phenolic and flavonoid content found in the n-hexane extract of 25.68 ± 0.29 mg GAE/g and 65.84 ± 0.96 mg QE/g respectively. Meanwhile, methanol extract of red betel leaf became the best extract in this study with the greatest inhibition among all extracts with a percent α-glucosidase inhibition value of 43.87 ± 1.83%.

Integrating sodium cholate-modified MOF hybrid lipase and solubilization of hydrophobic candidates into a step for liganding fishing lipase inhibitors from Nelumbinis Folium

Enzyme immobilization by metal organic frameworks (MOFs) is an efficient way for screening active constituents in natural products. However, the enzyme’s biocatalysis activity is usually decreased due to unfavorable conformational changes during the immobilization process. In this study, sodium cholate was firstly used as the modifier for zeolitic imidazolate framework-8 (ZIF-8) immobilized lipase to increase both the stability and activity. More importantly, with the help of solubilization of sodium cholate, a total of 3 flavonoids and 6 alkaloids candidate compounds were fished out. Their structures were identified and the enzyme inhibitory activities were verified. In addition, the binding information between the candidate compound and the enzyme was displayed by molecular docking. This study provides valuable information for the improvement of immobilized enzyme activity and functional active ingredients in complicated medicinal plant extracts.

Synthesis of N-[trisubstitutedphenyl]-4-methyl Aniline Derivatives as Novel Anti-Breast Cancer Agents

A series of N-(substituted)-4-methyl aniline derivatives (4a,b, 5a,b, 6, 7, 8, and 9) has been designed and synthesized, and their biological activities were also evaluated as potential anti-tumor and tubulin enzyme inhibitors. Among all compounds, compound (8) showed the most potent tubulin aromatase enzyme inhibitory activity in vitro with an IC50 of 157.3 pg/mL compared to the reference inhibitor Dox (IC50 = 227.4 pg/mL). A docking simulation was performed to insert compound (8) into the crystal structure of human aromatase at the active site to determine the probable binding model. Based on the previous results, compound (8) with potent inhibitory activity on tumor growth could be employed as a potential anticancer agent.

Effect of Various Fruit Extracts on Angiotensin I-Converting Enzyme (ACE) and Kallikrein (KLK) Activities.

Hypertension is one of the main risk factors for cardiovascular disease and causes widespread morbidity and mortality worldwide. The aim of this work was to screen the fruit with high angiotensin I-converting enzyme (ACE) inhibitory activity and kallikrein (KLK) promotion activity by three different extraction methods from 22 kinds of fruits. Results showed that the aqueous extracts of fresh kiwifruit significantly inhibited ACE activity (47.71%), whereas the KLK activity was also inhibited (4.56%). This indicated that the substances inhibiting ACE activity existed in kiwifruit might be small molecular substances such as polyphenols. The nonpolar substance existed in the ethanol extracts of grape inhibited ACE activity significantly. The enzymatic hydrolysates of red grape significantly promoted KLK activity, whereas its ethanol extracts significantly inhibited KLK activity. This results suggested that the components that lower blood pressure and raise blood pressure are generally presented in the same fruit, the former are mostly water-soluble substances, while the latter are generally alcohol-soluble substances. If certain or individual components can be isolated from edible fruits, they may significantly affect blood pressure in humans.

Unveiling the diverse bioactivity of cobalt oxide nanoparticles produced through carboxymethyl cellulose extraction

This study explores an eco-friendly method for synthesizing Cobalt oxide nanoparticles (Co3O4NPs) using extracted carboxymethyl cellulose (CMC) as a reducing and stabilizing agent. The Co3O4NPs, characterized via various analyses, demonstrated a crystalline structure with sizes ranging from 10.9 to 28.2 nm. Microscopic imaging confirmed a uniform spherical morphology with an average diameter of 27.2 nm. The biological activities of Co3O4NPs were investigated extensively, highlighting their superior antibacterial efficacy compared to amoxicillin-clavulanic acid. These nanoparticles exhibited potent antioxidant properties and demonstrated safety for potential applications based on erythrocyte viability results. Additionally, Co3O4NPs displayed significant potency against Michigan Cancer Foundation-7 (MCF-7) breast cancer cells and showed promising α-amylase enzyme inhibitory activity, highlighting their multifunctional therapeutic potential as antioxidant, antibacterial, anticancer, and alpha-amylase inhibition assay.

Functional Peptides from Yak Milk Casein: Biological Activities and Structural Characteristics.

The average content of casein in yak milk is 40.2 g/L. Casein can be degraded by enzymatic digestion or food processing to produce abundant degradation peptides. International researchers have studied the degradation peptides of yak milk casein by using multiple techniques and methods, such as in vitro activity tests, cellular experiments, proteomics, bioinformatics, etc., and found that the degradation peptides have a wide range of functional activities that are beneficial to the human body, such as angiotensin-converting enzyme (ACE) inhibitory, antioxidant, anti-inflammatory, antidiabetic, antimicrobial, anticancer, and immunomodulatory activities, etc., and it has been proved that the types and strengths of functional activities are closely related to the structural characteristics of the peptides. This paper describes the characteristics of yak milk proteins, the functional activities, and mechanism of action of degraded peptides. Based on the types of functional activities of yak milk casein degradation peptides, we classified and elucidated the effects of structural factors, such as peptide molecular weight, peptide length, amino acid sequence, physicochemical properties, electrical charge, hydrophobicity, spatial conformation, chain length, and the type of enzyme on these activities. It reveals the great potential of yak milk casein degradation peptides as functional active peptide resources and as auxiliary treatments for diseases. It also provides important insights for analyzing yak casein degradation peptide activity and exploring high-value utilization.

Investigating the inhibitory effects of carotenoids-fortified Helix aspersa slime on oxidative stress, collagenase and tyrosinase enzyme activities.

The investigations of snail slime and its possible biological activities have been performed recently. This study aimed to evaluate the properties of Helix aspersa snail slime (HAS), and carotenoids-fortified slime (HASC). Snails were fed with carrots for 10 days. Slime was collected and extracted using water. Saponins identification, antioxidant, collagenase, and tyrosinase enzyme inhibition activities, carotenoids, total phenols, and flavonoids content, were determined. UHPLC-MS/MS analysis was performed for phytochemical characterization. Saponins were detected in the HAS extract only. However, HASC was shown to contain a higher carotenoid content than HAS (29.51 ± 0.4 vs. 18.11 ± 0.2 μg/g). similarly, total phenolic and flavonoid content were higher for the the HASC extract compared to the HAS (182.3 ± 5.2 vs. 150.28 ± 3.3 mg/g equivalent to gallic acid), and (77.62 ± 1.2 vs. 14.19 ± 0.9 mg/g equivalent to quercetin). As expected, the HASC extract exhibited higher antioxidant activity compared to the HAS, using DPPH and the ABTS assays (IC50 = 7.75 ± 0.14 vs. 20.1 ± 0.4 μg/mL), and (IC50 = 7.6 ± 0.26 vs. 19.57 ± 1.4 μg/mL). UHPLC-MS/MS analysis revealed the presence of several phytocomponents of which, hexadecanoic acid and ascorbic acid, were observed in the HASC extract. Furthermore, HASC extract exhibited superior inhibitory activity compared to HAS against collagenase and tyrosinase enzymes (IC50 = 8.4 ± 1.19 vs. 15.3 ± 1.12 μg/mL) and (IC50 = 30.1 ± 0.91 vs. 35 ± 1.3 μg/mL). These findings highlight the potential of HASC as a valuable ingredient in various pharmaceutical applications, due to their content of various phenolic, antioxidants, carotenoids, hexadecanoic, and ascorbic acids. The latter is well known for its great cosmeceutical applications used for slowing the process of skin aging.

In-silico based Designing of benzo[d]thiazol-2-amine Derivatives as Anal-gesic and Anti-inflammatory Agents.

Benzo[d]thiazoles represent a significant class of heterocyclic com-pounds renowned for their diverse pharmacological activities, including analgesic and anti-inflammatory properties. This molecular scaffold holds substantial interest among medicinal chemists owing to its structural versatility and therapeutic potential. Incorporating the benzo[d]thiazole moiety into drug molecules has been extensively investigated as a strategy to craft novel therapeutics with heightened efficacy and minimized adverse effects. The aim of the present research work was to design, synthesize and characterize the new benzo[d]thiazol-2-amine derivatives as potent analgesic and anti-inflammatory agents. The synthesis of the presented benzo[d]thiazol-2-amine derivatives was performed by condensing-(4-chlorobenzylidene) benzo[d]thiazol-2-amine with a number of substituted phenols in the presence of potassium iodide and anhydrous potassium carbonate in dry acetone. IR spectroscopy, 1HNMR spectroscopy, 13CNMR spectroscopy and Mass spectroscopy methods were used to characterize the structural properties of all 13 newly syn-thesized derivatives. The molecular properties of these newly synthesized derivatives were estimated to study the attributes of drug-like candidates. Benzo[d]thiazol-2-amine derivatives were molecularly docked with selective enzymes COX-1 and COX-2. Analgesic and anti-inflammatory activities of synthesized compounds were evaluated by us-ing albino rats. Findings of the research suggested that compounds G3, G4, G6, G8 and G11 possess higher binding affinity than diclofenac sodium, when docking was performed with enzyme COX-1. Compounds G1, G3, G6, G8andG10 showed lower binding affinity than Indometha-cin when docking was performed with enzyme COX-2.In vitro evaluation of the COX-1 and COX-2 enzyme inhibitory activities was performed for synthesized compounds. Compounds G10 and G11 exhibited significant COX-1 and COX-2 enzyme in-hibitory action with an IC50 value of 5.0 and 10 μM, respectively. Using the hot plate method and the carrageenan-induced rat paw edema model, the synthesized compounds were screened for their biological activities, including analgesic and anti-inflammatory activities. Highest analgesic action was exhibited by derivative G11 and the compound G10 showed the highest anti-inflammatory response. Inhibition of COX may be considered as a mechanism of action of these compounds. It was concluded that synthesized derivatives G10 and G11 exhibited significant analgesic and anti-inflammatory effect; therefore, the said compounds may be subjected to further clinical investigation for establishing these as future compounds for the treatment of pain and inflammation.

Presence of Modified Peptides with High Bioavailability and Angiotensin-Converting Enzyme Inhibitory Activity in Japanese Fermented Soybean Paste (Miso).

Not only free amino acids and normal short-chain peptides but also modified amino acids, such as N-acetyl- and N-formyl amino acids, monoamines, polyamines, and modified peptides, such as isomerized aspartyl peptides, pyroglutamyl peptides, and diketopiperazines, were identified in Japanese fermented soy paste (miso) prepared using different fungal starters, rice, barley, and soybean-koji. One hour after oral administration of water extract of soybean-koji miso to rats, the modified peptides increased significantly in the lumen upon the ingestion, while the normal peptides did not. In the blood from the portal vein and abdominal vena cava, 17 and 15 diketopiperazines, 16 and 12 isomerized aspartyl peptides, and 2 and 1 pyroglutamyl peptides significantly increased to approximately 10-400 nM, respectively. The modified peptides, which increased in rat blood, showed angiotensin-converting enzyme (ACE) inhibitory activity in a dose-dependent manner, indicating multiple ACE inhibitory peptides with high bioavailability in miso. Among them, l-β-Asp-Pro showed the highest ACE inhibitory activity (IC50 4.8 μM).

The leaf essential oil of Ecuadorian Ophryosporus peruvianus (J.F. Gmel.) R.M. King & H. Rob: chemical composition, enantioselective analysis, and in vitro enzymatic inhibitory activity

ABSTRACT An Ecuadorian specimen of Ophryosporus peruvianus produced an essential oil with a yield of 0.4% of the weight of the fresh plant material. A total of thirty-two compounds were detected and quantified. The chemical composition showed the predominance of monoterpene hydrocarbons, with sabinene (22.5%), β-pinene (15.1%), limonene (8.3%), β-phellandrene (29.7%), δ-elemene (2.1%), and epi-α-cadinol (2.7%) being the main components, expressed as mean values on two stationary phases of different polarity. This composition was very different from that reported in the literature for the essential oil of a Peruvian specimen, which was dominated by sesquiterpene hydrocarbons. These results indicate the existence of different chemotypes of O. peruvianus. Moreover, an enantioselective analysis of the major chiral constituents was performed, which revealed (R)-(-)-β-phellandrene, (R)-(-)-β-phellandrene and (1R,9R,E)-(-)-β-caryophylleneas enantiomerically pure compounds. On the other hand, β-thujene, β-pinene, β-pinene, sabinene, limonene, and terpinen-4-ol were scalemic mixtures. Finally, a preliminary screening of enzymatic inhibitory activity was performedin vitro, showing modest but interesting inhibition of both butyrylcholinesterase and lipase.

Comparative study on physicochemical properties and hypoglycemic activities of intracellular and extracellular polysaccharides from submerged fermentation of Morchella esculenta

The structural characteristic, physicochemical properties and structure-hypoglycemic activity relationship of intracellular (IPS) and extracellular (EPS) from submerged fermentation of Morchella esculenta were systematically compared and assessed. Both IPS and EPS were neutral, with a triple-helical conformation, and composed of galactose, glucose and mannose monosaccharides in different molar ratios. The molecular weight and particle size of IPS were higher than those of EPS. FTIR and SEM showed that the main functional group absorption peak intensity, glycosidic bond type and surface morphology of the two polysaccharides differed. Analysis of rheological and thermal properties revealed that the viscosity of IPS was higher than that of EPS, while thermal stability of EPS was greater than that of IPS. Hypoglycemic activity analysis in vitro showed that both IPS and EPS were non-competitive inhibitors of α-amylase and α-glucosidase. EPS showed strong digestive enzyme inhibitory activity due to its higher sulphate content and molar ratio of galactose, lower Mw and particle size. Meanwhile, with its higher Mw and apparent viscosity, IPS showed stronger glucose adsorption capacity and glucose diffusion retardation. These results indicate that IPS and EPS differed considerably in structure and physicochemical properties, which ultimately led to differences in hypoglycemic activity. These results not only suggested that IPS and EPS has the potential to be functional foods or hypoglycemic drugs, but also provided a new target for the prevention and treatment of diabetes with natural polysaccharides.

ESSENTIAL OIL CONTENTS AND BIOLOGICAL ACTIVITIES OF THYMUS CANOVIRIDIS JALAS AND THYMUS SIPYLEUS BOISS.

Objective: Members of the Lamiaceae family are considered to be major sources of bioactive therapeutic agents. Many of them are important medicinal and aromatic plants used in traditional and modern medicine and in the food, cosmetic and pharmaceutical industries. The aim of this study was to investigate in detail the biological activities and chemical composition of the essential oils of Thymus canoviridis Jalas and Thymus sipyleus Boiss. species belonging to the genus Thymus, one of the most important genera of the Lamiaceae family. Material and Method: The essential oil content of the species was determined by GC-MS. Antioxidant activities of the essential oils were determined using lipid peroxidation, DPPH free radical, ABTS cation radical and CUPRAC methods. In addition, cytotoxic activities against breast cancer (MCF-7) and colon cancer (HT-29) cell lines and anticholinesterase (against AChE and BChE enzymes), urease, tyrosinase, elastase, collagenase and angiotensin converting enzyme inhibition activities were determined. Result and Discussion: When the essential oil composition of T. sipyleus was analyzed, the major compounds were 1,8-cineole (eucalyptol) (18.16%), camphor (15.08%) and endo-borneol (11.63%), while T. canoviridis was found to be rich in carvacrol (72.88%). T. canoviridis showed high antioxidant activity in lipid peroxidation (IC50: 45.72±0.12 μg/ml), ABTS (IC50: 6.12±0.03 μg/ml) and CUPRAC (IC50: 5.31±0.01 μg/ml) methods. The selectivities of T. canoviridis and T. sipyleus species against MCF-7 cell line were 4.39 and 6.81, respectively. In the enzyme inhibition studies, both Thymus species showed moderate inhibition activity against BChE enzyme (Inhibition%: 57.88±1.14, 39.21±0.89, respectively). In addition, T. sipyleus showed moderate inhibition of elastase enzyme (Inhibition%: 25.33±0.79). When the results are evaluated in general, it can be said that T. canoviridis essential oil with its rich carvacrol content and high cytotoxic and antioxidant activity can be preferred as a safer and natural option instead of synthetic preservatives in food, pharmaceutical and cosmetic industries to extend shelf life and ensure food safety.

Phytochemical profile, bioactivity, and molecular docking studies of natural edible mushrooms grown in Tokat and Sivas provinces of Turkey.

Mushrooms have been essential to the human diet because they contain balanced chemical components and some biologically active substances. In this work, we investigated the phenolics, essential oils, metal contents, antioxidant, antibacterial, DNA protective, and enzyme inhibition activities for Clitocybe geotropa, Ramaria aurea, Rhizopogon luteolus (RL), Russula delica (RD), Verpa bohemica, and Marasmius oreades mushrooms. Results exhibited a higher content for citric and succinic acids in all tested kinds. Further, we detected a high content of cis-9-oleic acid, linoleate, and cis-11-eicosanoate. All mushroom species contain a significant percentage of both Cu and Zn. Moreover, RL and RD recorded the highest phenolic and flavonoid contents. Furthermore, all samples showed standard to good antioxidant activity, and the same is true for the antibacterial and DNA protective activities. Enzyme inhibition activity was generally high and significantly higher against the urease than the thiourea. We applied molecular docking between the highest phenolic molecules with the urease to determine the mushroom extracts' high inhibition mechanism. In conclusion, all mushroom species revealed a variety in chemical content that is probably related to their multi-bioactivity.