Search

A new fungal species, Penicillium psychrofluorescens sp. nov. is described as a member of section Torulomyces. The new species is sister to P. catalonicum, and was isolated from soil collected from Robinson Ridge, East Antarctica, following enrichment cultivation under oligotrophic conditions supplemented with excess hydrogen gas. Penicillium psychrofluorescens is named for its intense autofluorescence derived from a combination of compounds that may include NADPH, porphyrins, and secondary metabolites, such as polyketides. Comparative genomics with both Antarctic and mesophilic Penicillium spp. shows that Penicillium psychrofluorescens has a wide repertoire of glycoside hydrolases, but almost no polysaccharide lyases, has comparably large effector proteins, lacks the machinery to use nitrate as an N-source, but has the genes for the assimilation of phosphorus from phosphonates via oxidative pathway. The strain was found to have 30 biosynthetic gene clusters (BGCs), the majority of which were unrelated to known compound BGCs. Given the remarkable diversity of natural products already characterised from Penicillium spp. and the presence of >30 BGCs with low similarity to known genes, there is biotechnological potential within this novel species that is yet to be explored. [ABSTRACT FROM AUTHOR]

Endophytes, symbiotically with their host plants, are frequently found in the roots of Panax ginseng. To explore ginsenosides biotransformation by endophytic fungi, 26 such fungi were isolated from ginseng roots sourced from four distinct planting regions, and their glycosyl hydrolysis activities were measured. Of these endophytic, 20 isolates exhibited glycosidase enzymes capable of cleaving glycosidic bonds of glucose, arabinofuranose and arabinopyranose. Notably, the glycosidase BglNh gene was isolated and cloned from Nectria haematococca, one of the endophytic fungi. Enzymatic assessments unveiled that BglNh specifically catalyzes the hydrolysis of glucose residues located external to the C-3 position of protopanaxadiol ginsenosides under optimal reaction conditions (pH 6.0 and temperature 35 °C). Our findings demonstrate the efficient conversion of major ginsenosides Rb1, Rb2 and Rc to minor ginsenosides Gyp17, CO and CMc1, highlighting the potential of these fungi for ginsenoside biotransformation and bioactive compound production. [ABSTRACT FROM AUTHOR]

Zhejiang, China, has a tradition of wine-fermented foods, including Jinhua Dajiao steamed bread (JDSB). The traditional leavening agent, jiaotou, confers its properties and taste to JDSB. We examined microorganisms in jiaotou, their effects on processing, and the metabolome using metagenomic and metabolomic analyses. Metagenomics of microorganisms in jiaotou revealed a high average diversity, with Rhizopus sp. being the dominant bacteria. The enriched genes were most abundant in genes related to carbohydrate and amino acid metabolism, with a greater number of non-redundant genes for glycoside hydrolases and glycosyl transferases. The enriched genes may have a direct impact on the organoleptic quality of JDSB. Functional enrichment analysis of different metabolites revealed that pathways associated with linoleic acid, ABC transporter, alanine, aspartate, glutamate, and galactose metabolism were enriched during JDSB processing. We identified a strong correlation between metagenomic functional level and metabolomics pathway enrichment analyses.The results contribute to the improvement of JDSB processing. [ABSTRACT FROM AUTHOR]

The content of malvin (malvidin-3,5-diglucoside) was determined in a set of wines obtained from Cabernet Cortis and other three recently introduced grape-resistant hybrids (Cabernet Volos, Merlot Khantus and Merlot Khorus) produced in South Tyrol (Italy), to establish their conformity to legal requirements and suggest winemaking approaches for their production and use. Different skin maceration times and ageing periods were considered for the wines investigated. Malvin content exceeded the limit of 15 mg/L, imposed by the Italian government for the commercialization of wines, in 18 out of 21 samples and showed a significant decrease during wine ageing (by about 40–50% every 12-month period) with the scarce effect of maceration time and fermentation temperature. Single-cultivar wines became suitable for commercialization after ca. 7 years ageing, following traditional winemaking approaches. The use of two commercial enzymatic pectolytic preparations indicated for aroma enhancement and possessing β-glucosidase activity was also investigated at two different dosages, to increase the degradation rate of malvin in wines after winemaking. They are unsuitable for significant malvin content decrease within a 6-month time lapse. [ABSTRACT FROM AUTHOR]

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

Astragalus membranaceus is a traditional Chinese medicine with multiple pharmacological activities. Modern pharmacological research has found that Astragalus membranaceus extract has an inhibitory effect on α-glucosidase, however, which component can inhibit the activity of α-glucosidase and its degree of inhibition are unknown. To address this issue, this study used affinity ultrafiltration screening combined with UPLC-ESI-Orbitrap-MS technology to screen α-glucosidase inhibitors in Astragalus membranaceus. Using affinity ultrafiltration technology, we obtained the active components, and using UPLC-ESI-Orbitrap-MS technology, we quickly analyzed and identified them. As a result, a total of 8 ingredients were selected as α-glucosidase inhibitors. [ABSTRACT FROM AUTHOR]

AbstractAlpha glucosidases are multifunctional glycoside hydrolases with hydrolysis and transglycosylation ability. It can be utilized for the glycosidic bond synthesis or glycosylation of Ascorbic acid/Vitamin C to its stable analogue, Ascorbic acid 2 glucoside (AA2G), a compound with wide applications in cosmetics and pharma. The application of α-glucosidases for industrial scale transglycosylation is limited due to the low transglycosylation yield of free enzymes. Enzyme immobilization techniques could enable the development of efficient, reusable catalysts. Only a few glycoside hydrolases have been studied in immobilized form for transglycosylation reactions, and α-glucosidases are probably the least explored in this form. Transglycosylation activity of immobilized α-glucosidase from Aspergillus carbonarius BTCF 5 was studied for AA2G synthesis, where different immobilization techniques like calcium alginate encapsulation, adsorption on chitosan beads, covalent cross-linking on magnetic nanoparticles, and cross-linked enzyme aggregates (CLEA) were employed for the immobilization. The immobilization yield of calcium alginate encapsulated enzyme, enzyme immobilized on Fe-MNP support, enzyme immobilized on chitosan beads and as CLEA were 107%, 99%, 46% and 486%, respectively. CLEA was identified as the best immobilization technique for this bi-substrate reaction due to the high immobilization yield and activity retention (30% activity retained after 5 consecutive cycles). Enzyme immobilization increased the transglycosylation activity by 38%, yielding 118 mM AA2G against 72 mM by the free enzyme. This indicates the potential of immobilized α-glucosidase as a catalyst for synthesizing AA2G at an industrial scale. [ABSTRACT FROM AUTHOR]

Phenolics produced during xylooligosaccharide production might inhibit xylanases and enhance the antioxidant and antimicrobial activities of XOS. The effects of phenolic compounds on xylanases may depend on the type and concentration of the compound, the plant biomass used, and the enzyme used. Understanding the effects of phenolic compounds on xylanases and their impact on XOS is critical for developing viable bioconversion of lignocellulosic biomass to XOS. Understanding the complex relationship between phenolic compounds and xylanases can lead to the development of strategies that improve the efficiency and cost-effectiveness of XOS manufacturing processes and optimise enzyme performance. [ABSTRACT FROM AUTHOR]

Aureobasidium pullulans LB83 is a versatile biocatalyst that produces a plethora of bioactive products thriving on a variety of feedstocks under the varying culture conditions. In our last study using this microorganism, we found cellulase activity (FPase, 2.27 U/ml; CMCase, 7.42 U/ml) and other plant cell wall degrading enzyme activities grown on sugarcane bagasse and soybean meal as carbon source and nitrogen, respectively. In the present study, we provide insights on the secretome analysis of this enzymatic cocktail. The secretome analysis of A. pullulans LB83 by Liquid Chromatography coupled to Mass Spectroscopy (LC-MS/MS) revealed 38 classes of Carbohydrate Active enZymes (CAZymes) of a total of 464 identified proteins. These CAZymes consisted of 21 glycoside hydrolases (55.26%), 12 glycoside hydrolases harboring carbohydrate-binding module (31.58%), 4 carbohydrate esterases (10.53%) and one glycosyl transferase (2.63%). To the best of our knowledge, this is the first report on the secretome analysis of A. pullulans LB83. [ABSTRACT FROM AUTHOR]

Phytochemical study on 90% ethanol extract from the green walnut husks of Juglans mandshurica Maxim. resulted into the isolation of three undescribed triterpenoids, juglansmanoids A–C (1–3). Structural elucidation of all the compounds were performed by spectral methods such as 1D and 2D (1H-1H COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated components were evaluated in vitro for anti-hyaluronidase activities. As a result, triterpenoid 1 exhibited potent anti-hyaluronidase activity (IC50 = 9.78 μg/ml) three times more than the positive control drug oleanolic acid (IC50 = 40.12 μg/ml). [ABSTRACT FROM AUTHOR]

Two new sesquiterpenoid glycosides, 8α (H)-eudesmane-1,3,11 (13)-triene-2-one -12-O-β-D-glucopyranoside (1) and dmetelisproside B (2), together with ten known compounds (3–12) were isolated from calyces of Physalis alkekengi L. var. franchetii (Mast.) Makino (PAF). Their structures were unambiguously elucidated through HR-ESI-MS, UV, IR, and NMR spectral data. Compounds 1, 10, and 12 exhibited DPPH scavenging ability with IC50 values of 33.69 ± 6.65, 6.29 ± 0.06, and 25.66 ± 3.06 μM, respectively. Additionally, 10 and 12 demonstrated weak α-glucosidase inhibition activity with IC50 values of 250.9 ± 6.60 and 347.6 ± 2.48 μM, respectively. [ABSTRACT FROM AUTHOR]

Senescence can promote hyperplastic pathologies, such as cancer. Prostate cancer is the second most common type of cancer in men. The p21-mediate cellular senescence, facilitated through the tumor suppressor p53-dependent pathway, is considered the primary mechanism for cancer treatment. Aloe-emodin, has been reported to exert anticancer effects in various types of cancers. This study aimed to investigate the bioactivity of aloe-emodin in LNCaP cells via the activation of p21-mediated cellular senescence. Aloe-emodin treatment increased the percentage of cells in the G1 phase while decreasing the percentage in the S phase. This effect was reflected in the expression levels of proteins associated with cell cycle progression, such as p21CIP, retinoblastoma protein, and cyclin-dependent kinase2/4 in LNCaP cells. However, aloe-emodin-treated LNCaP cells did not induce cell cycle arrest at G2/M checkpoint. Moreover, increased senescence-associated-galactosidase activity was observed in a dose-dependent manner following treatment with aloe-emodin. Aloe-emodin also induced DNA damage by modulating the expression of histone H2AX and lamin B1. Furthermore, aloe-emodin inhibited the proliferation of LNCaP cells, contrasting with the exponential growth observed in the nontreated cells. Importantly, this inhibition did not impact the immune system, as evidenced by the increased proliferation of splenocytes isolated from mice. These findings provide preliminary evidence of the anticancer effect of aloe-emodin in LNCaP cells, necessitating further investigations into the underlying mechanisms in vivo and human subjects. [ABSTRACT FROM AUTHOR]

Tetraclinis articulata essential oil proved to be effective in controlling tomato grey mould, so we would investigate its effect on some tomato defense mechanisms. The pretreatment of Botrytis cinerea infected tomato plants with TAEO emulsion enhanced the activity of antioxidant enzymes activity SOD, CAT, APX, and GPX, and total polyphenols content and it decreased IC50 of free radical-scavenging activity and H2O2 content. Results showed amelioration in antioxidant status in TAEO emulsion treated and B. cinerea infected plants indicating that treatment decreased infection in tomato plants. The qRT-PCR analysis of defense genes expression Chitinase SlChi, transcription factors SlWRKY and SlAP2/ERF, Lipoxygenase SlLOX, and Thioredoxin SlTRX showed that they were up-regulated as early as 12 hpi sustained with a second increase at 48 hpi in TAEO emulsion pretreated and infected plants. These results suggest the potential use of TAEO emulsion as natural product to induce tomato antioxidant status and activate defense genes. [ABSTRACT FROM AUTHOR]

Glycosides are widely used in many fields due to their favorable biological activity. The traditional plant extractions and chemical methods for glycosides production are limited by environmentally unfriendly, laborious protecting group strategies and low yields. Alternatively, enzymatic glycosylation has drawn special attention due to its mild reaction conditions, high catalytic efficiency, and specific stereo-/regioselectivity. Glycosyltransferases (GTs) and retaining glycoside hydrolases (rGHs) are two major enzymes for the formation of glycosidic linkages. Therein GTs generally use nucleotide phosphate activated donors. In contrast, GHs can use broader simple and affordable glycosyl donors, showing great potential in industrial applications. However, most rGHs mainly show hydrolysis activity and only a few rGHs, namely non-Leloir transglycosylases (TGs), innately present strong transglycosylation activities. To address this problem, various strategies have recently been developed to successfully tailor rGHs to alleviate their hydrolysis activity and obtain the engineered TGs. This review summarizes the current modification strategies in TGs engineering, with a special focus on transglycosylation activity enhancement, substrate specificity modulation, and product polymerization degree distribution, which provides a reference for exploiting the transglycosylation potentials of rGHs. [ABSTRACT FROM AUTHOR]

Four new phloroglucinol derivatives (1 − 4) were isolated from the leaves of Syzygium fluviatile. Their structures were elucidated by means of extensive spectroscopic data. Among them, compounds 1 and 3 showed significant inhibitory activity against α-glucosidase with IC50 values of 10.60 and 5.07 µM, respectively. The structure-activity relationship was also discussed briefly. [ABSTRACT FROM AUTHOR]

The aim of the current study was to determine whether daily fucoidan supplementation (Undaria pinnatifida extract containing >85% fucoidan, 1 g/day) for three-weeks in a double blind-placebo controlled cross-over trial (ACTRN12621000872831) could modulate alterations in faecal (calprotectin, lysozyme and IgA) and salivary (lactoferrin, lysozyme and IgA) markers of mucosal immune competence typically observed in response to both acute physical activity, and a period of intensified exercise training, in healthy recreationally active men (n = 12). Participants responded positively to the intensified training with 16–19% improvement in mean power that was not different between supplement groups. Faecal biomarkers and concentrations of lactoferrin, lysozyme and IgA from resting saliva samples were largely stable over the supplementation period. Concentrations of salivary biomarkers varied significantly over time in response to acute exercise, however differences between supplementation groups were modest. For salivary lysozyme, there was a trend for a lower magnitude of increase post-exercise (p = 0.08) and limited return towards pre-exercise in response to fucoidan. For salivary IgA, a greater acute exercise response was noted for IgA in response to fucoidan (~2.7-fold higher; p = 0.02). Different dosage and supplementation protocols and inclusion of additional immune markers should be considered in subsequent assessments of any potential benefits of fucoidan supplementation in healthy active adults. [ABSTRACT FROM AUTHOR]

1. The caecal microbiota in geese play a crucial role in determining the host's health, disease status and behaviour, as evidenced by extensive epidemiological data. The present investigation conducted 10× metagenomic sequencing of caecal content samples obtained from three distinct goose species, namely Landes geese, Roman geese and Zhedong White geese (n = 5), to explore the contribution of the gut microbiome to carbohydrate metabolism. 2. In total, 337GB of Illumina data were generated, which identified 1,048,575 complete genes and construction of 331 metagenomic bins, encompassing 78 species from nine phyla. Firmicutes, Bacteroidetes, Actinobacteria, Proteobacteria and Bacteria were identified as the dominant phyla while Prevotella, Bacteroides, Streptococcus, and Subdoligranulum were the most abundant genera in the caecum of geese. 3. The genes were allocated to 375 pathways using the Kyoto Encyclopedia of Genes and Genome (KEGG) analysis. The most abundant classes in the caecum of geese were confirmed to be glycoside hydrolases (GHs), glycosyl transferases (GTs), as identified through the carbohydrate-active enzyme (CAZyme) database mapping. Subdoligranulum variabile and Mediterraneibacter glycyrrhizinilyticus were discovered to potentially facilitate carbohydrate digestion in geese. 4. Notwithstanding, further investigation and validation are required to establish a connection between these species and CAZymes. Based on binning analysis, Mediterraneibacter glycyrrhizinilyticus and Ruminococcus sp. CAG:177 are potential species in LD geese that contribute to the production of fatty liver. [ABSTRACT FROM AUTHOR]

A new oleanane-type triterpenoid saponin, 21β, 22α-di-O-angeloyl-15α, 16α, 28-trihydroxyolean-12-ene 3β-O-α-L-rhamnopyranosyl-(1→3)-α-D-xylopyranosyl-(1→3)-β-D-glucopyranoside (1), together with five known compounds (2-5), were isolated from Camellia nitidissima. Their structures were elucidated based on spectroscopic methods, including extensive NMR and MS spectra. Compound 1 showed potential inhibitory activity on α-glucosidase with the IC50 values of 185.9 ± 44.5 µmol/L. [ABSTRACT FROM AUTHOR]

Black Bengal goats possess a rich source of rumen microbiota that helps them to adapt for the better utilization of plant biomaterial into energy and nutrients, a task largely performed by enzymes encoded by the rumen microbiota. Therefore the study was designed in order to explore the taxonomic profile of rumen microbial communities and potential biomass degradation enzymes present in the rumen of back Bengal goat using Illumina Nextseq-500 platform. A total of 83.18 million high-quality reads were generated and bioinformatics analysis was performed using various tools and subsequently, the predicted ORFs along with the rRNA containing contigs were then uploaded to MG-RAST to analyze taxonomic and functional profiling. The results highlighted that Bacteriodetes (41.38–59.74%) were the most abundant phyla followed by Firmicutes (30.59–39.96%), Proteobacteria (5.07–7.61%), Euryarcheaota (0.71–7.41%), Actinobacteria (2.05–2.75%). Genes that encode glycoside hydrolases (GHs) had the highest number of CAZymes, and accounted for (39.73–37.88%) of all CAZymes in goat rumen. The GT families were the second-most abundant in CAZymes (23.73–23.11%) and followed by Carbohydrate Binding module Domain (17.65–15.61%), Carbohydrate Esterase (12.90–11.95%). This study indicated that goat rumen had complex functional microorganisms produce numerous CAZymes, and that can be further effectively utilised for applied ruminant research and industry based applications. [ABSTRACT FROM AUTHOR]

Venom hyaluronidase is an enzyme belonging to the glycoside hydrolase family that plays a critical role in systemic envenomation by spreading toxins in tissue and destruction of the extracellular matrix. The roles of venom hyaluronidase during envenomation have been widely studied, but the identification of its variants and isoforms is still under investigation. In this study, we developed a filtering method to identify the exon-intron pattern, alternative splicing events and isoforms of hyaluronidase in A. crassicauda and H. lepturus scorpions using the RNA-seq technique. Furthermore, in silico analysis was performed to identify and characterize the hyaluronidases. The most important findings were that the scorpion hyaluronidase gene contains 5 exons, 4 introns and undergo to alternative splicing events. In A. crassicauda and H. lepturus datasets, a sequence denominated AcHase-1 and three denominated HLHase1, HLHase2 and HLHase3 were identified as hyaluronidase variants respectively, which were found to have multiple isoforms that differed in the coding, non-coding or untranslated regions. The results showed that exon skipping, intron retention and alternative 3' splice site led to dysregulation of gene expression. To clarify the evolutionary history of scorpions based on hyaluronidase molecular phylogenetic studies, we used the phylogenetic tree to deduce the origins of this protein in different species of scorpions, spiders and bees. Hyaluronidase gene performed well for divergences and accurately separated closely related species. Our work provides insights into the diversity of Hase proteins during scorpion evolution and may direct further studies consisting of synthesis, purification and recombinant production of Hase proteins. [ABSTRACT FROM AUTHOR]

One new phenylpropanoid glycoside, myxosmoside I (1) and six known compounds, arenarioside (2), verbacoside (3), 3-formylindole (4), 5-hydroxymethyl furfural (5), D-manitol (6), and glycerol monooleate (7) were isolated from the roots of Myxopyrum smilacifolium (Wall.) Blume. Their chemical structures were determined by 1D-, 2D-NMR, and mass spectra, chemical methods, and compared with those reported in the literature. All compounds were evaluated for α-glucosidase inhibitory effect. Among them, phenylpropanoid glycosides 1–3 significantly inhibited α-glucosidase activity with IC50 values of 30.0 ± 0.9, 66.6 ± 2.3, and 36.9 ± 2.0 µM, respectively. [ABSTRACT FROM AUTHOR]

The aim of study was to investigate the antidiabetic and antioxidant properties of extracts obtained from dried Prosopis farcta fruit and seeds against streptozotocin-induced diabetes in rats. According to the results, glucose, haemoglobin A1c, α-glycosidase activity, liver and kidney damage biomarkers, and malondialdehyde contents of all of the diabetic groups were found to have increased significantly according to the control group. Furthermore, the insulin and C-peptide secretions increased, and liver malondialdehyde level decreased, which were determined as the result of fluctuations in the antioxidant enzyme activities with a dose of 400 mg/kg fruit extract, while seed extract dosages of 100 and 400 mg/kg caused an increase in hepatic demage biomarkers. It was concluded that fruit extract may have insulin secretion stimulating and lipid peroxidation inhibitory effects, whereas seed extract might have caused hepatocyte damage changes to the transport functions and membrane permeability of these cells, thus causing enzymes to leak. [ABSTRACT FROM AUTHOR]

Two new prenylated xanthones, mangoxanthones A-B (1-2), together with four known compounds 3-6, were isolated from the ethanol extract of the pericarp of Garcinia mangostana. The structures of these compounds have been elucidated based on spectroscopic analysis. The analysis results of chiral HPLC revealed compounds 1 and 2 were scalemic mixtures respectively. All isolated compounds were biologically evaluated for their α-glucosidase and α-amylase inhibitory effects using in-vitro assays. Compound 1 showed moderate inhibitory activities against α-glucosidase and α-amylase with IC50 of 29.06 ± 1.86 and 22.74 ± 2.07 μM, respectively. Molecular docking predicted the binding sites of compound 1 to α-glucosidase and α-amylase. A preliminary structure-activity relationship was discussed. [ABSTRACT FROM AUTHOR]

A new aurone glycoside named licoagroaurone 6-O-α-ʟ-arabinopyranoside (1), together with six known compounds (2–7), was isolated from EtOAc-soluble extract of the aerial parts of Saussurea involucrata. Their structures were elucidated on the basis of spectroscopic methods. All compounds were evaluated for their inhibitory activities against α-glucosidase in vitro. Among them, compounds 1 and 6 showed significant inhibitory activities on α-glucosidase with the IC50 values of 47.1 and 57.7 μM, respectively. [ABSTRACT FROM AUTHOR]

The consumption of glucosinolate (GL)-rich foods, including Brassica vegetables, such as mustard, broccoli, and maca, is associated with decreased risk of developing cancer. The GL content in maca, which is recognized as a "superfood", is approximately 100-times higher than that in other brassicas. Although maca is a potential dietary source of GLs, limited studies have examined the bioactivity of maca GLs using the combination of chemical characterization and bioassays. In this study, the fractions (Lm-II and Lm-III) rich in intact GLs (glucotropaeolin and glucolimnanthin) were isolated and characterized from maca ethanolic extracts using chromatography and mass spectrometry. Additionally, the growth-inhibitory effects of Lm-II and Lm-II fractions against hepatocellular carcinoma (HepG2/C3A) and colon adenocarcinoma (HT29) cell lines were examined in the absence or presence of myrosinase (MYR). Fractions lacking low molecular weight sugars dose-dependently exerted cytotoxic effects in the presence of MYR. The half-maximal inhibitory concentration values of Lm-II and Lm-III against HepG2/C3A were 118.8 and 69.9 µg/mL, respectively, while those against HT29 were 102.6 and 71.5 µg/mL, respectively. These results suggest that the anticancer properties of maca can be attributed to GLs and corroborate the categorization of maca as a "superfood." Supplemental data for this article is available online at https://doi.org/10.1080/01635581.2021.1952444 [ABSTRACT FROM AUTHOR]

A series of metal complexes containing a 1,10-phenanthroline scaffold [ML] (L-1,10-Phenanthroline derivative comprises conjugated aromatic core and electron withdrawing –NO2 group); M = Cu(II), Zn(II), Co(II), and Zn(II) ions were designed and synthesized to obtain effective anti-cholinesterase efficiencies of metal chelates. Analytical and spectroscopic studies were used to determine the structural features. An octahedral structure with moderate distortion was attributed to the above metal chelates based on spectroscopic data. S. aureus, A. niger, C. albicans, B.subtilis, A. flavus, and E. coli were used to test the antibacterial efficacy of the synthesized ligands and metal complexes. Using agarose gel electrophoresis, the DNA fragmentation proficiency of prepared metal complexes was tested on pUC 18 DNA. The distorted octahedral geometry of the copper(II) complex to DNA (Kb = 4.11 × 105 M−1) is stronger than that of ethidium bromide (EB) to DNA (Kb = 3.3 × 105 M−1) and other metal complexes, respectively. The synthesized 1,10-phenanthroline derivative had the best inhibitory effects against acetylcholinesterase and butyrylcholinesterase, with IC50 values of 0.45 and 3.6 M, respectively, which were lower than the reference molecules. Our experimental results may contribute to the development of new drug molecules particularly in the treatment of neurological disorders including glaucoma, Alzheimer's disease and diabetes. The actions of inhibitors on the glycosidase enzyme help to delay the breakdown and release of sugar molecules into the bloodstream, and they can be used as therapeutic factors in the treatment of diabetes. [ABSTRACT FROM AUTHOR]

From the lichen Parmotrema praesorediosum, one new diphenyl peroxide, named praesordin A (1), together with four depsidones, including virensic acid (2), protocetraric acid (3), 8'-O-methylprotocetraric acid (4), and furfuric acid (5) were purified. Their structures were chacracterized using extensive HR-ESI-MS and NMR spectroscopic methods. The isolated compounds (2-5) possessed stronger α-glucosidase inhibitory activity (IC50 = 43.7-110.1 μM) than the standard drug acarbose (IC50 = 214.5 μM). [ABSTRACT FROM AUTHOR]

In plants, β-glucosidases (BGLUs) are important glycoside hydrolases involved in several biological phenomena, including the response to stresses via the activation of phytohormones and the release of alpha-hydroxy nitriles to protect against stresses. Due to the importance of BGLUs in plant growth and stress response, genome-wide analyses have been conducted in Arabidopsis and rice, while not in tomato (Solanum lycopersicum). In this study, we identified 20 BGLU genes in the tomato that were unevenly distributed on nine chromosomes and divided into five subgroups. There were a variety of plant hormones and stress response cis-elements in the promoter region of the SlBGLU gene, indicating that the BGLU gene may be involved in several aspects of the tomato stress response. SlBGLU gene expression analysis showed that the BGLU gene of tomato was expressed in many tissues, especially in the roots and leaves. Transcriptome data and results of real-time quantitative reverse transcription-polymerase chain reaction showed that most SlBGLU genes could be induced by abscisic acid, chlorothalonil, NaCl and cold (4 °C), especially SlBGLU13 and SlBGLU19, which may be key BGLU genes in response to stress and hormonal stimulation in the tomato. In addition, we constructed a competing endogenous RNA (ceRNA) network, which confers a new direction for studies on the function of SlBGLU genes. These findings not only further clarify the potential function of the BGLU gene family in mediating abiotic stresses in the tomato, but also provide valuable information for the study of functional genomics of the tomato in the future. [ABSTRACT FROM AUTHOR]

The current study aims at exploring enzyme inhibition of four species of medicinal herbs, namely Senna bicapsularis, Thevetia peruviana, Nerium oleander and Vinca major. Plant selection was done on the basis of their therapeutic uses by local practitioners. The crude methanolic extracts of these plants were tested for their α-glycosidase and urease enzyme inhibition potential. The observed urease inhibitory potential for the crude extract of S. bicapsularis, T. peruviana and N. oleander were 8.3 ± 0.33 μg, 6.98 ± 0.98 μg and 9.56 ± 1.43 μg, respectively while the V. major did not show any inhibition. In addition, the IC50 value for Thiourea was 22.3 ± 1.14 μg. The crude extracts of S. bicapsularis, T. peruviana, N. oleander, V. major were shown to inhibit α-glycosidase activity with an IC50 value of 630.3 ± 0.03 μg, 700.7 ± 2.43 μg, 430.4 ± 3.97 μg, and the standard (acarbose) 880 ± 1.03 μM, respectively. Based on the TLC profile, the extract of S. bicapsularis was subjected to column chromatography and the major component named rhein (1) was identified. Compound 1 exhibited excellent urease and α-glycosidase inhibitory activity with an IC50 value of 7.4 ± 0.32 and 622.3 ± 1.03 μM, respectively. [ABSTRACT FROM AUTHOR]

Breast cancer is a hormonally-driven cancer, and various dietary factors are associated with estrogen metabolism, including dietary fiber. Several studies report associations between dietary fiber and breast cancer; however, research on whether fiber influences circulating estrogens through the gut microbiota is rare. The objective of this cross-sectional study among 29 newly-diagnosed (stage 0-II), post-menopausal breast cancer patients is to examine associations between dietary fiber and the gut microbiota that are linked with β-glucuronidase activity, and purportedly increase circulating estrogens. Spearman's and partial correlations controlling for body mass index and age were performed using dietary recall data, Illumina MiSeq generated microbiota relative abundance, and HPLC-mass spectrometry-derived estradiol and estrone levels. Major findings are: (1) total dietary fiber is inversely associated with Clostridium hathewayi (r= −0.419; p = 0.024); (2) soluble fiber is inversely associated with Clostridium (r=-0.11; p = 0.02); (3) insoluble fiber is positively associated with Bacteroides uniformis sp. (r = 0.382; p = 0.041); and (4) serum estradiol and estrone levels are not correlated with species/genera or dietary fiber, though there is a trend toward an inverse association between soluble fiber and estradiol levels (r= −0.30; p = 0.12). More studies are needed to understand the complex interaction between dietary fiber, intestinal microbiota, and hormonal levels in older females. [ABSTRACT FROM AUTHOR]

From the EtOH-soluble extract of the roots of Piper nigrum, one new dimeric alkamide, pipercyclobutanamide D (1) was isolated. Its structure was elucidated on the basis of NMR spectroscopic interpretation. The relative configuration of 1 was determined based on the NOESY analysis. Compound 1 showed α-glucosidase inhibitory activity with an IC50 value of 158.5 µM. In addition, compound 1 exhibited cytotoxicity against the MCF-7 and HepG2 cell lines with the IC50 values of 45.6 and 63.9 µM, respectively. Plausible biosynthetic pathway for the formation of 1 was proposed based on regioselective [2 + 2] cycloaddition reaction. [ABSTRACT FROM AUTHOR]

The highly demanding conditions of industrial processes may lower the stability and affect the activity of enzymes used as biocatalysts. Enzyme immobilization emerged as an approach to promote stabilization and easy removal of enzymes for their reusability. The aim of this review is to go through the principal immobilization strategies addressed to achieve optimal industrial processes with special care on those reported for two types of enzymes: β-galactosidases and fructosyltransferases. The main methods used to immobilize these two enzymes are adsorption, entrapment, covalent coupling and cross-linking or aggregation (no support is used), all of them having pros and cons. Regarding the support, it should be cost-effective, assure the reusability and an easy recovery of the enzyme, increasing its stability and durability. The discussion provided showed that the type of enzyme, its origin, its purity, together with the type of immobilization method and the support will affect the performance during the enzymatic synthesis. Enzymes' immobilization involves interdisciplinary knowledge including enzymology, nanotechnology, molecular dynamics, cellular physiology and process design. The increasing availability of facilities has opened a variety of possibilities to define strategies to optimize the activity and re-usability of β-galactosidases and fructosyltransferases, but there is still great place for innovative developments. [ABSTRACT FROM AUTHOR]

Three new compounds (methyl-3β,25-dihydroxycycloart-23-en-29-oate 3-sulfate (1), methyl-3β-hydroxy-25-methoxycycloart-23-en-29-oate 3-sulfate (2) and 3β-hydroxy-25-methoxycycloart-23-ene 3-sulfate (3)) and a known one (3β-hydroxycycloart-24-en-23-one 3-sulfate (4)) were isolated from Vietnamese red alga Tricleocarpa fragilis. All isolated compounds 1-4 showed potent inhibitory activity against yeast α-glucosidase with IC50 values of 16.62 ± 2.80, 36.34 ± 4.04, 30.19 ± 5.01 and 6.52 ± 0.17 µM, respectively. The docking data showed that the substitutions at C-3 and the differences in the side chain of cycloartane-skeleton could influence the interaction of molecule with enzyme, which was consistent with the experimental findings. [ABSTRACT FROM AUTHOR]

A new aurone named (2Z)-2-[(4'-hydroxy-3'-methoxyphenyl) methylene]-6-methoxy-7-prenyl-3(2H)-benzofurane (1), together with five known compounds (2–6), were isolated from EtOAc-soluble extract of the stems of Acanthopanax senticosus. The chemical structures were elucidated on the basis of spectroscopic analyses. All isolates were evaluated for in vitro inhibitory activity on α-glucosidase. Among them, compounds 1 and 4 were found to exhibit moderate inhibitory activity on α-glucosidase with IC50 value of 64.1 ± 1.2 and 48.9 ± 1.1 μM, respectively. [ABSTRACT FROM AUTHOR]

Three new flavonoid glycosides, embeliaflavosides A-C (1–3), together with eight known flavonoid glycosides (4–11), were isolated from the fruits of Embelia ribes. Their structures were established based on the analyses of spectroscopic data. Compounds 1–11 were evaluated for antioxidant and α-glucosidase inhibitory activities. The results revealed that compounds 1–11 owned significant ABTS radical scavenging activity with IC50 values of 2.52–9.78 µM, and DPPH scavenging activity with IC50 values of 7.56–26.47 µM, respectively. However, α-glucosidase inhibition assay indicated that all the isolates were inactive. [ABSTRACT FROM AUTHOR]

In the present study, two medicinal plants from Africa, namely Bersama abyssinica Fresen. and Scoparia dulcis L., were extracted using ethyl acetate, methanol, and water. The antioxidant, enzyme (α-amylase, α-glucosidase, acetyl- and butyrylcholinesterase, lipase, and tyrosinase) inhibitory action, and phytochemical profiles of extracts of Bersama abyssinica and Scoparia dulcis were determined. The aqueous (180.62 and 61.81 mg gallic acid equivalent/g extract, for B. abyssinica and S. dulcis respectively) and methanol (75.21 and 57.81 mg rutin equivalent/g extract, for B. abyssinica and S. dulcis, respectively) extracts contained high concentrations of phenolic and flavonoids, respectively. The ethyl acetate extracts of both plants were potent inhibitors of α-glucosidase and tyrosinase. Several phytochemical groups were determined by HPLC-MS/MS. The study tend to suggest that B. abyssinica and S. dulcis are potential candidates for the development of novel therapeutical agents. [ABSTRACT FROM AUTHOR]

In this study, we report the synthesis of novel tris-chalcones and testing of human carbonic anhydrase I, and II isoenzymes (hCA I, and hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase (α-Gly) inhibitors for the development of novel chalcone structures towards for treatment of some diseases. The compounds demonstrated Ki values between 13.6 ± 1.1 and 50.0 ± 17.1 nM on hCA I, 9.9 ± 0.8 and 39.5 ± 15.1 nM on hCA II, 3.1 ± 0.2 and 20.1 ± 1.9 nM on AChE, 4.9 ± 0.4 and 14.7 ± 5.2 nM on BChE and 3.9 ± 0.2 and 22.4 ± 10.7 nM on α-Gly enzymes. The results revealed that novel tris-chalcones can have promising drug potential for glaucoma, leukaemia, epilepsy; Alzheimer's disease that was associated with the high enzymatic activity of hCA I, hCA II, AChE, and BChE enzymes. [ABSTRACT FROM AUTHOR]

One pair of new amides enantiomers (1a and 1b) and two known amides were isolated from the rhizomes of Polygonum cuspidatum. Their structures were established using UV, IR, HRESIMS, and NMR data. Notably, compound 1 possesses unique C-C connection between feruloyltyramine and resveratrol. Their absolute configurations were determined by the ECD method. All compounds were evaluated for their α-glucosidase inhibitory activity and compounds 2 and 3 showed significant inhibitory activity with IC50 values of 2.82 and 13.06 μmol/L, respectively (positive control acarbose, IC50 385 μmol/L). [ABSTRACT FROM AUTHOR]

Two new compounds named asperpenes D (1) and E (2) were isolated from the marine-derived fungus Aspergillus sp. SCS-KFD66. Their structures were determined on the basis of spectroscopic methods. Compound 2 represents the first natural product bearing a 2-substituted-5-oxo-4-phenyl-2,5-dihydrofuran-3-carboxylic acid skeleton. All the compounds were tested for enzyme inhibitory activity against AChE and α-glucosidase and DPPH radical scavenging activity, respectively. [ABSTRACT FROM AUTHOR]

The genus Carduus is traditionally used in the Anatolian folk medicine for treating various diseases. Therefore, the enzyme inhibiting potential, antioxidant-antimicrobial activity, and phytochemical profile of Carduus lanuginosus extracts were investigated. The analysis of phenolic compounds was carried out by using RP-HPLC for the chemical characterization of methanol extract. The total polyphenols, total phenolic and flavonoid contents, antioxidant activity (ABTS and DPPH assay), α-amylase, and α-glucosidase inhibition activities were determined using colorimetric methods. Moreover, the antimicrobial activity was examined using the disc diffusion and microdilution methods. The ethylacetate extract was found to have the highest flavonoid and phenolic content. The water and hexane extracts showed strong enzyme inhibitory activity against the α-amylase and α-glucosidase. The methanol extract was found to contain high concentration of chlorogenic acid. The hexane and ethylacetate extracts showed to have significant MIC values on Enterococcus faecium. In conclusion, the extracts of C. lanuginosus might have a significant potential for the use as a natural pharmaceutical agent. [ABSTRACT FROM AUTHOR]

This study to investigate chemical constituents from the aerial of Bupleurum marginatum led to the isolation of a new trierpenoid and a new flavonoid, namely 3β-hydroxy-cycloart-24-en-26-acetyloxy (1), and 3, 3′, 5′-trimethoxyl-myricetin 7-O-β-D–glucopyranoside (2) along with eight known compounds (3–10). Their structures were established by spectral data analyses (MS, 1D and 2D NMR), as well as by comparison of spectral data with those of the related known compounds. The 24-en-lanostane type triterpenoid with a cyclopropane ring (1 and 3) was firstly reported from this specie, which might be chemotaxonomic markers of this specie. In addition, compounds 1 and 2 were examined for their anti-inflammatory activity. Compounds 1 and 2 inhibited the NF κB induction by 60.61% and 24.30%. [ABSTRACT FROM AUTHOR]

The advanced glycation end products (AGEs) constitute a wide variety of substances synthesized from interactions between amino groups of proteins and reducing sugars, which excess induces pathogenesis of chronic diseases. Brazil is the major producer of citrus, a low-cost source of hesperidin, which is a polyphenol recognized for its capacity to inhibit AGEs formation. This is the first work to evaluate the effects of a polyphenolic fraction derived from citrus wastes on the antiglycation and on the inhibition properties of digestive enzymes on the possibility to process these wastes in high value-added products. At concentrations of 10, 15 and 20 mg/mL inhibition of AGEs was higher than 60%. The extracts were able to inhibit by 76% the activity of pancreatic lipase and by 98% the activity of α-glucosidase. For the α-amylase the inhibition capacity was lower than 50%. Strong correlation was obtained among anti-glycation with polyphenolic content and antioxidant capacity. [ABSTRACT FROM AUTHOR]

Environmental, genetic, oxidative and biochemical factors play an important role in the atherosclerotic process. We investigated the association of serum fibroblast growth factor (FGF-23), klotho, fetuin-A, osteoprotegerin (OPG), osteopontin (OPN) and high-sensitive-CRP (Hs-CRP) markers with coronary artery disease and whether one was superior to others or not. A study group of 52 patients with coronary artery disease (CAD) and a control group of 30 patients with angiographically normal epicardial coronary arteries were included in the study. Serum FGF-23, klotho, fetuin-A, OPN, OPG and Hs-CRP marker levels were studied. Patients with CAD were classified in two groups as low (SYNTAX ≤22, n = 29) and moderate-high (SYNTAX ≥ 23, n = 23) according to anatomic SYNTAX score. FGF-23 (p = .033), klotho (p < .001), fetuin-A (p = .005) and OPG (p = .001) serum marker levels were significantly lower in CAD patients than the control group. Serum levels of FGF-23 (p = .012), klotho (p = .001), fetuin-A (p = .015) and OPG (p = 0.002) were significantly different between SYNTAX tertiles and control group. Klotho (p = .025, odd ratio (OR) = 0.542, 95% confidence interval (CI): 0.317-0.926) and HT (p = .004, OR = 34.598, 95%CI:1.054-1135.657) were the independent predictors of CAD presence. Serum klotho levels of 91.48 pmol/L predicts the presence of CAD with 60% sensitivity and 96.55% specificity (p < .001, area under curve = 0.864, 95% CI = 0.768, 0.931). We found that serum klotho level is an independent predictor of presence, extent and severity of CAD. [ABSTRACT FROM AUTHOR]

The carbohydrate-active enzyme (CAZyme) genes of Trametes contribute to polysaccharide degradation. However, the comprehensive analysis of the composition of CAZymes and the biosynthetic gene clusters (BGCs) of Trametes remain unclear. Here, we conducted comparative analysis, detected the CAZyme genes, and predicted the BGCs for nine Trametes strains. Among the 82,053 homologous clusters obtained for Trametes, we identified 8518 core genes, 60,441 accessory genes, and 13,094 specific genes. A large proportion of CAZyme genes were cataloged into glycoside hydrolases, glycosyltransferases, and carbohydrate esterases. The predicted BGCs of Trametes were divided into six strategies, and the nine Trametes strains harbored 47.78 BGCs on average. Our study revealed that Trametes exhibits an open pan-genome structure. These findings provide insights into the genetic diversity and explored the synthetic biology of secondary metabolite production for Trametes. [ABSTRACT FROM AUTHOR]

In this study, with the aid of a constitutive promoter, and the co-expression of chaperone and transcription factor (TF) genes, the expression and enzymatic activity of recombinant κ-carrageenase in Pichia pastoris containing truncated κ-carrageenase gene cgkZΔPst (GS115/pPIC9K-cgkZΔPst) was enhanced. The recombinant P. pastoris strain containing constitutive glyceraldehyde-3-phosphate dehydrogenase (GAP) promoter enabled the expression of recombinant κ-carrageenase without methanol induction, the enzymatic activity was 2.73 U/mL after 96 h of shake flask fermentation at 22 °C. The enzymatic activity increased to 7.96 U/mL under methanol induction during P. pastoris growth, showing a 1.4-fold increase compared to that of the control group. With the co-expression of a series of chaperone genes and TFs that could promote protein folding, prevent protein aggregation, and counteract oxidative stress, the expression level of cgkZΔPst showed a 1.29- to 1.93-fold increase from that in the control group. The enzymatic activity of the recombinant κ-carrageenase increased to 7.07–7.70 U/mL. The use of the inducible PAOX1 in combination with the constitutive PGAP can further improve the productivity of recombinant κ-carrageenase. The rational selection of molecular chaperones and TFs can also promote recombinant κ-carrageenase secretion in P. pastoris. This work can be useful for the heterologous expression of other marine-origin glycoside hydrolases in P. pastoris. [ABSTRACT FROM AUTHOR]

One strategy for developing glycoside hydrolase (GH) inhibitors is to mimic the conformation of the transition state (TS) along the hydrolysis reaction coordinate. We present a DFT-based model to understand the conformational space of the oxocarbenium cation as a TS in carbohydrate chemistry. Using Bolzano's theorem, we have demonstrated the existence of a function that divides the puckering coordinate space. These results are compared with the available experimental crystal structures of GH-inhibitor complexes, and a contradictory case (GH92) was computationally studied. Our mathematical model opens a door to design more specific inhibitors and to decipher the catalytic pathways of controversial cases. [ABSTRACT FROM AUTHOR]

Two new nordammarane-type triterpenoids, 3β-acetoxy-20-oxo-21-nordammaran-23-carboxylic acid methyl ester (1) and 3β-acetoxy-17β-dammaranic acid (2), along with two known cycloartane-type triterpenoids (3–4), were isolated from the petroleum ether-soluble extract of Artemisia argyi. Their structures were elucidated based on 1D and 2D NMR spectroscopic data analysis. All compounds were evaluated for their α-glucosidase inhibitory activity in vitro. Compounds 1–4 exhibited significant inhibitory effects on α-glucosidase with IC50 values ranging from 38.34 ± 0.23 to 105.54 ± 0.33 μM. [ABSTRACT FROM AUTHOR]

A new coumestan named bavacoumestan D (1), together with five known compounds (2-6), was isolated from EtOAc-soluble extract of seeds of Psoralea corylifolia. Their structures were elucidated on the basis of spectroscopic and physico-chemical analyses. All compounds were evaluated for in vitro inhibitory activity against DGAT1, DGAT2 and α-glucosidase. Among them, compounds 1–2, 5–6 showed potential inhibitory activity on DGAT1 with IC50 values ranging from 52.3 ± 1.3 to 81.0 ± 1.0 μM. Compounds 1–3, 6 displayed the significant inhibitory activity on α-glucosidase with IC50 values ranging from 31.2 to 89.1 μM. [ABSTRACT FROM AUTHOR]

This study characterized the functional properties of ethyl acetate-methanol (EA-MeOH) and chloroform extracts of the muricid gastropod Chicoreus ramosus and buccinid Babylonia spirata. The EA-MeOH extract of B. spirata was a potent quencher of radical cation (IC90 < 1 mg/mL), whereas that of C. ramosus held greater anti–inflammatory potential (IC90 5-lipoxygenase inhibition 1.74 mg/mL) than the buccinid gastropod. The EA-MeOH extract of C. ramosus displayed potent antidiabetic activities as deduced by its attenuation properties against carbolytic enzymes α-amylase and α-glycosidase (IC90 1.06 and 2.25 mg/mL, respectively) than those exhibited by B. spirata (IC90 2.32 and 4.50 mg/mL, respectively). The spectroscopic dereplication studies to determine probable chemical groups in the solvent extracts of the studied gastropods revealed the presence of functionalities, which might augment the electronic properties of the bioactive principles present within the extract, thereby enhancing their activity. Thus, the present study recognized that marine gastropods C. ramosus and B. spirata have potential functional implications against oxidative stress-induced diseases, such as diabetes and inflammation. This research supports further investigation of these previously uncharacterized marine gastropod species to isolate potential bioactive leads for use against various biological targets and to develop functional food formulations. [ABSTRACT FROM AUTHOR]

Polyphenols, as one group of secondary metabolite, are widely distributed in plants and have been reported to show various bioactivities in recent year. Starch digestion not only is related with food industrial applications such as brewing but also plays an important role in postprandial blood glucose level, and therefore insulin resistance. Many studies have shown that dietary phenolic extracts and pure polyphenols can retard starch digestion in vitro, and the retarding effect depends on the phenolic composition and molecular structure. Besides, dietary polyphenols have also been reported to alleviate elevation of blood glucose level after meal, indicating the inhibition of starch digestion in vivo. This review aims to analyze how dietary polyphenols affect starch digestion both in vitro and in vivo. We can conclude that the retarded starch digestion in vitro by polyphenols results from inhibition of key digestive enzymes, including α-amylase and α-glucosidase, as well as from interactions between polyphenols and starch. The alleviation of postprandial hyperglycemia by polyphenols might be caused by both the inhibited starch digestion in vivo and the influenced glucose transport. Therefore, phenolic extracts or pure polyphenols may be alternatives for preventing and treating type II diabetes disease. [ABSTRACT FROM AUTHOR]