Disease-related Enzymes Research Articles

Synthesis, Characterization, and Biological Evaluation of N-Methyl Derivatives of Norbelladine.

Norbelladine derivatives have garnered attention in recent years due to their diverse biological activities and pivotal role in the biosynthetic pathway of Amaryllidaceae alkaloids. This study reports the synthesis and biological evaluation of four O,N-methylated derivatives of norbelladine. These derivatives were synthesized through a three-step process: forming imine intermediates from benzaldehydes with tyramine, hydrogenating them to secondary amines, and N-methylating these amines. The products were purified and characterized by 1H and 13C NMR spectroscopy. Their biological activities were assessed by evaluating their ability to inhibit Alzheimer's disease-related enzymes acetylcholinesterase and butyrylcholinesterase. Additionally, the cytotoxic activity of the novel derivatives was tested against cancer cell lines derived from hepatocarcinoma (Huh7), adenocarcinoma (HCT-8), and acute myeloid leukemia (THP-1) cells, and their antiviral properties against a human coronavirus (HCoV-OC43), a flavivirus (dengue virus), and a lentivirus (pseudotyped HIV-1). Docking analysis was performed to understand the impact of the N-methylation on their pharmacological relevance. The results indicate that while N-methylation does not significantly affect antiviral activity, it enhances butyrylcholinesterase inhibition for N-methylnorbelladine and 4'-O,N-dimethylnorbelladine. Overall, this work enhances our understanding of norbelladine derivatives, provides new tools for Alzheimer's disease research, and lays the groundwork for future pharmaceutical developments.

Metabolomic Analyses Reveal That IAA from Serratia marcescens Lkbn100 Promotes Plant Defense during Infection of Fusarium graminearum in Sorghum.

Global sorghum production has been significantly reduced due to the occurrence of sorghum root rot caused by the fungus Fusarium graminearum. The utilization of biocontrol microorganisms has emerged as an effective strategy. However, the underlying mechanisms remain unclear. Therefore, the aim of this study was to investigate the effectiveness of biocontrol bacteria in inducing sorghum resistance against sorghum root rot and explore the potential induced resistance mechanisms through metabolomics analysis. The results revealed that the biocontrol bacteria Lnkb100, identified as Serratia marcescens (GenBank: PP152264), significantly enhanced the resistance of sorghum against sorghum root rot and promoted its growth, leading to increased seed weight. Targeted metabolomics analysis demonstrated that the highest concentration of the hormone IAA (indole-3-acetic acid) was detected in the metabolites of Lnkb100. Treatment with IAA enhanced the activity of disease-related enzymes such as SOD, CAT, POD and PPO in sorghum, thereby improving its resistance against sorghum root rot. Further untargeted metabolomic analysis revealed that IAA treatment resulted in higher concentrations of metabolites involved in the resistance against F. graminearum, such as geniposidic acid, 5-L-Glutamyl-taurine, formononetin 7-O-glucoside-6″-O-malonate, as well as higher concentrations of the defense-related molecules volicitin and JA. Additionally, "secondary bile acid biosynthesis" and "glycerophospholipid metabolism" pathways were found to play significant roles in the defense response of sorghum against fungal infection. These findings provide a reliable theoretical basis for utilizing biocontrol microorganisms to control sorghum root rot.

Synthesis, in vitro activity, and molecular docking of caffeic acid and resveratrol derivatives against Alzheimer’s disease-related enzymes

Synthesis, in vitro activity, and molecular docking of caffeic acid and resveratrol derivatives against Alzheimer’s disease-related enzymes

Evaluation of 3,4-diethoxy substituted thioureas and their thiazole derivatives as potent anti-Alzheimer's agents: Synthesis, DFT, biological activity and molecular modeling investigations

The current research project aims to develop 3, 4-diethoxy substituted thioureas (15–20) and thiazoles (22–23, 25–26) analogs as potential anti-Alzheimer's agents. A total of ten derivatives were synthesized and were further characterized with TLC, FTIR, and NMR techniques. In addition, density functional theory (DFT) calculations and molecular modeling were performed to evaluate the electronic properties and anti-Alzheimer's disease potential of the compounds within the active pockets of the targeted enzymes, respectively. During in-vitro testing, it was determined that all analogs exhibited some degree of inhibitory potential, and analogs (15), (16), (19), and (26) were found to have excellent potency in inhibiting Alzheimer's disease-related enzymes i.e., monoamine oxidase-A, monoamine oxidase-B, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). Analog (15) demonstrated an IC50 of 1.33 ± 0.04 µM for MAO-A; (16) showed an IC50 of 1.67 ± 0.06 µM for MAO-B, (19) represented an IC50 of 0.31 ± 0.02 µM for AChE, and (26) showed an IC50 of 0.51 ± 0.01 µM for BChE. These compounds have shown a comparable potential with the reference compounds i.e., Clorgyline (for MAO-A), Deprenyl (for MAO-B) and donepezil in case of AChE and BChE, respectively. The study also established a structure-activity relationship and determined that the potency of the analogs depends on the nature, position, number, and electron-donating/-withdrawing effects of the phenyl ring substituents. The identified compounds also exhibited strong binding interactions during molecular docking investigations. Moreover, the most potent complexes of respective targets were found stable during molecular dynamics simulation studies. The findings of the current study revealed that new thioureas and thiazoles analogs exhibited a reactive electronic property, which is essential for anti-cholinesterase activity.

Application of Enzyme Inhibition Therapy in the Management/Treatment of Neurological Conditions, Diseases, and Disorders

Enzyme inhibition therapy uses specific molecules to inhibit enzyme activity, targeting disease-related enzymes in medical treatments like cancer treatment and infectious disease management. Different types of inhibitors, competitive and non-competitive, bind to different sites and alter enzyme function. The success of this therapy depends on the inhibitor's specificity and delivery to the target site. Further research could lead to more effective treatments. Nowadays, the majority of medications are enzyme inhibitors and are in the clinical or pre-clinical stages of drug development. Enzyme inhibitors are often prescribed medications for a variety of illnesses, including neurological problems. There is only symptomatic therapy available for many neurological conditions, particularly neuro-degenerative disorders, as opposed to therapy based on knowledge of the underlying mechanisms of these diseases. Enzyme inhibitors are useful as they block the function of certain enzymes whose aberrant activity could be contributing to the illness. They also alleviate the symptoms and stop the disease’s progression. This review discusses the mechanism of action of several enzyme inhibitors that have been prescribed as medications for neurological illnesses as well as some that are still in research stages.

Phenolic compounds recovery from date seed and assessment of their antioxidant and enzyme inhibitory properties

Date fruit is a highly important crop cultivated in arid and semi-arid regions, known for its nutritional value and health benefits. Dates' benefits extend beyond their edible portion and include seeds, which are a by-product of different industries, often considered waste, and have untapped potential. This work aimed to optimize the extraction conditions of antioxidant compounds from date seeds and assess their ability to inhibit disease-related enzymes. The optimization was carried out by examining the main parameters, including solvent type (acetone, ethanol, methanol, and water), solvent concentration (25–100%), sample-to-solvent ratio (10–60/20 mg/ml), and extraction time (15–90 min). Phenolic content (PC) was determined using the Folin-Ciocalteu method, while antioxidant activity was evaluated by ABTS and DPPH scavenging assays, as well as ferric reducing power (FRP). Based on the statistical analysis, 75% acetone, 10 mg/20 ml, and 45 min were found to be the best extraction conditions, manifesting a PC of 128.65 mg GAE/g dw, antiradical powers of 244.91 mg TE/g dw (ABTS) and 64.27 mg GAE/g dw (DPPH), and a FRP of 64.27 mg GAE/g dw. Moreover, the extract of date seed demonstrated a promising inhibitory property against some key enzymes such as tyrosinase, acetylcholinesterase, and α-glucosidase, which may be considered a good candidate for managing diabetes, Alzheimer's disease, and neurodegenerative disorders.

Fabrication of a Magnetic Porous Organic Polymer for α-Glucosidase Immobilization and Its Application in Inhibitor Screening

The technology based on immobilized enzymes was employed to screen the constituents inhibiting disease-related enzyme activity from traditional Chinese medicine, which is expected to become an important approach of innovative drug development. Herein, the Fe3O4@POP composite with a core-shell structure was constructed for the first time with Fe3O4 magnetic nanoparticles as the core, 1,3,5-tris (4-aminophenyl) benzene (TAPB) and 2,5-divinylterephthalaldehyde (DVA) as organic monomers, and used as the support for immobilizing α-glucosidase. Fe3O4@POP was characterized by transmission electron microscopy, energy-dispersive spectrometry, Fourier transform infrared, powder X-ray diffraction, X-ray photoelectron spectroscopy, and vibrating sample magnetometry. Fe3O4@POP exhibited a distinct core-shell structure and excellent magnetic response (45.2 emu g-1). α-Glucosidase was covalently immobilized on core-shell Fe3O4@POP magnetic nanoparticles using glutaraldehyde as the cross-linking agent. The immobilized α-glucosidase possessed improved pH stability and thermal stability as well as good storage stability and reusability. More importantly, the immobilized enzyme exhibited a lower Km value and enhanced affinity for the substrate than the free one. The immobilized α-glucosidase was subsequently used for inhibitor screening from 18 traditional Chinese medicines in combination with capillary electrophoresis analysis among which Rhodiola rosea exhibited the highest enzyme inhibitory activity. These positive results demonstrated that such magnetic POP-based core-shell nanoparticles were a promising carrier for enzyme immobilization and the screening strategy based on immobilized enzyme provided an effective way to rapidly explore the targeted active compounds from medicinal plants.

N-Hydroxy-N-Propargylamide Derivatives of Ferulic Acid: Inhibitors of Cholinesterases and Monoamine Oxidases.

Alzheimer's disease (AD) is a complex disorder characterized by impaired neurotransmission in cholinergic and monoaminergic neurons, which, in combination with the accumulation of misfolded proteins and increased oxidative stress, leads to the typical features of the disease at the biomolecular level. Given the limited therapeutic success of approved drugs, it is imperative to explore rationally supported therapeutic approaches to combat this disease. The search for novel scaffolds that bind to different receptors and inhibit AD disease-related enzymes could lead to new therapeutic solutions. Here, we describe N-hydroxy-N-propargylamide hybrids 1-6, which were designed by combining the structures of Contilisant-a multifunctional anti-AD ligand-and ferulic acid, a natural antioxidant with various other biological activities. Among the synthesized compounds, we identified compound 4 as a micromolar inhibitor of hAChE with a potent radical-scavenging capacity comparable to resveratrol and Trolox. In addition, compound 4 chelated copper(II) ions associated with amyloid β pathology, mitochondrial dysfunction, and oxidative stress. The promising in vitro activity combined with favorable drug-like properties and predicted blood-brain barrier permeability make compound 4 a multifunctional ligand that merits further studies at the biochemical and cellular levels.

Cut-off values of neonatal lysosomal storage disease-related enzymes detected by tandem mass spectrometry.

To establish cut-off values of lysosomal storage disease (LSD)-related enzymes by tandem mass spectrometry. A total of 26 689 newborns and 7 clinically confirmed LSD children underwent screening for LSDs (glycogen storage disease typeⅡ, Fabry disease, mucopolysaccharidosis type Ⅰ, Krabbe disease, Niemann-Pick disease A/B and Gaucher disease). The activities of LSD-related enzymes were detected by tandem mass spectrometry. The 20% of the median enzyme activity of each batch of acid β-glucocerebrosidase, acid sphingomyelinase, β-galactocerebroside, α- L-iduronidase and acid α-glucosidase, and the 30% of the median enzyme activity of α-galactosidase were taken as cut-off values of corresponding enzymes. The genetic diagnosis was performed in neonates whose enzyme activity was lower than 70% of the cut-off value. The enzyme activities of 7 clinically confirmed cases were all lower than the cut-off values. Among 26 689 newborns, 142 cases (0.53%) were suspected positive for LSDs, including 25 cases of β-galactocerebroside deficiency, 1 case of α- L-iduronidase deficiency, 19 cases of α-galactosidase deficiency, and 97 cases of acid α-glucosidase deficiency. Eight infants were genetically diagnosed with LSDs, including 3 cases of glycogen storage disease type Ⅱ, 3 cases of Krabbe disease, and 2 cases of Fabry disease, with a positive predictive value of about 5.6%. Cut-off values ​​of the 6 LSD enzyme activities all showed a downward trend from March to August, and an upward trend from September to December. There was a statistically significant difference in LSD enzyme activity among different months ( P<0.05). The established cut-off values of LSD-related enzyme activities detected by tandem mass spectrometry can be used for screening LSDs in neonates, and the enzyme activity would be affected by temperature and humidity.

Electrochemical biosensors based on peptide-kinase interactions at the kinase docking site

Kinases are important cancer biomarkers and are conventionally detected based on their catalytic activity. Kinases regulate cellular activities by phosphorylation of motif-specific multiple substrate proteins, resulting in a lack of selectivity of activity-based kinase biosensors. We present an alternative approach of sensing kinases based on the interactions of their allosteric docking sites with a specific partner protein. The new approach was demonstrated for the ERK2 kinase and its substrate ELK-1. A peptide derived from ELK-1 was bound to a gold electrode and ERK2 sensing was performed by electrochemical impedance spectroscopy. We performed a detailed analysis of the interaction between the ELK-1 peptide and the kinase on gold surfaces. Atomic force microscopy, variable angle spectroscopic ellipsometry, X-ray Photoelectron Spectroscopy, and polarization modulation IR reflection-absorption spectroscopy analysis of the gold surface revealed the adsorbed layer of the ERK2 on the peptide monolayer. The sensors showed a high level of target selectivity for ERK2 compared to the p38γ kinase and BSA. ERK2 was detected in its cellular concentration range, 0.5–2.0 μM, and the limit of detection was calculated to be 0.35 μM. Using the flexibility of peptide design, our method is generic for developing sensitive and substrate-specific biosensors and other disease-related enzymes based on their interactions.

Inhibitory Activities of Sulfur Compounds in Garlic Essential Oil against Alzheimer's Disease-Related Enzymes and Their Distribution in the Mouse Brain.

Alzheimer's disease (AD) is the most common neurodegenerative disease. Garlic reportedly has various physiological effects, including a role in protecting against dementia. However, the action mechanisms of garlic on AD are not entirely clear. In this study, we investigated the inhibitory activity of garlic essential oil (GEO) against AD-related enzymes and evaluated the distribution of active substances in GEO to the brain. We found that several sulfur compounds in GEO significantly inhibited AD-related enzymes. Sulfur compounds were detected in the serum and brain 6 h post administration. The ratios of allyl mercaptan (24.0 ± 3.9%) and allyl methyl sulfide (49.8 ± 15.6%) in the brain were significantly higher than those in GEO, while those of dimethyl trisulfide (0.89 ± 34.8%), allyl methyl trisulfide (0.41 ± 19.0%), and diallyl trisulfide (0.43 ± 72.8%) in the brain were significantly lower than those in GEO. Similar results were observed in the serum, suggesting that the organosulfur compounds were converted to allyl mercaptan or allyl methyl sulfide in the body. Although allyl mercaptan and allyl methyl sulfide are not the main components of GEO, they might be key molecules to understand the bioactivities of GEO in the body.

Cover Feature: Real‐Time and Label‐Free Measurement of Deubiquitinase Activity with a MspA Nanopore (ChemBioChem 17/2021)

Ubiquitination plays a prominent role in cell signaling networks. Enzymes governing ubiquitination include the conjugation machinery along with the deconjugating enzymes - deubiquitases. A MspA nanopore is demonstrated as a sensor for discriminating and quantifying various ubiquitin proteins. Real-time measurement of polymeric ubiquitin chain disassembly by a deubiquitinating enzyme was performed and enzyme kinetics were determined. The implementation of MspA into arrays could enable high throughput characterizations of unknown deubiquitinases as well as drug screening against disease-related enzymes. More information can be found in the Communication by Min Chen et al.

Bacillus subtilis HSY21 can reduce soybean root rot and inhibit the expression of genes related to the pathogenicity of Fusarium oxysporum

Soybean root rot occurs globally and seriously affects soybean production. To avoid the many disadvantages of chemical fungicides, the addition of Bacillus is gradually becoming an alternative strategy to tackle soybean root rot. However, the molecular mechanism of phytopathogenic fungi in this process by Bacillus inhibition is rarely reported. In this study, we isolated a strain of B. subtilis HSY21 from soybean rhizosphere soil, which had an inhibition rate of 81.30 ± 0.15% (P < 0.05) against Fusarium oxysporum. The control effects of this strain against soybean root rot under greenhouse and field conditions were 63.83% and 57.07% (P < 0.05), respectively. RNA-seq analysis of F. oxysporum after treatment with strain HSY21 revealed 1445 downregulated genes and 1561 upregulated genes. Among them, genes involved in mycelial growth, metabolism regulation, and disease-related enzymes were mostly downregulated. The activities of cellulase, β-glucosidase, α-amylase, and pectin-methyl- galacturonase as well as levels of oxalic acid and ergosterol in F. oxysporum were significantly decreased after HSY21 treatment. These results demonstrated that B. subtilis HSY21 could effectively control F. oxysporum by inhibiting its growth and the expression of pathogenic genes, thus indicating that this strain may be an ideal candidate for the prevention and control of soybean root rot.

In vitro Antioxidant and Anticholinesterase Activities of Senecio massaicus Essential Oil and Its Molecular Docking Studies as a Potential Inhibitor of Covid-19 and Alzheimer’s Diseases

The composition of the essential oil obtained from the dried aerial parts of Senecio massaicus was analyzed by GC/MS. Twenty-two components have been identified and represented 97.41 % of the total oil composition. The major constituents of the essential oil were m-cymene (30.58 %), n-hexadecanoic acid (14.88 %) and docosane-11-decyl (10.43 %). Four methods were used to determine the antioxidant activity: DPPH, ABTS, CUPRAC and reducing power assay. The results indicate that the essential oil extract has moderate to low activity compared to the reference antioxidant compounds. In vitro anticholinesterase activity of the essential oil has also been studied. It exhibited higher inhibitory activity against butyrylcholinesterase (BChE) than against acetylcholinesterase (AChE). Docking studies conducted for Alzheimer's disease-related enzymes have displayed that compounds docosane-11-decyl and octaethyleneglycol monododecyl ether have strong potency, and compounds 15,15’Bi1,4,7,10,13-pentaoxacyclohexadecane and n-Hexadecanoic acid have moderate inhibitory potential. In addition, these three compounds (Docosane-11-decyl, octaethyleneglycol monododecyl ether and 15,15’Bi1,4,7,10,13-pentaoxacyclohexadecane) of the essential oil displayed strong interaction against SARS-CoV-2 main protease and Nsp15 endoribonuclease. Therefore, it could be useful to provide anticholinesterase agent and anti-coronavirus candidate drugs.

Real-Time and Label-Free Measurement of Deubiquitinase Activity with a MspA Nanopore.

Covalently attaching ubiquitin (Ub) to cellular proteins as a post-translational modification can result in altered function of modified proteins. Enzymes regulating Ub as a post-translational modification, such as ligases and deubiquitinases, are challenging to characterize in part due to the low throughput of in-vitro assays. Single-molecule nanopore based assays have the advantage of detecting proteins with high specificity and resolution, and in a label-free, real-time fashion. Here we demonstrate the use of a MspA nanopore for discriminating and quantifying Ub proteins. We further applied the MspA pore to measure the Ub-chain disassembly activity of UCH37, a proteasome associated deubiquitinase. The implementation of this MspA system into nanopore arrays could enable high throughput characterizations of unknown deubiquitinases as well as drug screening against disease related enzymes.

Mechanisms of Proteolytic Enzymes and Their Inhibition in QM/MM Studies.

Experimental evidence for enzymatic mechanisms is often scarce, and in many cases inadvertently biased by the employed methods. Thus, apparently contradictory model mechanisms can result in decade long discussions about the correct interpretation of data and the true theory behind it. However, often such opposing views turn out to be special cases of a more comprehensive and superior concept. Molecular dynamics (MD) and the more advanced molecular mechanical and quantum mechanical approach (QM/MM) provide a relatively consistent framework to treat enzymatic mechanisms, in particular, the activity of proteolytic enzymes. In line with this, computational chemistry based on experimental structures came up with studies on all major protease classes in recent years; examples of aspartic, metallo-, cysteine, serine, and threonine protease mechanisms are well founded on corresponding standards. In addition, experimental evidence from enzyme kinetics, structural research, and various other methods supports the described calculated mechanisms. One step beyond is the application of this information to the design of new and powerful inhibitors of disease-related enzymes, such as the HIV protease. In this overview, a few examples demonstrate the high potential of the QM/MM approach for sophisticated pharmaceutical compound design and supporting functions in the analysis of biomolecular structures.

Inhibitory Potential of Acroptilon repens against Key Enzymes involved in Alzheimer and Diabetes, Phytochemical Profile, Radical Scavenging, and Antibacterial Activity.

Background:This study was devoted to assessing the inhibitory potential of acetone, methanol, and ethanol extracts of Acroptilon repens against disease-associated enzymes, as well as their antioxidant/antibacterial activity and phytochemical composition. Methods:Comparative assessment using various antioxidant evaluation methods, including FRAP, scavenging ability on DPPH radical and hydrogen peroxide, and RP, indicated that the acetone extract presented the highest antioxidant activity, due to its highest total antioxidant content. Results:The TPC and TFC of these extracts were 3.44 ± 0.32 mg GAE/g DW and 2.09 ± 0.2 mg QE/g DW, respectively. The hydrodistillation essential oil from A. repens was analyzed by GC/MS, and 17 compounds were identified. All extracts showed good inhibitory activities against disease-related enzyme acetylcholinesterase and α-amylase, with the lowest IC50 for acetonic extract. Extracts of A. repens exhibited inhibiting activities against the Gram-positive bacteria, with the most effect of acetone extract. Conclusion:Our findings suggest A. repens as a promising source of natural antioxidant, antimicrobial, anti-cholinesterase and anti-amylase agents for the management of oxidative damage, and pharmaceutical, food, and cosmeceutical purposes.

Unravelling the Enzymatic Degradation Mechanism of Supramolecular Peptide Nanofibers and Its Correlation with Their Internal Viscosity.

Enzyme-responsive supramolecular peptide biomaterials have attracted growing interest for disease diagnostics and treatments. However, it remains unclear whether enzymes target the peptide assemblies or dissociated peptide monomers. To gain further insight into the degradation mechanism of supramolecular peptide amphiphile (PA) nanofibers, cathepsin B with both exopeptidase and endopeptidase activities was exploited here for degradation studies. Hydrolysis was found to occur directly on the PA nanofibers as only surface amino acid residues were cleaved. The number of cleaved residues and the degradation efficiency was observed to be negatively correlated with the internal viscosity of the PA nanofibers, quantified to be between 200-800 cP (liquid phase) using fluorescence lifetime imaging microscopy combined with an environmentally sensitive molecular rotor, BODIPY-C10. These findings enhance our understanding on the enzymatic degradation of supramolecular PA nanofibers and have important implications for the development of PA probes for the real-time monitoring of disease-related enzymes.

Chemical profile, antioxidant, antimicrobial, enzyme inhibitory, and cytotoxicity of seven Apiaceae species from Turkey: A comparative study

Several Apiaceae species, used as both food and in complementary and alternative medicine, represents a rich source of potential valuable phytopharmaceuticals which necessitates scientific contemplation. In the present study, the antioxidant, enzyme inhibitory, antimicrobial, and cytotoxic properties of methanol extracts of seven Apiaceae species, (Chaerophyllum macrospermum (Willd. ex Spreng.) Fisch. & C.A.Mey. ex Hohen, Ferula rigidula Fisch. ex DC., Ferula orientalis L., Prangos ferulacea Lindl., Prangos peucedanifolia Fenzl., Ferulago setifolia K. Koch, and Pimpinella anthriscoides Boiss.) were evaluated. Species belonging to the Prangos genus exhibited the highest total phenolic content, namely P. peucedanifolia and P. ferulacea, with values of 47.90 and 44.44 mg gallic acid equivalent/g extract, respectively. P. peucedanifolia also displayed the highest radical scavenging capacity (81.53 and 102.70 mg Trolox equivalent [TE]/g extract for 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), respectively) and reducing power (165.87 and 100.09 mg TE/g extract for cupric reducing antioxidant capacity (CUPRAC) and ferric reducing antioxidant power (FRAP), respectively). C. macrospermum showed the most potent inhibition against Alzheimer’s disease related enzymes, namely acetylcholinesterase (4.53 mg galantamine equivalent [GALAE]/g extract) and butyrylcholinesterase (3.22 mg GALAE/g extract). P. ferulacea (131.94 mg kojic acid (KAE) equivalent/g extract) and P. peucedanifolia (4.97 mmol acarbose equivalent (ACAE)/g extract) were potent inhibitors of tyrosinase and α-glucosidase, respectively. In general, studied species were able to reduce cellular viabilities. P. peucedanifolia possessed promising antibacterial potential against Bacillus cereus (Minimum inhibition concentration (MIC): 0.37 mg/mL), L. monocytogenes (MIC: 0.56 mg/mL), P. aeruginosa and Escherichia coli (MIC: 0.27 mg/mL), Salmonella typhimurium and Enterobacter cloacae (MIC: 0.75 mg/mL). F. rigidula showed the highest antifungal effect against Aspergillus ochraceus and Trichoderma viride (MIC: 0.10 mg/mL). The present findings could be the scientific starting point towards the pharmaceutical and/or commercial utilization of these Apiaceae species.

Nanocatalyst sensor produces simple cancer test

Detecting some cancers early can improve a patient’s chance of survival, but conventional detection methods can involve costly tests and equipment, making them inaccessible for people in low-resource areas. Researchers have now developed a diagnostic test that can detect a molecular signature of cancer and other diseases with a simple readout: it turns urine blue (Nat. Nanotechol. 2019, DOI: 10.1038/s41565-019-0527-6). Molly Stevens of Imperial College London teamed up with Sangeeta Bhatia of the Massachusetts Institute of Technology to create nanoparticle-protein complexes that, once injected, can reveal the presence of disease-related enzymes through a simple urine test. The team used peptides to link gold nanoclusters to neutravidin, a protein carrier. They designed the linkers so that enzymes called matrix metalloproteinases (MMPs) can cleave them. The presence of MMPs has been proposed as an early warning sign of several cancers. To test their sensors, the team injected the complexes into healthy mice