Chelating Properties Research Articles

Synthesis and antifungal activity of novel amide derivatives from quinic acid against the sweet potato pathogen Ceratocystis fimbriata.

Ceratocystis fimbriata is a fungal pathogen that infects sweet potato roots, producing enormous economic losses. Cyclic polyhydroxy compound quinic acid is a common metabolite synthesized in plant tissues, including sweet potato tubers, showing weak antifungal properties. Although several O-acylated quinic acid derivatives have been synthesized and found in nature and their antifungal properties have been explored, derivatives based on modification of the carboxylic acid have never been evaluated. In this study, amide derivatives were synthesized via linkage of amines with the carboxylic acid moiety of quinic acid. Derivatives with high dipolar moments and a low number of rotatable bonds showed greater antifungal activities toward C. fimbriata in vitro than quinic and chlorogenic acids. Derivative 5b, which was synthesized by coupling p-aminobenzoic acid (pABA) with quinic acid, had the greatest antifungal activity. 5b showed iron(II)-chelating properties and reduced ergosterol content in C. fimbriata cells, causing irregularities in the fungal cell wall and inhibiting conidia agglutination. Application of 3 mm 5b reduced black rot symptoms in sweet potatoes by 70.1%. Collectively, derivatization of the carboxylic acid from quinic acid was demonstrated to be a suitable strategy to improve the antifungal properties of this compound. This study reveals a new efficient strategy for management of the sweet potato pathogen C. fimbriata. © 2024 Society of Chemical Industry.

Antioxidant activities of developed natural smoothies and their effects on blood glucose levels and expression of pro-inflammatory genes in streptozotocin-induced diabetic rats

Fruits and vegetables are laden with antioxidants and have been used to quench reactive oxygen species. The combination of two or more fruits and vegetables to produce smoothies is expected to yield a synergistic effect that could further improve functionality. This study investigated the antioxidative and blood glucose-lowering potentials of smoothies made from selected fruits and vegetables as well as their effect on the expression of pro-inflammatory genes in streptozotocin-induced diabetic Wistar rats. Standard procedures were used for the in vitro antioxidant determination while pancreas tissue was excised for molecular study. The inclusion of beetroot increased the total phenolic contents by 30-50% while the flavonoid content was increased by more than 3-fold. Similarly, smoothies with beetroot and bitter gourd exhibited stronger free radical scavenging abilities as shown by DPPH (1, 1- diphenyl-2-picrylhydrazyl), ABTS (2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic) acid), Nitric oxide (NO) scavenging ability, metal chelation (Fe2+) and ferric reducing antioxidant properties (FRAP) compared to the sample devoid of the duo. The blood glucose levels of the rats fed the smoothie were significantly lowered with a similar trend in the animals that were administered metformin. The smoothies significantly (p<0.05) reduced the malondialdehyde (MDA) content thus reducing lipid peroxidation in the animals. The endogenous antioxidant enzymes; catalase (CAT), superoxide dismutase (SOD) and glutathione peroxidase (GPX) in the pancreas were all significantly (p<0.05) increased when the animals were fed smoothies. The expression of pro-inflammatory genes, IL-1β, IL-6 and TNF-α, was down-regulated in the animals fed with smoothies. The findings showed that the smoothies made from the combination have the potential for managing type-2 diabetes mellitus.Graphical

Corrective role of endophytic exopolysaccharides from Clerodendrum infortunatum L. on arsenic-induced ovarian steroidogenic dysfunction and associated inflammatory responses

The present investigation aimed to evaluate the therapeutic potential of exopolysaccharides (EPSs) derived from endophytic fungi against arsenic [As(III)]-mediated metabolic and reproductive ailments. Two endophytic fungi, Diaporthe arengae (CleR1) and Fusarium proliferatum (CleR3), were isolated from Clerodendrum infortunatum (Cle), and used for the extraction of two types of EPSs. GC–MS analysis confirmed the presence of hydroxymethyl furfural (HMF) and α-d-glucopyranose in the EPS1 (CleR1) and EPS2 (CleR3), respectively. FTIR analysis revealed the potential As(III)-chelation properties of both EPSs. EPS1 and EPS2 significantly mitigated As(III)-induced oxidative stress and lipid peroxidation by restoring the activities of antioxidative enzymes. EPSs successfully corrected the gonadotropin imbalance and steroidogenic alterations. The downregulation of proinflammatory (NF-κB and TNF-α) and proapoptotic (BAX) mediators and the upregulation of antiapoptotic (Bcl-2) markers were also detected following the treatment with EPSs. Histomorphological restoration of reproductive and metabolic organs was also observed in both the EPS groups. Moreover, the As(III)-induced increase in the immunoreactivity of the androgen receptor (AR) was successfully reversed by these EPSs. Molecular docking predicted that HMF and α-d-glucopyranose of EPS1 and EPS2 interact with the active site of AR by limiting its activity. Hence, EPS could be effective for developing new therapeutic strategies for managing As(III) toxicity.

Multifunctional property of N,N-bis (carboxymethyl) glutamic acid modified biomass material: adsorption and degradation removals of cationic dyes in wastewater

As a common type of pollutants in industrial wastewater, cationic dyes have attracted great attentions. Using biodegradable N,N-di (carboxymethyl) glutamic acid (GLDA) as ligand and corn stalk (CS) as matrix, a novel and green biomass modified material GLDA-CS was successfully prepared. The multifunctional property of GLDA-CS for removing methylene blue (MB), malachite green (MG) and alkaline red 46 (R-46) from wastewater was evaluated. The dyes were removed by the electrostatic adsorption based on the cationic adsorption properties of GLDA-CS. The removal rates of MB, MG and R-46 can quickly reach 90.4%, 96.8% and 94.8% in short time. especially for MG and R-46 even only 20 min. The adsorption capacities of the dyes still remain more than 86.5% of the initial values after 5 cycles. In a heterogeneous system, the dyes were removed by Fenton-like degradation based on the metal chelating property of GLDA-CS. 100% degradation rates of the dyes can be achieved in 35 min under the acidic region. Even if at pH 7, degradation rates are 44.1%, 47.1% and 56.6% higher than those under the conventional homogeneous system, and the degradation rate remained at 83.7% after 5 cycles. Regardless of the adsorption or degradation, GLDA-CS shows strong anti-anion interference ability. The potential mechanisms of adsorption and degradation for the dyes by GLDA-CS were deduced by quantization calculation. It is concluded that the adsorption removal of the dyes by GLDA-CS follows MG > R-46 > MB, and mainly depends on the electrostatic interaction between -COOH in GLDA-CS and -N- in the dye molecules. Based on the degradation mechanism of Fenton-like reaction, the possible active sites of the dyes attacked by free radicals and their possible degradation intermediates were predicted by the calculations of Fukui function.

Efficacy of Radical‐Scavenging Activity in Novel Diorganotin(IV) Complexes of Schiff Bases of Salicylaldehyde

AbstractBiopotent hybrid diorganotin(IV) complexes, derived from salicylaldehyde Schiff bases having general formula R2SnL, where LH = (OH)C6H4HC: NCR′(R″)CHR‴OH] [where R = Me or Bu], were logically designed, generated, and characterized using spectroscopic techniques, single‐crystal X‐ray investigations, and DFT studies. Different diorganotin(IV) complexes were synthesized because of interaction between diorganotin(IV) dichloride and sodium salts of Schiff bases of salicylaldehyde ligand in anhydrous refluxing THF at 1:1 and 1:2 molar ratio (Product A and B). The chelating property of Schiff bases replaces organo group from diorganotin(IV) dichloride. It creates an O2SnL type of complex when diorganotin(IV) dichloride and ligand interact in 1:2 ratio, which is this study's most fascinating aspect. The characterization of these complexes is aided by physicochemical and spectroscopic investigations, including IR and NMR (1H, 13C, and 119Sn). Single‐crystal X‐ray investigations, mass spectrum studies, and DFT investigations suggest the dimeric structure of these compounds. These diorganotin(IV) complexes have a dimeric structure containing hexacoordinated central tin atom. Two µ2─O atoms bridge the gap between two Sn(IV) atoms in the dimeric dimethyltin(IV) complexes. The DPPH assay results for radical scavenging activity and IC50 values demonstrate the antioxidative potential of diorganotin(IV).

Synergistic removal of malachite green and Cr(Ⅵ) using ethylenediamine disuccinic acid functionalized silica gel

As common industrial raw materials, malachite green (MG) and Cr(Ⅵ) generally coexist in waste liquids discharged from the paper printing, leather, and textile industries, causing serious harm to humans and the environment. Therefore, developing an effective method for the synergistic removal of MG and Cr(Ⅵ) from aquatic environments is of great research value. In this work, the non-homogeneous Fenton-like catalysts, namely, EDDS-Silica and EDDS-Co2+-Silica were successfully prepared using ethylenediamine disuccinic acid (EDDS) and silica gel (Silica) as raw materials, and a non-homogeneous Fenton-like catalytic method was developed for the efficient and synergistic removal of MG and Cr(Ⅵ) from wastewater. EDDS-Silica and EDDS-Co2+-Silica were analyzed using Fourier infrared spectroscopy and X-ray photoelectron spectroscopy to determine their structural composition and elemental contents. The catalytic degradation and removal effects of these materials in an MG single-waste system were also investigated. The results demonstrated that the incorporation of both materials can overcome the limitation of the conventional Fenton reaction, which is its applicability to acidic environments only. Moreover, EDDS-Co2+-Silica showed better degradation effects on MG than EDDS-Silica. Quantitative calculations based on density functional theory were used to predict the optimal coordination forms between Co2+and EDDS-Silica as well as the MG structure. The lowest unoccupied and highest occupied molecular orbitals of the catalysts were then used to predict the active sites on which MG tends to capture or release electrons during the degradation reaction. The optimal conditions for the synergistic removal of MG and Cr(Ⅵ) from a binary system using EDDS-Co2+-Silica were further investigated under different influencing factors. The results showed that EDDS-Co2+-Silica still had excellent catalytic effect on the degradation rate of MG in the range of pH 3-7, and the optimal conditions were as follows: solution pH, 7; degradation time, 1 h; temperature, 25 ℃; H2O2 concentration, 20 mmol/L; and the initial mass concentration of Cr(Ⅵ), 25 mg/L. Under the above conditions, the degradation rate was increased from 87.25% to 96.67% compared with that in the MG monosystem. Obvious enhancements in degradation effect and efficiency confirmed that the incorporation of EDDS-Co2+-Silica was favorable for the synergistic removal of MG and Cr(Ⅵ) in the binary system. Strongly oxidizing Cr(Ⅵ) can participate in the Fenton reaction, thus promoting MG degradation over a wide pH range. Thus, a positive synergistic effect exists between MG and Cr(Ⅵ). Considering that a large number of metal ions remained in the solution after the degradation reaction, EDDS-Silica was added to the degradation solution, and adsorption experiments were performed for 4 h at 30 ℃to adsorb and remove Cr and Fe via the strong chelating property of EDDS. The total residual mass concentrations of Cr and Fe were 4.96 and 1.02 mg/L, respectively, which meet national emission standards. These findings indicate that EDDS-Silica has good effects on the removal of residual metal ions after the nonhomogeneous Fenton reaction. As heterogeneous Fenton-like catalysts, the aminopolycarboxylic acid-modified materials proposed in this study can simultaneously promote the Fenton reaction and remove residual metal ions, thereby effectively removing MG and Cr(Ⅵ) from the binary system while ensuring that the content of residual metal ions in the system meets environmental emission standards. This study has broad application prospects in dye degradation and heavy-metal-ion wastewater treatment, and provides a reference value and theoretical basis for the development of other similar ligand-modified materials.

The Development of Clioquinol Labeled-Gold Nanoparticles for the Treatment of Alzheimer’s Disease

Clioquinol has emerged as a prominent metal-chelating agent for Alzheimer’s Disease. While clioquinol was once a popular antibiotic for skin infections, it has recently been investigated as a potential therapeutic for Alzheimer’s Disease. Its metal chelating property can restore metal homeostasis and prevent copper (Cu2+) and zinc (Zn2+) from interacting with amyloid-β (Aβ) peptides. Here, we propose labeling gold nanoparticles with clioquinol as a novel therapeutic approach for Alzheimer’s Disease to enable effective delivery of the agent across the blood-brain barrier. Based on previous studies on the individual efficacies of clioquinol and gold nanoparticles, we anticipate that this approach will prevent the formation of Aβ oligomers by disrupting metal-protein interactions. Our proposed clioquinol-labeled gold nanoparticles provide a novel curative approach for Alzheimer’s Disease and insights into subsequent therapeutic developments.

Iron chelating, antioxidant, and anti-inflammatory properties of brazilin from Caesalpinia sappan Linn

BackgroundIron overload and inflammation are severe conditions that can lead to various chronic diseases. However, the current iron chelator drugs have their limitations. The phytochemical compounds from herbals, such as brazilin, the major active compound in Caesalpinia sappan Linn., have significant therapeutic potential in various chronic diseases. Our study was designed to examine the effect of brazilin on iron chelating properties, antioxidant activity in hepatocytes, and anti-inflammatory potential in macrophages. MethodsThis study focused on the isolation, purification, and evaluation of brazilin, the principal bioactive constituent found in C. sappan wood. Brazilin was extracted via methanol maceration followed by column chromatography purification. The purified compound was characterized using high-performance liquid chromatography (HPLC), nuclear magnetic resonance (NMR) spectroscopy, and mass spectrometry (MS). The antioxidant potential of brazilin was assessed by in vitro assays, including 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azinobis-(3-ethylbenzthiazolin-6-sulfonic acid (ABTS), and ferric-reducing antioxidant power (FRAP). Furthermore, its cellular antioxidant activity was evaluated using hydrogen peroxide-induced oxidative stress in the hepatocellular carcinoma cell line (Huh-7). The iron-chelating capacity of brazilin was determined spectrophotometrically, and Job's plot method was used to elucidated the stoichiometry of the iron-brazilin complex formation. The anti-inflammatory properties of brazilin were investigated in lipopolysaccharide (LPS)-stimulated macrophages (RAW 264.7). Nitric oxide (NO) inhibition was quantified using the Griess reagent, while the expression levels of pro-inflammatory cytokines, interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α), were evaluated by RT-qPCR. ResultsThe results demonstrated that brazilin exhibited potent antioxidant activity in vitro and hepatocytes in a concentration-dependent manner. It also showed anti-inflammatory activity, in which NO production was significantly reduced and IL-6 and TNF-α expression in LPS-induced macrophages were repressed. Furthermore, it can bind ferric and ferrous ions. Brazilin acts as a bidentate iron chelator that forms a complex with iron in a 2:1 ratio, and two water molecules are used as additional chelators in this complex. ConclusionsOur findings have significant implications. Brazilin can potentially alleviate the harmful effects of iron-induced oxidative stress and inflammatory disorders.

Exploiting the potential of rivastigmine-melatonin derivatives as multitarget metal-modulating drugs for neurodegenerative diseases

The multifaceted nature of the neurodegenerative diseases, as Alzheimer's disease (AD) and Parkinson's disease (PD) with several interconnected etiologies, and the absence of effective drugs, led herein to the development and study of a series of multi-target directed ligands (MTDLs). The developed RIV-IND hybrids, derived from the conjugation of an approved anti-AD drug, rivastigmine (RIV), with melatonin analogues, namely indole (IND) derivatives, revealed multifunctional properties, by associating the cholinesterase inhibition of the RIV drug with antioxidant activity, biometal (Cu(II), Zn(II), Fe(III)) chelation properties, inhibition of amyloid-β (Aβ) aggregation (self- and Cu-induced) and of monoamine oxidases (MAOs), as well as neuroprotection capacity in cell models of AD and PD. In particular, two hybrids with hydroxyl-substituted indoles (5a2 and 5a3) could be promising multifunctional compounds that inspire further development of novel anti-neurodegenerative drugs.

Platinum(II) complexes based on derivatives of natural chlorins with pyridine-containing chelate groups as prototypes of drugs for combination therapy in oncology

Objectives. To synthesize Pt-containing derivatives of natural chlorins as potential agents for the combination therapy in oncology. Platinum compounds are known to occupy an important place as chemotherapeutic agents in the treatment of oncological diseases. However, Pt(II) complexes are highly toxic to the body and are not selectively accumulated in tumor cells. If photodynamic and chemotherapy methods are combined in a single drug, the pigments are responsible for the selectivity of conjugate accumulation in the tumor, while a chemotherapeutic agent based on Pt(II) complexes is responsible for the cytotoxic effect on tumor cells. This will not affect healthy cells and thereby minimize the systemic toxicity of the drug to the body.Methods. Methods for the synthesis of pyridine-containing derivatives of natural chlorins and their metal complexes for use as potential binary agents in oncology were applied. As part of the study, the structures of the compounds obtained were confirmed by mass spectrometry, nuclear magnetic resonance spectroscopy, ultraviolet spectroscopy, and high-resolution chromatography-mass spectrometry. Preparative methods, including thin-layer and column chromatography, centrifugation and recrystallization, were used to isolate and purify the compounds obtained.Results. Platinum(II) complexes of pyridine-containing derivatives of natural chlorins were obtained for application in combination therapy in oncology. The schemes for synthesizing the target photosensitizers were optimized, in order to increase the yields and for subsequent transfer to industrial sites.Conclusions. It was found that pyridine-containing derivatives of natural chlorins could be obtained in high yields, that they possess chelating properties for platinum, and can be considered as binary agents in cancer therapy after successful preclinical trials.

Design, synthesis, and biological evaluation of imidazolylacetophenone oxime derivatives as novel brain-penetrant agents for Alzheimer's disease treatment

Alzheimer's disease (AD, also known as dementia) has become a serious global health problem along with population aging, and neuroinflammation is the underlying cause of cognitive impairment in the brain. Nowadays, the development of multitarget anti-AD drugs is considered to be one effective approach. Imidazolylacetophenone oxime ethers or esters (IOEs) were multifunctional agents with neuroinflammation inhibition, metal chelation, antioxidant and neuroprotection properties against Alzheimer's disease. In this study, IOEs derivatives 1−8 were obtained by structural modifications of the oxime and imidazole groups, and the SARs showed that (Z)-oxime ether (derivative 2) had stronger anti-neuroinflammatory and neuroprotective ability than (E)-congener. Then, IOEs derivatives 9−30 were synthesized based on target-directed ligands and activity-based groups hybridization strategy. In vitro anti-AD activity screening revealed that some derivatives exhibited potentially multifunctional effects, among which derivative 28 exhibited the strongest inhibitory activity on NO production with EC50 value of 0.49 μM, and had neuroprotective effects on 6-OHDA-induced cell damage and RSL3-induced ferroptosis. The anti-neuroinflammatory mechanism showed that 28 could inhibit the release of pro-inflammatory factors PGE2 and TNF-α, down-regulate the expression of iNOS and COX-2 proteins, and promote the polarization of BV-2 cells from pro-inflammatory M1 phenotype to anti-inflammatory M2 phenotype. In addition, 28 can dose-dependently inhibit acetylcholinesterase (AChE) and Aβ42 aggregation. Moreover, the selected nuclide [18F]-labeled 28 was synthesized to explore its biodistribution by micro-PET/CT, of which 28 can penetrate the blood-brain barrier (BBB). These results shed light on the potential of 28 as a new multifunctional candidate for AD treatment.

A new application of MoS2@AG@PA prepared by irradiation: Synergizing with magnesium hydroxide to enhance fire safety and other key properties of EVA composites

AbstractTwo‐dimensional molybdenum disulfide (MoS2) nanosheets are seen as highly promising nanofillers for enhancing polymer properties, yet there is a need for methods that are low‐cost, simple, and environmentally friendly to facilitate the large‐scale production of MoS2 nanosheets. Furthermore, it is necessary to functionalize the MoS2 surface to ensure good interfacial compatibility with the polymer matrix. In this study, MoS2@Ag@PA hybrids were created by generating silver nanoparticles directly on the surface of MoS2 via radiation, followed by encapsulation on the surface of MoS2@Ag through the chelating properties of phytic acid. It is significant to note that, due to the excellent lubrication and physical cross‐linking effects of the MoS2@Ag@PA hybrids, adding one part of MoS2@Ag@PA hybrids can enhance the melt flow rate and elongation at break of the ethylene vinyl acetate copolymer (EVA)/MH composites by 140% and 17.3%, respectively. The simultaneous addition of one part of MoS2@Ag@PA hybrids decreased the peak heat release rate, total heat release, and total smoke release of the EVA composites by 48.7%, 42.7%, and 41.2%, respectively. Moreover, the toxic gasses (e.g., CO) generated by burning EVA composites were significantly reduced compared to pure EVA, indicating improved fire safety. This research not only provides significant opportunities for the green mass production of MoS2 nanosheets but also expands their potential applications in high‐performance nanocomposites.

A comprehensive review and recent advancement in the application of tannins for treating Parkinson disease

IntroductionParkinson's disease (PD) is a neurodegenerative disorder characterized by progressive loss of dopaminergic neurons in the substantia nigra. Despite extensive research, the etiology of PD remains elusive, and current treatments focus primarily on symptomatic relief rather than disease modification. MethodsThe papers were searched in Web of Science, Scopus, PubMed, PubMed Prime, Cochrane library, Sciencedirect and Google Scholar as web resources. This article includes information about tannins research and reviews in the treatment of PD. However, other paper related to CNS have been avoided. ResultsIn recent years, there has been growing interest in exploring the therapeutic potential of natural compounds, such as tannins, for the management of PD. Tannins, polyphenolic compounds found abundantly in various plant species, have demonstrated neuroprotective effects through their antioxidant, anti-inflammatory, and metal chelating properties. This review provides a comprehensive overview of the current understanding of PD pathophysiology, existing treatment modalities, and the potential role of tannins in PD management. Additionally, recent advancements in the application of tannins, including in vitro and in vivo studies, clinical trials, and novel delivery systems, are discussed. Furthermore, challenges and future perspectives regarding the translation of tannin-based therapies into clinical practice are addressed. DiscussionOverall, this review highlights the promising therapeutic potential of tannins in the treatment of Parkinson's disease and underscores the need for further research to elucidate their mechanisms of action and optimize their clinical efficacy.

THP as a sensor for the electrochemical detection of H2O2

Hydrogen peroxide (H2O2) detection is paramount in biological and clinical domains due to its pivotal role in various physiological and pathological processes. This molecule is a crucial metabolite and effector in cellular redox mechanisms, influencing diverse cellular signaling pathways and bolstering the body’s defense mechanisms against infection and oxidative stress. Organic molecule-based electrodes present unique advantages such as operational versatility and scalability, rendering them attractive candidates for sensor development across diverse fields encompassing food safety, healthcare, and environmental monitoring. This study explores the electrochemical properties of a tris(3-hydroxypyridin-4-one) THP, which has been unexplored in electrochemical sensing. Leveraging THP’s chelating properties, we aimed to develop an electrochemical probe for hydrogen peroxide detection. Our investigations reveal promising results, with the developed sensor exhibiting a low limit of detection (LOD) of 144 nM, underscoring its potential utility in sensitive and selective H2O2 detection applications. In addition, the new sensor was also tested on fetal bovine serum (FBS) to emphasize future applications on biological matrices. This research signifies a significant stride in advancing electrochemical sensor technologies for hydrogen peroxide detection with several novelties related to the usage of THP, such as high sensitivity and selectivity, performance in biological matrices, repeatability, stability, and reproducibility, economical and practical advantages. This research opens new avenues for enhanced biomedical diagnostics and therapeutic interventions.

Implications of White Light-Emitting Diode-Based Photoirradiation on Green Synthesis of Silver Nanoparticles by Methanol- and Aqueous-Based Extracts of Bergenia ciliata Leaves.

Bergenia ciliata (BC) is a perennial herb that is frequently used as a traditional medicine. Its leaves and rhizomes are reported to have significant antioxidant, metal-reducing, and chelating properties. Although the rhizomes have the potential to synthesize silver nanoparticles (AgNPs), the leaves are yet to be studied for the green synthesis of metal nanoparticles. Likewise, photoirradiation also plays a significant role in the green synthesis of metal nanoparticles. In the current study, we intended to demonstrate the implications of photoirradiation by white light-emitting diode (LED) on the aqueous and methanol extracts (AE and ME, respectively) of BC leaf-mediated green synthesis of AgNPs. In this regard, the AgNP synthesis of the two extracts was performed in the dark and under 250-lumen (lm) and 825 lm LED bulbs. The physicochemical characterization of the synthesized nanoparticles was also performed, wherein percent nanoparticles yield, morphology of the nanoparticles, shape, size, percent elemental composition, crystallinity, and nanoparticle stability were studied. The nanoparticle-synthesizing potential of the two extracts contradicted significantly in the presence and absence of light, while the AE produced a significantly high number of nanoparticles in the dark (17.26%), and increasing light intensities only attenuated the nanoparticle synthesis, whereas ME synthesized comparatively negligible silver nanoparticles in the dark (1.23%). However, increasing light intensities significantly enhanced the number of nanoparticles synthesized in 825 lms (7.41%). The GCMS analysis further gave a comparative insight into the phytochemical composition of both extracts, wherein catechol and pyrogallol were identified as major reducing agents for nanoparticle synthesis. The influence of light intensities on the physiochemical characterization of AgNPs was predominant. While the size of both the AE- and ME-mediated AgNPs increased considerably (20-50 nm diameter) with increasing light intensities, the percent of silver atoms decreased significantly with increasing light intensities in both the AE- and ME-mediated AgNPs with ranges of 13-18% and 14-24%, respectively. The nanoparticle stability studies suggested that both the AE- and ME-mediated AgNPs were stable for up to 15 days when stored at 4 °C. The stability of both nanoparticles was attributed to the presence of a wide range of phytochemicals. In conclusion, the AE of BC leaves was reported to have significantly higher AgNP-synthesizing potential as compared to the ME. However, AE-mediated AgNP synthesis is attenuated by photoirradiation, whereas ME-mediated AgNP synthesis is enhanced by photoirradiation. The photoirradiation by white LED light increases the size of the AgNPs, while the percent silver composition declines, irrespective of the extract type. Both extracts, however, have nanoparticle stabilizing potential, thereby producing stable nanoparticles.

New applications of Clioquinol in the treatment of inflammation disease by directly targeting arginine 335 of NLRP3

The NOD-like receptor protein 3 (NLRP3) inflammasome is essential in innate immune-mediated inflammation, with its overactivation implicated in various autoinflammatory, metabolic, and neurodegenerative diseases. Pharmacological inhibition of NLRP3 offers a promising treatment strategy for inflammatory conditions, although no medications targeting the NLRP3 inflammasome are currently available. This study demonstrates that clioquinol (CQ), a clinical drug with chelating properties, effectively inhibits NLRP3 activation, resulting in reduced cytokine secretion and cell pyroptosis in both human and mouse macrophages, with a half maximal inhibitory concentration (IC50) of 0.478 μM. Additionally, CQ mitigates experimental acute peritonitis, gouty arthritis, sepsis, and colitis by lowering serum levels of interleukin-1β (IL-1β), IL-6, and tumour necrosis factor-α (TNF-α). Mechanistically, CQ covalently binds to Arginine 335 (R335) in the NACHT domain, inhibiting NLRP3 inflammasome assembly and blocking the interaction between NLRP3 and its component protein. Collectively, this study identifies CQ as an effective natural NLRP3 inhibitor and a potential therapeutic agent for NLRP3-driven diseases.

Protein Hydrolysates from Salmon Heads and Cape Hake By-Products: Comparing Enzymatic Method with Subcritical Water Extraction on Bioactivity Properties.

Fish by-products can be converted into high-value-added products like fish protein hydrolysates (FPHs), which have high nutritional value and are rich in bioactive peptides with health benefits. This study aims to characterise FPHs derived from salmon heads (HPSs) and Cape hake trimmings (HPHs) using Alcalase for enzymatic hydrolysis and Subcritical Water Hydrolysis (SWH) as an alternative method. All hydrolysates demonstrated high protein content (70.4-88.7%), with the degree of hydrolysis (DH) ranging from 10.7 to 36.4%. The peptide profile of FPHs indicated the breakdown of proteins into small peptides. HPSs showed higher levels of glycine and proline, while HPHs had higher concentrations of glutamic acid, leucine, threonine, and phenylalanine. Similar elemental profiles were observed in both HPHs and HPSs, and the levels of Cd, Pb, and Hg were well below the legislated limits. Hydrolysates do not have a negative effect on cell metabolism and contribute to cell growth. HPSs and HPHs exhibited high 2,2'-azino-bis(3 ethylbenzthiazoline-6)-sulfonic acid (ABTS) radical scavenging activity, Cu2+ and Fe2+ chelating activities, and angiotensin-converting enzyme (ACE) inhibitory activity, with HPHs generally displaying higher activities. The α-amylase inhibition of both FPHs was relatively low. These results indicate that HPHs are a promising natural source of nutritional compounds and bioactive peptides, making them potential candidates for use as an ingredient in new food products or nutraceuticals. SWH at 250 °C is a viable alternative to enzymatic methods for producing FPHs from salmon heads with high antioxidant and chelating properties.

Moringa oleifera flowers: insights into their aroma chemistry, anti-inflammatory, antioxidant, and enzyme inhibitory properties

BackgroundMoringa oleifera is a highly nutritious plant widely used in traditional medicine.ResultsThe aroma constituents present in the fresh flowers of M. oleifera versus the hydrodistilled oil and hexane extract were studied using GC-MS. Aldehydes were the major class detected in the fresh flowers (64.75%) with E-2-hexenal being the predominant component constituting > 50%. Alkane hydrocarbons, monoterpenes, and aldehydes constituted > 50% of the hydrodistilled oil, while alkane hydrocarbons exclusively constitute up to 65.48% of the hexane extract with heptacosane being the major component (46.2%). The cytotoxicity of the hexane extract was assessed on RAW 264.7 macrophages using the MTT assay which revealed no significant cytotoxicity at concentrations of 1 µg/mL and displayed IC50 value at 398.53 µg/mL as compared to celecoxib (anti-inflammatory drug) with IC50 value at 274.55 µg/ml. The hexane extract of Moringa flowers displayed good anti-inflammatory activity through suppression of NO, IL-6, and TNF-α in lipopolysaccharide-induced RAW 264.7 macrophages. The total phenolic and flavonoid content in the hexane extract was found to be 12.51 ± 0.28 mg GAE/g extract and 0.16 ± 0.01 mg RuE/g extract, respectively. It displayed moderate antioxidant activity as indicated by the in vitro DPPH, ABTS, CUPRAC, FRAP, and phosphomolybdenum (PBA) assays. No metal chelating properties were observed for the extract. The enzyme inhibitory potential of the hexane extract was evaluated on acetyl- and butyrylcholinesterases (for neuroprotective assessment), α-amylase and α-glucosidase (for antihyperglycemic assessment), and tyrosinase (for dermoprotective assessment) revealing promising results on cholinesterases, tyrosinase, and α-glucosidase.ConclusionOur findings suggested that M. oleifera leaves can be considered as a multidirectional ingredient for preparing functional applications.Graphical abstract

Biosynthesis of a clickable pyoverdine via in vivo enzyme engineering of an adenylation domain

The engineering of non ribosomal peptide synthetases (NRPS) for new substrate specificity is a potent strategy to incorporate non-canonical amino acids into peptide sequences, thereby creating peptide diversity and broadening applications. The non-ribosomal peptide pyoverdine is the primary siderophore produced by Pseudomonas aeruginosa and holds biomedical promise in diagnosis, bio-imaging and antibiotic vectorization. We engineered the adenylation domain of PvdD, the terminal NRPS in pyoverdine biosynthesis, to accept a functionalized amino acid. Guided by molecular modeling, we rationally designed mutants of P. aeruginosa with mutations at two positions in the active site. A single amino acid change results in the successful incorporation of an azido-l-homoalanine leading to the synthesis of a new pyoverdine analog, functionalized with an azide function. We further demonstrated that copper free click chemistry is efficient on the functionalized pyoverdine and that the conjugated siderophore retains the iron chelation properties and its capacity to be recognized and transported by P. aeruginosa. The production of clickable pyoverdine holds substantial biotechnological significance, paving the way for numerous downstream applications.

Physiological and molecular mechanisms of carbon quantum dots alleviating Cu2+ toxicity in Salvia miltiorrhiza bunge

Excessive Cu2+ is toxic to plants. Carbon quantum dots (CQDs) exhibit certain chelating properties towards heavy metals, and they also demonstrate antioxidant activities. To explore the mechanism for alleviating the Cu2+ toxicity of Salvia miltiorrhiza Bunge mediated by CQDs, CQDs that contained CC, CO, H–O, C–N and C–O functional groups with particle size less than 10 nm and that emitted blue fluorescence were prepared. S. miltiorrhiza seedlings were treated with 200 μM of Cu2+ and 500 mg/L of CQDs to relieve stress. Exogenous CQDs effectively restored plant phenotype; reduced Cu2+, H2O2 and malondialdehyde contents and restored total superoxide dismutase, peroxidase and catalase activities under Cu2+ toxicity. Simultaneously, an association network of Cu2+ transport-related and metabolic pathway genes of phenolic acids and terpenoids was established on the basis of cross-species transcriptome analysis. Combined with reverse transcription quantitative real-time polymerase chain reaction analysis, the potential molecular mechanism of CQDs, i.e. promoting phenolic acid biosynthesis to alleviate Cu2+ toxicity, was revealed by activating the expression of key enzyme genes of phenolic acid synthesis. This study provides a theoretical basis for Cu2+ pollution prevention and control in plants. It also laid a foundation for alleviating Cu stress by using CQDs in agricultural production.