Search

Leontice smirnowii is a member of the Berberidaceae family. In the current study we investigated the possible antiradical and antioxidant activity of the monodesmosides (MLS) and crude extract (CELS) of [...]

Amaç: Bu araştırmanın amacı, hemşirelik öğrencilerinin terapötik iletişim becerilerini belirlemektir. Yöntem: Tanımlayıcı tipte olan bu araştırma, 7-18 Haziran 2021 tarihinde bir üniversitenin sağlık yüksekokulu hemşirelik bölümünde okuyan ve araştırmaya katılmaya gönüllü olan 143 öğrenci ile gerçekleştirildi. Araştırma için üniversitenin etik kurulundan ve kurumdan yazılı izin alındı. Çalışma verileri Google Forms üzerinden hazırlanan anket aracılığıyla online olarak toplandı. Veri toplamak için araştırmacılar tarafından hazırlanan “Öğrenci Tanıtıcı Bilgi Formu” ve “Hemşirelik Öğrencileri İçin Terapötik İletişim Becerileri Ölçeği” kullanıldı. Bulgular: Araştırmaya katılan öğrencilerin tümü 18 yaş ve üstü, %87,4’ünü kadın, %49,7’sinin 3. sınıf öğrencisi olduğu belirlendi. Öğrencilerin %79,7’sinin iletişim veya kişilerarası ilişkiler dersi aldığı ve akademik başarı algı durumlarına bakıldığında %50,3’ünün başarılı olduğunu belirttiği görüldü. Öğrencilerin %44,1’i iyi düzeyde sosyal ilişkilere sahip olduğunu ifade etti. Hemşirelik Öğrencileri İçin Terapötik İletişim Becerileri Ölçeği’nden minimum 16 maximum 97 puan alan öğrencilerin puan ortalaması 66,76 (±13,66) bulundu. Öğrencilerin sosyal ilişki düzeyi algısına göre Hemşirelik Öğrencileri İçin Terapötik İletişim Becerileri Ölçeği puan ortalamaları arasında istatistiksel açıdan anlamlı fark olduğu belirlendi. Sonuç: Çalışmada hemşirelik öğrencilerin terapötik iletişim ölçek puan ortalamasının orta düzeyde olduğu görüldü.

Grapes (Vitis vinifera), grape extracts, and grape products are known to possess beneficial effects. Antioxidant activity and enzyme inhibition activities of Tayfi grape (Vitis vinifera) extracts were studied and compared to standards. The IC50 values of the ethanol extract of the Tayfi grape’s scavenging abilities for ABTS˙+ and DPPH˙ radicals were found to be 5.9 and 16.1 μg/mL, respectively, higher than those of positive controls. Also, the phenolic and flavonoid ingredients of the Tayfi grape seed ethanol extract were measured to be 82.8 mg GAE/g and 91 mg QE/g. The Tayfi grape seed water and ethanol extracts exhibited IC50 values of 5.3 and 5.8 μg/mL toward α-glycosidase, respectively; 385.2 and 567.6 μg/mL toward α-amylase; 27.1 and 13.8 μg/mL toward acetylcholinesterase (AChE); and 54.7 and 12.6 μg/mL toward CA II. Twenty-two biomolecules were detected by LC-MS/MS. The four types of conventional antibiotics utilized by hospitals proved ineffective against Staphylococcus aureus and Escherichia coli bacteria. The Tayfi grape ethanol and water extracts had high AChE, α-glycosidase, and CA II inhibitions in addition to having antioxidant activity. The use of Tayfi grape extracts for pharmacological purposes in individuals with the diseases mentioned above can be sustained by clinical pharmacology studies.

Streptococcus mutans is important in dental caries. Although the role of cytokines in the pathogenesis of dental caries is not clear, components of S. mutans were found to stimulate production of pro-inflammatory cytokines. We examined the associations of interleukin (IL)-1β, IL-1 receptor antagonist (IL-1ra), and IL-10 with dental caries. Unstimulated whole saliva and blood samples were obtained from 108 children aged 6-12 years with high caries (decayed, missing, or filled teeth [dmft/DMFT] index >4, n = 37), moderate caries (dmft/DMFT = 1-4, n = 37), or caries-free (dmft/DMFT = 0, n = 34). S. mutans level was classified as low (<105 colony-forming units [CFU]/mL) or high (>105 CFU/mL). Saliva and serum concentrations of IL-1β, IL-1ra, and IL-10 were determined by ELISA. IL-1β, IL-1ra, and IL-10 gene polymorphisms were genotyped using PCR and restriction fragment length polymorphism analysis. The chi -square, Mann-Vhitney U, one-way ANOVA, posthoc, Fisher's exact, and t tests were used in statistical analysis. Dental caries was not correlated with salivary or serum concentrations of the studied cytokines. S. mutans level positively correlated with saliva IL-1β concentration and inversely correlated with saliva IL-1ra concentration. There was no correlation of IL-1β, IL-1ra, or IL-10 gene polymorphisms with dental caries. S. mutans is important in stimulating saliva IL-1β and inhibiting IL-1ra. Future studies of associations between cytokines and dental caries should investigate additional cytokines and enroll a larger number of participants. [ABSTRACT FROM AUTHOR]

The antioxidant activity of a triterpenoid glycoside [3-O-(beta-D-glucopyranosyl)-hederagenin; OGH] isolated from the berries of Hedera colchica, an ivy species endemic in Georgia, was investigated. The antioxidant properties of OGH were evaluated using different antioxidant assays: 1,1-diphenyl-2-picryl-hydrazyl free radical (DPPH.) scavenging, total antioxidant activity, reducing power, superoxide anion radical (O2*-)) scavenging, hydrogen peroxide (H2O2) scavenging and metal chelating activities. The total antioxidant activity was measured according to the ferric thiocyanate method. alpha-Tocopherol and trolox, a water-soluble analogue of tocopherol, were used as reference antioxidant compounds. At a 30 microg/mL concentration, the inhibitory effects of OGH on the peroxidation of linoleic acid emulsion was found to be 95.3%, whereas alpha-tocopherol and trolox exhibited 88.8% and 86.2% inhibition of peroxidation in the system, respectively. In addition, OGH had effective DPPH. scavenging, superoxide anion radical scavenging, hydrogen peroxide scavenging, total reducing power and metal chelation of ferrous ions activities. These various antioxidant activities were compared with alpha-tocopherol and trolox. [ABSTRACT FROM AUTHOR]

Abstract Background In situ hybridization (ISH) is a powerful method for visualizing gene expression patterns at the organismal level with cellular resolution. When automated, it is capable of determining the expression of a large number of genes. Results The expression patterns of 662 genes that encode enzymes were determined by ISH in the mid-gestation mouse embryo, a stage that models the complexity of the adult organism. Forty-five percent of transcripts encoding metabolic enzymes (n = 297) showed a regional expression pattern. A similar percentage was found for the 190 kinases that were also analyzed. Many mRNAs encoding glycolytic and TCA cycle enzymes exhibited a characteristic expression pattern. The annotated expression patterns were deposited on the Genepaint database and are retrievable by user-defined queries including gene name and sites of expression. Conclusion The 662 expression patterns discussed here comprised gene products with activities associated with catalysis. Preliminary analysis of these data revealed that a significant number of genes encoding housekeeping functions such as biosynthesis and catabolism were expressed regionally, so they could be used as tissue-specific gene markers. We found no difference in tissue specificity between mRNAs encoding housekeeping functions and those encoding components of signal transduction pathways, as exemplified by the kinases.

Objectives: Five solvent extracts (n-hexane, ethyl acetate, ethanol, ethanol/water (70%), and water) of Gladiolus italicus Mill. from Turkey were evaluated for chemical and biological properties., Methods: Antioxidant activities, inhibitory properties against key enzymes involved in the etiology of chronic diseases were tested, as well as cytotoxic effects on different cell lines. Chemical characterization was also carried out to determine the most abundant compounds of each extract., Results: The highest total phenolic content (TPC) was observed in the water extract while highest TFC in ethanol/water extract. The most abundant compounds in the extracts were hyperoside (69041.06 mg kg -1 ), isoquercitrin (46239.49 mg kg -1 ), delphindin-3,5-diglucoside (42043.81 mg kg -1 ), myricetin (21486.61 mg kg -1 ), and kaempferol-3-glucoside (21199.76 mg kg -1 ). Molecular dynamic (MD) simulations confirmed the structural stability and dynamic conformational integrity of these complexes over a period of 100 ns. In network pharmacology, A total of 657 unique target genes were screened: 52 associated with programmed cell death-1 (PD-1), 85 with vascular endothelial growth factor receptor-2 (VEGFR2), and 130 with fibroblast growth factor receptor-2 (FGFR2), identifying crucial gene interactions for these proteins. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted, revealing significant interactions and pathways such as the advanced glycation end products (AGE) and their receptors (RAGE) signaling pathway in diabetic complications and T- helper 17 (Th17) cell differentiation, among others. This elucidation of complex networks involving key genes like AKT Serine/Threonine Kinase 1 (AKT1), MYC proto-oncogene (MYC), tumor protein 53 (TP53), Interleukin 6 (IL6), and tumor necrosis factor (TNF) provides a promising foundation for the development of targeted therapies in the treatment of non-communicable diseases., Conclusion: These results show that G. italicus could be a natural source of potent antioxidants and enzyme inhibitors which need to be further explored for the development of biopharmaceuticals.

An important research topic is the discovery of multifunctional compounds targeting different disease-causing components. This research aimed to design and synthesize a series of 2-aryl-6-carboxamide benzoxazole derivatives that inhibit cholinesterases on both the peripheral anionic and catalytic anionic sides. Compounds (7-48) were prepared from 4-amino-3-hydroxybenzoic acid in three steps. The Ellman test, molecular docking with Maestro, and molecular dynamics simulation studies with Desmond were done (Schrodinger, 12.8.117). Compound 36, the most potent compound among the 42 new compounds synthesized, had an inhibitory concentration of IC 50 12.62 nM for AChE and IC 50 25.45 nM for BChE (whereas donepezil was 69.3 nM and 63.0 nM, respectively). Additionally, compound 36 had docking values ​​of - 7.29 kcal/mol for AChE and - 6.71 kcal/mol for BChE (whereas donepezil was - 6.49 kcal/mol and - 5.057 kcal/mol, respectively). Furthermore, molecular dynamics simulations revealed that compound 36 is stable in the active gorges of both AChE (average RMSD: 1.98 Å) and BChE (average RMSD: 2.2 Å) (donepezil had average RMSD: 1.65 Å and 2.7 Å, respectively). The results show that compound 36 is a potent, selective, mixed-type dual inhibitor of both acetylcholinesterase and butyrylcholinesterase. It does this by binding to both the catalytically active and peripheral anionic sites of cholinesterases at the same time. These findings show that target compounds may be useful for establishing the structural basis for new anti-Alzheimer agents., Competing Interests: Declarations. Conflict of interest: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2024. The Author(s).)

The present study reveals in vitro antioxidant properties and the phytochemical content of a novel Rheum species ( Rheum telianum ), which grows in Southeastern Anatolia. To perform the analysis, dried leaves and seeds of the plants were ground and extracted with ethanol to obtain plant secondary metabolites and antioxidant activity. Then, dried extracts were subjected to in vitro DPPH scavenging and Cupric reducing (CUPRAC), Fe 3+ , and Ferric reducing antioxidant power (FRAP). In addition to the antioxidant capacity assays, quantitative phenolic, flavonoid, and secondary metabolite were determined through spectrophotometric and LC-MS/MS chromatographic methods. IC 50 values showed that both leaves and the seeds of the R. telianum have high inhibitory properties over DPPH radicals with 20.79 and 5.67 μg/mL, respectively. The samples' dominant secondary metabolites were evaluated through the LC-MS/MS analysis results. The inhibition effects of both leaves and the seeds of the R. telianum extracts on acetylcholinesterase and butyrylcholinesterase, α-glycosidase and human carbonic anhydrases II isoenzyme enzymes, which associated with some global diseases including Alzheimer's disease, type-2 diabetes mellitus and glaucoma were determined. In conclusion, the extracts' contents and functional relationship and the plants' possible usage in the food, medicine, and cosmetic industries was revealed., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2025 The Authors.)

In current study antioxidant, antidiabetic, antimicrobial, anticholinesterase, and human carbonic anhydrase I, and II (hCA I and II) isoenzymes inhibition activities of Astrodaucus orientalis different parts were investigated. Achetylcholinesterse (AChE) and butyrylcholinesterse (BChE) inhibitory activities of octyl acetate were determined via molecular docking. Quantitative assessment of specific secondary metabolites was conducted using LC-MS/MS. An examination of chemical composition of essential oils was carried out by GC-MS/MS. A thorough exploration of plant's anatomical characteristics was undertaken. The highest phenolics level and DPPH antioxidant capacity were seen in root and fruit. Fruit essential oil demonstrated the highest AChE inhibition (44.13±3.61 %), while root dichloromethane sub-extract had the best inhibition towards BChE (86.13±2.58 %). Cytosolic hCA I, and II isoenzymes were influentially inhibited by root oil with 1.974 and 2.207 μM IC 50 values, respectively. The most effective extracts were found to be root all extract/sub-extracts (except water) against C. tropicalis and C. krusei strains with MIC value 160>μg/mL. Sabinene (29.4 %), α-pinene (20.2 %); octyl acetate (54.3 %); myrcene (28.0 %); octyl octanoate (71.3 %) were found principal components of aerial parts, roots, flowers, and fruits, respectively. Flower essential oil, fruit dicloromethane and ethyl acetate exhibited potent α-glucosidase inhibitory activity with 900, 40, and 937 μg/mL IC 50 values, respectively., (© 2023 Wiley-VHCA AG, Zurich, Switzerland.)

Baicalin is the foremost prevalent flavonoid found in Scutellaria baicalensis . It also frequently occurs in many multi-herbal preparations utilized in Eastern countries. The current research has assessed and compared the antioxidant, antidiabetic, anticholinergic, and antiglaucoma properties of baicalin hydrate. Baicalin hydrate was tested for its antioxidant capacity using a variety of techniques, including N,N-dimethyl-p-phenylenediamine dihydrochloride radical (DMPD •+ ) scavenging activity, 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonate) radical (ABTS •+ ) scavenging activity, 1,1-diphenyl-2-picrylhydrazyl radical (DPPH • ) scavenging activity, potassium ferric cyanide reduction ability, and cupric ions (Cu 2+ ) reducing activities. Also, for comparative purposes, reference antioxidants, such as butylated hydroxyanisole (BHA), Trolox, α-Tocopherol, and butylated hydroxytoluene (BHT) were employed. Baicalin hydrate had an IC 50 value of 13.40 μg/mL (r 2 : 0.9940) for DPPH radical scavenging, whereas BHA, BHT, Trolox, and α-Tocopherol had IC 50 values of 10.10, 25.95, 7.059, and 11.31 μg/mL for DPPH • scavenging, respectively. These findings showed that baicalin hydrate had comparably close and similar DPPH • scavenging capability to BHA, α-tocopherol, and Trolox, but it performed better than BHT. Additionally, apart from these studies, baicalin hydrate was tested for its ability to inhibit a number of metabolic enzymes, including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase II (CA II), and α-glycosidase, which have been linked to several serious illnesses, such as Alzheimer's disease (AD), glaucoma, and diabetes, where the K i values of baicalin hydrate toward the aforementioned enzymes were 10.01 ± 2.86, 3.50 ± 0.68, 19.25 ± 1.79, and 26.98 ± 9.91 nM, respectively.

Onion contains many dietary and bioactive components including phenolics and flavonoids. Spiraeoside (quercetin-4-O-β-D-glucoside) is one of the most putative flavonoids in onion. Several antioxidant techniques were used in this investigation to assess the antioxidant capabilities of spiraeoside, including 1,1-diphenyl-2-picrylhydrazyl radical (DPPH·) scavenging, N,N-dimethyl-p-phenylenediamine radical (DMPD •+ ) scavenging, 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonate) radical (ABTS •+ ) scavenging activities, cupric ions (Cu 2+ ) reducing and potassium ferric cyanide reduction abilities. In contrast, the water-soluble α-tocopherol analogue trolox and the conventional antioxidants butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), and α-tocopherol were utilized as the standards for evaluation. Spiraeoside scavenged the DPPH radicals an IC 50 of 28.51 μg/mL (r 2 : 0.9705) meanwhile BHA, BHT, trolox, and α-tocopherol displayed IC 50 of 10.10 μg/mL (r 2 : 0.9015), 25.95 μg/mL (r 2 : 0.9221), 7.059 μg/mL (r 2 : 0.9614) and 11.31 μg/mL (r 2 : 0.9642), accordingly. The results exhibited that spiraeoside had effects similar to BHT, but less potent than α-tocopherol, trolox and BHA. Also, inhibitory effects of spiraeoside were evaluated toward some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase II (CA II) and α-glycosidase, which are related to a number of illnesses, such as Alzheimer's disease (AD), diabetes mellitus and glaucoma disorder. Spiraeoside exhibited IC 50 values of 4.44 nM (r 2 : 0.9610), 7.88 nM (r 2 : 0.9784), 19.42 nM (r 2 : 0.9673) and 29.17 mM (r 2 : 0.9209), respectively against these enzymes. Enzyme inhibition abilities were compared to clinical used inhibitors including acetazolamide (for CA II), tacrine (for AChE and BChE) and acarbose (for α-glycosidase). Spiraeoside demonstrated effective antioxidant, anticholinergic, antidiabetic and antiglaucoma activities. With these properties, it has shown that Spiraeoside has the potential to be a medicine for some metabolic diseases., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2023 The Author(s).)

Determining the antioxidant abilities and enzyme inhibition profiles of medicinally important plants and their oils is of great importance for a healthy life and the treatment of some common global diseases. Kiwifruit ( Actinidia deliciosa ) oil was examined and researched using several bioanalytical methods comprehensively for the first time in this research to determine its antioxidant, antiglaucoma, antidiabetic and anti-Alzheimer's capabilities. Additionally, the kiwifruit oil inhibitory effects on acetylcholinesterase (AChE), carbonic anhydrase II (CA II), and α-amylase, which are linked to a number of metabolic illnesses, were established. Furthermore, LC-HRMS analysis was used to assess the phenolic content of kiwifruit oil. It came to light that kiwifruit oil contained 26 different phenolic compounds. According to the LC-HRMS findings, kiwifruit oil is abundant in apigenin (74.24 mg/L oil), epigallocatechin (12.89 mg/L oil), caryophyllene oxide (12.89 mg/L oil), and luteolin (5.49 mg/L oil). In addition, GC-MS and GC-FID studies were used to ascertain the quantity and chemical composition of the essential oils contained in kiwifruit oil. Squalene (53.04%), linoleoyl chloride (20.28%), linoleic acid (2.67%), and palmitic acid (1.54%) were the most abundant compounds in kiwifruit oil. For radical scavenging activities of kiwifruit oil, 1,1-diphenyl-2-picryl-hydrazil (DPPH • ) and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS •+ ) radicals scavenging techniques were examined. These methods effectively demonstrated the potent radical scavenging properties of kiwifruit oil (IC 50 : 48.55 μg/mL for DPPH • , and IC 50 : 77.00 μg/mL for ABTS •+ scavenging). Also, for reducing capabilities, iron (Fe 3+ ), copper (Cu 2+ ), and Fe 3+ -2,4,6-tri(2-pyridyl)-S-triazine (TPTZ) reducing abilities were studied. Moreover, kiwifruit oil showed a considerable inhibition effect towards hCA II (IC 50 : 505.83 μg/mL), AChE (IC 50 : 12.80 μg/mL), and α-amylase (IC 50 : 421.02 μg/mL). The results revealed that the use of kiwifruit oil in a pharmaceutical procedure has very important effects due to its antioxidant, anti-Alzheimer, antidiabetic, and antiglaucoma effects.

In addition to the first synthesis of the natural bromophenol butyl 2-(3,5-dibromo-4-hydroxyphenyl)acetate (1), indene derivatives 34 and 35 were synthesized from 3-phenylpropenal derivatives in BBr 3 medium. Five known natural bromophenols and some derivatives were synthesized by known methods. Cholinesterase (ChEs) inhibitors reduce the breakdown of acetylcholine and are used in the treatment of Alzheimer's disease (AD) and dementia symptoms. The inhibition effects of all obtained compounds were examined towards acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and α-glycosidase enzymes. All synthesized compounds demonstrated the strong inhibition effects against both cholinergic enzymes. For determination of Ki values of novel bromophenols Lineweaver-Burk graphs were obtained. Ki values were found in the ranging of 0.13-14.74 nM for AChE, 5.11-23.95 nM for BChE, and 63.96-206.78 nM for α-glycosidase, respectively. All bromophenols and their derivatives exhibit effective inhibition profile when compared to positive controls., (© 2023 Wiley-VHCA AG, Zurich, Switzerland.)

In an attempt to identify potential active anticancer agents with low cytotoxic properties and CA inhibitors, a new series of hybrid compounds incorporating imidazole ring and hydrazone moiety as part of their structure were synthesized by aza-Michael addition reaction followed by intramolecular cyclization. The structure of synthesized compounds was elucidated using various spectral techniques. Synthesized compounds were evaluated for their in vitro anticancer (prostate cell lines; PC3) and CA inhibitory (hCA I and hCA II) activity. Among them, some compound displayed remarkable anticancer activity and CA inhibitory activity with K i values in range of 17.53±7.19-150.50±68.87 nM against cytosolic hCA I isoform associated with epilepsy, and 28.82±14.26-153.27±55.80 nM against dominant cytosolic hCA II isoforms associated with glaucoma. Furthermore, the theoretical parameters of the bioactive molecules were calculated to establish their drug-likeness qualities. The proteins used for the calculations are prostate cancer protein (PDB ID: 3RUK and 6XXP). ADME/T analysis was carried out to examine the drug properties of the studied molecules., (© 2023 Wiley-VHCA AG, Zurich, Switzerland.)

Astragalus species are traditionally used for diabetes, ulcers, leukemia, wounds, stomachaches, sore throats, abdominal pain, and toothaches. Although the preventive effects of Astragalus species against diseases are known, there is no record of the therapeutic effects of Astragalus alopecurus . In this study, we aimed to evaluate the in vitro antiglaucoma, antidiabetic, anti-Alzheimer's disease, and antioxidant activities of the methanolic (MEAA) and water (WEAA) extracts of the aerial part of A. alopecurus . Additionally, its phenolic compound profiles were analyzed by liquid chromatography-tandem mass spectrometry (LC-MS/MS). MEAA and WEAA were evaluated for their inhibition ability on α-glycosidase, α-amylase, acetylcholinesterase (AChE), and human carbonic anhydrase II (hCA II) enzymes. The phenolic compounds of MEAA were analyzed by LC-MS/MS. Furthermore, total phenolic and flavonoid contents were determined. In this context, the antioxidant activity was evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), N,N-dimethyl-p-phenylene diamine (DMPD), ferric reducing antioxidant power (FRAP), cupric ions (Cu 2+ ) reducing antioxidant capacity (CUPRAC), ferric ions (Fe 3+ ) reducing, and ferrous ions (Fe 2+ ) chelating methods. MEAA and WEAA had IC 50 values of 9.07 and 2.24 μg/mL for α-glycosidase, 693.15 and 346.58 μg/mL for α-amylase, 1.99 and 2.45 μg/mL for AChE, and 147.7 and 171.7 μg/mL for hCA II. While the total phenolic amounts in MEAA and WEAA were 16.00 and 18.50 μg gallic acid equivalent (GAE)/mg extract, the total flavonoid contents in both extracts were calculated as 66.23 and 33.115 μg quercetin equivalent (QE)/mg, respectively. MEAA and WEAA showed, respectively, variable activities on DPPH radical scavenging (IC 50 : 99.02 and 115.53 μg/mL), ABTS radical scavenging (IC 50 : 32.21 and 30.22 µg/mL), DMPD radical scavenging (IC 50 : 231.05 and 65.22 μg/mL), and Fe 2+ chelating (IC 50 : 46.21 and 33.01 μg/mL). MEAA and WEAA reducing abilities were, respectively, Fe 3+ reducing (λ 700 : 0.308 and 0.284), FRAP (λ 593 : 0.284 and 0.284), and CUPRAC (λ 450 : 0.163 and 0.137). A total of 35 phenolics were scanned, and 10 phenolic compounds were determined by LC-MS/MS analysis. LC-MS/MS revealed that MEAA mainly contained isorhamnetin, fumaric acid, and rosmarinic acid derivatives. This is the first report indicating that MEAA and WEAA have α-glycosidase, α-amylase, AChE, hCA II inhibition abilities, and antioxidant activities. These results demonstrate the potential of Astragalus species through antioxidant properties and enzyme inhibitor ability traditionally used in medicine. This work provides the foundation for further research into the establishment of novel therapeutics for diabetes, glaucoma, and Alzheimer's disease.

Sepsis is a serious systemic inflammatory response to infections. In this study, effects of thymol treatments on sepsis response were investigated. A total of 24 rats were randomly divided into 3 different treatment groups, namely as Control, Sepsis and Thymol. A sepsis model was created with a cecal ligation and perforation (CLP) in the sepsis group. For the treatment group, 100 mg/kg dose of thymol was administered via oral gavage and sepsis was established with a CLP after 1 h. All rats were sacrificed at 12 h post-opia. Blood and tissue samples were taken. ALT, AST, urea, creatinine and LDH were evaluated to assess the sepsis response in separated sera. Gene expression analysis was conducted for ET-1, TNF-α, IL-1 in lung, kidney and liver tissue samples. ET-1 and thymol interactions were determined by molecular docking studies. The ET-1, SOD, GSH-Px and MDA levels were determined by ELISA method. Genetic, biochemical and histopathological results were evaluated statistically. The pro-inflammatory cytokines and ET-1 gene expression revealed a significant decrease in the treatment groups, while there was an increase in septic groups. SOD, GSH-Px and MDA levels of rat tissues were significantly different in the thymol groups as compared to the sepsis groups (p < 0.05). Likewise, ET-1 levels were significantly reduced in the thymol groups. In terms of serum parameters, present findings were consistent with the literature. It was concluded based on present findings that thymol therapy may reduce sepsis-related morbidity, which would be beneficial in the early phase of the sepsis., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Ilhami Gulcin reports was provided by Ataturk University., (Copyright © 2023. Published by Elsevier B.V.)

Zivzik pomegranate ( Punica granatum ) has recently sparked considerable interest due to its nutritional and antioxidant properties. To evaluate the antioxidant capacities of P. granatum juice, ethanol (EEZP), and water (WEZP) extracts from peel and seed, the antioxidant methods of 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid radical (ABTS •+ ) scavenging, 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH • ) scavenging, Fe 3+ -2,4,6-tris(2-pyridyl)-S-triazine (TPTZ) reducing, Fe 3+ reducing, and Cu 2+ reducing methods were used. The antioxidant capacities of samples were compared with the most commonly used synthetic antioxidants, i.e., BHA, BHT, α-tocopherol, and Trolox. In terms of setting an example, the IC 50 values of EEZP for ABTS •+ and DPPH • scavenging activities were found to be lower than standards, at 5.9 and 16.1 μg/mL, respectively. The phenolic and flavonoid contents in EEZP peel were 59.7 mg GAE/g and 88.0 mg QE/g, respectively. Inhibition of α-glycosidase, α-amylase, acetylcholinesterase, and human carbonic anhydrase II (hCA II) enzymes was also investigated. EEZP demonstrated IC 50 values of 7.3 μg/mL against α-glycosidase, 317.7 μg/mL against α-amylase, 19.7 μg/mL against acetylcholinesterase (AChE), and 106.3 μg/mL against CA II enzymes. A total of 53 phenolic compounds were scanned, and 30 compounds were determined using LC-MS/MS. E. coli and S. aureus bacteria were resistant to all four antibiotics used as standards in hospitals.

The widespread usage of Schiff bases in chemistry, industry, medicine, and pharmacy has increased interest in these compounds. Schiff bases and derivative compounds have important bioactive properties. Heterocyclic compounds containing phenol derivative groups in their structure have the potential to capture free radicals that can cause diseases. In this study, we designed and synthesized eight Schiff bases ( 10 - 15 ) and hydrazineylidene derivatives ( 16 - 17 ), which contain phenol moieties and have the potential to be used as synthetic antioxidants, for the first time using microwave energy. Additionally, the antioxidant effects of Schiff bases ( 10 - 15 ) and hydrazineylidene derivatives ( 16 - 17 ) were studied using by the bioanalytical methods of 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) cation radical (ABTS •+ ) and 1,1-diphenyl-2-picrylhydrazyl (DPPH • ) scavenging activities, and Fe 3+ , Cu 2+ , and Fe 3+ -TPTZ complex reducing capacities. In the context of studies on antioxidants, Schiff bases ( 10 - 15 ) and hydrazineylidene derivatives ( 16 - 17 ) were found to be as powerful DPPH (IC 50 : 12.15-99.01 μg/mL) and ABTS •+ (IC 50 : 4.30-34.65 μg/mL). Additionally, the inhibition abilities of Schiff bases ( 10 - 15 ) and hydrazineylidene derivatives ( 16 - 17 ) were determined towards some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCAs I and II), enzymes that are linked to some global disorders including Alzheimer's disease (AD), epilepsy, and glaucoma. In the context of studies on enzyme inhibition, it was observed that the synthesized Schiff bases ( 10 - 15 ) and hydrazineylidene derivatives ( 16 - 17 ) inhibited AChE, BChE, hCAs I, and hCA II enzymes with IC 50 values in ranges of 16.11-57.75 nM, 19.80-53.31 nM, 26.08 ± 8.53 nM, and 85.79 ± 24.80 nM, respectively. In addition, in light of the results obtained, we hope that this study will be useful and guiding for the evaluation of biological activities in the fields of the food, medical, and pharmaceutical industries in the future.

Propolis is a complex natural compound that honeybees obtain from plants and contributes to hive safety. It is rich in phenolic and flavonoid compounds, which contain antioxidant, antimicrobial, and anticancer properties. In this study, the chemical composition and antioxidant activities of propolis were investigated; ABTS •+ , DPPH • and DMPD •+ were prepared using radical scavenging antioxidant methods. The phenolic and flavonoid contents of propolis were 53 mg of gallic acid equivalent (GAE)/g and 170.164 mg of quercetin equivalent (QE)/g, respectively. The ferric ion (Fe 3+ ) reduction, CUPRAC and FRAP reduction capacities were also studied. The antioxidant and reducing capacities of propolis were compared with those of butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), α-tocopherol and Trolox reference standards. The half maximal inhibition concentration (IC 50 ) values of propolis for ABTS •+ , DPPH • and DMPD •+ scavenging activities were found to be 8.15, 20.55 and 86.64 μg/mL, respectively. Propolis extract demonstrated IC 50 values of 3.7, 3.4 and 19.6 μg/mL against α-glycosidase, acetylcholinesterase (AChE) and carbonic anhydrase II (hCA II) enzyme, respectively. These enzymes' inhibition was associated with diabetes, Alzheimer's disease (AD) and glaucoma. The reducing power, antioxidant activity and enzyme inhibition capacity of propolis extract were comparable to those demonstrated by the standards. Twenty-eight phenolic compounds, including acacetin, caffeic acid, p-coumaric acid, naringenin, chrysin, quinic acid, quercetin, and ferulic acid, were determined by LC-MS/MS to be major organic compounds in propolis. The polyphenolic antioxidant-rich content of the ethanol extract of propolis appears to be a natural product that can be used in the treatment of diabetes, AD, glaucoma, epilepsy, and cancerous diseases.

In this study, for the first time, the antioxidant and antidiabetic properties of the essential oil from cinnamon ( Cinnamomum zeylanicum ) leaves were evaluated and investigated using various bioanalytical methods. In addition, the inhibitory effects of cinnamon oil on carbonic anhydrase II (hCA II), acetylcholinesterase (AChE), and α-amylase, which are associated with various metabolic diseases, were determined. Further, the phenolic contents of the essential oil were determined using LC-HRMS chromatography. Twenty-seven phenolic molecules were detected in cinnamon oil. Moreover, the amount and chemical profile of the essential oils present in cinnamon oil was determined using GC/MS and GC-FID analyses. ( E )-cinnamaldehyde (72.98%), benzyl benzoate (4.01%), and trans -Cinnamyl acetate (3.36%) were the most common essential oils in cinnamon leaf oil. The radical scavenging activities of cinnamon oil were investigated using 1,1-diphenyl-2-picryl-hydrazil (DPPH • ), 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid), and (ABTS •+ ) bioanalytical scavenging methods, which revealed its strong radical scavenging abilities (DPPH • , IC 50 : 4.78 μg/mL; and ABTS •+ , IC 50 : 5.21 μg/mL). Similarly, the reducing capacities for iron (Fe 3+ ), copper (Cu 2+ ), and Fe 3+ -2,4,6-tri(2-pyridyl)-S-triazine (TPTZ) were investigated. Cinnamon oil also exhibited highly effective inhibition against hCA II (IC 50 : 243.24 μg/mL), AChE (IC 50 : 16.03 μg/mL), and α-amylase (IC 50 : 7.54μg/mL). This multidisciplinary study will be useful and pave the way for further studies for the determination of antioxidant properties and enzyme inhibition profiles of medically and industrially important plants and their oils.

In this work, nine new bromophenol derivatives were designed and synthesized. The alkylation reactions of (2-bromo-4,5-dimethoxyphenyl)methanol ( 7 ) with substituted benzenes 8 - 12 produced new diaryl methanes 13 - 17 . Targeted bromophenol derivatives 18 - 21 were synthesized via the O-Me demethylation of diaryl methanes with BBr3. Moreover, the synthesized bromophenol compounds were tested with some metabolic enzymes such as acetylcholinesterase (AChE), carbonic anhydrase I (CA I), and II (CA II) isoenzymes. The novel synthesized bromophenol compounds showed Ki values that ranged from 2.53 ± 0.25 to 25.67 ± 4.58 nM against hCA I, from 1.63 ± 0.11 to 15.05 ± 1.07 nM against hCA II, and from 6.54 ± 1.03 to 24.86 ± 5.30 nM against AChE. The studied compounds in this work exhibited effective hCA isoenzyme and AChE enzyme inhibition effects. The results show that they can be used for the treatment of glaucoma, epilepsy, Parkinson's as well as Alzheimer's disease (AD) after some imperative pharmacological studies that would reveal their drug potential.

Studies have shown an inverse correlation among age-related illnesses like coronary heart disease and cancer and intake of fruit and vegetable. Given the probable health benefits of natural antioxidants from plants, research on them has increased. Dactylorhiza osmanica is consumed as a food and traditional medicine plant in some regions of Turkey, so evaluation of the biological ability of this species is important. In this study, the amount of phenolic content (LC-HRMS), antioxidant activities and enzyme inhibitory properties of an endemic plant, D. osmanica , were investigated. The antioxidant capacities of an ethanol extract of D. osmanica aerial parts (EDOA) and roots (EDOR) were evaluated with various antioxidant methods. Additionally, the enzyme inhibitory effects of EDOA and EDOR were examined against acetylcholinesterase (AChE), α-glycosidase, and α-amylase enzymes, which are associated with common and global Alzheimer's disease and diabetes mellitus. The IC 50 values of EDOA against the enzymes were found to be 1.809, 1.098, and 0.726 mg/mL, respectively; and the IC 50 values of EDOR against the enzymes were found to be 2.466, 0.442, and 0.415 mg/mL, respectively. Additionally, LC-HRMS analyses revealed p -Coumaric acid as the most plentiful phenolic in both EDOA (541.49 mg/g) and EDOR (559.22 mg/g). Furthermore, the molecular docking interaction of p -coumaric acid, quercitrin, and vanillic acid, which are the most plentiful phenolic compounds in the extracts, with AChE, α-glucosidase, and α-amylase, were evaluated using AutoDock Vina software. The rich phenolic content and the effective antioxidant ability and enzyme inhibition potentials of EDOA and EDOR may support the plant's widespread food and traditional medicinal uses., Competing Interests: The authors declare no conflict of interest.

Eight new aminothiols (4a-g and 5) and three new sulfonic acid derivatives (6a-c) were synthesized, and their structures were characterized. Inhibitory effects of the obtained compounds on carbonic anhydrase I and II isoforms (hCA I and hCA II), butyrylcholinesterase (BChE) and acetylcholinesterase (AChE), enzymes were investigated. The newly synthesized compounds have inhibited hCA I with K i s ranging from 7.11 ± 1.46 nM (6a) to 670.52 ± 300.41 nM (4b) and, hCA II with K i s ranging from 16.83 ± 5.72 nM (6a) to 453.34 ± 208.56 nM (4c). Acetazolamide was employed as the positive control for both hCA isoforms (K i for hCA I 198.81 ± 14.13 nM and K i for hCA II 211.42 ± 13.10 nM), and among the new compounds obtained, it was observed that there were compounds that were active at much lower nM levels. All compounds were also evaluated for inhibition of AChE and BChE. They inhibited AChE and BChE enzymes in the range of Ki 5.24 ± 2.27 (6c) - 48.44 ± 21.82 (4g) for AChE and 4.86 ± 0.64 (6c) - 51.75 ± 12.56 (4a) for BChE, and the results were compared with the standard inhibitor Tacrine (K i : 14.20 ± 8.83 nM toward AChE and K i : 3.39 ± 1.91 nM for BChE). Cholinesterase (BChE and AChE) inhibitory abilities of all synthesized molecules were also performed in situ and molecular docking and molecular dynamics (MD) simulation studies. The molecular coupling scores of the compounds and the free binding energies calculated by MM/GBSA were found to be compatible. Examining the results obtained from this study shows that it may have the potential to develop new drugs to treat some global patients such as glaucoma and Alzheimer's disease (AD)., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2022 Elsevier B.V. All rights reserved.)

Enzyme inhibition is a very active area of research in drug design and development. Chalcone derivatives have a broad enzyme inhibitory activity and function as potential molecules in the development of new drugs. In this study, the synthesized novel halogenated chalcones with bromobenzyl and methoxyphenyl moieties were evaluated toward the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes and human erythrocyte carbonic anhydrase I (hCA I), and II (hCA II) isoenzymes. They showed highly potent inhibition ability toward AChE with Ki values of 1.83 ± 0.21-11.19 ± 0.96 nM and BChE with Ki values of 3.35 ± 0.91-26.70 ± 4.26 nM; hCA I with Ki values of 29.41 ± 3.14-57.63 ± 4.95 nM, and hCA II with Ki values of 24.00 ± 5.39-54.74 ± 1.65 nM. Among the tested enzyme inhibitions, compounds 14 and 13 were the most active compounds against AChE and BChE. Docking studies were performed to the most active compounds against AChE, BChE, hCA I and hCA II to propose a binding mode in the active site and molecular dynamics simulations were studied to check the molecular interactions and the stability of the ligands in the active site. The results may contribute to the development of new drugs particularly to treat some global disorders including Alzheimer's disease (AD), glaucoma, and diabetes., Competing Interests: Declaration of Competing Interest There is no conflict of interest., (Copyright © 2022 Elsevier Ltd. All rights reserved.)

Magnofluorine, a secondary metabolite commonly found in various plants, has pharmacological potential; however, its antioxidant and enzyme inhibition effects have not been investigated. We investigated the antioxidant potential of Magnofluorine using bioanalytical assays with 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS •+ ), N , N -dimethyl- p -phenylenediamine dihydrochloride (DMPD •+ ), and 1,1-diphenyl-2-picrylhydrazyl (DPPH • ) scavenging abilities and K 3 [Fe(CN) 6 ] and Cu 2+ reduction abilities. Further, we compared the effects of Magnofluorine and butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), α-Tocopherol, and Trolox as positive antioxidant controls. According to the analysis results, Magnofluorine removed 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals with an IC 50 value of 10.58 μg/mL. The IC 50 values of BHA, BHT, Trolox, and α-Tocopherol were 10.10 μg/mL, 25.95 μg/mL, 7.059 μg/mL, and 11.31 μg/mL, respectively. Our results indicated that the DPPH· scavenging effect of Magnofluorine was similar to that of BHA, close to that of Trolox, and better than that of BHT and α-tocopherol. The inhibition effect of Magnofluorine was examined against enzymes, such as acetylcholinesterase (AChE), α-glycosidase, butyrylcholinesterase (BChE), and human carbonic anhydrase II (hCA II), which are linked to global disorders, such as diabetes, Alzheimer's disease (AD), and glaucoma. Magnofluorine inhibited these metabolic enzymes with Ki values of 10.251.94, 5.991.79, 25.411.10, and 30.563.36 nM, respectively. Thus, Magnofluorine, which has been proven to be an antioxidant, antidiabetic, and anticholinergic in our study, can treat glaucoma. In addition, molecular docking was performed to understand the interactions between Magnofluorine and target enzymes BChE (D: 6T9P), hCA II (A:3HS4), AChE (B:4EY7), and α-glycosidase (C:5NN8). The results suggest that Magnofluorine may be an important compound in the transition from natural sources to industrial applications, especially new drugs.

This paper presents experimental and molecular docking studies on the inhibitory effects of tyrosol, hydroxytyrosol, luteolin, diosmetin, caffeic acid, luteolin 7-O-glycoside, and apigenin 7-O-glycoside from olive (Olea europaea L.) leaf against human carbonic anhydrase (hCA, E.C.4.2.1.1) isozymes I and II. After these isozymes were separately purified, their activities were determined using the esterase activity. IC 50 values for hCA I and II were calculated as 2.02-11.38 µM and 2.23-9.05 µM, respectively. The compounds were identified as CA inhibitors, with K i values in the ranges of 1.66-9.17 µM for the hCA I isozyme and 1.49-14.21 µM for hCA II. The inhibitory effects of these natural compounds were also compared to acetazolamide, which is a potent inhibitor of both CA isozymes. Our results may contribute to the synthesis of new CA inhibitors and pave the way for new drug design in the treatment of a number of diseases including cancer, obesity, diabetes, and glaucoma., (© 2022 Deutsche Pharmazeutische Gesellschaft.)

Coumestrol (3,9-dihydroxy-6-benzofuran [3,2-c] chromenone) as a phytoestrogen and polyphenolic compound is a member of the Coumestans family and is quite common in plants. In this study, antiglaucoma, antidiabetic, anticholinergic, and antioxidant effects of Coumestrol were evaluated and compared with standards. To determine the antioxidant activity of coumestrol, several methods-namely N,N-dimethyl-p-phenylenediamine dihydrochloride radical (DMPD •+ )-scavenging activity, 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonate) radical (ABTS •+ )-scavenging activity, 1,1-diphenyl-2-picrylhydrazyl radical (DPPH • )-scavenging activity, potassium ferric cyanide reduction ability, and cupric ion (Cu 2+ )-reducing activity-were performed. Butylated hydroxyanisole (BHA), Trolox, α-Tocopherol, and butylated hydroxytoluene (BHT) were used as the reference antioxidants for comparison. Coumestrol scavenged the DPPH radical with an IC 50 value of 25.95 μg/mL (r 2 : 0.9005) while BHA, BHT, Trolox, and α-Tocopherol demonstrated IC 50 values of 10.10, 25.95, 7.059, and 11.31 μg/mL, respectively. When these results evaluated, Coumestrol had similar DPPH • -scavenging effect to BHT and lower better than Trolox, BHA and α-tocopherol. In addition, the inhibition effects of Coumestrol were tested against the metabolic enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase II (CA II), and α-glycosidase, which are associated with some global diseases such as Alzheimer's disease (AD), glaucoma, and diabetes. Coumestrol exhibited K i values of 10.25 ± 1.94, 5.99 ± 1.79, 25.41 ± 1.10, and 30.56 ± 3.36 nM towards these enzymes, respectively.

In the design of novel drugs, the formation of hybrid molecules via the combination of several pharmacophores can give rise to compounds with interesting biochemical profiles. A series of novel quinazolin-sulfonamid derivatives ( 9a-m ) were synthesized, characterized and evaluated for their in vitro antidiabetic, anticholinergics, and antiepileptic activity. These synthesized novel quinazolin-sulfonamid derivatives ( 9a-m ) were found to be effective inhibitor molecules for the α-glycosidase, human carbonic anhydrase I and II (hCA I and hCA II), butyrylcholinesterase (BChE) and acetylcholinesterase (AChE) enzyme, with Ki values in the range of 100.62 ± 13.68-327.94 ± 58.21 nM for α-glycosidase, 1.03 ± 0.11-14.87 ± 2.63 nM for hCA I, 1.83 ± 0.24-15.86 ± 2.57 nM for hCA II, 30.12 ± 3.81-102.16 ± 13.87 nM for BChE, and 26.16 ± 3.63-88.52 ± 20.11 nM for AChE, respectively. In the last step, molecular docking calculations were made to compare biological activities of molecules against enzymes which are achethylcholinesterase, butyrylcholinesterase and α-glycosidase.Communicated by Ramaswamy H. Sarma.

The compounds ( 3 - 6 ) used in this study were re-synthesized in accordance with our previous study. The inhibitory effect of the complexes on some metabolic enzymes was examined and it was demonstrated that the enzymes inhibited by ligands and their complex molecules at micromolar level. The best Ki value for α-glycosidase enzyme was absorved 1.01±0.08 µM for compound 6 . The biological activity of ligand and metal complexes against enzymes was compared with molecular docking method. The enzymes used against ligand and metal complexes respectively: Achethylcholinesterase for ID 4M0E (AChE), butyrylcholinesterase for ID 5NN0 (BChE), α-glycosidase for ID 1XSI (α-Gly). ADME analysis was performed to examine the drug properties of the compounds ( 3 - 6 ). Besides, the anticancer properties of the complexes were studied. The doses of all compounds caused significant reductions in MCF-7 cell viability. The 3 and 5 compounds administered to PC-3 cells exhibited a more pronounced cytotoxic effect than the other two compounds ( 4 and 6 ). Furthermore, antibacterial activities of these compounds against Escherichia coli and Staphylococcus aureus were examined.Communicated by Ramaswamy H. Sarma.

Four new and four known isoxazoline derivatives were synthesized from the reactions of benzonorbornadiene with nitrile oxides formed from the corresponding benzaldehydes. Three new and one known pyrazoline derivatives were also synthesized from the reactions of the benzonorbornadiene with nitrile imines formed from the corresponding compounds. The synthesized nitrogen-based novel heterocyclic compounds were evaluated against the human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes. The synthesized nitrogen-based novel heterocyclic compounds showed IC 50 values in the range of 2.69-7.01 against hCA I, 2.40-4.59 against hCA II, 0.81-1.32 µM against AChE, and 20.83-1.70 µM against BChE enzymes. On the contrary, nitrogen-based novel heterocyclic compounds demonstrated K i values between 2.93 ± 0.59-8.61 ± 1.39 against hCA I, 2.05 ± 0.62-4.97 ± 0.95 against hCA II, 0.34 ± 0.02-0.92 ± 0.17 nM against AChE, and 0.50 ± 0.04-1.20 ± 0.16 µM against BChE enzymes. The synthesized nitrogen-based novel heterocyclic compounds exhibited effective inhibition profiles against both indicated metabolic enzymes. These results may contribute to the development of new drugs particularly to treat some disorders, which are widespread in the world including glaucoma and Alzheimer's diseases., (© 2021 Wiley Periodicals LLC.)

In this study, the antioxidant and antiradical properties of some phyto lignans (nordihydroguaiaretic acid, secoisolariciresinol, secoisolariciresinol diglycoside, and α-(-)-conidendrin) and mammalian lignans (enterodiol and enterolactone) were examined by different antioxidant assays. For this purpose, radical scavenging activities of phyto and mammalian lignans were realized by 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) radical (ABTS •+ ) scavenging assay and 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) scavenging assay. Additionally, the reducing ability of phyto and mammalian lignans were evaluated by cupric ions (Cu 2+ ) reducing (CUPRAC) ability, and ferric ions (Fe 3+ ) and [Fe 3+ -(TPTZ)2] 3+ complex reducing (FRAP) abilities. Also, half maximal inhibitory concentration (IC 50 ) values were determined and reported for DPPH • and ABTS •+ scavenging influences of all of the lignan molecules. The absorbances of the lignans were found in the range of 0.150-2.320 for Fe 3+ reducing, in the range of 0.040-2.090 for Cu 2+ reducing, and in the range of 0.360-1.810 for the FRAP assay. On the other hand, the IC 50 values of phyto and mammalian lignans were determined in the ranges of 6.601-932.167 µg/mL for DPPH • scavenging and 13.007-27.829 µg/mL for ABTS •+ scavenging. In all of the used bioanalytical methods, phyto lignans, as secondary metabolites in plants, demonstrated considerably higher antioxidant activity compared to that of mammalian lignans. In addition, it was observed that enterodiol and enterolactone exhibited relatively weaker antioxidant activities when compared to phyto lignans or standard antioxidants, including butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), Trolox, and α-tocopherol.

In this work, the inhibitory effect of some symmetric sulfamides derived from phenethylamines were determined against human carbonic anhydrase (hCA) I, and II isoenzymes, and compared with standard compound acetazolamide. IC 50 values were obtained from the Enzyme activity (%)-[Symmetric sulfamides] graphs. Also, K i values were calculated from the Lineweaver-Burk graphs. Some symmetric sulfamides compounds (11-18) demonstrated excellent inhibition effects against hCA I, and II isoenzymes. These compounds demonstrated effective inhibitory profiles with IC 50 values in ranging from 21.66-28.88 nM against hCA I, 14.44-30.13 nM against hCA II. Among these compounds, the best K i value for hCA I (K i : 8.34±1.60 nM) and hCA II (K i : 16.40±1.00 nM) is compound number 11. Besides, the IC 50 value of acetazolamide used as a standard was determined as hCA I, hCA II 57.75 nM, 49.50 nM, respectively. Moreover, in silico ADME-Tox study showed that all synthesized compounds (11-18) had good oral bioavailability in light of Jorgensen's rule of three, and of Lipinski's rule of five., (© 2021 Wiley-VHCA AG, Zurich, Switzerland.)

This work is devoted to definition of the direction of reaction between 1-benzenesulfonylimino pyridinium chloride and α- or β-halo-containing sulfamides, chloroacetic acid, 1-chloro-2,3-dihydroxypropane, etc. The optimal conditions for the synchronous reaction of heterocyclization are determined. Benzenesulfonyliminopyridinium chloride was obtained to form pyrazolopyridines with 1,2-polarophiles, and pyridazine pyridines with 1,3-polarophiles. These novel derivatives were found as effective inhibitors of the α-glycosidase with K i values in the range of 13.66 ± 2.63-60.63 ± 12.71 nM. The molecules ( II-X ) against enzyme were compared theoretically with the help of molecular docking to compare biological activities. The results were compared with the numerical values of the parameters obtained from molecular docking calculations and found to be in great agreement with the experimental results. However, ADME analysis of molecules was performed. Also, the compounds exhibited significant anticancer effect depending on the doses administered.Communicated by Ramaswamy H. Sarma.

In order to evaluate the antioxidant activity of evaporated ethanolic extract (EESB) and lyophilized water extract (WESB) of Shaggy bindweed ( Convulvulus betonicifolia Mill. Subs), some putative antioxidant methods such as DPPH· scavenging activity, ABTS •+ scavenging effect, ferric ions (Fe 3+ ) reduction method, cupric ions (Cu 2+ ) reducing capacity, and ferrous ions (Fe 2+ ) binding activities were separately performed. Also, ascorbic acid, α-tocopherol and BHT were used as the standard compounds. Additionally, some phenolic compounds that responsible for antioxidant abilities of EESB and WESB were screened by liquid chromatography-high resolution mass spectrometry (LC-HRMS). At the same concentration, EESB and WESB demonstrated effective antioxidant abilities when compared to standards. In addition, EESB demonstrated IC 50 values of 1.946 μg/mL against acetylcholinesterase (AChE), 0.815 μg/mL against α-glycosidase and 0.675 μg/mL against α-amylase enzymes., Competing Interests: The authors declare no conflict of interest., (© 2021 The Author(s).)